DRUG MOA and INDICATION ADVERSE EFFECTS NOTABLE PROPERTIES

1. AUTONOMIC DRUGS
Cholinomimetics
A. Direct Acting Choline Esters
i. Acetylcholine Muscarinic agonist; activates M1 through M3
receptors in all peripheral tissues. Results to increased
secretion, smooth muscle contraction (except in
vascular smooth muscles where it causes relaxation)
and changes in heart rate
ii.Betanechol Muscarinic agonist; activates M1 through M3
receptors in all peripheral tissues (same as Ach) ; for
Bladder and bowel atony
iii. Carbachol Nonselective muscarinic and nicotinic agonist; similar
to betanechol; used topically for glaucoma treatment
CNS stimulation, miosis, cyclospasm, brochoconstriction, very short lived DOA: 5-30sec,
excessive GI and GU smooth muscle contraction, increased apidly hydrolyzed by AChE; acts on
secretory activity of sweat gland, airways etc, vasodilation both M and N receptors
Cylospasm, diarrhea, urinary urgency, vasodilation, reflex Results in smooth muscle
tachycardia, sweating contraction except in vascular
smooth muscles where it causes
relaxation; resistant to AChE, orally
active, act on M receptors only
Cylospasm, diarrhea, urinary urgency, vasodilation, reflex acts on both M and N receptors,
tachycardia, sweating DOA: 30mins-2hrs

B. Direct Acting Muscarinic Alkaloids

i. Pilocarpine Partial muscarinic agonist; used for treatment of Miosis, blurring of vision good lipid solubility compared to
Glaucoma, Sjogren's syndrome and Sicca syndrome choline esters

C. Direct Acting Nicotinic Agonists

i. Nicotine Agonist at both NN and NM receptos; activates Generalized ganglionic stimulation (hypertension, tachycardia, Able to enter the CNS and activates
autonomic post ganglionic neurons (both sympathetic nausea, vomiting, diarrhea) NN receptors ; DOA: 1-6h only
and parasympathetic) and skeletal muscle
neuromuscular end plates ; for Smoking Cessation
ii. Varenicline Selective partial agonist at nicotinic receptors; used Generalized ganglionic stimulation (hypertension, tachycardia, longer DOA than nicotine: 12-24h
exclusively for smoking cessation nausea, vomiting, diarrhea)
D. Short Acting Cholinesterase Inhibitor (Alcohol)
i. Edrophonium Binds briefly to active site of acetylcholinesterase Miosis, salivation, nausea, vomiting, diarrhea, bradycardia parenteral, very short lived DOA: 5-
(AChE) and prevents access of acetylcholine (Ach); 15min
Amplifies all actions of Ach; increases
parasympathetic activity and somatic neuromuscular
transmission ; for Myasthenia gravis diagnosis
(Tensilon test)
E. Intermediate Acting Cholinesterase Inhbitors

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(Carbamates)
i. Neostigmine Forms covalent bonds with AChE, but is hydrolyzed Miosis, salivation, nausea, vomiting, diarrhea, bradycardia poor lipid solubility, oral, DOA:
and released; Longer acting than Edrophonium ; for 30min-2h
Myasthenia gravis treatment; reversal of
nondepolarizing muscular blockade, Ogilvie syndrome
ii. Pyridostigmine Longer acting effect compared to Neostigmine Miosis, salivation, nausea, vomiting, diarrhea, bradycardia poor lipid solubility, oral, DOA: 4-8h

iii. Physostigmine Natural alkaloid tertiary amine, similar to neostigmine Miosis, salivation, nausea, vomiting, diarrhea, bradycardia good lipid solubility: able to enter
the CNS, DOA: 4-8h
F. Long Acting Cholinesterase Inhibitors
(Organophosphates)
i. Echothiophate Similar to neostigmine but with slower release Miosis, salivation, nausea, vomiting, diarrhea, bradycardia moderate lipid solubiliy, DOA: 2-
7days
ii. Malathion, Parathion malathion: scabicide, parathion: insecticide Miosis, salivation, nausea, vomiting, diarrhea, bradycardia high lipid solubiliy, DOA: 7-30 days

Cholinoceptor Blocking Drugs

i. Scopolamine Competitively blocks all muscarinic receptors, Drowsiness, blurring of vision, dry eyes, constipation, dry mouth, known as Hyoscine-N-Butyl-
antagonizes histamine and serotonin ; for motion urinary retention Bromide (Buscopan)
sickness, dec. acid secretion in the GIT
ii. Atropine Nonselective competitive antagonism at all muscarinic Tachycardia, mydriasis, cyloplegia, skin flushing, delirium, DOC for organophosphate
receptors in the CNS and peripheral tissues; causes hallucinations, urinary retention, constipation poisoning; notorious for causing
mydriasis and cycloplegia; mandatory antidote for hyperthermia
severe cholinesterase inhibitor poisoning ; Mydriatic,
cycloplegic, antidote for organophosphate poisoning
(DOC), for bradycardia, hypersalivation and to
decrease airway secretion during general anesthesia
iv. Homatropine Similar to atropine but with a shorter duration of Mydriatic, cycloplegic
action (12-24h) ; Mydriatic, cycloplegic in eye
examinations
v. Cyclopentolate Similar to atropine but with a shorter duration of Mydriatic, cycloplegic
action (3-6h), Mydriatic, cycloplegic in eye
examinations
vi. Tropicamide Similar to atropine but with the shortest duration of shorter DOA among cholineceptor
action (15-60min); Mydriatic, cycloplegic in eye blockers (15-60min)
examinations

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 vii. Ipratropium Competitive nonselective antagonist at muscarinic
receptors ; for BA and COPD
viii. Tiotropium Similar to Ipratropium but with longer duration of
action
ix. Oxybutinin Nonselective muscarinic antagonist which reduces
detrussor smooth muscle tone spasms ; for
decreasing urgency in mild cystitis and dec. bladder
spasm after urologic surgery
x. Pralidoxime Regenerates active acetylcholinesterase; can relieve
skeletal muscle and endplate block ; Usual antidote
for early stage cholinesterase inhibitor poisoning
xi. Hexamethonium, Mecamylamine, Trimethaptan Competitively blocks all Nn nicotinic Ach receptors ;
for Hypertensive emergencies (obsolete)
Sympathomimetics
i. Epinephrine Non-selective, direct acting sympathomimetic;
activates A and B adrenergic receptors; A1 -
vasoconstriction and increased BP; B1 - increased HR,
conduction and contractility; B2 - bronchodilatation ;
used for Cardiac arrest, anaphylaxis, asthma, COPD,
Hemostasis
ii. Norepinephrine Non-selective, direct acting sympathomimetic;
activates A and B adrenergic receptors; A1 -
vasoconstriction and increased BP; B1 - increased HR,
conduction and contractility; B2 - bronchodilatation ;
used for Neurogenic shock, cardiogenic shock
iii. Dopamine Non-selective, direct acting sympathomimetic;
activates A, B and D1 adrenergic receptors; A1 -
vasoconstriction and increased BP; B1 - increased HR,
conduction and contractility; D1 - vasodilation in
splanchnic and renal blood vessels ; for cardiogenic
Shock and heart failure
Dry mouth, cough, nasal dryness not as effective as SABAs but less
tachycardia and arrhythmia ; few
muscarinic effects outside the lungs
Dry mouth, cough, nasal dryness not as effective as SABAs but less
tachycardia and arrhythmia ; few
muscarinic effects outside the lungs
Tachycardia, mydriasis, cyloplegia, skin flushing, delirium, for urinary urgency and
hallucinations, urinary retention, constipation incontinence
muscle weakness Must be administered before 6-8
hours of organophosphate bond
with cholinesterase occurs ; has
oxime group which has high affinity
for phosphorus
Postural hypotension, dry mouth, blurred vision, constipation, first successful agents in treating
sexual dysfunction HTN
Hypertension, tachycardia, ischemia, hyperglycemia DOC for Anaphylaxis ; inactive per
orem ; do not enter CNS
significantly ; short DOA
Extreme vasospasm, tissue necrosis, excessive BP increase, Compensatory vagal reflexes tend
arrhythmias, infarction, reflex bradycardia to overcome the direct postive
chronotropic effects ; alpha activity
> beta activity; inactive per orem ;
do not enter CNS significantly ;
short DOA
Cardiovascular disturbances, arrhythmias inactive per orem ; do not enter
CNS significantly ; short DOA; very
effective in renal failure associated
with shock
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 iv. Isoproterenol Beta nonselective sympathomimetic; nonselectively
activates B adrenergic receptors; B1 - increased HR,
conduction and contractility; B2- bronchodilatation ;
for Asthma
vi. Phenylephrine A1 agonist used for short term maintenance of BP in
acute hypotension; also used intranasally to produce
local vasoconstriction as a decongestant ; mydriatic,
for drug-induced hypotension, spinal shock
vii. Clonidine A2 agonist that inhibits adenylyl cyclase and interacts
with other intracellular pathways; marked
vasodilation by central sympatholytic effect ; for
Hypertension, Cancer pain, opioid withdrawal
viii. Methyldopa, Guanfacine and Guanabenz Central sympatholytics analogous to clonidine ;
Methyldopa is used for Pre-eclampsia
xi. Apraclonidine, Brimonidine A2 agonist; reserved for ophthalmologic use in
glaucoma for reduction of intraocular pressure
xii. Dobutamine B1 agonist that activates adenylyl cyclase, increasing
myocardial contractility; with positive inotropic effect
; Clinically used for cardiogenic shock and acute heart
failure
xiii. Albuterol/Salbutamol B2 agonist with adenylyl cyclase activation; results to
bronchial smooth muscle dilation ; for Bronchial
Asthma
xiv. Fenoldopam D1 agonist that activates adenylyl cyclase; results to
vascular smooth muscle relaxation ; for Hypertension
Cardiovascular disturbances, arrhythmias synthetic catecholamine, not readily
taken up into nerve endings
Rebound nasal congestion (Rhinitis medicamentosa), Mydriasis without cycloplegia
hypertension, stroke, MI
Sedation, rebound hypertension, dry mouth When taken per orem, there is
initial inc in BP then will go down
once the drug enters the CNS
Sedation, positive Coomb's test (Hemolytic anemia) Methyldopa - positive Coomb's test
(Hemolytic anemia)
eye discomfort, hyperemia and pruritus, blurred vision NONE
Tachyarrhythmia, Hypertension, Eosinophilic myocarditis, Beta1 selective
Premature ventricular beats, Angina, Dyspnea, Fever, Headache,
Nausea, Palpitation
Nausea , Fever, Bronchospasm, Vomiting, Headache, Dizziness, Rapid development of tolerance;
Cough, Allergic reactions DOC as Asthma reliever
Angina, Cardiac dysrhythmia, Dizziness, Flushing, Heart failure, D1 agonist
Hypotension, Myocardial infarction, Tachycardia

xv. Bromocriptine D2 agonist that inhibits adenylyl cyclase and interacts Nausea, Hypotension, Headache, Dizziness D2 agonist
with other intracellular pathways; restores dopamine
actions in the CNS for Parkinson's disease,
prolactinemia
Sympatholytics
i. Phenoxybenzamine Irreversibly blocks A1 and A2 receptors resulting to Orthostatic hypotension, Reflex tachycardia, GI irritation Irreversible blockade
indirect baroreflex activation. Decreases blood
pressure but increases heart rate due to baroreflex
activation ; for Pheochromocytoma
ii. Phentolamine Reversible A1 and A2 receptor antagonist with low Orthostatic hypotension, Reflex tachycardia, GI irritation Reversible blockade
half life ; for Pheochromocytoma and Rebound
hypertension

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 iii. Prazosin, Doxazosin, Terazosin
iv. Tamsulosin
vi. Labetalol
vii. Propranolol, Nadolol, Timolol
viii. Metoprolol, Atenolol, Alprenolol, Betaxolol,
Nebivolol
x. Pindolol, Acebutolol, Carteolol, Bopindolol,
Oxprenolol, Celiprolol, Penbutolol
xi. Carvedilol, Medoxalol, Bucindolol, Labetalol
xii. Esmolol
2. CARDIOVASCULAR-RENAL DRUGS
Antihypertensives
A. Diuretics
i.Thiazide: Hydrochlorothiazide, Chlorthalidone,
Metolazone, Indapamide
Blocks A1 but not A2 receptors; leads to reduction in
blood pressure ; for Benign Prostatic Hyperplasia,
Hypertension
Slightly selective A1a blockade causing relaxation of
prostatic smooth muscles > vascular smooth muscle ;
for BPH
Beta blockade > A1 blockade; still with BP depressant
effects and limited HR increase
Blocks B1 and B2 receptors; lowers both HR and BP
and reduces the release of renin ; for Angina
prophylaxis, hypertension, arrhythmias, migraine,
performance anxiety, hyperthyroidism
B1 > B2 blockade; lowers both HR and BP, reduces the
release of renin BUT is considered safer for patients
with asthma ; for Angina prophylaxis, hypertension,
arrhythmias, migraine, performance anxiety,
hyperthyroidism
B1, B2 with intrinsic sympathomimetic (partial
agonist) effect; lowers BP with modest reduction in
HR
Beta blockade > A1 blockade; still with BP depressant
effects and limited HR increase ; for Heart Failure
B1 > B2 blockade; for rapid control of BP and
arrhythmias, thyrotoxicosis and myocardial ischemia
intraoperatively ; for Supraventricular tachycardia
lower BP by decreasing volume and a direct vascular
effect that is not yet fully understood
Inhibit Na/Cl transporter in distal convoluted tubule.
Cause moderate diuresis and reduced excretion of
calcium; for mild to moderate hypertension (FIRST
LINE), Heart failure, Nephrogenic Diabetes Insipidius,
Renal calcium stones
Dizziness, Drowsiness, Headache, Weakness, Asthenia, Nausea, Used in patients with HTN and BPH
Palpitation, Edema, Orthostatic hypotension at the same time
Headache, Orthostatic hypotension, Rhinitis, Abnormal Slightly selective A1a blockade
ejaculation, Dizziness, Arthralgia, Infection causing relaxation of prostatic
smooth muscles > vascular smooth
muscle
Bronchospasm, cardiac depression, AV block, hypotension, safe in pregnant patients
dizziness, headache; Use in caution with DM Px: Masks symptoms
of hypoglycemia in diabetics
Propranolol has local anesthetic
effect
Nebivolol has vasodilating effect ;
metoprolol reduce moratlity in
heart failure
Pindolol is a partial agonist,
therefore safer in bronchial asthma
Carvedilol reduce mortality in heart
failure
Used in for perioperative thyroid
storm
causes hypercalcemia in contrast
Hypokalemic metabolic alkalosis, Dilutional hyponatremia, with loop diuretics which cause
Potassium wasting, hyperlipidemia, hyperuricemia, sulfa allergy, hypocalcemia ; FIRST LINE for mild
hyperglycemia, hypercalcemia to moderate hypertension
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ii. Loop: Furosemide, Torsemide, Bumetanide, Ethacrynic
Acid
B. Sympathoplegics
i.Sympathetic Outflow Blocker: Clonidine, Methyldopa
ii. Ganglion blockers: Hexamethonium,Trimethaphan
iii. Nerve terminal blockers: Reserpine, Guanethidine,
Guanadrel
iv. Adrenergic antagonists: Prazosin,Doxazosin,
Terazosin, Tamsulosin, Silodosin
C. Vasodilators
i. Oral Vasolidator: Hydralazine
Minoxidil
ii. Calcium Channel Blockers
Non-dihydropyridine calcium channel blocker:
Verapamil, Diltiazem
Dihydropyridine calcium channel blocker: Nifedipine,
Amlodipine, Nicardipine, Nisoldipine, Isradipine,
Felodipine
Inhibit Na/K/2Cl transporter in thick ascending limb of
loop of Henle, Cause powerful diuresis and increased
CA excretion; for heart failure, hypertension, acute
renal failure, Pulmonary edema, hypercalcemia, Anion
overdose
decrease venous return, decrease HR, decrease
contractile force, decrease cardiac output, decrease
TPR
activates a2 adrenergic receptors ; for hypertensive
urgency (clonidine), pre eclampsia (methyldopa)
competetively blocks Nn nicotinic Ach receptors; for
hypertension (obsolete), hypertensive emergencies
Reserpine Irreversibly blocks the vesicular
monoamine transporter (VMAT) while Guanethidine
and Guanadrel inhibit the vesicular release of NE from
the presynaptic neuron; for Hypertension (obsolete)
selectively blocks a1 adrenergic receptors; for
hypertension, benign prostatic hyperplasia
Release NO from endothelial cells, Relaxes arteriolar
smooth muscle, causing vasolidation. Decreases
afterload ; for pre-eclampsia, hypertension, heart
failure
Opens K+ channels in vascular smooth muscle,
causing hyperpolarization, muscle relaxation and
vasolidation; for alopecia / male pattern baldness,
hypertension
block voltage-gated L-type calcium channels (cardiac >
vascular); for Angina, Supraventricular tachycardia,
migraine, hypertension
block voltage-gated L-type calcium channels (vascular
> cardiac); for Angina, hypertension
Hypokalemic metabolic alkalosis, Potassium wasting, ototoxicity, causes hypocalcemia in contrast
hyperuricemia, nephrotoxicity, dehydration, hypomagnesemia, with thiazide diuretics which cause
sulfa allergy hypercalcemia
Taper use prior to discontinuation
dry mouth, sedation, rebound hypertension, hemolytic anemia: to avoid rebound hypertension ;
(+) Coomb's test (methyldopa), sedation readily enter the CNS
Postural hypotension, blurred vision, constipation, dry mouth,
sexual dysfunction NONE
Sedation, suicidal ideation, severe psychiatric depression NONE
Tamsulosin is most selective for
prostatic smooth muscle ;
Reflex tachycardia (less chance), first dose orthostatic Doxazosin and Terazosin has longer
hypotension duration of action than prazosin
combination treatment with ISDN
Edema, myocardial ischemia, drug induced lupus (hydralazine), for heart failure is more effective
reflex tachycardia than ACEIs in blacks
require concomitant use of diuretics
Edema, Angina, Reflex tachycardia, Pulmonary hypertension, and BBs to block compensatory
Pericarditis, Hirsutism, salt and water retention responses
Constipation, Nausea, flushing,gingival hyperplasia, AV block, excessive cardiac depression may
sinus node depression, Pretibial edema, dizziness occur
greater vasodilator effect that
Nausea, Flushing, dizziness, pretibial edema, constipation cardiodepressant effect
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 iii. Parenteral Vasodilators
Nitroprusside
Diazoxide
Fenoldopam
D. Angiotensin antagonists and renin inhibitor
i. ACE inhibitors: Captopril, Enalapril, Lisinopril,
Benazepril
ii. Angiotensin receptor blocker: Losartan, Valsartan,
Irbesartan, Candesartan
iii. Renin inhibitor: Aliskerin
Vasodilators and anti-Angina Pectoris
A. Nitrates
i. Ultrashort-acting nitrate: Amyl Nitrite
ii. Short-acting nitrate: Nitroglycerin, Isosorbide
Dinitrate, Isosorbide Mononitrate
relaxes venous and arteriolar smooth muscle; for
acute heart failure, controlled hypotension,
cardiogenic shock, hypertensive emergency
Opens K+ channels in vascular smooth muscle,
causing hyperpolarization, muscle relaxation and
vasolidation; for hypertension
causes arteriolar vasolidation of the afferent and
efferent arterioles. Increases renal blood flow; for
hypertensive emergency
inhibit angiotensin converting enzyme ; for
hypertension, heart failure
competetively blocks Angiotensin 1 receptor site ; for
hypertension
inhibitor of renin's action on its substrate
angiotensinogen
releases nitric oxide (NO), relaxes smooth muscle,
especially vascular, increases cGMP (cyclic guanosine
monophosphate); for cyanide poisoning
releases nitric oxide (NO), increases cGMP (cyclic
guanosine monophosphate) and relaxes smooth
muscle especially vascular; for Angina, acute coronary
syndromes
not commonly used because it is
very light sensitive, has short
Duration of action ; given as
hypotension, headache, CN toxicity continuous infusion
a thiazide derivative without a
diuretic effect ; also reduces insulin
release (can be used to treat
hypoglycemia in insulin-producing
hypotension, headache tumors)
hypotension, hypokalemia short duration of action: 10mins
cough, hyperkalemia, rash, hypotension, palpitations, renal slows down the progression of DM
damage in patients with preexisting renal vascular disease but is nephropathy and cardiac
protective for DM nephropathy ; CI in pregnancy remodelling in heart failure
fatigue / weakness, hypoglycemia, anemia, diarrhea, cough, CI in
pregnancy as effective as ACEi but less cough
no reproductive toxicity but is also
diarrhea, cough, rash, hyperkalemia, increase in serum creatinine, CI because of the toxicity of ACEi
renal impairment, angioedema and ARBs
inhalational route, but now rarely
Reflex tachycardia, Orthostatic hypotension, methemoglobinemia used
Dangerous hypotension with PDE
inhibitors such as Sildenafil ; First
Reflex tachycardia, orthostatic hypotension, headache, tolerance Pass effect is ~90% (NTG), NTG also
(transdermal) decrease platelet aggregation
Page 7 of 87
B. Calcium Channel Blockers
block voltage-gated L-type calcium channels (cardiac >
i. Non-dihydropyridine calcium channel blocker: vascular); for Angina, Supraventricular tachycardia, Constipation, Nausea, flushing,gingival hyperplasia, AV block, excessive cardiac depression may
Verapamil, Diltiazem migraine, hypertension sinus node depression, Pretibial edema, dizziness occur

ii. Dihydropyridine calcium channel blocker: Nifedipine,

Amlodipine, Nicardipine, Nisoldipine, Isradipine, block voltage-gated L-type calcium channels (vascular
Felodipine > cardiac); for Angina, hypertension
Drugs used in Heart Failure
Other drugs for heart failure include Diuretics
(Furosemide is the DOC for acute heart failure),
Angiotensin Antagonists (ACEi is the DOC for chronic
heart failure), Beta1 blockers (dopamine and
dobutamine), Non-selective Beta Blockers (Carvedilol,
Labetalol, Metoprolol), PDEi (Inamrinone, Milrinone),
A. Cardiac Glycoside Vasodilators (Nitroprusside, Nitroglycerin)
inhibits Na/K ATPase; increases intracellular Ca,
increasing cardiac contractility; for heart failure,
i. Digoxin Nodal arrythmias
Anti-Arrhythmics
A. Class 1 Antiarryhtmics
Use- and state-dependent block of INa channels;
some block of Ik channels. Slowed conduction velocity
and pacemaker activity; prolonged action potential
duration and refractory period; for atrial and
ventricular arrhythmias especially after myocardial
i. Class 1A: Procainamide, Disopyramide, Quinidine, infarction
highly selective use and state-dependent INa block;
minimal effect in normal tissue; no effect on IK; DOC
for ventricular arrhythmia post-myocardial infarction,
Digoxin-induced arrhythmia ; Mexilitine can be used
ii. Class 1B: Lidocaine, Mexiletene, Tocainide, Phenytoin for neuropathic pain
Selective use and state-dependent block of INa;
iii. Class 1C: Flecainide, Propafenone, Encainide, slowed conduction velocity and pacemaker activity;
Moricizine for refractory arrhythmias
greater vasodilator effect that
Nausea, Flushing, dizziness, pretibial edema, constipation cardiodepressant effect
Arrhythmogenesis increased by
Narrow therapeutic index, Arrhythmias, diarrhea, vomiting, visual hypokalemia, hypercalcemia,
changes hypomagnesemia
Arrhythmias, lupus-like syndrome (procainamide), hypotension,
cinchonism (quinidine), thrombocytopenia (quinidine),
antimuscarinic effect (disopyramide), quinidine reduces digoxin Hyperkalemia exacerbates cardiac
clearance toxicity
Hyperkalemia, exacerbates cardiac
toxicity. Lidocaine is the least
cardiotoxic among conventional
anti-arrhythmics ; only affect
ischemic tissue; lidocaine is never
CNS stimulation, Allergy, Arrhythmias, depression, given P.O due to significant first
Agranulocytosis pass effect
hyperkalemia exacerbates cardiac
toxicity contraindicated for post MI
Increased arrhythmias (proarrhythmic effect), CNS excitation arrhythmias

Page 8 of 87
B. Class 2 Antiarrythmics
i. Propranolol, Esmolol
C. Class 3 Arrhythmics
i. Dofetilide, Ibutilide,
ii. Sotalol
iii. Amiodarone, Dronedarone
D. Class 4 Antiarrythmatics
i. Non-dihydropyridine calcium channel blocker:
Verapamil, Diltiazem
E.Miscellaneous Antiarrythmics
i. Adenosine
Diuretics
A. Carbonic Anhydrase Inhibitors
i. Acetazolamide, Dorzolamide, Brinzolamide,
Dichlorphenamide, Methanolamide
Block of beta-receptors, decrease in cAMP results to
decreased Na and Ca current and suppression of
cardiac pacemaker activity; for Post MI prophylaxis
against sudden death, thyrotoxicosis, acute
perioperative and thyrotoxic arrhythmias,
Supraventricular tachycardia
Selective Ik block ; prolonged action potential and QT
interval; for treatment and prophylaxis of atrial
fibrillation
Ik block and beta-adrenoceptor block; for ventricular
arrhythmias, Supraventricular tachycardia, Atrial
fibrillation
Strong Ik block produces marked prolongation of
action potential and refractory period. Group 1
activity slows conduction velocity; groups 2 and 4
activity confer additional anti arrhythmic activity; for
refractory arrhythmia, used off label in many
arrhythmia
Block voltage-gated L-type calcium channels (cardiac
>vascular), decreased AV conduction velocity ; for
Angina, Hypertension, Supraventricular tachycardia,
migraine, Raynaud's Phenomenon, Vasospasm
Increase in diastolic Ik of AV node that causes marked
hyperpolarization and conduction block; reduced ICa;
For AV nodal arrhythmias, DOC for paroxysmal
supraventricular tachycardia
Inhibits carbonic anhydrase. In proximal tubule, In
glaucoma, secretion of aqueous humor is reduced and
in mountain sickness, metabolic acidosis increases
respiration; for glaucoma, diuresis for edema with
alkalosis.
In CHF, reduces progression and
decreases incidence of potentially
fatal arrhythmias. Sotalol is a beta-
blocker anti arrhythmic that has
Bronchospasm, AV block, Hypotension, Cardiac depression class 3 properties
Group with the greatest risk for TDP
Torsade de pointes NONE
Dose-related torsade de pointes, excessive beta-blockade (sinus
bradycardia, asthma) NONE
Amiodarone has Class 1, 2 3 and 4
activity therefore is the MOST
EFFICACIOUS of all anti-arrhythmics,
Microcrystalline deposits in cornea and skin, paresthesias, amiodarone has longest among all
Pulmonary fibrosis, Tremor, Thyroid dysfunction (hyper- or hypo-) anti-arrhythmics (1-10 weeks)
Constipation, Pretibial edema, Nausea, Flushing, Gingival
hyperplasia, heart failure, AV block, dizziness, sinus node should be avoided in Ventricular
depression tachycardia
DOC for paroxysmal
supraventricular tachycardia,
Flushing, Transient chest pain, Dyspnea, Hypotension Duration of action is only 15sec
Drowsiness, Sulfa Allergy, Renal calcium stones, Paresthesias,
hyperchloremic metabolic acidosis, hepatic encephalopathy in diuresis is self-limiting after 2-3
cirrhotic patients, potassium wasting days
Page 9 of 87
B. Loop Diuretic
i.Furosemide, Bumetanide, Torsemide
C. Thiazide Diuretics
i. Hydrochlorothiazide, Chlorthalidone, Indapamide,
Metolazone
D. Potassium-Sparing Diuretics
i. Spironolactone, Eplerenone (Aldosterone Antagonist)
ii. Amiloride, Triamterene (Na channel Blocker)
E. Osmotic Diuretics
i. Mannitol, Glycerin, Isosorbide, Urea
F. ADH Agonists/ Antagonists
i. Antidiuretic hormone, Desmopressin, Vasopressin
Inhibit Na/K/2Cl transporter in thick ascending limb of
loop of Henle, Cause powerful diuresis and increased
Ca excretion; for Heart failure, Hypertension,
Pulmonary Edema, Hypercalcemia, Acute renal failure,
Anion overdose
Inhibit Na/Cl transporter in distal convolutes tubes.
Causes moderate diuresis and reduced excretion of
calcium; For hypertension Hypercalciuria, Heart
failure, Nephrogenic diabetes insipidius, renal calcium
stones
Steroid inhibitors of cytoplasmic aldosterone receptor
in cortical collecting ducts. Reduce K excretion; for
Hyperaldosteronism, Heart failure, Hypokalemia,
Hypertension
Inhibitor of ENaC (Epithelial sodium channels) in
cortical collecting duct, reduces Na reabsorption and
K excretion; for hypokalemia
Osmotically retains water in tubule by reducing
reabsorption in proximal tubule, descending limb of
Henle's loop, and collecting ducts; in the periphery,
mannitol extracts water from cells; for
Rhabdomyolysis, Hemolysis, Increased intracranial
pressure, Acute glaucoma
Agonists at V1 and V2 ADH receptors. Activate
insertion of aquaporin water channels in collecting
tubule. Vasoconstriction; For central diabetes
insipidus, hemophilia, Nocturnal enuresis, von
Willebrand's disease
Synergistic ototoxicity with
aminoglycosides. Efficacy decreased
Hypokalemic metabolic alkasis, dehydration, Ototoxicity, by NSAIDs ; causes hypocalcemia in
Potassium wasting, Sulfa allergy, Hyperuricemia, Hypocalcemia, contrast with thiazide diuretics
Hypomagnesemia, Nephritis which cause hypercalcemia
Synergistic effect with loop
diurectics. Efficacy decreased by
Hypokalemic metabolic alkalosis, Potassium wasting, dilutional NSAIDs ; causes hypercalcemia in
hyponatremia, Hyperglycemia, hyperuricemia, sulfa allergy, contrast with loop diuretics which
hyperlipidemia cause hypocalcemia
Hyperkalemia, impotence, Benign prostatic hyperplasia, Eplerenone reduces progression of
Hyperchloremic metabolic acidosis, anti-androgenic effect DM nephropathy and reduces
(Spironolactione) mortality post MI
Hyperkalemia, kidney stones, metabolic acidosis, Acute renal
failure (with indomethacin), should never be given with potassium should never be given with
supplements potassium supplements
Transient volume expansion (hyponatremia, pulmonary edema;
followed by hypernatremia) nausea, headache, dehydration,
vomiting used to maintain high urine flow
Increases the factor VIII activity of
patients with mild hemophilia A or
Hypertension, Hyponatremia von Willebrand disease
Page 10 of 87

G. ADH Antagonists: Conivaptan, Tolvaptan, Lixivaptan,
Demeclocycline, Lithium
3. DRUGS WITH IMPORTANT ACTION ON SMOOTH MUSCLES
Histamine, Serotonin and the Ergot Alkaloids
A. H1 antagonists
i. 1st Generation: Diphenhydramine, Dimenhydrinate,
Chlorpheniramine, Meclizine, Promethazine
ii. 2nd Generation: Loratadine, Desloratadine, Cetirizine,
Levocertirizine, Fexofenadine
B. H2 antagonists
Antagonist at V1, V2 receptors; for SIADH and
Hyponatremia
diminish or abolish the major actions of histamine in
the body by competitive, reversible blockade of
histamine H1-receptor sites on tissues ; used primarily
for the alleviation of conditions such as urticarial
rashes and nasal allergy that are characterised by type
I hypersensitivity ; are of value in preventing urticaria
and are used to treat urticarial rashes and mild
angioedema
Reversible blockade of histamine H1-receptor sites on
tissues ; anti-nausea and antiparkinsonism effect, for
allergic reactions, for sedation and motion sickness
(Diphenhydramine Dimenhydrinate, Cyclizine,
Meclizine, Promethazine), for chemotherapy-induced
vomiting (Diphenhydramine)
Reversible blockade of histamine H1-receptor sites on
tissues ; for allergic reactions
Infusion site reactions, hyperkalemia, Nephrogenic diabetes Central Pontine Myelinosis may
insipidus, Bone and Teeth abnormalities(demeclocycline), Renal occur with rapid correction of
failure (Lithium, demeclocycline) hyponatremia
Sedation, should not be given to neonates because they are more Possess antimuscarinic, adrenaline-
susceptible to antimuscarinic effects antagonising, serotonin
antagonising, and local anaesthetic
effects. Some have calcium-channel
blocking activity ; Sedating
antihistamines may enhance the
sedative effects of CNS depressants
including alcohol, barbiturates,
hypnotics, opioid analgesics,
anxiolytic sedatives, and
antipsychotics ; all are PO but can
be given topical (nose and eyes) ;
negligible effect on H2 receptors
Anticholinergic effects, orthostatic hypotension (promethazine), more likely to block autonomic
sedation receptors, also has alpha1 blocking
and local anesthetic effect ;
Cyclizine (more anti-motion
sickness action less sedative and
and autonomic effects);
Promethazine (less anti-motion
sickness, more sedative and
autonomic effects ; Usual half-life:
4-12h
headache, dry mouth, hyperkinesia, malaise, may cause No sedation and antimuscarinic
arrhythmia due to blockade of cardiac potassium channels effects ; usual half-life: 12-24h
(acrivastine, astemizole, cetirizine, loratadine, and terfenadine)
No blocking action on H1 receptor
Page 11 of 87
 i. Cimetidine, Ranitidine, Famotidine, Nizatidine Surmountable competitive pharmacologic block of H2
receptors, reduction of nocturnal acid secretion in
gastirc and duodenal ulcer, accelerate healing and
prevent recurrences ; for PUD, GERD and ZES
C. Serotonin Agonists
i. 5HT1D receptor agonist: Sumatriptan, Naratriptan, Agonist at the 5HT1D receptor in the blood vessels
Almotriptan, Eletriptan, Frovatriptan, Rizatriptan, causing vasocontriction ; 1st line treatment for Acute
Zolmitriptan migraine and cluster headache attacks
D. Serotonin Antagonists
i. 5HT3 receptor antagonist: Ondansetron, Granisetron, Selectively block 5HT3 receptors ; For antiemesis in
Dolasetron, Alosetron patients post-chemotherapy or post-operation
E. Ergot Alkaloids most are partial agonists at alpha receptors and 5HT
receptors but some are potent agonist at dopamine
receptors
i. Vasoselective: Ergotamine Mixed partial agonist effects at 5-HT2 and a-
adrenoceptors, causes vasoconstriction; For Migraine
attacks (but 5HT1D are preferred)
ii. Uteroselective: Ergonovine Mixed partial agonist effects at 5-HT2 and a-
adrenoceptors, causes vasoconstriction; For control of
post-partum bleeding
CYP450 inhibitor, antiandrogen effects, decreased hepatic blood used in the ICU setting to prevent
flow (cimetidine), weak enzyme inhibitory effect (Ranitidine) gastric erosion and hemorrhage ;
usual half-life: 1-3h
Injection site reaction, paresthesia, dizziness, warm/hot sensation, all are per orem only except for
chest pain, coronary vasospasm Sumatriptan which can also be
given intranasally, transdermal and
IV ; All has 2-27hrs DOA exc for
sumatriptan DOA: 2-4h
Constipation, headache, malaise Dolasetron can increase QRS and
QT (proarrhythmic effect) duration
so never use in patients with heart
disease
gangrene (secondary to ischemia) in overdose, unusual can cause epinephrine reversal due
hyperplasia of the retroperitoneal, retropleural or subendocardial to partial agonist effect on alpha
cavity --> hydronephrosis, cardiac valvular and conduction system receptors (REMEMBER: All partial
malfunction agonist will act as antagonist in the
present of a full agonist)
marked uterine contraction, GI upset (nausea, vomiting, diarrhea) uterus becomes more sensitive to
ergots during pregnancy, produce
very powerful and long-lasting
contraction leading to decreased
bleeding, Never give before delivery
of placenta
Page 12 of 87
The Eicosanoids: Prostaglandins, Thromoboxanes, Leukotrienes and related compounds
A. Prostaglandin E1 analog
i. Misoprostol, Gemeprost PGE1 analogue, activated EP receptor, causes
increased HCO3 and mucus secretion in stomach and
uterine contraction; For prevention of ulcer in
patients who take high doses of NSAIDs due to
arthritis, abortifacient
ii. Alprostadil PGE1 analogue, causes vascular smooth muscle
relaxation and vasolidation; For Maintenance of
patent ductus arteriosus (PDA), Erectile dysfunction
B. Prostaglandin E2 analog
i. Dinoprostone, Sulprostone Low concentrations contract, higher concentrations
relax uterine and cervical smooth muscle, soften
cervix at term before induction with oxytocin; For
cervical ripening, induction of labor, abortifacient
C. Prostaglandin F2a analog
i. Latanoprost, Arboprost, Bimatoprost, Travoprost, PGF2a analogue, increases outflow of aqueous humor
Unoprostone thus reduces intraocular pressure; For glaucoma
D. Prostaglandin I2 analog
i. Epoprostenol, Beraprost, Iloprost, Treprostinil PGI2 analogue, activates IP receptor, causes
vasolidation and reduces platelet aggregation; For
severe pulmonary Hypertension and reducing platelet
aggregation in dialysis machines
E. Leukotriene antagonists
i. Lipoxygenase inhibitor: Zileuton see entry on Drugs used for Asthma
Abdominal pain, Uterine cramping, teratogen, miscarriage
Apnea, hypotension, priapism, lightheadedness, arrhythmia
Cramping, Fetal trauma
vomiting, diarrhea, transient bronchoconstriction
Hypotension, headache, flusing
Misoprostol's intended use is for
NSAID-induced gastritis, may also
be used together with Mifepristone
or Methotrexate as safe
abortifacient
given as injection into the
cavernosa for erectile dysfunction
approved abortifacient in the 2nd
trimester, although effective in
inducing labor, it produces more SE
than other oxytocics
Latanoprost may cause changes in
the color of the iris and may
lengthen eyelashes
used primarily for pulmonary
hypertension (esp Treprostinil IV)

ii. LT receptor blocker: Montelukast, Zafirlukast see entry on Drugs used for Asthma

F. Corticosteroids see entry on Drugs used for Asthma

G. Non-steroidal anti-inflammatory drugs see entry on Analgesics

Page 13 of 87
Drugs used in Asthma
A. Beta2-selective agonist (short-acting)
i. Albuterol/Salbutamol, Levalbuterol, Terbutaline,
Metaproterenol, Pirbuterol, Procaterol, Fenoterol
B. Beta2-selective agonist (long acting)
ii. Salmeterol, Formoterol, Cleneterol, Bambuterol
C. Muscarinic receptor agonist
i. Ipratropium, Tiotropium
C. Methylxanthine
i. Theophylline, Aminophylline, Pentoxifylline
D. Mast cell Stabilizer
i. Cromolyn, Nedocromil, Lodoxamide
Activates beta2-receptors in bronchial smooth muscle
leading to bronchodilation ; DOC for acute asthma
attacks
Activates beta2-receptors in bronchial smooth muscle
leading to bronchodilation, potentiates corticosteroid
action; For Asthma prophylaxis
Blocks muscarinic receptors in bronchial smooth
muscle and prevent bronchoconstriction mediated by
vagal discharge; For acute BA attack and COPD
Phosphodiesterase inhibitor, Adenosine receptor
antagonist, causes bronchodilation and increased
strength of contraction of diaphragm; For asthma
especially in nocturnal attacks, Intermittent
claudication (pentoxifylline), very useful in COPD
Prevents calcium influx and stabilizes mast cells,
preventing degranulation and release of histamine,
leukotrienes and mediators; for Asthma prophylaxis
and allergies (oral, nasal and ophthalmic drops)
Tachycardia, Nervousness, tremors, restlessness, arrhythmias Increase toxicity when used for
when used excessively, loss of responsiveness (tolerance, COPD (May precipitate arrythmias)
tachyphylaxis) and in patients with heart disease;
usual DOA: 2-4hrs, all are given
inhalational, Salbutamol and
terbutaline is also available PO,
terbutaline can also be given IV
Tachycardia, Nervousness, tremors, restlessness, arrhythmia Increase asthma mortality when
when used excessively, loss of responsiveness (tolerance, used alone; May precipitate
tachyphylaxis) arrhythmias; usual DOA: 12hrs
anti-muscarinic effects (dry mouth, blurred vision etc.) More effective and less toxic than
beta agonists for COPD, Tiotropium
has longer DOA than Ipratropium,
Ipratropium given as aerosol has
little systemic effects, has no effect
on the chronic inflammation aspect
of BA
CNS stimulation (Insomnia, seizure, Anorexia), Cardiac stimulation Antidote in overdosage is BB.
(Arrhythmias), Tremors, increased BP, diuresis, inc GI motility Higher clearance in adolescents and
smokers. Narrow therapeutic
window; usual DOA: 12hrs
Cough, Airway irritation No bronchodilator action but can
prevent bronchoconstriction caused
by antigens (both in the early and
late BA responses), unusually
insoluble chemicals so rarely used
Page 14 of 87
E. Corticosteroid
i. Fluticasone, Beclomethasone, Budesonide, Flunisolide,
Mometasone, Triamcinolone, Ciclosenide
F. Leukotriene synthesis inhibitor
i. Zileuton
G. Leukotriene Antagonist
i. Montelukast, Zafirlukast, Pranlukast
H. Anti-IgE antibody
i. Omalizumab
4. DRUGS THAT ACT ON THE CENTRAL NERVOUS SYSTEM
Sedative-Hypnotics
A. Short-acting benzodiazepines
i. Midazolam, brotizolam, triazolam, oxazepam, etizolam
Inhibit synthesis of arachidonic acid by inhibiting
Phospholipase A2, Reduces expression of COX and LT,
inc responsiveness of Beta receptors in the airway,
bind to intracellular receptors and activate
Glucocorticoid response elements in the nucleus
leading to synthesis of substances that prevent full
expression of inflammation and allergy ; DOC for
Asthma prophylaxis, First line treatment for
moderate to severe BA, COPD, Allergic rhinitis, also
used as anti-inflammatory for other conditions such
as auto-immune diseases and cancer, also for immune
suppression
Inhibitor of 5-lipoxygenase. Reduces synthesis of
leukotrienes. Prevents airway inflammation and
bronchoconstriction; For asthma prophylaxis
Blocks leukotriene-1 receptor, prevents airway
inflammation and bronchoconstriction; For asthma
prophylaxis
Binds IgE antibodies on sensitized mast cells and
prevents activation by BA triggers and subsequent
release of inflammatory mediators; For prophylaxis of
severe, refractory asthma not responsive to all other
drugs
bind GABA-A receptor subunits to increase frequency
of chloride channel opening which causes membrane
hyperpolarization ; For acute anxiety, panic attacks,
anesthesia induction and preoperative sedation (esp
Midazolam), insomnia (Triazolam)
Oropharyngeal candidiasis, mild growth retardation observed in For status asthmaticus: use IV
children, Minimal systemic steroid steroid toxicity (eg, adrenal prednisolone or hydrocortisone ;
suppression), Mild growth retardation prednisolone is the active
metabolite of prednisone
Flulike syndrome, headache, drowsiness, dyspepsia, hepatitis, No bronchodilator action, not
elevation of liver enzymes (more than LT receptor blockers) recommended for acute BA attack
Gastrointestinal upset, Insomnia, elevation of liver enzymes No bronchodilator action, not
recommended for acute BA attack
Long term toxicity not yet well documented humanized murine monoclonal
antibody, very expensive and only
administered IV
additive CNS depression if used
with ethanol, antihistamines,
antipsychotics, opioids and TCAs,
causes anterograde amnesia, decreased psychomotor skills, decreased REM sleep, use lower
unwanted daytime sedation, tolerance, dependence liability and doses in the elderly when used for
rebound insomnia or anxiety. insomnia
Page 15 of 87
B. Intermediate-acting benzodiazepines
i. Lorazepam, Alprazolam, Estazolam, Clonazepam,
Lormetazepam, Nitrazepam, Temazepam
C. Long-acting Benzodiazepine
i. Diazepam, chlorazepate, chlordiazepoxide, flurazepam,
quazepam, flunitrazepam
D. Benzodiazepine antagonist
i. Flumazenil
E. Ultrashort-acting barbiturates
i. Thiopental, Methohexital, Thiamylal
F. Short and intermediate-acting barbiturates
bind GABA-A receptor subunits to increase frequency
of chloride channel opening which causes membrane
hyperpolarization; For anxiety disorders even panic
disorders (Alprazolam and Clonazepam), insomnia
(Estazolam), skeletal muscle relaxation, seizure
disorders (Clonazepam), status epilepticus
(Lorazepam), tranquilizers, Bipolar disorder
(Clonazepam), infantile spasm (Clonazepam)
bind GABA-A receptor subunits to increase frequency
of chloride channel opening which causes membrane
hyperpolarization; For anxiety disorders, insomnia
(Flurazepam), skeletal muscle relaxation (e.g. cerebral
palsy - Diazepam), seizure disorders, tranquilizers, for
status epilepticus (Diazepam), anesthesia (Diazepam),
alcohol withdrawal (Diazepam and Chlordiazepoxide)
antagonist at benzodiazepine sites on GABA-A
receptor ; for benzodiazepine overdose.
bind to GABA-A receptor sites (distinct from
benzodiazepines) to increase duration of chloride
channel opening, block glutamic acid
neurotransmission, at high doses can block NA
channels ; For anesthesia induction (esp Thiopental)
additive CNS depression if used
with ethanol etc, decreased REM
sleep, High dose BZD and Barbs may
suppress seizure but at the
expenses of marked sedation
EXCEPT Clonazepam and
Phenobarbital, Lorazepam is
preferred over Diazepam in Status
Epilepticus due to its long
causes anterograde amnesia, decreased psychomotor skills, distribution halflife, use lower doses
unwanted daytime sedation, tolerance, dependence liability and in the elderly when used for
unwanted daytime sedation. insomnia
additive CNS depression if used
with ethanol etc., decreased REM
causes anterograde amnesia, decreased psychomotor skills (esp sleep, Flunitrazepam is used as a
Diazepam and Flurazepam), unwanted daytime sedation, date-rape drug, use lower doses in
tolerance, dependence liability and rebound insomnia or anxiety. the elderly when used for insomnia
Seizures and arrhythmias may occur
when administered in patients who
agitation, confusion, and precipitates benzodiazepine withdrawal took both TCAs and
syndrome for those with benzodiazepine dependence. benzodiazepines
additive CNS depression if used
with ethanol etc., CYP450 inducer,
dependence liability is greater than benzodiazepine, acute Thiopental has highest lipid
intermittent porphyria. solubility
Page 16 of 87

i. Pentobarbital, secobarbital, amobarbital, butalbital,
butabarbital, talbutal, aprobarbital
G. Long-acting barbiturate
i. Phenobarbital, mephobarbital, primidone
H. Imidazopyridine sedative-hypnotics
i. Zolpidem, Zaleplon, Eszopiclone
I. Atypical Sedative-Hypnotics
i. Partial Serotonin Agonist: Buspirone
bind to GABA-A receptor sites (distinct from
benzodiazepines) to increase duration of chloride
channel opening, block glutamic acid
neurotransmission, at high doses can block Na
channels ; For insomnia and preoperative sedation
(Secobarbital), for status epilepticus (Phenobarbital)
bind to GABA-A receptor sites (distinct from
benzodiazepines) to increase duration of chloride
channel opening, block glutamic acid
neurotransmission, at high doses can block Na
channels ; For insomnia, seizure disorders
(Phenobarbital), status epilepticus (Phenobarbital)
bind selectively to a subgroup of GABA-A receptors,
acting like benzodiazepines to enhance membrane
hyperpolarization, only interact with GABA-A
receptors with alpha-1 subunit ; For insomnia and
sleep disorder esp. when sleep onset is delayed
partial agonist at 5-HT1A receptors and possibly D2
receptors, precise MOA of anxiolytic effect is unkown
; For generalized anxiety disorders
dependence liability is greater than benzodiazepine, acute additive CNS depression if used
intermittent porphyria. with ethanol etc., CYP450 inducer
additive CNS depression if used
with ethanol, CYP450 inducer,
Phenobarbital may be excreted
unchanged in the urine, High dose
BZD and Barbs may suppress
dependence liability is greater than benzodiazepine, acute seizure but at the expenses of
intermittent porphyria, severe respiratory and cardiovascular marked sedation EXCEPT
depression Clonazepam and Phenobarbital
lack anti-convulsant, anti-anxiety
and muscle relaxant effects, effects
are reversed with Flumazenil, very
rapid onset of action, may dec. REM
sleep, rebound inc on withdrawal
from chronic use, increasing use
due to rapid onset with minimal
day-after psychomotor depression, few amnestic effects; effects on the sleep pattern and
tolerance, dependence liability and withdrawal symptoms is less cause less daytime cognitive
than that of benzodiazepines impairment as compared to BZD
minimal abuse liability, minimal CNS
depressant effects, tolerance and
withdrawal ; no anticonvulsant or
muscle relaxant property ; slow
non-specific chest pain, tachycardia, palpitations, dizziness, onset of action (>1week),
nervousness, tinnitus, GI distress, paresthesias, dose-dependent metabolized by CYP3A4, safe for
pupillary constriction pregnant patients
Page 17 of 87

ii. Melatonin receptor agonist: Ramelteon
Antiseizure Drugs
i. Phenytoin, Fosyphenytoin, Mephenytoin, Ethotoin
ii. Carbamazepine, Oxcarbazepine
iii. Valproic acid
iv. Phenobarbital
v. Ethosuximide, Phensuximide, Methsuximide
activates melatonin receptors (MT1 and MT2
receptors) in the suprachiasmatic nuclei in the CNS -->
decreased latency of sleep onset
block voltage-gated Na channel ; DOC for generalized
tonic-clonic seizures, DOC for partial seizures, status
epilepticus, arrhythmias, migraine
block voltage-gated Na channels and decreases
glutamate release ; DOC for trigeminal neuralgia, DOC
for generalized tonic-clonic seizures, DOC for partial
seizures, for bipolar disorders
blocks high-frequency firing of neurons which
modifies amino acid metabolism ; DOC for bipolar
disorder (acute mania), DOC for generalized tonic-
clonic seizures and absence seizure, partial seizures,
myoclonic seizures, also used for Bipolar disorders
see notes above ; For status epilepticus in children
inhibit low threshold (T-type) Ca currents esp in
thalamic neurons ; DOC for absence seizure
minimal rebound insomnia or
withdrawal symptoms, minimal
abuse liability, metabolized by
CYP450 (increased levels in the
presence of CYP1A2 or CYP2D6
Dizziness, fatigue, decreased testosterone, increased prolactin inhibitors
CYP450 inducer , metabolism is
non-linear (elimination shift from
1st order to zero order at moderate
to high dose levels) , Fosphenytion
is a water-soluble prodrug of
phenytoin ; phenytoin is preferred
nystagmus, diplopia, sedation, gingival hyperplasia, hirsutism, in prolonged therapy for status
anemias, peripheral neuropathy (absent DTRs), osteoporosis, fetal epilepticus because it is less
hydantoin syndrome, abnormalities in Vit D metabolism sedating.
CYP450 inducer, Oxcarbazepine has
less drug interactions, metabolism
may be inhibited by other drugs
diplopia, cognitive dysfunction, drowsiness, ataxia, blood such as Propoxyphene and valproic
dyscrasias, Stevens-Johnson syndrome, erythematous rash, acid ; may be used for acute manic
teratogen (spina bifida and craniofacial anomalies), hyponatremia phase and as prophylaxis in the
(Oxcarbazepine) depressive phase
CYP450 inhibitor ; also have the
same effect on Ca currents like
Ethosuximide ; Other MOA include
enhancing K channel permeability ;
BZDs are commonly required at
drowsiness, nausea, tremor, alopecia, weight gain, hepatotoxicity initiation therapy of valproic acid ;
(esp in infants), neural tube defects DOC for acute manic illness
May also act on Na channels and as
antagonist at some glutamate
receptors ; primary anticonvulsant
in infants, children and pregnant
cognitive dysfunction, dependence patients
GI distress, lethargy, headache and behavioural changes. Long half-life
Page 18 of 87
 vi. Diazepam see entry on Sedative-Hypnotics
blocks Ca++ channels, increases GABA release ; For
neuropathic pain such as postherpetic neuralgia,
vii. Gabapentin, Pregabalin partial seizures, migraine
blocks Na and Ca++ channels and decreases glutamate
, Zonisamide only blocks Na channels ; For generalized
tonic-clonic seizures, DOC for partial seizures,
myoclonic seizures, absence seizures, bipolar
viii. Lamotrigine, Zonisamide disorder.
Bind synaptic protein selectively inhibiting
hypersynchronization of epileptiform burst firing ; For
ix. Levetiracetam generalized tonic-clonic seizures, partial seizures
multiple actions on synaptic function, probably via
actions on phosphorylation (Na, Ca, GABA, AMPA-
glutamate, carbonic anhydrase), Felbamate also
facilitate the inhibitory actions of GABA but its exact
MOA is still unknown ; For generalized tonic-clonic
seizures, partial seizures, absence seizures, migraine ;
x. Topiramate, Felbamate Felbamate is only for severe refractory seizure states
Irreversibly inactivates GABA aminotransaminase
(GABA-T) which terminates the action of GABA ; For
xi. Vigabatrin GTC seizure
Inhibits GABA transporter (GAT-1) in neurons and glia
thus inhibiting its reuptake, leading to prolongation of
xii. Tiagabine GABA effects ; For partial seizures
General Anesthetics
A. Inhalational General Anesthetics
Facilitates GABA-mediated inhibition, block brain
NMDA and Ach-N receptors; used as anesthesia for
i. Nitrous Oxide minor surgery and dental procedures
eliminated in the kidneys in their
unchanged form ; structural
analogues of GABA but does not
activate GABA receptor directly ;
also have the same effect on Ca
dizziness, sedation, ataxia, nystagmus, tremor currents like Ethosuximide
primarily undergoes
glucuronidation reaction ;
Lamotrigine may be used for acute
dizziness, ataxia, nausea, rash, SJS / TEN (lamotrigine), severe skin manic phase and as prophylaxis in
reaction (Zonisamide) the depressive phase
It is not metabolized by CYP450
enzymes, eliminated in the kidneys
dizziness, sedation, weakness, irritability, hallucinations, psychosis in their unchanged form
Antiseizure drugs with the most
number of MOA, undergo both
hepatic and renal metabolism,
Topiramate can also block Na
drowsiness, dizziness, ataxia, psychomotor slowing, memory channels and potentitae action of
impairment, paresthesias, weight loss, acute myopia, glaucoma, GABA and block glutamate
myopia, urolithiasis ; felbamate causes hepatic failure and receptor, Felbamate may also block
hematotoxic (can cause ITP, aplastic anemia) glutamate receptors
visual field defects None
asthenia or weakness, dizzines None
This group in general increase the threshold for firing of CNS
neurons
Lowest Potency (highest MAC) and
least cardiotoxic; additive CNS
depression with many agents
megaloblastic anemia on prolonged exposure; Euphoria (laughing especially opioids and sedative-
gas), bronchodilation hypnotics
Page 19 of 87

Facilitates GABA-mediated inhibition, block brain
ii. Desflurane NMDA and Ach-N receptors ; For general anesthesia
Facilitates GABA-mediated inhibition, block brain
iii. Sevoflurane NMDA and Ach-N receptors; For general anesthesia
Facilitates GABA-mediated inhibition, block brain
iv. Isoflurane NMDA and Ach-N receptors ; For general anesthesia
Facilitates GABA-mediated inhibition, block brain
v. Enflurane NMDA and Ach-N receptors ; For general anesthesia
Facilitates GABA-mediated inhibition, block brain
vi. Halothane NMDA and Ach-N receptors ; For general anesthesia
Facilitates GABA-mediated inhibition, block brain
vii. Methoxyflurane NMDA and Ach-N receptors ; For general anesthesia
B. Intravenous General Anesthetics
i. Barbiturates: Thiopental, Methohexital, Thiamylal see notes above
ii. Benzodiazepine: Midazolam, Brotizolam, Triazolam,
Oxazepam, Etizolam see notes above
Blocks excitation by glutamate at NMDA receptors;
For dissociative anesthesia (analgesia, amnesia and
iii. Phencyclidine derivative: Ketamine catatonia but with retained consciousness)
Modulates GABA-A receptors containing beta3
subunits; For general anesthesia to patients with
iv. Imidazole derivative: Etomidate limited cardiac or respiratory reserve
additive CNS depression with many
agents especially opioids and
sedative-hypnotics ; all inhaled
anesthetcis cause bronchodilation
bronchospasm, peripheral vasodilation except Desflurane
additive CNS depression with many
peripheral vasodilation, renal insufficiency (due to Flourine agents especially opioids and
release), bronchodilation sedative-hypnotics
additive CNS depression with many
catecholamine-induced arrhythmias, peripheral vasodilation, agents especially opioids and
bronchodilation sedative-hypnotics
additive CNS depression with many
spike-and-wave activity in EEG, muscle twitching, breath-holding, agents especially opioids and
myocardial depression, renal insufficiency (due to Flourine sedative-hypnotics ; has pungent
release), dec cardiac output, bronchodilation odor which limits its use
additive CNS depression with many
catecholamine-induced arrhythmias, myocardial depression, post- agents especially opioids and
operative hepatitis, dec cardiac output, bronchodilation sedative-hypnotics
Highest potency and lowest MAC
(very slow onset and recovery);
additive CNS depression with many
agents especially opioids and
renal insufficiency (due to Flourine release), bronchodilation sedative-hypnotics
are respiratory and circulatory depressants --> dec cerebral blood
flow --> dec ICP rapid entry into the brain (<1min)
Midazolam is a usual adjunct with
inhalational anesthetics and IV
opioids, has a slow onset but longer
see notes above DOA
CV stimulation, hypertension, increased ICP, delirium, Dissociative Reduces delirium by pretreatment
anesthesia, post-op effects: disorientation, hallucination, with benzodiazepine, congener of
excitation Phencyclidine / angel dust
pain at injection site, myoclonus, postoperative nausea and Minimal effects on CV and
vomiting, adrenocortical suppression (on prolonged respiratory functions, no analgesic
administration) properties, short DOA
Page 20 of 87

Interacts with mu, sigma, kappa receptors for
v. Opioid analgesics: Fentanyl, morphine, alfentanil, endogenous opioid peptides ; For high risk patients
remifentanil who might not survive general anesthesia
Potentiates GABA-A receptors, blocks Na channels;
For prolonged sedation esp in ICU patients and also in
vi. Propofol, Fospropofol OPD surgeries
Local Anesthetics
A. Ester Local Anesthetics
Blockade of Na channels slows which prevents axon
i. Procaine potential propagation; For local anesthesia
Blockade of Na channels slows which prevents axon
potential propagation; For local anesthesia, topical
ii. Benzocaine anesthesia
Blockade of Na channels slows which prevents axon
potential propagation, with intrinsic
sympathomimetic activity; For local anesthesia,
iii. Cocaine topical anesthesia
Blockade of Na channels slows which prevents axon
potential propagation; For local anesthesia, spinal
anesthesia, epidural anesthesia, topical ophthalmic
iv. Tetracaine anesthesia
B. Amide Local Anesthetics
Antidote is Naloxone / Naltrexone ;
Neuroleptanesthesia (analgesia +
amnesia) happens when Fentanyl,
Droperidol and Nitrous oxide are
given together ; faster recovery
respiratory depression, chest wall rigidity (which may cause with remifentanil ; these drugs have
impaired ventilation) and constipation fast onset of action
"milk of anesthesia", additive
effects with sedative-hypnotic drugs
; as rapid as thiopental and also
with fast recovery ; antiemetic
bradycardia, vasodilation, hypotension, negative inotropism, pain action ; Fospropofol is the water-
at injection site, anterograde amnesia, dystonia, priapism, soluble prodrug form of propofol
paresthesia (Fospropofol) but with slower onset and recovery
this group can cause antibody
formation in some patients
light-headedness, sedation, restlessness, nystagmus, seizures, Shortest half-life among local
respiratory, CV depression anesthetics
light-headedness, sedation, restlessness, nystagmus, seizures, Use cautiously in sunburns, Topical
respiratory, CV depression only
with intrinsic sympathomimetic
activity so it does not need an alpha
agonist (like epinephrine) to limit its
systemic absorption; causes mood
elevation due to action on
light-headedness, sedation, restlessness, nystagmus, seizures, dopamine receptor ; All local
respiratory, CV depression, abuse liability, severe hypertension, anesthetics are vasodilators EXCEPT
cerebral hemorrhage, cardiac arrhythmia, MI cocaine ; Topical only
light-headedness, sedation, restlessness, nystagmus, seizures, also available as Ophthalmic
respiratory, CV depression solution
Page 21 of 87

i. Lidocaine
ii. Prilocaine
iii. Bupivacaine
iv. Ropivacaine
Skeletal Muscle Relaxant
A. Depolarizing Neuromuscular Blocker
i. Succinylcholine
B. Non-Depolarizing Neuromuscular Blocker
i. Mivacurium (short-acting: 10-20mins DOA)
ii. Atracurium (intermediate-acting)
iii. Vecuronium (intermediate-acting)
Blockade of Na channels slows which prevents axon
potential propagation; For local anesthesia,
antiarrhythmia (group 1B activity), used for post-MI
and for digitalis toxicity
Blockade of Na channels slows which prevents axon
potential propagation; For local anesthesia, dental
anesthesia
Blockade of Na channels slows which prevents axon
potential propagation; For local anesthesia, epidural
anesthesia, intrathecal anesthesia
Blockade of Na channels slows which prevents axon
potential propagation; For local anesthesia, epidural
anesthesia
Agonist at Ach-N receptors causing initial twitch then
persistent depolarization ; For skeletal muscle
relaxation during intubation and general anesthesia
Competitive antagonists at skeletal muscle nicotinic
acetylcholine receptors; For skeletal muscle relaxation
during intubation and general anesthesia
Frequently administered with
light-headedness, sedation, restlessness, nystagmus, seizures, Epinephrine to avoid systemic
respiratory, CV depression absorption
light-headedness, sedation, restlessness, nystagmus, seizures, causes methemoglobinemia
respiratory, CV depression (antidote: methylene blue)
Use with caution in pregnant
light-headedness, sedation, restlessness, nystagmus, seizures, women and patients with cardiac
respiratory, CV depression, severe CV toxicity, hypotension and disease (may cause heartblock,
arrhythmias arrhyhtmia and hypotension)
light-headedness, sedation, restlessness, nystagmus, seizures, Longest half-life among local
respiratory, CV depression, cardiotoxicity anesthesia
Metabolized by
muscle pain, hyperkalemia, increased intragastric pressure leading pseudocholinesterase ; may cause
to regurgitation (aspiration), increased intraocular pressure, malignant hyperthermia if given
malignant hyperthermia together with inhaled anesthetics
effects are easily reversed by giving
AChE inhibitors such as
a common SE for this group is Histamine release Neostigmine
Metabolized by
pseudocholinesterase; reverse
respiratory paralysis, apnea, and moderate histamine release effects with Neostigmine
Undergoes Hoffman elimination
(rapid spontaneous breakdown);
reverse effects with Neostigmine ;
respiratory paralysis, apnea, and moderate histamine release and converted to Laudanosine which
bronchospasm can cause seizures
Undergoes elimination in bile;
respiratory paralysis and apnea reverse effects with Neostigmine
Page 22 of 87

iv. Rocuronium (intermediate-acting)
v. Tubocurarine (long-acting)
Competitive antagonists at skeletal muscle nicotinic
acetylcholine receptors; For skeletal muscle relaxation
during intubation and general anesthesia, euthanasia,
vi. Pancuronium (long-acting) lethal injection, strychnine poisoning
Anti-Parkinsonism and other drugs for movement disorders
A. Dopamine Precursor
Levodopa is a dopamine precursor, carbidopa inhibits
peripheral metabolism via dopa decarboxylase; Drug
i. Levodopa-carbidopa of choice for parkinsons disease
B. Dopamine Agonist
Partial agonist at dopamine D2 receptors in brain; For
Parkinsons disease which is levodopa intolerance,
i. Bromocriptine, Pergolide hyperprolactinemia
Partial agonist at dopamine D3 receptors in brain,
ii. Pramipexole, Ropinirole Roprinole is a D2 agonist; For Parkinsons disease
reverse effects with Neostigmine;
Suggamadex is a novel reversal
agent for rocuronium; most rapid
respiratory paralysis and apnea, hypersensitivity onset time (60-120 sec)
Relatively contraindicated in
myocardial ischemia; reverse
respiratory paralysis, apnea, hypotension and recurarization effects with neostigmine
respiratory paralysis, apnea, tachycardia, hypertension, Reverse effects with Neostigmine,
recurarization may cause heart block
Contraindicated in patients with
history of psychosis; hypertensive
crisis occurs when used with MAO
inhibitors, ameliorates signs of
parkinsonism and decreases
GI upset (emesis), dyskinesia (choreoathetosis), behavioural mortality rate ; patient response
changes (anxiety, agitation, confusion, delusion), on-off decreases with time but is improved
phenomena, wearing-off phenomena, postural hypotension, when given together with COMT
tachycardia inhibitors
anorexia, nausea, vomiting, dyskinesia, postural hypotension,
behavioural changes, erythromelalgia (Bromocriptine), pulmonary
infiltrate (Bromocriptine) Ergot alkaloids
Contraindicated for patients with
active peptic ulcer disease,
psychotic illnesss or recent MI ;
decrease dose in renal dysfunction ;
anorexia, nausea, vomiting, dyskinesia, postural hypotension, Neuroprotective ; Ropirinole is
behavioural changes (more prominent compared to levodopa) metabolized by CYP1A2
Page 23 of 87
 Partial agonist at dopamine D3 receptors, antagonist
at 5-HT and alpha adrenoceptors; For off-periods of
Parkinsons disease, alcoholism, opiate addiction,
iii. Apomorphine erectile dysfunction, alzheimers disease
C. MAO type B inhibitor
Selective inhibitors of MAO type B leading to
decreased degradation of dopamine, increases
response to levodopa/carbidopa; Only as adjunct to
levodopa for parkinsons disease but Rasigiline can be
i. Selegiline, Rasagiline given alone (more potent)
D. COMT inhibitor
Block L-dopa metabolism by inhibiting catechol-O-
methyltransferase in periphery and CNS, prolongs
response to levodopa; used in the wearing-off
phenomena of parkinsons disease, as adjuncts to
i. Entacapone, Tolcapone levodopa
E. Antiviral
enhances dopaminergic transmission by unknown
mechanism, maybe by influencing the synthesis,
release or reuptake of dopamine; For Parkinsons
i. Amantadine disease and influenza
F. Anticholinergic
Decrease the excitatory actions of cholinergic neurons
on cells in the striatum by blocking muscarinic
receptors; as adjunct for parkinsons disease and
i. Benztropine, Biperiden, Trihexyphenidyl, Orphenadrine extrapyramidal symptoms caused by antipsychotics
Antipsychotics and Lithium
A. Typical Antipsyhotics may also be used for pruritus and as sedatives
Blocks D2 receptors >> 5-HT2 receptors; For
i. Phenothiazine: Chlorpromazine schizophrenia and other psychotic disorders
Premedicate with
Trimethobenzamide to prevent
severe nausea, dyskinesia, hypotension, drowsiness and sweating severe nausea
serotonin syndrome occurs when
used with SSRI and Meperidine ;
Selegiline is hepatically metabolized
into desmethyl selegiline (which is
insomnia, mood changes, dyskinesias, GI distress and hypotension neuroprotective) and amphetamine
dyskinesias, GI distress, postural hypotension, sleep disturbance, Entacapone only acts in the
orange discoloration of urine, hepatotoxicity (tolcapone only), periphery while Tolcapone acts
neuroleptic malignant syndrome, rhabdomyolysis both in the periphery and CNS.
behavioural changes (restlessness, agitation, insomnia, May improve bradykinesia, rigidity
hallucination, psychosis), livedo reticularis, GI disturbances, and tremor ; has antimuscarinic
urinary retention, postural hypotension, peripheral edema action
Exacerbate tardive dyskinesias that
result from prolonged use of
antipsychotic drugs; improve
drowsiness, inattention, confusion, delusions, hallucinations, tremor and rigidity with little effect
atropine-like effects on bradykinesia
has no effect on negative symptoms
extrapyramidal dysfunction, tardive dyskinesia,
hyperprolactinemia, atropine-like effects, failure of ejaculation,
postural hypotension, marked sedation, corneal and lens deposits, prototype of all typical
neuroleptic malignant syndrome, contact dermatitis antipsychotics
Page 24 of 87

ii. Other Phenothiazines: Thioridazine, Fluphenazine,
Perphenazine, Prochlorperazine, Trifluoperazine
iii. Butyrophenol: Haloperidol, Droperidol
B. Atypical Antipsychotics
i. Clozapine
ii. Olanzapine
Blocks D2 receptors >> 5-HT2 receptors; For
schizophrenia and other psychotic disorders,
antiemesis (prochlorperazine)
Blocks D2 receptors >> 5-HT2 receptors; For
schizophrenia and other psychotic disorders,
huntingtons disease and tourettes syndrome
may be used for mania and psychotic symptoms in
Alzheimer's dementia and Parkinsons disease
Blocks 5-HT2 receptors >> D2 receptors; For
schizophrenia (refractory, suicidal) and other
psychotic disorders
Blocks 5-HT2 receptors >> D2 receptors; For
schizophrenia, bipolar disorders, anorexia nervosa
and depression
Thioridazine has the Strongest
autonomic effects; only
antipsychotic with fatal overdose ;
Fluphenazine and Trifluoperazine
extrapyramidal dysfunction, tardive dyskinesia, have very significant parkinson-like
hyperprolactinemia, atropine-like effects, failure of ejaculation, effect ; Fluphenazine has less
postural hypotension, retinal deposits (thioridazine), sedation compared to other anti-
cardiotoxicity (arrhythmias - thioridazine) psychotics
causes the most extrapyramidal
symptoms of all typical anti-
extrapyramidal dysfunction, tardive dyskinesia, psychotics ; has the weakest
hyperprolactinemia, neuroleptic malignant syndrome autonomic effects
cure both negative and positive
symptoms
Only antipsychotic that reduces the
Extrapyramidal dysfunction (less), hyperprolactinemia (less), risk of suicide ; may be effective for
postural hypotension, weight gain, hyperglycemia, drug-resistant types ; weight gain,
hyperlipidemia, myocarditis, agranulocytosis, seizures, ileus, agranulocytosis, seizure and
hypersalivation (sialorrhea) hyperglycemia is prominent
Extrapyramidal dysfunction (less), hyperprolactinemia (less), weight gain and hyperglycemia is
postural hypotension, weight gain, hyperglycemia, hyperlipidemia prominent, safe in pregnancy

Extrapyramidal dysfunction (less), hyperprolactinemia (less),

Blocks 5-HT2 receptors >> D2 receptors; For
iii. Quetiapine schizophrenia, bipolar disorders (manic)
Blocks 5-HT2 receptors >> D2 receptors; For
schizophrenia, bipolar disorders, depression,
iv. Risperidone intractable hiccups, tourette syndrome
Blocks 5-HT2 receptors >> D2 receptors; For
v. Ziprasidone schizophrenia, bipolar disorders (acute mania)
Blocks 5-HT2 receptors >> D2 receptors; For
schizophrenia, bipolar disorders, depression, autism,
vi. Aripiprazole cocaine dependence
postural hypotension, weight gain, somnolence, fatigue, sleep
paralysis, hypnagogic hallucinations, cataracts, priapism, QT
prolongation (TDP) can cause TDP, safe in pregnancy
Extrapyramidal dysfunction (less), hyperprolactinemia (marked), Only antipsychotic approved for
insomnia, photosensitivity schizophrenia in the youth
Increased mortality in elderly
Extrapyramidal dysfunction (less), postural hypotension, QT patients with dementia-related
prolongation (TDP) psychosis ; can cause TDP
Extrapyramidal dysfunction (less), GI upset, tremor, Least sedating atypical
hypersensitivity (rare) antipsychotics

Page 25 of 87

vii. Lithium (mood stabilizer)
Antidepressants
A. Tricyclic Antidepressants
i. Imipramine, Clomipramine, Desipramine,
Amitryptyline, Nortryptiline
B. SSRI
i. Fluoxetine, Paroxetine, Citalopram, Escitalopram,
Sertraline, Fluvoxamine
Uncertain MOA but the proposed MOA is by inhibiting
the enzyme involved in the recycling of neuronal
membrane phosphoinositides which causes depletion
of phosphatidylinositol bisphosphate, thus
consequently decreasing IP3 and DAG --> decrease in
neurotransmission ; For bipolar disorder, recurrent
depression, schizoaffective disorder
Block NE and 5-HT transporters leading to
potentiation of NT action at postsynaptic receptors;
For MDD (most effective), bipolar disorder, acute
panic attacks, ADHD, chronic pain states, as sleeping
aid, OCD (Clomipramine) ; this group is very useful for
patients with psychomotor retardation, sleep
disturbance, poor appetite and weight loss
Inhibits neuronal reuptake of serotonin by inhibiting
Serotonin Transporter (SERT); DOC for OCD, for MDD,
anxiety, panic attacks, phobias, PTSD, GAD, bulimia,
premenstrual dysphoric disorder, alcohol dependence
Contraindicated in sick sinus
syndrome; treat overdose with
hemodialysis ; high volume of
distribution ; clinical benefit is seen
only after weeks of use ;
antipsychotic agents or BZDs are
Tremor, sedation, ataxia, aphasia, thyroid enlargement, commonly required at initiation
hypothyroidism, reversible nephrogenic diabetes insipidus, therapy of Li and valproic acid ;
edema, acneiform skin eruption, leukocytosis, teratogen Contraindicated in lactation ;
(ebsteins anomaly), bradycardia, some drugs (NSAIDs, ACEi, Natriuresis stimulates reflex
diuretis etc) can increase Lithium toxicity while caffeine and increase in the reabsorption of Li
theophylline can decrease its toxicity and Na in the PCT
Additive depression of the CNS with
other central depressants ;
Imipramine is metabolized to
desipramine while amitriptyline is
metabolized to nortriptyline ;
longterm use may lead to down-
regulation of Beta receptors leading
to a decrease in BP and depression
of cardiac conduction ; has
significant muscarinic receptor
excessive sedation, fatigue, confusion, sympathomimetic effects, blocking effect esp Amitriptyline ;
atropine-like effects, orthostatic hypotension, cardiomyopathies, lower seizure threshold ; may
arrhythmias, tremors, paresthesias, weight gain ; 3Cs of overdose: interfere with antihypertensive
Coma, Cardiotoxicity, Convulsions action of Clonidine
Serotonin syndrome when used
with MAOIs ; minimal inhibitory
effect on cholinergic or adrenergic
receptors ; lower seizure threshold ;
this group can decrease appetite
leading to weight loss ; Increased
risk for suicide in children and
nausea, vomiting, headache, anxiety, agitation, drowsiness, adolescents ; Fluoxetine,
insomnia, erectile dysfunction, EPS, QT prolongation (citalopram), Fluvoxamine and Paroxetine are
withdrawal syndrome CYP450 inhibitors
Page 26 of 87
C. SNRI
Inhibits neuronal reuptake of serotonin and
norepinephrine by binding to transporters for both
5HT and NE; For MDD, fibromyalgia, neuropathic pain,
i. Venlafaxine, Duloxetine, Desvenlafaxine menopausal symptoms
D. Serotonin antagonist
Blocks 5-HT2A receptors, weak inhibitor of NE and
5HT transporters; For MDD, as sleeping aid
i. Trazodone, Nefazodone (trazodone)
E. Tetracyclics
Strong norepinephrine reuptake inhibitor and weak
serotonin reuptake inhibitor, blocks dopamine D2
i. Amoxapine receptors; For MDD
Increases amine release from nerve endings by
antagonism of presynaptic a2 adrenoceptors, also
blocks serotonin 5-HT2A receptors; For MDD, appetite
ii. Mirtazapine stimulation, as sleeping aid
Inhibits neuronal reuptake of dopamine and
norepinephrine, increase dopamine and
norepinephrine activity; For MDD and smoking
iii. Bupropion cessation, alcohol dependence
F. MAO Inhibitors
venlafaxine has less affinity for NE
transporter than desvenlafaxine
dizziness, insomnia, sedation, GI distress, hypertension and duloxetine ; differ from TCA in
(venlafaxine), hepatotoxicity (duloxetine), withdrawal syndrome lacking blockade of H1, M and alpha
even in just one missed dose, CNS stimulation (Venlafaxine), liver receptors ; Increased risk for suicide
dysfunction (Duloxetine) in children and adolescents
May cause arrhythmias in px with
pre-existing cardiac disease ; short
t1/2 so given BID to TID, has
significant muscarinic receptor
blocking effect esp Nefazodone ;
CYP450 inhibitors ; Trazodone also
sedation, GI disturbance, orthostatic hypotension, priapism, has significant alpha1 and H1
hyperprolactinemia, liver dysfunction (nefazodone) blocking effect
Increased risk for suicide in children
and adolescents
Lowers seizure threshold, has
autonomic effects, akathisia, parkinsonism (due to dopamine significant muscarinic receptor
receptor blockade), seizures, cardiotoxicity blocking effect
weight gain, marked sedation, dizziness, blurred vision and has significant muscarinic receptor
nightmares and alpha2 blocking effect
Lowers seizure threshold, for
smoking cessation ; no effect on
weight loss, agitation, anxiety, dizziness, dry mouth, aggravation 5HT or NE receptors or amine
of psychosis, seizures, priapism transporters ; CYP450 inhibitor
Page 27 of 87

Inhibits MAO type A and type B, increases CNS levels
of NE and serotonin, Phenelzine and Tranylcypromine
are nonselective MAO inhibitors while Selegiline is a
MAO-B selective inhibitor; For MDD unresponsive to
other agents ; useful in patients with significant
i. Phenelzine, tranylcypromine, selegiline anxiety, phobic features and hypochondriasis
Opioid Analgesics and Antagonists
A. Full Agonist
Strong agonist at u receptors; For severe pain, pain
i. Morphine associated with acute MI, for pulmonary edema
Strong agonist at u receptors; For severe pain, adjunct
in anesthesia, chronic pain and breakthrough cancer
ii. Fentanyl pain
Strong agonist at u and k receptors, inhibits pain
neurotransmission, muscarinic blocking actions; For
moderate to severe pain, labor analgesia, spasmodic
iii. Meperidine pain (biliary, renal), preoperative sedation
Strong agonist at u receptors, inhibits pain
neurotransmission, binds NMDA receptors and
antagonizes the effects of glutamate; For moderate to
iv. Methadone severe pain, opioid dependence, opioid withdrawal
B. Partial Agonist / Moderate Agonist
Hypertensive crisis when taken with
tyramine-rich food, serotonin
syndrome when taken with SSRI ;
this group is structurally related to
amphetamine ; CYP450 inhibitors ;
longterm use may lead to down-
regulation of Beta receptors
(leading to decrase in BP) ; lower
dizziness, insomnia, orthostatic hypotension, blurred vision, seizure threshold ; selegiline may be
arrhythmia, diarrhea, hyperthermia, CNS stimulation, seizure given as skin patch
Additive CNS depression with other
TRIAD: miosis, coma, respiratory depression depressants
Exerts hemodynamic effects on the
pulmonary circulation ; significant
first-pass effect ; metabolized in the
miosis, restlessness, respiratory depression, increased ICP, body to morphine-6-glucuronide
postural hypotension, urinary retention, pruritus, addiction which has equal analgesic activity as
liability morphine
May be given transdermally or via
restlessness, respiratory depression, increased ICP, postural lollipop; ohmefentanyl is the most
hypotension, urinary retention, pruritus, addiction liability potent opioid
Only opioid that does not cause
miosis and biliary contraction ;
opioid of choice for pain relief in
pancreatitis ; metabolized to
normeperidine which can cause
seizure therefore contraindicated in
patients with seizure disorder ; if
restlessness, respiratory depression, increased ICP, postural given with MAOi --> Hyperpyrexic
hypotension, urinary retention, pruritus, addiction liability, coma, if given with SSRI -->
seizures Serotonin syndrome
Used in methadone maintenance
therapy (MMT) for opioid
miosis, restlessness, respiratory depression, increased ICP, dependence; currently being
postural hypotension, urinary retention, pruritus, addiction investigated as a novel treatment
liability for leukemia
Page 28 of 87
 Strong agonist at u receptors, inhibits pain
neurotransmission, binds NMDA receptors and
antagonises the effects of glutamate; For moderate to
i. Hydrocodone, oxycodone severe pain, opioid dependence, opioid withdrawal
Decreases sensitivity of cough receptors, depressing
the medullary cough center through sigma receptors
ii. Dextrometorphan, codeine stimulation; For cough suppression
C. Weak Agonist
Weak agonist at u receptors, inhibits pain
i. Propoxyphene, levopropoxyphene, neurotransmission; For mild to moderate pain,
dextropropoxyphene restless leg syndrome
D. Mixed Agonist-Antagonist
Strong agonist at k receptors, weak antagonist activity
at u receptors; For moderate to severe pain, opioid
dependence, alcohol dependence, balance
anesthesia, for opioid withdrawal states
i. Nalbuphine, buprenorphine, butorphanol, pentazocine (buprenorphine)
E. Opioid Antagonist
Competitively blocks u, sigma and k receptors, rapidly
reverses effects of opioid agonists; For opioid
overdose, opioid and alcohol dependence
i. Naloxone, naltrexone, nalmefene (naltrexone)
F. Dual-acting
Weak agonist at u receptors, inhibits neuronal
reuptake of serotonin and norepinephrine; For
moderate pain, chronic pain syndrome, neuropathic
i. Tramadol pain
5. DRUGS USED TO TREAT DISEASES OF THE BLOOD, INFLAMMATION, & GOUT
Agents Used in Anemias and Hematopoietic Growth Factors
A. Hematopoietic growth factor
Required for the biosynthesis of heme and heme
i. Ferrous sulfate, Ferrous gluconate, Ferrous Fumarate, containing proteins, including hemoglobin and
Iron dextran, Sodium Ferric Gluconate complex, Iron myoglobin; For Iron deficiency anmia, iron
sucrose supplementation
miosis, restlessness, respiratory depression, increased ICP, there is genetic variation in the
postural hypotension, urinary retention, pruritus, addiction metabolism of codeine and its
liability derivatives
hallucination, confusion, excitation, increased or decreased pupil
size, nystagmus, seizures, coma, respiratory depression, addiction codeine is metabolized by CYP2D6
liability to morphine
miosis, respiratory depression, increased ICP, postural
hypotension, urinary retention, pruritus, addiction liability, fatal Withdrawn because of fatal
arrythmias cardiotoxicity
Buprenorphine reduces craving in
sedation, dizziness, sweating, nausea, anxiety, hallucinations, alcohol dependence,
nightmares, respiratory depression (less), tolerance, dependence buprenorphine and nalbuphine is
liability resistant to Naloxone
Precipitates abstinence syndrome in
Px with opioid dependence ;
Naloxone and Nalmefene is IV
(DOA: 12-24 hrs) while Naltrexone
pruritus, nausea, vomiting is PO (DOA: 48h)
Lower seizure threshold ; CI in Px
taking SSRI and those with history
seizures, nausea, dizziness, pruritus, constipation of seizure
Black stools, shock, lethargy, dyspnea, abdominal pain, necrotizing
gastroenteritis, death, organ failure, hemochromatosis, metabolic
acidosis None
Page 29 of 87
B. Heavy metal chelator
Chelates excess iron; For acute and chronic iron Hypotension, Neurotoxicity, ARDS, Increased susceptibility to
i. Deferoxamine, Deferasirox poisoning infections None
C. Hematopoietic growth factor
Cofactor required for essential enzymatic reactions
that form tetrahydrofolate, convert homocysteine to Hydroxocobalamin has a longer t1/2
methionine and metabolize methylmalonyl-CoA; For than cyanocobalamin ; has a
i. Cyanocobalamin, Hydroxocobalamin vitamin B12 deficiency, megaloblastic anemia No significant toxicity storage of up to 5yrs in the liver
D. Hematopoietic growth factor
Precursor of an essential donor of methyl groups used
for synthesis of amino acids, purines and
deoxynucleotide; For Megaloblastic anemia,
prevention of neutral tube defects (spina bifida), only modest amounts are stored in
i. Folic acid, Folacin (Pteroylglutamic acid), Folinic acid prevention of coronary artery disease No significant toxicity the body
E. Hematopoietic growth factor
Performance-enhancing drug in
athletes ; darbepoietin is once a
week administration, while
Agonist of erythropoietin receptors expressed by red Methoxy Polyethylene Glycol-
i. Epoetin Alfa, Darbepoetin alfa, Methoxy Polyethylene cell progenitors; For Anemia, associated with chronic Epoetin Beta is 1-2x per month
Glycol- Epoetin Beta renal failure, cancer, HIV infection and prematurity Hypertension, Thrombosis, Pure red cell aplasia administration
F. Myeloid growth factor
Binds receptors on myeloid progenitors and
stimulates cell maturation and proliferation ;
Accelerates neutrophil recovery and reduces
incidence of infection; For neutropenia associated
i. (G-CSF) Filgrastim, Sargamostim (GM-CSF), with chemotherapy, myelodysplasia, and aplastic
Pegfilgrastim anemia Edema, Fever, Arthralgia Pegfilgrastim has longer t1/2
G. Megakaryocyte growth factor
Recombinant form of an endogenous cytokine;
activates IL -11 receptors ; For secondary prevention
of thrombocytopenia in patients undergoing fatigue, headache, anemia, fluid accumulation in the lungs,
i. Oprelvekin(IL-11), Thrombopoietin chemotheraphy dizziness, transient atrialarrythmias given SC OD

Page 30 of 87
Agents Used in Dyslipidemia

has direct anti-atherosclerotic

A. HMG-CoA Reductase Inhibitors: Simvastatin,
Atorvastatin, Rosuvastatin, Fluvastatin, Pravastatin,
Lovastatin, Pitavastatin, Cerivastatin,
B. Bile Acid Binding Resin: Colesevelam, Colestipol,
Cholestyramine
C. NPC1L1 transporter inhibitor: Ezetimibe
D. Sterol absorption blocker: Sitosterol
Inhibits rate-limiting enzyme in cholesterol
biosynthesis (HMG-CoA reductase), Increased hepatic
cholesterol uptake, Increased high affinity LDL
receptors which leads to decreased LDL levels ; DOC
for hypercholesterolemia (high LDL), decreases risk of
acute coronary syndromes, ischemic stroke
non-absorbable polymers that bind bile acids and
similar steroids in the intestines preventing their
reabsorption, increases cholesterol utilization for
replacement, modestly lowers LDL levels by increasing
hepatic LDL receptors ; For hypercholesterolemia
(high LDL), pruritus in cholestasis, digitalis toxicity
Selective inhibitor of the NPC1L1 transporter
decreasing intestinal absorption of cholesterol and
other phytosterols, decreases cholesterol hepatic
pool, increases hepatic LDL receptors ; For
Hypercholesterolemia (High LDL), phytosterolemia
Cholesterol analog, takes the place of dietary and
billiary cholesterol, decreasing intestinal absorption of
cholesterol and other phytosterols ; For
Hypercholesterolemia (high LDL), phytosterolemia
Hepatoxicity, Myopathy, Rhabdomyolysis, Gastrointestinal
distress, Teratogen
Constipation, Bloating, Gritty taste, Gallstone formation,
steatorrhea, malabsortion of fat soluble substances (vitamin k,
folate)
Hepatoxicity (increased with statin use), Myositis
Gastrointestinal upset, bloating, impotence (rare), coronary
events
effect, and can prevent bone loss ;
Increased risk of myopathy and
rhabdomyolysis when used with
fibrates ; Given before bedtime
because cholesterol synthesis
predominantly occurs at night ;
simvastatin and lovastatin are
prodrugs, all the rest are in their
active form already ; Rosuvastatin,
Atorvastatin and Simvastatin have
greater maximal effect than other
statins ; if given together with resins
give at least 1hr before or 4hrs after
resin administration (resins
decrease the absorption of statins) ;
has CYP450 dependent metabolism
Increases TGs and VLDL in patients
with high TGs and combined
hyperlipidemia ; Treat constipation
with fiber supplements/psyllium ;
Avoid in patients with diverticulitis
Synergistic LDL-lowering effect with
statins ; is a prodrug
NONE

Page 31 of 87

E. Nicotinic Acid derivatives: Niacin
F. Fibrates: Gemfibrozil, Fenofibrate, Bezafibrate
Drugs for Coagulation
A. Antiplatelet
i. Aspirin
ii. GPIIb-IIIa inhibitor: Abciximab, Eptifibatide,Tirofiban
iii. PDE III inhibitor: Dipyridamole, Cilostazol
Decreases VLDL synthesis and LDL cholesterol
concentrations, decreases hormone-sensitive lipase
activity leading to decreased LDL levels, Increases HDL
cholesterol by decreasing its catabolism ; DOC for
increasing HDL levels, for Hypercholesterolemia (low
HDL, high LDL/VLDL), hypertriglyceridemia
Activates PPAR- and increases expression of
lipoprotein lipase and apolipoproteins (apoA-I, apoA-
II) leading to enhanced clearance of TG-rich
lipoproteins, Lowers triglycerides, Increases HDL ;
DOC for hypertriglyceridemia
For arterial thrombosis only
Nonselective, irreversible COX 1&2 inhibitor. Reduces
platelet production of thromboxane A2, temporarily
inhibit Prostacyclin synthesis ; For prevention or
arterial thrombosis (MI, TIA, CVD), Inflammatory
disorders (rheumatic fever, juvenile rheumatoid
arthritis, kawasaki disease)
Reversbily inhibits the binding of fibrin and other
ligands to the platelet GPIIb-IIIa receptor ; For
antithrombosis during PCI, Acute coronary syndromes
(unstable angina, NSTEMI)
Inhibits phosphodiesterase III and increases cAMP in
platelets and blood vessels, Inhibits platelet
aggregation and causes vasolidation ; For prevention
of thromboembolic complications of cardiac valve
replacement (as adjunct to warfarin), secondary
prevention of ischemic stroke (with aspirin),
Intermittent claudication (Cilostazol only)
decreases fibrinogen and increases
t-PA ; NSAIDs pre-treatment
reduces flushing ; Avoid in patients
with peptic ulcer disease ;
Flushing, nausea, vomiting, Pruritus, Acanthosis nigricans, Rashes, Potentiates effects of
Gastrointestinal irritation, Hepatoxicity (mild), Hyperuricemia, antihypertensives (vasodilators,
Impaired glucose tolerance, Arrhythmias, Ambylopia ganglion blockers)
Increased risk of myopathy and
rhabdomyolysis when used with
statins ; Avoided in patients with
hepatic or renal dysfunction ; may
increase LDL in patients with
familial combined
hyperlipoproteinemia ; has little or
no effect on LDL ; higher risk of
Nausea, Rashes, Leukopenia, nausea, vomiting, increased risk of gallstone formation if given
cholesterol gallstones together with resins
Uncoupler of oxidative
Gastrointestinal toxicity, nephrotoxicity, tinnitus, phosphorylation, associated with
hyperventilation, hypersensitivity, HAGMA, Increased bleeding Reye syndrome in children ; Do not
time, Nephrotoxicity (AKI and Interstitial Nephritis) use as NSAID for gout
Bleeding, Thrombocytopenia Adjunct to thrombolysis
additional MOA: inhibit uptake of
adenosine by endothelial cells and
RBC, thus increasing adenosine
levels leading to inhibition of
platelet aggregation ; Cilostazol is
Headache, palpitations contraindicated in heart failure
Page 32 of 87

iv. ADP inhibitor: Clopidogrel,Ticlopidine, Prasugel
B. Anticoagulant
i. Heparin (indirect thrombin inhibitor)
ii. LMWH: Enoxaparin, Dalteparin, Tinzaparin,
Fondaparinux
iii. Direct Thrombin Inhibitors: Lepirudin, Desirudin,
Bivalirudin, Argatroban, Dabigatran
iv. Direct Oral Factor Xa inhibitor: Rivaroxaban, Apixaban
v. Warfarin, Dicumarol
C. Antidote
i. Protamine Sulfate
Irreversibly inhibits binding of ADP to platelet
receptors,thus reducing platelet aggregation ; For
prevention and treatment of arterial thrombosis
(stroke, TIA, unstable angina), Acute coronary
syndromes, Prevention of re-stenosis after PCI
For both venous and arterial thrombosis
Activates antithrombin III which Inactivates thrombin
or factor IIa, factor IXa & factor Xa by forming stable
complexes with them ; For deep venous thrombosis,
myocardial dysfunction, Pulmonary embolism,
adjuvant to percutaneous coronary intervention (PCI)
and thrombolytics, Atrial fibrillation, Pulmonary
embolism, given with thrombolytics for
revascularization procedures, given with GPIIb-IIIa
inhibitors for angioplasty and stent placement
Binds and potentiates effect of antithrombin III on
factor Xa (more selective for Xa); For Deep venous
thrombosis, Pulmonary embolism, unstable angina,
myocardial infarction, adjuvant to percutaneous
coronary intervention (PCI) and thrombolytics, Atrial
fibrillation
Binds to thrombin's ative site and inhibits its
enzymatic action; For anticoagulation in patients with
heparin induced thrombocytopenia (HIT),
percutaneous coronary angioplasty (Bivalirudin with
aspirin)
bind to free and bound factor Xa ; For prevention of
Venous thrombosis, in stroke patients with Afib
Inhibits vitamin K epoxide reductase (responsible for
y-carboxylation of the vitamin K- dependent clotting
(factors II, VII, IX, X, Protein C & Protein S) ; For
chronic anticoagulation (DVT, atrial fibrillation, valve
replacement) EXCEPT in pregnancy
Chemical antagonist of heparin. Reverses excessive
anticlotting activity of unfractionated heparin; For
heparin overdosage
GI & Hematologic SE are more
Bleeding, nausea, hematologic (neutropenia, leukopenia), common with ticlopidine. Additive
thrombotic thrombocytopenic purpura (Ticlopidine), dyspepsia effects with aspirin
DOC for anticoagulation during
pregnancy ; administered IV or SC ;
Bleeding, transient Heparin-induced thrombocytopenia, Monitor with aPTT, Antidote:
Osteoporosis with chronic use Protamine Sulfate
Does not require aPTT monitoring,
Protamine sulfate is only partially
effective in reversing effects ;
advantage over regular heparin is
higher bioavailability and t1/2 ;
Bleeding, less risk of thrombocytopenia Fondaparinux is given SC OD
Monitor with aPTT. No reversal
agents exist ; Dabigatran is PO while
all the rest are parenteral ;
Bivalirudin also inhibits platelet
Bleeding, Anaphylactic reactions, Effect-prolonging antibodies activation
bleeding No reversal agent
Monitor effects with PT-INR.
Antidote is vitamin K or FFP. Narrow
Bleeding, Teratogen (bone defects, hemorrhage), warfarin- therapeutic window ; 99% protein-
induced skin necrosis (transient hypercoagulability) bound
hypotension, flushing, bradycardia, dyspnea, hypersensitivity Partially reverses effect of LMWHs
Page 33 of 87

ii. Endogenous Vitamin: Vitamin K1, K2, K3
(Phytonadione, Menaquinone, Menadione)
D. Thrombolytic: Alteplase, Anistreplase, Reteplase,
Streptokinase, Tenecteplase, Urokinase
E. Antiplasmin drug: Tranexamic acid
F. ADH agonist: Desmopressin
Non-steroidal Anti-Inflammatory Drugs, Disease-Modifying Anti-rheumatic Drugs, Non-opioid Analgesics & Drugs Used in Gout
A.Non-selective NSAID
i. Aspirin, Sodium Salicylate
Increases supply of reduced vitamin K, which is
required for synthesis of functional vitamin K-
dependent clotting and anticlotting factors ; For
Vitamin K deficiency, Antidote to warfarin, prevention
of hemorrhagic diatheses in newborns
Tissue plasminogen activator analog. Converts
plasminogen to plasmin, which degrades the fibrin
and fibrinogen, causing thrombolysis ; For acute
myocardial infarction, pulmonary embolism, Ischemic
stroke
Competitively inhibits plasminogen activation thus
inhibiting fibrinolysis ; For prevention and treatment
of acute bleeding episodes in patients with high risk of
bleeding (hemophilia, intracranial aneurysms,
menstrual, obstetrics, thrombolytics, postperative)
Vasopressin V2 receptor agonist, Increases factor VIII
activity of patients with mild hemophilia A or VWD;
For hemophillia A, von Willebrand's disease, central
diabetes insipidus
See entry on Drugs for caogulation Disorder
Severe infusion reaction when administered at a fast rate
(dyspnea, chest and back pain) Vit K1 may be given PO or IV
Tx should be done within 6 hrs,
better if within 3hrs ; Antidote is
AMINOCAPROIC ACID ;
Streptokinase forms a complex with
endogenous plasminogen, thus
catalyzing the conversion of
plasminogen to plasmin ; tPA is
Bleeding, Reperfusion, Cerebral hemorrhage, Arrhythmias ; Loss selective for fibrin-bound
of effectiveness (on 2nd use) and allergic reactions (streptokinase) plasminogen
Contraindicated in disseminated
intravascualr coagulation (DIC) and
Thrombosis, hypotension, Myopathy, Diarrhea genitourinary bleeding
may cause immunologic reactions
headaches, nausea, flushing, seizures, hyponatremia and infections
low doses undergo first order
kinetics while high doses undergo
zero order reaction ; Long term use
See entry on Drugs for caogulation Disorder reduces the risk of colon cancer
Page 34 of 87

ii. Ibuprofen, Diclofenac, Diflunisal, Etodolac,
Fenoprofen, Flurbiprofen, Ketoprofen, Meloxicam,
Nabumetone, Naproxen, Oxaprozin, Piroxicam, Sulinidac,
Tolemtin, Mefenamic acid, Ketorolac
iii. Indomethacin
B. COX-2 Selective NSAID: Celecoxib, Etoricoxib, Parecoxib
C. Non-opioid Analgesic (COX3 inhibitor) Paracetamol
(Acetaminophen)
D. Disease Modifying Anti-Rheumatic Drug
i. Methotrexate
ii. TNF-alpha inhibitor: Infliximab, Adalimumab,
Etanercept
Nonselective reversible COX-1 and COX-2 inhibitor.
Inhibits prostaglandin and thromboxane synthesis ;
For analgesia, fever and as anti inflammatory
Nonselective reversible COX-1 and COX-2 inhibitor.
Inhibits prostaglandin synthesis and inhibit crystal
phagocytosis by macrophages ; For anti inflammatory
(gout arthritis, ankylosing spondylitis), for closing PDA
Selective COX-2 inhibitor. Inhibits prostaglandin
synthesis ; For Analgesia, Anti inflammatory,
Antipyretic
Selectively inhibits COX-3 in the CNS, Weak COX-1 and
COX-2 inhibitor in the periphery, Inhibits
prostaglandin synthesis ; For Analgesia and antipyretic
Inhibits AICAR transformylase and thymidylate
synthase, with secondary effects on
polymorphonuclear chemotaxis ; For rheumatoid
arthritis, SLE, JRA, psoriatic arthritis, Ankylosing
spondylitis, Polymyositis
Binds or inhibits to TNF-a ; For Crohn's disease,
rheumatoid arthritis, other rheumatic disease
Ibuprofen and Indomethacin can be
used to close PDA ; Ibuprofen and
naproxen have moderate
effectiveness ; Ibuprofen is
relatively safe but with short half-
life of 2hrs ; Naproxen and
Piroxicam have longer half-lives ;
Ketorolac has significant analgesic
effect but not anti-inflammatory
effect ; use Ketorolac only for 72hrs
due to GI and renal damage ;
Gastrointestinal bleeding (less than aspirin), Nephrotoxicity (AKI NSAIDs may interfere with ASA's
and Interstitial Nephritis), Hypersensitivity reaction antithrombotic action
Indomethacin has greater anti-
Gastrointestinal toxicity, pancreatitis, Nephrotoxicity, Serious inflammatory effect compared to
hematologic reactions, BM suppression other NSAIDs
Rofecoxib and Valdecoxib
Gastrointestinal bleeding, Nephrotoxicity (same risk as withdrawn due to incereased
nonselective NSAIDs), Myocardial infarction and stroke incidence of thrombosis
Preferred antipyretic in children
Hepatoxicity (antidote: NAC), Renal papillary necrosis and (does not cause reye's syndrome) ;
Interstitial nephritis, Methemoglobinemia, Hemolytic anemia t1/2 is only 2-3h
DMARD of choice for Rheumatoid
Nausea, Mucosal ulcers, hepatoxicity, hypersensitivty, arthritis, Rescue agent: Leucovorin
Pseudolymphomatous reaction, teratogen, hematotoxicity (Folinic acid)
Bacterial infections (URTIs), reactivation of latent tuberculosis,
lymphoma, Demyelination, Reactivation of Hepatitis B, Auto
antibody formation (ANA, anti dsDNA), infusion reactions, Synergistic effects with
hepatoxicity, hematotoxicity, cardiotoxicity methotrexate
Page 35 of 87

iii. Azathioprine
iv. Chloroquine, Hydroxychloroquine
v. Cyclophosphamide
vi. Cyclosporine
vii. Mycophenolate Mofetil
viii. Sulfasalazine
E. Antigout drugs
Forms 6-thioguanine, suppressing inosinic acid
synthesis, B-cell and T-cell function, Immunoglobulin
production and interleukin-2 secretion ; For
rheumatoid arthritis, psoriatic arthritis, reactive
arthritis, polymyositis, SLE
Suppression of T-lymphocyte leading to decreased
leukocyte chemotaxis, stabilization of lysosomal
enzymes, inhibition of DNA and RNA synthesis,
trapping of free radicals ; For rheumatiod arthritis,
SLE, Sjogren's syndrome, Malaria
Forms phospharamide mustard, which cross links DNA
to prevent cell replication, Supresses T-cell and B-cell
function ; For Rheumatoid arthritis, SLE vasculitis,
Wegener's granulomatosis, severe rheumatic diseases
Inhibits interleukin-1 and iterleukin-2 receptor
production and secondarily inhibits macrophage-T-cell
interaction and T-cell responsiveness ; For rheumatoid
arthritis, SLE, Tissue transplantation
active product inhibits inosine monophosphate
dehydrogenase and inhibits T-cell lymphocyte
proliferation ; For SLE nephritis, vasculitis, Wegener's
granulomatosis, rheumatoid arthritis
active metabolite inhibits the release of inflammatory
bowel cytokines; For rheumatoid arthritis,
inflammatory bowel disease, JRA, ankylosing
spondylitis
Cannot give allopurinol with
azathioprine (allopurinol reduces
xanthine oxidase catabolism of
Bone marrow supression, increased risk of infections, increased purine analogs, increasing 6-
incidence of lymphoma, Fever, rash, hepatotoxicity, allergic thioguanine nucleotides, leading to
reactions severe leukopenia)
Ocular toxicity, Dyspepsia, Nausea, vomiting, abdominal pain,
rashes, nightmares, myopathy, neuropathy, ocular toxicity safe for pregnant women
Hemorrhagic cystitis, Rescue agent
Hemorrhagic cystitis is Mesna
Nephrotoxicity, hypertension, hyperkalemia, hepatoxicity,
Gingival hyperplasia, hirsutism NONE
Gastrointestinal disturbances, headache, hypertension, reversible
myelosupression NONE
Nausea, vomiting headache,rash, hemolytic anemia,
methemoglobinemia, neutropenia, leukopenia,
thrombocytopenia, pulmonary toxicity, autoantibody formation
(anti dsDNA), Reversible infertility in men anti-IBD drugs
Page 36 of 87

i. Microtubule assembly inhibtor: Colchicine
ii. Uricosuric agent: Probenecid, Sulfinpyrazone
iii. Xanthine oxidase inhibitor: Allopurinol, Febuxostat
Inhibits microtubule assembly and LTB4 production
leading to decreased macrophage migration and
phagocytosis ; For gout
are weak acids that compete with uric acid for
reabsorption in the PCT leading to increased uric acid
excretion ; For gout
Active metabolite (alloxanthine) irreversibly inhibits
xanthine oxidase and lowers production of uric acid;
1st line treatment of chronic gout, tumor lysis
syndrome
a general mitotic poison, may also
Diarrhea, nausea, vomiting, abdominal pain, hepatic necrosis, be used for Familial Mediterranean
acute renal failure, disseminated intravascular coagulation, Fever ; diarrhea is the adverse
seizures, hair loss, bone marrow depression, peripheral neuritis, effect which signals toxicity from
myopathy colchicine
May precipitate acute gout during
early phase of drug action (prevent
by coadministering with colchicine
or indomethacin) ; may be given
together with antimicrobial agents
(particularly Penicillins) to prolong
therapeutic effect by inhibiting
Gastrointestinal irritation, rashes, nephrotic syndrome, aplastic renal tubular secretion of
anemia ; sulfa allergy antibiotics
Inhibits metabolism of
mercaptopurine and azathioprine.
Witheld for 1-2 wk after an acute
episode of gouty arthritis
(coadministered with colcichine or
indomethacin to avoid an acute
attack) ; Feboxustat is a newer non-
Gastrointestinal upset, Rash, Peripheral neuritis, Vasculitis, bone purine inhbitor of Xanthine Oxidase
marrow dysfunction, Aplastic anemia, liver dysfunction ; Febuxostat is more effective than
(Febuxostat) Allopurinol
Page 37 of 87
6. ENDOCRINE DRUGS
Hypothalamic and Pituitary Hormones
Recombinant Growth hormone, Increases release of
IGF-1 in the liver and carilage, stimulates skeletal
muscle growth, amino acid transport, protein
synthesis and cell proliferation ; For GH deficiency in
children and genetic disease associated with short
stature (Turner syndrome, Prader-Willi syndrome),
failure to thrive due to chronic renal failure or SGA,
AIDS wasting, improve GI function in patients who
underwent intestinal resection that led to
i. Somatropin malabsorption syndrome
Recombinant IGF-1 ; For children unresponsive to GH
ii. Mecasermin therapy
Somatostatin analog, suppresses the release of
growth hormones, glucagon, insulin, gastrin, IGF-1,
serotonin and gastrointestinal peptides ; For
Acromegaly, pituitary adenoma, carcinoid,
iii. Octreotide, Lanreotide gastrinoma, glucagonoma, variceal bleeding
iv. Pegvisomant GH receptor antagonist ; For acromegaly
Gonadotropin analog (FSH analog); activates FSH
receptors and mimics effects of endogenous FSH ; For
Controlled ovarian hyperstimulation, infertility due to
v. Follitropin alfa, Follitropin beta, Urofollitropin hypogonadism in men
Gonadotropin analog (LH analog); activates LH
receptors and mimics effects of endogenous LH ; For
vi. Menotropins, Human chorionic gonadotropin (HCG), Controlled ovarian hyperstimulation (ovulation
Choriogondaotropin alfa, Lutropin induction), hypogonadotripic hypogonadism
Peripheral edema, Myalgia, Arthralgia, Intracranial hypertension, used as Performance enhancing
pseudotumor cerebri, slipped capital femoral epiphysis, drug since it increases muscle mass
progression of scoliosis, hyperglycemia ; given SC
remedy to hypoglycemia: give
Hypoglycemia, increased LFT, intracranial HTN patient some snacks prior to dose
regular release: given BID-QID SC, if
slow release: every 4wks IM ; are
long-acting synthetic analogs of
GI upset, gallstone, cardiac condution abnormality somatostatin
Diarrhea, nausea, flu-like syndrome, elevated LFTs, hypesensitivity onset of action is expected within
reaction 2wks of use
Follitropin alfa and beta are
recombinant FSH forms while
Headache, depression, edema, ovarian hyperstimulation Urofollitropin is a purified
syndrome (ovarian enlargement, ascites, hypovolemia, shock), preparation from urine of
multiple pregnancies in women, gynecomastia in men postmenopausal women
menotropins are mixtures of FSH
and LH from postmenopausal
women ; Choriogondaotropin alfa
Headache, depression, edema, ovarian hyperstimulation is a recombinant hCG while Lutropin
syndrome, multiple pregnancies in women, gynecomastia in men is a recombinant LH ; hCG given IM
Page 38 of 87

vii. Leuprolide, Gonadorelin, Goserelin, Histrelin,
Nafarelin, Triptorelin
GnRH analog, increased LH and FSH secretion with
intermittent administration , reduced LH and FSH
secretion with prolonged continuous administration
(due to downregulation of GnRH receptors in the
pituitary cells that normally release LH and FSH ; For
Controlled ovarian hyperstimulation, endometriosis,
myoma uteri, precocious puberty, prostate CA
there is exacerbation of symptoms
in males with prostate CA and
children with precocious puberty
during the first few weeks of
therapy (remedy: co-administer
Flutamide, an androgen receptor
antagonist) ; Gonadorelin is a
Hot flushes, sweats, headaches, osteoporosis, gynecomastia, synthetic human GnRH ; Leuprolide
reduced libido, decreased hematocrit has a long agonist activity

Does NOT cause tumor flare-up whe

viii. Ganirelix, Cetrorelix, Degarelix
GnRH antagonist, blocks GnRH receptors, reduces
endogenous production of LH and FSH ; For
Controlled ovarian hyperstimulation (prevents
premature LH surge), advanced prostate CA
used for treatment of advanced
prostate cancer, also less likely to
cause ovarian hyperstimulation
syndrome ; Degarelix is used for
Nausea, headache, hypersensitivity, hot flushes, gynecomastia, prostate CA while Ganirelix prevent
decreased libido, decreased hematocrit, osteoporosis LH surge in controlled ovulation

Dopamine agonist, partial agonist at dopamine D2

receptors in brain, inhibits prolactin release ; For
Hyperprolactinemia, Pituitary adenoma, acromegaly,
ix. Bromocriptine, Carbegoline Parkinson's disease
Activates oxytocin receptors, stimulates uterine
contraction and labor, stimulates mammary glands,
lactation and milk let-down ; For Labor induction,
labor augmentation, control of uterine hemorrhage
x. Oxytocin post-delivery
Nausea, headache, lightheadedness, orthostatic hypotension,
fatigue, behavioral changes, erythromelalgia, Raynaud's
phenomenon, pulmonary infiltrates
Fetal distress, placental abruption, uterine rupture, fluid
retention, hyponatremia, heart failure, seizures, hypotension
Slightly inhibits GH release if given
in high doses ; CI in patients with
history of psychotic illness
ATOSIBAN - an oxytocin antagonist
used in preterm labor

ADH agonist, Vasopressin V2 receptor agonist which

xi. Desmopressin, Vasopressin
causes insertion of water channels in the collecting
duct leading to more water reabsoprtion, also
regulates the release of factor VIII and VWF ; For
Central DI, Hemophilia A, von Willebrand's disease,
Variceal bleeding, colon diverticula, primary nocturnal
seizures
also contracts vascular smooth
muscles via V1 receptor leading to
vasoconstriction, used as treatment
for esophageal varices or colon
Headaches, flushing, nausea, hyponatremia, seizures diverticula

Page 39 of 87
 ADH antagonist, Antagonist at V1a and V2 receptors ;
For SIADH, Hyponatremia, offset fluid retention in
acute heart failure and SIADH which causes
xii. Conivaptan, Tolvaptan, Lixivaptan hyponatremia (dilutional)
Thryoid & Antithyroid Drugs
Thryoid hormone, activation of nuclear receptors
results in gene expression with RNA formation and
protein synthesis ; For Hypothyroidism, myxedema
i. Levothyroxine (T4), Liothyronine (T3) coma
Inhibits thyroid peroxidase reactions, blocks iodine
organification, inhibits peripheral conversion of T4
ii. Propylthiouracil (PTU) into T3 ; For Hyperthyroidism, thyroid storm
Inhibits thyroid peroxidase reactions, blocks iodine
iii. Methimazole, Carbimazole organification ; For Hyperthyroidism, thyroid storm
Inhibit iodine organification and hormone release
leading to reduced size and vascularity of thyroid
gland ; For Hyperthyroidism, thyroid storm,
preparation for surgical thyroidectomy to reduce the
iv. Lugol Solution (Iodine in Potssium Iodide), Potassium size and vascularity of the thyroid gland, radiation
Iodide prophylaxis
Central pontine myelinolysis may
occur with rapid correction of
hyponatremia, tolvaptan is more
Infusion site reactions, hyperkalemia selective for V2 receptors
T4 dose must be lowered in
patients with cardiovascular disease
or longstanding hypothyroidism
(increased cardiosensitivity) ;
Dry skin, sweatng, tachycardia, nervousness, tremor, weight loss, Liothyronine has a faster onset but
weakness, heat intolerance shorter half-life
Drug of choice for pregnant
Maculopapular pruritic rash, gastrointestinal distress, fulminant hyperthyroid patients (does not
hepatitis, agranulocytosis, urticaria, vasculitis, lupus-like eneter placenta and breastmilk);
syndrome, lymphadenopathy, hypoprothrombinemia, Exfoliative slow onset of action (3-4 weeks for
dermatitis, polyserositis, arthralgia, hypothyroidism full effect)
Maculopapular pruritic rash, gastrointestinal distress, fulminant Methimazole and Carbimazole are
hepatitis, dose-dependent, agranulocytosis, urticaria, vasculitis, teratogens (causes Aplasia Cutis
lupus-like syndrome, lymphadenopathy, hypoprothrombinemia, Congenita) ; given as once daily
Exfoliative dermatitis, polyserositis, arthralgia, hypothyroidism dosing
onset is more rapid (2-7 days) but
effect is transient (thyroid gland
escapes iodide block after several
weeks of treatment) ; Should not be
used alone (escape in 2-8 weeks);
Iodism, acneiform rash, swollen salivary glands, mucous prevents radiation induced thryoid
membrane ulcerations, conjunctivitis, rhinorrhea, drug fever, damage; prenatal exposure causes
metallic taste, bleeding disorders, anaphylactoid reactions fetal goiter
Page 40 of 87

v. Propranolol, Esmolol, Metoprolol, Atenolol
vi. Radioactive Iodine
Adrenocorticosteroids & Adrenocortical Antagonists
i. Low Potency: Desonide
ii. Med Potency: Fluticasone, Mometasone
iii. High Potency: Desoximetasone, Clobetasol
iv. Synthetic GCs: Prednisone, Prednisolone,
Methylprednisolone, Meprednisone, Dexamethasone,
Betamethasone, Triamcinolone, Beclomethasone,
Budesonide
Beta blocker control HR and other cardiac
abnormalities of severe thyrotoxicosis, slows
pacemaker activity; inhibits peripheral conversion of
T4 into T3 ; For Hyperthyroidism, thyroid storm, post
MI prophylaxis, hypertension
Iodide, emits beta rays causing destruction of thyroid
parenchyma ; For hyperthyroidism, permanent cure
of thyrotoxicosis without surgery and no effect on
other tissues
Glucocorticoid, activates glucocorticoid receptors,
leading to altered gene transcription, Suppresses
inflammation, Replaces cortisol when deficient ; For
Acute adrenal insufficiency associated with life-
threatening shock, chronic adrenal insufficiency
(Addison's disease), congenital adrenal hyperplasia,
insect bites, contact dermatitis, status asthmaticus,
thyroid storm
Glucocorticoid; For supressession of inflammation and
immune response, hematopoeitic cancers, transplant
rejection, collagen and rheumatic disease, lung
maturation in preterm labor (betamethasone and
dexamethasone), bronchial asthma, chemotherapy-
induced vomiting, hypercalcemia, mountain sickness
Esmolol may be used to treat
thyrotoxicosis-related arrhythmias;
causes clinical improvement
WITHOUT altering thyroid hormone
Bronchospasm, cardiac depression, AV block, hypotension levels
Preferred treatment for most
patients due to ease of
administration, effectiveness, low
expense and absence of pain;
contraindicated in pregnant women
Permanent hypothyroidism, sore throat or nursing mothers
Effects: stimulate gluconeogenesis,
increased fat deposition, muscle
protein and bone catabolism,
lymphoid connective tissue fat and
skin wasting inhibit cell-mediated
immunologic functions,
lymphotoxic, increased neutrophils,
decreased lymphocytes eosinophils
basophils and monocytes, inhibit
leukocyte migration, inhibit PLA2,
delay rejection in transplant
patients, increased GI acid secretion
(ulcer) ; Biochemical effects:
induced synthesis of an inhibitor of
PLA2, decreased mRNA for COX2,
Adrenal suppression, growth inhibition, DM, muscle wasting, decrease in IL-2 and IL-3 and
osteoporosis, salt retention, glucose intolerance, behavioral decrease in Platelet Activating
changes Factor (PAF)
prednisolone is the active
metabolite of prednisone ; this
Adrenal suppression, growth inhibition, muscle wasting, group has a long t1/2, reduced salt-
osteoporosis, salt retention, glucose intolerance, behavioral retaining effect and better
changes (psychosis) penetration of lipid barriers
Page 41 of 87

v. Mineralocorticoid: Fludrocortisone,
Deoxycorticosterone
Corticosteroid Antagonists
vi. Aminoglutethimide
vii. Ketoconazole
viii. Metyrapone
ix. Mifepristone (RU486)
x. Spironolactone, Eplerenone
strong agonist of mineralocorticoid receptors and
moderate activation of glucorticoid receptors,
Increases Na reabsorption, K and H excretion ; For
Chronic adrenal insufficiency (Addison's disease),
Congenital adrenal hyperplasia, adrenal replacement
therapy post-adrenalectomy
Glucorticoid synthesis inhibitor, inhibits desmolase
activity, blocking conversion of cholesterol to
pregnenolone ; For Breast CA, Cushing syndrome
Glucorticoid synthesis inhibitor; azole antifungal;
inhibits cholesterol side chain cleavage, cytochrome
P450 enzymes and other enzymes necessary for
synthesis of all steroids ; For Adrenal CA, Hirsutism,
Breast CA, steroid-responsive metastatic Prostate CA,
Cushing's syndrome, Fungal infections, hirsutism
Glucorticoid synthesis inhibitor, selective inhibitor of
steroid-11 hydroxylation, interfering with cortisol and
corticosterone synthesis ; As diagnostic test for
adrenal function
competitive inhibitor at the GC receptor as well as
progesterone receptor ; For Cushing's syndrome
Aldoesterone antagonist ; For hypokalemia due to
other diuretics, for post-MI, hyperaldoteronism- see
entry -
Additive hypokalemia with loop
diurectics and thiazides ;
Deoxycorticosterone is the
precursor of aldosterone ;
Fludrocortisone also has significant
glucocorticoid activity ; Aldosterone
Salt and fluid retention, Hypokalemia, Congestive heart failure, is implicated in myocardial and
muscle wastng, osteoporosis, glucose intolerance, behavioral vascular fibrosis and baroreceptor
changes dysfunction
Also inhibits synthesis of all
Skin rash, hepatotoxicity, hypothyroidism hormonally active steroids
Hepatotoxicity, many drug interactions, androgenic effect Potent inhibitor of CYP450 enzymes
DOC for pregnant patients with
Dizziness, GI disturbances Cushing's syndrome
also used as an approved
abdominal pain and cramping, uterine cramping, nausea, abortifacient for medical abortion
headache, vomiting, diarrhea, dizziness, vaginal bleeding (usually together with misoprostol)
also with weak antagonist effect at
Hyperkalemia, gynecomastia (spironolactone) - see entry - the androgen receptor
Page 42 of 87
Gonadal Hormones and Inhbitors
A. Estrogen compounds
i. Ethinyl Estradiol, Mestranol, Estradiol cypionate,
Premarin
Activates etrogen receptors, leads to changes in rates
of trasncription of estrogen-regulated genes ; For
Primary hypogonadism, Postmenopausal hormonal
replacement therapy, Osteoporosis and prevention of
bone loss, Contraception, Intractable dysmenorrhea
ii. Diethylstilbestrol Synthetic estrogen (nonsteroid); activates estrogen
receptors; leads to changes in rates of transcription of
estrogen-regulated genes ; For Atrophic vaginitis,
hormone replacement therapy, prevention of adverse
pregnancy outcomes, metastatic prostate CA
breakthrough bleeding, nausea, breast tenderness, migraine,
thromboembolism (DVTs), gallbladder disease,
hypertriglyceridemia, hypertension, premature closure of the
epiphysis in young females, increased risk of breast and
endometrial cancer (remedy: add progesterone to the
preparation)
breakthrough bleeding, nausea, breast tenderness, migraine,
thromboembolism (DVTs), gallbladder disease,
hypertriglyceridemia, hypertension, premature closure of the
epiphysis in young females, increased risk of breast and
endometrial cancer (remedy: add progesterone to the
preparation)
Increases risk of endometrial cancer
and breast cancer ; Ethinyl Estradiol
has low bioavailability,
PO/TD/IM/Intravaginal ; Estradiol
cypionate is IM with longer t1/2 ;
Premarin is a mixture of conjugated
estrogen used in HRT ; Ethinyl
estradiol undergoes enterohepatic
recirculation ; Effects of Estrogen:
growth of genital structures and
secondary sexual characteristics,
modifies serum protein levels and
decrease bone resorption,
enhances coagulability of blood,
increases TG and HDL levels while
decreasing LDL levels, if given as
continuous infusion will inhibt FSH
and LH release
associated with Infertility, ectopic
pregnancy, clear cell vaginal
adenocarcinoma in daughters of
women treated with DES
Page 43 of 87
B. Progestins
i. Norgestrel, Medroxyprogesterone, Norethindrone,
Norgestimate, Desogestrel, Megestrol
C. Combined Hormonal Contraceptives
i. Estradiol + Norethindrone
ii. Ethinyl Estradiol + Desogestrel
iii. Ethinyl Estradiol + Drospirenone
iv. Ethinyl Estradiol + Noregistmate
v. Medroxyprogesterone Acetate
vi. Levonorgestrel
D. Selective Estrogen Receptor Modulators (SERMs)
activates progesterone receptors, changes rate of
transcription of progesterone-regulated genes ; For
Hormone replacement therapy (given together with
Estrogen, to prevent estrogen-induced endometrial
cancer), contraception, assisted reproduction (for
maintenance of pregnancy), anovulation induction
(given in high doses to suppress FSH and LH)
Combined oral contraceptive, activates estrogen and
progesterone receptors, inhibits ovulation, effects on
cervical mucus gland, uterine tubes and endometrium
lead to decreased fertility, inhibit ovulation when
given before the LH surge ; For Contraception,
hypogonadism, acne, hirsutism, dysmenorrhea,
endometriosis
Progestin-only contraceptive, activates progresterone
receptors, Prevents conception by altering cervical
mucus and creating a hostile endometrium ; For
Contraception, hormone replacement therapy
Postcoital contraceptive, activates estrogen and/or
progesterone receptors, thickens cervical mucus,
inhibits ovulation ; For Emergency contraception
Prevents estrogen induced
endometrial cancer when used in
combination with estrogens;
Megesterol is used as an appetite
stimulant ; given PO or as vaginal
cream ; Medroxyprogesterone has a
better oral bioavilability ; L-
Norgestrel and Norethindrone has
more androgenic effect ; Norgestrel
undergoes enterohepatic
recirculation ; Effects of
progesterone: induces secretory
changes in the endometrium,
stabilize the endometrium, affect
carbohydrate metabolism and
stimulate deposition of fat, high
Hypertension, decreased HDL, weight gain, reversible decrease in doses suppress FSH and LH
bone mineral density, delayed resumption of ovulation after use secretion
maybe PO/IM/TD/vaginal rings/IUD
Lifetime risk of breast cancer is NOT
changed; Norethindrone is a
testosterone derivative while
Drospirenone is a spironolactone
derivative that is antiandrogenic ;
Norgestimate and Desogestrel are
breakthrough bleeding, nausea, breast tenderness, migraine, newer progestins ; combined OCPs
thromboembolism (DVTs), breast cancer (earlier onset), may be used for androgen-induced
headache, skin pigmentation, depression, weight gain acne and hirsutism ; Mestranol (Estrogen)
hirsutism for older OCPs may also be used in OCPs
Breakthrough bleeding, hair loss, dysmenorrhea, delayed return
of fertility, osteoporosis IM depot preparation
Severe nausea, vomiting, breast tenderness, irregular bleeding,
headache, dizziness (fewer SE compared to estrogen alone and Must be taken within 72 hours of
combi contraceptives) unprotected sexual intercourse
Page 44 of 87
 Estrogen antagonist actions in breast tissue and CNS,
Estrogen agonist effects in uterus, liver and bone ; For
Hormone responsive breast CA, prophylaxis of breast
i. Tamoxifen, Torimefene CA esp. in those with high risk
Estrogen antagonist actions in breast tissue, uterus,
and CNS, Estrogen agonist effects in liver and bone.
Increases bone mineral density ; For Osteoporosis esp
ii. Raloxifene on post menopausal women, breast CA prevention
prevent osteoporosis in post-
Hot flushes, thromboembolism, endometrial hyperplasia, menopausal women ; Torimefene is
endometrial cancer structurally related to Tamoxifen
No estrogenic effect on endometrial
Hot flushes, thromboembolism tissue unlike tamoxifen

may cause multiple pregnancies ;

Partial agonist in pituitary, reduces negative feedback FULVESTRANT: pure estrogen
by estradiol, increases FSH and LH output ; For receptor anatgonist in all tissues
Induction of ovulation in women who want to become Hot flushes, afterimages, headache, constipation, reversible hair used in breast CA resistant to
iii. Clomiphene pregnant loss, ovarian enlargement tamoxifen
Effective against brest CA that have
become tamoxifen-resistant ;
Reduces estrogen synthesis by inhibiting aromatase ; Exemestane is an IRREVERSIBLE
iv. Anastrozole, Letrozole, Exemestane For breast CA, precocious puberty Hot flushes, musculoskeletal disorders, osteoporosis, joint pains inhibitor
Ovarian inhibitor, weak cytochrome P450 inhibitor
and partial agonist of progestin and androgen
receptors ; For Endometriosis, Fibrocystic disease, Acne, hirsutism, weight gain, menstrual disturbances, hepatic May also act on Glucocorticoid
v. Danazol Hemophilia, Angioneurotic edema dysfunction receptors

Combined with misoprostol results

vi. Mifepristone (RU486)
vii. Leuprolide and Ganirelix
E. Androgens
in abortion of 95% of early
pregnancies ; as abortifacient in
early pregnancy (may be used up to
Glucocorticoid receptor antagonist, progesterone 49days after menses) ;
receptor antagonist ; For Medical abortion, Cushing's Vaginal bleeding, abdominal pain, GI upset (vomiting, diarrhea), complication: failure to induce
syndrome uterine cramping, nausea, vomiting, headache, dizziness, diarrhea complete abortion
see entry see entry see entry
may be given IV or as TD

Page 45 of 87

i. Testosterone, Fluoxymesterone, Methyltestosterone
ii. Oxandrolone, Stanozolol, Nandrolone
F. Anti-androgens
i. Flutamide, Bicalutamide, Nilutamide
ii. Cyproterone
iii. Finasteride, Dutasteride
iv. GnRH agonist and antagonists
v. Spironolactone
vi. Ketoconazole
Activates androgen receptors, promotes development
of male characteristics, increases body muscle bulk
and RBC production ; For Male hypogonadism,
delayed puberty, wasting syndromes (for weight
gain), certain types of anemias
Activates androgen receptors, promotes development
of male characteristics, increases body muscle bulk
and RBC production; increased ratio of anabolic-to-
androgenic activity in animals
For benign and malignant prostate disease,
precocious puberty, hair loss and hirsutism
Competitive antagonist at androgen receptor ; For
Prostate CA, surgical castration
Antagonist at androgen receptor. Marked
progestational effect that suppresses the feedback
enhancement of LH and FSH ; for Hirsutism,
component of combined oral contraceptives,
decreased sexual drive in men
Androgen synthesis inhibitor, inhibits 5a reducase
enzyme that converts testosterone to
dihydrotestosterone ; For BPH, Male pattern
baldness. Hirsutism
see entry
for treatment of hirsutism in women
inhibit gonadal and adrenal steroid synthesis
Effects of androgen: secondary
sexual characteristics, fertility and
libido, male pattern baldness,
increases muscle mass, increased
RBC production, decreased urea
nitrogen excretion, maintains
normal bone density ; used illegally
Virilization and menstrual irregularities in females, paradoxical by atheletes as performance
feminization in males, cholestatic jaundice, elevated LFTs enhancer
Virilization in females, paradoxical feminization in males; this group is called "anabolic
cholestatic jaundice, elevated liver enzymes, hepatocellular CA steroids"
GnRH analogs must be
coadministered with flutamide to
prevent acute flareups of prostate
CA ; Bicalutamide and Nilutamide
Gynecomastia, hot flushes, impotence, hepatotoxicity have less heaptotoxicity
Hepatotoxicity, Adrenal suppression, depression, gynecomastia,
galactorrhea, thromboembolism Orphan drug status
Dutasteride is newer with longer
t1/2 ; this group is less likely to
cause impotence, infertility and
Impotence, gynecomastia, depression decreased libido
see entry see entry
see entry see entry
Page 46 of 87
P ancreatic Hormones & Antidiabetic Drugs
A. Insulins
i. Rapid Acting Insulin: Lispro, Aspart, Glulisine
ii. Short Acting Insulin: Regular
Activates insulin receptors leading to a reducting of
iii. Intermediate Acting: NPH, Lente circulating glucose: promotes glucose transport and
oxidation; glycogen, lipid, protein synthesis and
regulation of gene expression ; For Diabetes mellitus,
iv. Long Acting Insulin: Detemir, Glargine, Ultralente, diabetic emergencies like DKA, HHS (rapid-acting),
Lantus Hyperkalemia
B. Sulfonylureas
2nd generation sulfonylurea, acts as an insulin
secretagogue, increases insulin secretion from
pancreatic beta cells by closing ATP sensitive K+
i. Glipizide, Glibenclamide, Glimepiride, Gliclazide, channels leading to depolarization of the B cell; For
Glyburide Type 2 Diabetes Mellitus
1st generation sulfonylurea, acts as an insulin
secretagogue; increases insulin secretion from
pancreatic beta cells by losing ATP sensitive K+
ii. Tolazamide, Tolbutamide, Chlorpropamide channels ; for Type 2 Diabetes Mellitus
C. Meglitinides
Insulin Secretagogue, similar to sulfonylureas with
some overlap in binding sites, reduces circulating
glucose, increases glycogen, fat and protein formation
i. Repaglinide and gene regulation ; For Type 2 Diabetes Mellitus
Insulin Secretagogue, similar to sulfonylureas with
some overlap in binding sites, reduces circulating
glucose, increases glycogen, fat and protein formation
ii. Nateglinide and gene regulation ; For Type 2 Diabetes Mellitus
D. Biguanides
Effects of insulin: increased
glycogen and protein synthesis,
decreased protein catabolism,
increased TG storage ; rapid acting
insulins are injected a few mins
prior to meals and they are the
preferred insulin for continuous SC
infusion devices ; short-acting
insulins are injected more than an
hour before a meal ; intermediate
acting insulins are often combined
Hypoglycemia (antidote: sugar or candy, IV glucose, IM glucagon), with regular and rapid acting
insulin allergy, immune insulin resistance, lipodystrophy at insulins ; long acting insulins are
injection site called "peakless" insulins
Less hypoglycemia, weight gain, photosensitivity, cholestatic Not effective in patients with
jaundice (glibenclamide) functional B cells
tolbutamide and chlorpropamide
are highly protein bound drugs,
Hypoglycemia, weight gain, disulfiram reaction, hyperemic flush, which may also cause allergic
dilutional hyponatremia, hematologic toxicity reactions and rash
Least Hypoglycemia, rapid onset
Least hypoglycemia, headache, URTI and short DOA
Has least incidence of
hypoglycemia, may be used in CKD
patients ; rapid onset and short
Least hypoglycemia, headache, URTI DOA
Page 47 of 87

i. Metformin
E. Alpha Glucosidase Inhibitors
i. Acarbose, Miglitol
F. Thiazolidinediones
i. Pioglitazone
ii. Rosiglitazone
G. Novel Antidiabetic Agents
i. Exenatide
ii. Sitagliptin, Linagliptin
Reduced hepatic and renal gluconeogenesis with
decreased endogenous glucose production, activates
AMP-stimulated protein kinase leading to inhibition of
gluconeogenesis ; For Type 2 DM, Diabetes
prevention, PCOS
Inhibits intestinal alpha-glucosidases , reduces
conversion of starch and disacchardies to
monosaccharidea, reduces post prandial
hyperglycemia ; For Type 2 DM, Diabetes prevention
Regulates gene expression by binding to PPAR-gamma
and PPAR-alpha which increases tissue sensitivity,
increases glucose uptake in muscle and adipose
tissue, inhibits hepatic gluconeogenesis, effects on
lipid metabolism and distribution of body fat, control
of fasting and postprandial glucose, decreased risk of
DM in high-risk patients ; For Type 2 DM, Diabetes
prevention
Regulates gene expression by binding to PPAR-gamma
ONLY ; for Type 2 DM, Diabetes prevention
Analog of GLP-1, Binds to GLP-1 receptors which leads
to reducetion of post-meal glucose excursions,
increases glucose-mediated insulin release, lowers
glucagon levels, slows gastric emptying time,
produces satiety ; For Type 2 DM
Dipeptidyl Peptidase-4 Inhibitors, blocks degradation
of GLP-1, raises circulating GLP-1 levels, reduces post-
meal glucose excursions, increases glucose mediated
insulin release, lowers glucagon levels, slows gastric
emptying time, decreases appetite ; For Type 2 DM
DOC for obese diabetics ; may also
cause slowing of glucose absorption
from GIT, decreased plasma
glucagon ; causes a decrease in
endogenous insulin production by
increasing insulin sensitivity of
tissues "Insulin Sparing Effect"
therefore does not have weight
GI disturbance, weight loss, lactic acidosis (esp in renally and gain as a SE ; do NOT cause
hepatically impaired patients), Vit B12 malabsorption hypoglycemia
relatively minor glucose lowering
effects ; impaired absoprtion of
GI disturbance, hypoglycemia, increased liver enzymes, flatulence, sucrose ; taken immediately before
diarrhea, abdominal pain a meal
binds to PPAR-gamma and PPAR-
alpha ; PPAR regulates transcription
of genes encoding proteins involved
in carbohydrate and lipid
metabolism ; may increase risk for
developing Bladder Cancer
Fluid retention, weight gain, congestive heart failure, fractures esp
in women, cardiovascular events, hepatotoxicity (Troglitazone),
macular edema, dyslipidemia, increased risk of MI (Rosiglitazone) binds to PPAR-gamma ONLY
usually combined with SU or
Hypoglycemia, acute pancreatitis, GI upset, nausea, vomiting metformin ; long-acting injectables
Headache, nasopharyngitis, URTI often combined with metformin
Page 48 of 87

iii. Pramlintide
iv. Colesevelam hydrochloride
Agents That Affect Bone Mineral Homeostasis
A. Vitamin D Metabolites and Analogs
i. Cholecalciferol, Ergocalciferol
ii. Calcitriol, Doxercalciferol, Paricalcitol, Calcipotriene
Analog of amylin, Binds to amylin receptors, reduce
post-meal glucose excursions, lowers glucagon levels,
slows gastric emptying, decreases appetite ; For Type
2 DM
Bile acid binder, lowers glucose through unknown
mechanisms ; For Type 2 DM
INACTIVE Vitamin D; Regulates gene tanscription via
the vitamin D receptor; stimulates intestinal calcium
absorption, bone resorption, renal calcium and
phosphate reabsorption, decreases PTH, promote
innate immunity ; For Vitamin D deficiency states
(intestinal osteodystrophy, CKD, chronic liver disease,
hypoparathyroidism, nephrotic syndrome)
osteoporosis, psoriasis
ACTIVE Vitamin D; Regulates gene tanscription via the
vitamin D receptor; stimulates intestinal calcium
absorption, bone resorption, rena calcium and
phosphate reabsorption, decreases PTH, promote
innate immunity ; For Secondary hyperparathyroidism
in CKD, hypocalcemia in hypoparathyroidism,
psoriasis
used with insulin to control post-
Hypoglycemia, GI disturbances prandial glucose
constipation, dyspepsia, myalgia, asthenia None
given topically for psoriasis ; given
with calcium supplements for
Hypercalcemia, hyperphosphatemia, hypercalciuria osteoporosis
The active form Calcitriol is
preferred in patients with CKD,
chronic liver disease and
hypoparathyroidism ;
Doxercalciferol is a prodrug that is
converted in the liver to 1,25-
dihydroxyvitaminD ; Paricalcitol,
Calcipotriene are analogs of
calcitriol and are used topically for
Hypercalcemia, hyperphosphatemia, hypercalciuria ; psoriasis and are being investigated
Doxercalciferol, Paricalcitol and Calcipotriene cause less for malignancies and inflammatory
hypercalcemia and hypercalciuria disorders
Page 49 of 87
B. Bisphosphonates
Suppress the activity of osteoclasts in part via
inhibition of farnesyl pyrophosphate synthesis, inhibit
resorption and formation of bone by acting on the
basic hydroxyapatite crystal structure ; For Paget's
i. Alendronate, Risedronate, Ibandronate, Pamidronate, disease of the bone, Hypercalcemia esp in
Zoledronate, Etidronate, Tiludronate, Zoledronic acid malignancies, Osteoporosis
C. Hormones
Recombinant PTH, Acts via cognate G protein coupled
receptors, stimulates bone formation when given in
i. Teriparatide low intermittent doses
Acts via cognate G protein coupled receptors;
suppresses bone resorption ; For Paget's disease of
the bone, hypercalcemia, osteoporosis, tumor marker
ii. Calcitonin for thyroid CA
D. Selective Estrogen Receptor Modulators (SERMs)
Interacts selectively with estrogen receptors, inhibits
PTH-stimulated bone resorption without stimulating
breast or endometrial hyperplasia, delay bone loss in
i. Raloxifene post-menopausal women
E. Rank Ligand (RANKL) Inhibitor
Monoclonal antibody, binds to RANKL and prevents it
from stimulating osteoclast differentiation and
function, blocks bone resorption ; For
i. Denosumab postmenopausal osteoporosis
F. Calcium Receptor Antagonist
Activates the calcium sensing receptors in the
parathyroid gland, inhibits PTH secretion ; For
secondary hyperparathyroidism in CKD,
i. Cinacalcet hypercalcemia in patients with parathyroid CA
Pamidronate, Zoledronic acid and
Etidronate are used IV for
hypercalcemia in Paget's disease
and cancer ; all other preparations
and Etidronate can be given PO but
with low bioavailability (<10%) ;
Treatment regimen: oral OD
(alendronate, risedronate,
ibandronate), weekly PO
(alendronate, risedronate), monthly
Adynamic bone, Esophagitis, Osteonecrosis of the Jaw, renal PO (ibandronate), quarterly
impairment, GI irritation (remedy: take lots of water and keep injection (ibandronate), annual IV
patient in an upright position for 30mins after intake of drug) (zoledronate)
hypercalcemia, arthralgia, rhinitis, nausea, weakness, dizziness,
pharyngitis, dyspepsia, rash used IV for osteoporosis
given as injection or as nasal spray ;
used for osteoporosis but is less
effective than bisphosphonates and
Rhinitis, Nausea, vomiting, facial flushing teriparatide
see entry see entry
as potent as bisphosphonates ;
given SC every 6months which
increased risk of infection avoid the GI SE
hypocalcemia, adynamic bone disease (profound decreae in bone considered a Calcimimetic
cell activity) (decreases PTH)

Page 50 of 87
7. CHEMOTHERAPEUTIC DRUGS
Beta-Lactam & Other Cell Wall-Active & Membrane-Active Antibiotics
A. Penicillin
i. Natural Penicillins: Penicillin G, Penicillin V (narrow
spectrum penicillin)
ii. Anti-Staphylococcal Penicillins: Methicillin, nafcillin,
oxacillin, cloxacillin (very narrow spectrum)
iii. Extended Spectrum Penicillin: Ampicillin, Amoxicillin
iv. Antipseudomonal Penicillin: Piperacillin, ticarcillin,
carbenicillin
B. Cephalosporins
i.First Generation: Cefazolin, cefadroxil, cephalothin,
cephapirin, cephradine, cephalexin
Binds to penicillin-binding proteins, inhibits
transpeptidation in bacterial cell walls ; DOC for
syphillis, for streptococcal, meningococcal, G+ bacilli,
spirochete infection
Binds to penicillin-binding proteins, inhibits
transpeptidation in bacterial cell walls; For
staphylococcal infections
Binds to penicillin-binding proteins, inhibits
transpeptidation in bacterial cell walls ; For
enterococci, Listeria, E. coli, Proteus, H. influenza,
Moraxella
Binds to penicillin-binding proteins, inhibits
transpeptidation in bacterial cell walls ; For
Pseudomonas, Enterobacter, Klebsiella
Binds to penicillin-binding proteins, inhibits
transpeptidation in bacterial cell walls ; For surgical
prophylaxis, bone infections, infections due to staph
and strep, E. coli, Klebsiella, G+ cocci
Bactericidal ; excreted unchanged in
the urine ; capable of entering the
blood brain barrier
Inactivated by beta-lactamase
(penicillinase) ; given IM but Pen V
can be given PO ; increased activity
against enterococci when given
hypersensitivity, GI disturbances together with aminoglycosides
Resistant to inactivation by beta-
lactamase (penicillinase) ; all
penicillins are excreted unchanged
hypersensitivity, GI disturbances, interstitial nephritis (methicillin), in the urine EXCEPT for Nafcillin
neutropenia (nafcillin) which is excreted in the bile
Inactivated by beta-lactamase
(penicillinase), enhanced effect
when used with beta-lactamase
inhibitors (clavulanic acid,
sulbactam) ; ampicillin undergoes
enterohepatic recirculation ;
hypersensitivity, GI disturbances, pseudomembranous colitis synergistic effect with
(ampicillin), rash (ampicillin) aminoglycosides
Inactivated by beta-lactamase
(penicillinase), enhanced effect
when used with beta-lactamase
inhibitors (clavulanic acid,
hypersensitivity, GI disturbances tazobactam)
Bactericidal ; mostly IV ; all have
renal excretion EXCEPT
Cefoperazone and Ceftriaxone
Increases nephrotoxicity of
aminoglycosides ; do not cross the
BBB ; minimal activity against G-
cocci, enterococci, MRSA and most
hypersensitivity, injection site reactions, phlebitis, GI upset G- rods
Page 51 of 87

ii. Second Generation: Cefamandole, cefaclor, cefonicid,
cefuroxime, cefprozil, loracarbef, ceforanide, cefoxitin,
cefmetazole, cefotetan
iii. Third Generation: Cefoperazone, cefotaxime,
ceftizoxime, ceftriaxone, cefixime, cefpodoxime proxetil,
cefdinir, ceftibuten
Binds to penicillin-binding proteins, inhibits
transpeptidation in bacterial cell walls ; For surgical
prophylaxis, bone infections, infections due to staph
strep and E. coli, Enterobacter, Neisseria, infections
against anaerobes (Bacteroides), sinus ear and
respiratory infections by Klebsiella andHemophilus
Binds to penicillin-binding proteins, inhibits
transpeptidation in bacterial cell walls ; decreased
gram + coverage, increased gram activity
(pseudomonas, bacteroides), against Providencia,
Serratia, Neiserria, Haemophilus ; DOC for gonorrhea
(Ceftriaxone and Cefixime)
Increases nephrotoxicity of
aminoglycosides ; do not cross the
BBB ; slight less activity against G+
but extended G- activity ;
Cefuroxime has improved action
against pneumococcus and H.
influenzae ; Cefotetan and Cefoxitin
hypersensitivity, injection site reactions, phlebitis, GI upset, have good activity against B. fragilis
Hypoprothrombinemia and Disulfiram rection (cefamandole, and thus are used for abdominal
cefotetan) and pelvic infections
Synergistic effect with
aminoglycosides ; all have renal
excretion EXCEPT Cefoperazone and
Ceftriaxone ; all can penetrate the
BBB EXCEPT Cefoperazone and
Cefixime ; Ceftriaxone and
Cefotaxime are the most active
Cephs against Penicillin resistant
Streptococcus pneumoniae ;
Ceftizoxime is commonly used
against Bacteroides ; should be
reserved against serious infection
EXCEPT ceftriaxone and cefixime ;
Ceftriaxone has very good CNS
hypersensitivity, GI upset, Hypoprothrombinemia and Disulfiram penetration ; Ceftazidime has very
rection (cefoperazone) good action on Pseudomonas
Page 52 of 87

iv. Fourth Generation: Cefipime, Ceftaroline
Binds to penicillin-binding proteins, inhibits
transpeptidation in bacterial cell walls ; wide coverage
against gram + and gram - bacteria
C. Other Beta-Lactams
i. Carbapenems: Imipenem-cilastatin , ertapenem,
meropenem
Binds to penicillin-binding proteins, inhibits
transpeptidation in bacterial cell walls, wide coverage
against gram + gram - bacteria and anaerobes ; For
infections resistant to other antibiotics EXCEPT MRSA,
DOC for Enterobacter, Citrobacter and Serratia
ii.Monobactam: Aztreonam Binds to penicillin-binding proteins, inhibits
transpeptidation in bacterial cell walls ; used against
Gram like klebsiella, pseudomonas and Serratia
iii. Beta-Lactamase Inhibitors: Clavulanic acid ,
sulbactam, tazobactam Inhibits inactivation of penicillins by bacterial beta-
lactamase (penicillinase); used against beta-lactamase
producing gonococci, streptococci, E. coli and H.
influenza
hypersensitivity, GI upset
hypersensitivity, GI upset, CNS toxicity (confusion,
encephalopathy, seizures)
GI upset, superinfection, vertigo, headache, skin rash and
hepatotoxicity
hypersensitivity and cholestatic jaundice
More resistant to beta-lactamase
produced by Enterobacter,
Haemophilus, Neisseria and
Pneumococcal ; Has improved
stability to chromosomal lactamase
; Ceftaroline used for MRSA
Reserved for serious ife-threatening
infections; cilastatin inhibits renal
metabolism of imipenem ; given IV ;
low susceptibility to B-lactamases ;
active against Pseudomonas and
Acinetobacter EXCEPT Ertapenem ;
Imipenem given with Cilastatin
which acts as Dehydropeptidase
enzyme inhibitor ; Partial cross-
allergenicity with Penicillins ;
Ertapenem has longer t1/2 but less
active against Enterococci and
Pseudomonas
Resistant to beta-lactamase, no
activity against gram + bacteria or
anaerobes ; given IV ; synergistic
with AG ; renal excretion ; No cross-
allergenicity with Pens
Most active against plasmid
encoded B lactamases (Gonococci,
Streptococci, E coli and H.
Influenzae ; not good inhibitor of
inducible chromosomal B
lactamases
(Enterobacter,Pseudomonas,
Serratia)
Page 53 of 87
D. Other Cell Wall Synthesis Inhibitors
i. Glycopeptides: Vancomycin, teicoplanin, telavancin,
dalbavancin
ii. Peptide Antibiotic: Bacitracin
iii. Antimetabolite: Cycloserine
iv. Antimetabolite: Fosfomycin
v. Cyclic lipopeptide: Daptomycin
Tetracyclines, Macrolides, Clindamycin, Chloramphenicol, Streptogramins & Oxazolidinones
A. Chloramphenicol (broad spectrum protein synthesis
inhibitor)
Inhibits cell wall synthesis by binding to the D-Ala-D-
Ala terminus of nascent peptidoglycan --> inhibit
transglycosylation --> prevent elongation and cross-
linking of peptidoglycan chain ; For MRSA, PRSP, as
alternative for pseudomembranous colitis
Interferes with a late stage oin cell wall synthesis in
gram + organisms ; For gram + bacteria
Blocks incorporation of D-Ala into the pentapeptide
side chain of the peptidoglycan ; For drug-resistant TB
inhibits cytosolic enolpyruvate transferase -->
prevents formation of N-acetylmuramic acid (a
peptidoglycan precursor molecule)
same spectrum of activity as Vancomycin ; For VRE,
VRSA, for G+ acitivity, against endocarditis and sepsis
Inhibits transpeptidation (catalyzed by peptidyl
transferase) by blocking the binding of aminoacyl
moiety of the charged tRNA to the acceptor site o
mRNA at 50S subunit, basteriostatic ; For meningitis
(Strep pneumonia, H influenza, Neisseria
meningitides), back up for Salmonella, Rickettsia,
Bacteroides, Wide spectrum antibiotic
Narrow spectrum Treat red man
syndrome by slowing the rate of
infusion ; VRSA and VRE are due to
D-Ala-D-Lactate formation ;
teicoplanin and telavancin are not
absorbed in the GIT thus used for
bacterial enterocolitis, they are also
eliminated unchanged in the urine ;
decrease dose for renally impaired
patients ; Dalbavancin has very long
t1/2 (6-11 days) which permits
red man syndrome, nephrotoxicity, ototoxicity, chills, fever, once-weekly dosing and is more
phlebitis active than Vancomycin
Reserved for topical use only due to
nephrotoxicity marked nephrotoxicity
only used as a second-line agent in
neurotoxicity (tremors, seizures and psychosis) TB
renal excretion ; resistance emerges
rapidly ; synergistic with Beta
Diarrhea lactam and quinolones
monitoring of CPK is needed, NOT
Bactericidal (only destabilizes
myopathy bacterial cell membrane)
given PO and IV ; able to cross the
placenta and BBB ; Inhibits hepatic
drug-metabolizing enzymes causing
many drug interactions ; resistance
is due to the formation of
acetyltransferase that inactivates
GI disturbance, aplastic anemia, gray baby syndrome drug ; usually used as topical agent
Page 54 of 87

B. Tetracyclines: Tetracycline, doxycycline, minocycline,
tigecycline, demeclocycline
Binds 30s ribosomal subunit thus preveting the
binding of tRNA to mRNA, bacteriostatic ; Broad/Wide
Spectrum (G+ and G-), For infections caused by
Mycoplasma pneumonia, Chlamydia, Rickettsia,
Vibrio, Spirochetes such as Leptospira, Peptic ulcer
disease, Lyme disease, Malaria prophylaxis,
Amoebiasis, Acne, Doxycycline is an alternative to
macrolides as initial treatment of CAP, Alternative in
syphilis, treatment of respiratory infection caused by
susceptible organism, prophylaxis against infection in
chronic bronchitis ; Selective uses: Tetracycline (H.
Pylori PUD), Doxycycline (Lyme disease and malaria
prevention), Minocycline (Meningococcal carrier
state), Demeclocycline (SIADH), Tigecycline (more
broad spectrum - MRSA, VRE, B-lactamase producing
G- bacteria, anaerobes, Chlamydiae, Mycobacteria)
GI disturbances (enetrocolitis, nausea, diarrhea, vomiting),
teratogen (tooth enamel dysplasia/discoloration), hepatotoxicity,
nephrotoxicity, photosensitivity n(esp. demeclocycline),
vestibulotoxicity, candidiasis, bacterial superinfection with S.
aureus and C. difficile, Fanconi syndrome
Tigecycline has the broadest
spectrum and has the longest t1/2
(30-36hrs); do not drink with milk
(decreased absorption with divalent
cations like calcium) ; high Vd, cross
the placenta, enterohepatic
recycling ; all are excreted renally
EXCEPT Doxycycline (bile) ;
Resistance is due to development of
efflux pumps for active extrusion of
tetracyclines and the formation of
ribosomal protection proteins that
interfere with tetracycline binding
(but not present with Tigecycline
EXCEPT in Proteus and
Pseudomonas) ; Tigecycline is given
IV only and is unaffected by
common tetracyclie resistace
mechanisms

Page 55 of 87
C. Macrolides
Binds 30s ribosomal subunit, inhibit transpeptidation,
bacteriostatic ; For community-acquired pneumonia,
pertussis, diphtheria, chlamydial infections ;
Eryhthromycin (Campylobacter, Chlamydia,
Mycoplasma, Legionella, Corynebacterium,
Chlamydophila, Legionella, Ureaplasma, Bordetella,
G+ cocci, some G-), Clarithromycin and Azithromycin
(coverage of Erythromycin plus greater activity
against Chlamydia, Mycobacterium avium,
Toxoplasma, Helicobacter, Haemophilus, Moraxella,
i. Erythromycin, azithromycin, clarithromycin, Neiserria) ; Azithromycin is used as an alternative
telithromycin Ceftriaxone in Gonorrhea and to Pen G in syphilis
a narrow spectrum macrolide, for G+ and anaerobe,
ii. Fidaxomicin low oral bioavailability
Ketolide, structurally related to macrolide, same MOA
and spectrum as erythromycin but macrolide-resistant
iii. Telithromycin organisms are susceptible to telithromycin ; For CAP
Binds 30s ribosomal subunit, inhibit transpeptidation,
bacteriostatic ; For anaerobic infections (Bacteroides),
alternative against gram + cocci (MRSA), endocarditis
prophylaxis esp in those allergic to Pens, PCP
pneumonia, toxoplasmosis (+ Pyrimethamine), skin
D. Lincosamides: Clindamycin, lincomycin and soft tissue infection
Binds 50s ribosomal subunit, constricting the channel
where polypeptides are extruded thus tRNA
synthetase is also inhibited --> decreased free tRNA ;
For infections caused by drug-resistant gram + cocci
E. Streptogramin: Quinupristin-Dalfopristin (MRSA, VRSA, PRSP, resistant E. faecium)
good oral bioavilability but
azithromycin absoprtion is impeded
by food ; All macrolides inhibit
CYP450 except azithromycin;
azithromycin has highest Vd and
slowest elimination; telithromycin is
used for macrolide-resistance ; Half-
lives: Erythromycin (2hrs),
Clarithromycin (6hrs), Azithromycin
(24-48hrs) ; Resistance is due to
development of efflux pumps and
production of methylase enzyme ;
Cross-resistance among macrolides:
GI disturbance, cholestatic hepatitis, QT prolongation, drug complete or partial resistance with
interaction drugs acting on the 50S
as effective as Vancomycin as
GI upset, rashes, eosinophilia, acute cholestatic hepatitis, enzyme treatment for C. difficile possibly
inhibitor with lower relapse rate
For CAP including multi-drug
resistant organisms, A ketolide not
QT prolongation, enzyme inhibitor, hepatic dysfunction a macrolide in chemical structure
Cross-resistance between
clindamycin and macrolides is
common ; Resistance is due to
methylation of binding sites and
enzymatic inactivation ; G- aerobes
GI disturbance, skin rash, neutropenia, hepatic dysfunction, are resistant because of poor
possible superinfection (Pseudomembranous colitis - C. difficile penetration through th eouter
overgrowth) membrane
Inhibits CYP450 enzymes causing
multiple drug interactions ;
Injection site reaction, anthralgia-myalgia syndrome BACTERICIDAL
Page 56 of 87

F. Oxazolidinone: Linezolid
Aminoglycosides & Spectinomycin
A. Gentamycin, tobramycin
B. Amikacin
C. Streptomycin
Binds 23S rRNA of 50s ribosomal subunit, inhibit
initiation by blockin formation of the tRNA-ribosome-
mRNA ternary complex, bacteriostatic ; Reserved for
infections caused by drug-resistant gram + cocci
(MRSA, VRE, PRSP), Listeria, Corynebacteria
General MOA of all aminoglycosides (AG) is by
inhibiting protein synthesis by binding to 30s subunit:
(1) block formation of the initiation complex (2) cause
misreading of the code on the mRNA template (3)
inhibit translocation, bactericidal ; For serious
infections caused by aerobic gram bacteria (E.coli,
Enterobacter, Klebsiella, Proteus, Providencia,
Pseudomonas, Serratia, Haemophilus, Moraxella,
Shigella), endocarditis, ocular infections ; If given
together with Pens, may be used for Listeria,
Enterococcus and G+ cocci
Inhibits protein synthesis by binding to 30s subunit,
bactericidal ; For serious infections caused by aerobic
gram bacteria (E.coli, Enterobacter, Klebsiella,
Proteus, Providencia, Pseudomonas, Serratia,
Haemophilus, Moraxella, Shigella), endocarditis,
ocular infections, multidrug resistant TB (2nd line) ; If
given together with Pens, may be used for Listeria,
Enterococcus and G+ cocci
Inhibits protein synthesis by binding to 30s subunit,
bactericidal ; For TB, tularaemia, bubonic plague,
brucellosis
Inhibits CYP450 enzymes causing
multiple drug interactions ;
Resistance is due to
Thrombocytopenia, neutropenia, serotonin syndrome, decreasedaffinity of drug to binding
neuropathy, optic neuritis site
AG are given IM or IV only, have
concentration dependent killing, is
not capabale of penetrating the
blood brain barrier, low tissue
penetration, SYNERGISTIC effect
with cell wall synthesis inhibitors
due to enhancement of transport to
the inside of the bacterial cell ;
mechanism of resistance of AG:
plasmid-mediated formation of
inactivating enzymes "group
transferase" --> catalyze the
acetylation of amine functions and
the transfer of phosphoryl or
nephrotoxicity (reversible - Acute Tubular Necrosis esp in elderly, adenylyl groups to the oxygen
if given with Amphotericin B, Cephalosporin and Vancomycin)), atoms of the hydroxyl groups of AG,
ototoxicity (irreversible), neuromuscular blockade (Curare-like For Streptomycin, resistance is due
block --> respiratory paralysis. Remedy: Calcium, Neostigmine and to changes in the ribosomal binding
Mechanical Ventilator) ; S. pneumoniae is resistant to Gentamicin, site ; Gentamicin and tobramycin
Enterococci is resistant to amikacin, gentamicin, tobramycin but are the most vestibulotoxic and
NOT streptomycin nephrotoxic
Least resistance and narrowest
nephrotoxicity (reversible), ototoxicity (irreversible), therapeutic window ; used for
neuromuscular blockade streptomycin-resistant TB
Administered intramuscularly ; if
hypersensitivity, nephrotoxicity (reversible), ototoxicity given together with Pens can be
(irreversible), neuromuscular blockade, teratogen (congenital used for enterococcal endocarditis,
deafness), injection site reactions TB plague and tularemia
Page 57 of 87

D. Neomycin, kanamycin, paromomycin
E. Spectinomycin
F. Netilmicin
Sulfonamides, Trimethoprim & Quinolones
A. Sulfonamides: Silver sulfadiazine, mafenide acetate
i. Short acting: Sulfisoxazole
ii. Intermediate acting: Sulfamethoxazole
iii. Long acting: Sulfadoxine
B. Combination: Co-trimoxazole (Sulfamethoxazole +
Trimethoprim)
C. Fluoroquinolones
Inhibits protein synthesis by binding to 30s subunit,
bactericidal ; For skin infections, bowel preparations
for elective surgeries, hepatic encephalopathy,
visceral leishmaniasis (paromomycin)
Inhibits protein synthesis by binding to 30s subunit,
bactericidal ; For drug-resistant gonorrhoea,
gonorrhoea in penicillin allergic patients
Inhibits protein synthesis by binding to 30s subunit,
bactericidal ; For serious infections caused by aerobic
gram bacteria
Inhibits dihydropteroate synthase, bacteriostatic ; For
burn infections, for G=, G-, Chlamydia and Nocardia,
Simple oral sulfas (UTI), Sulfacetamide (ocular
infection, topical), Mafenide and Silver sulfadiazine
(burn infection, topical), Sulfasalazine (Ulcerative
colitis and RA, oral), Sulfadizaine + Pyrimethamine +
Folinic acid (Toxoplasmosis, oral)
Sequential blockade of dihydropteroate synthase
(sulfamethoxazole) and dihydrofolate reductase
(trimethoprim), bactericidal ; For UTI, respiratory, ear
and sinus infections (Hemophilus, Moraxella,
Aeromonas), DOC for P. jiroveci pneumonia and
Nocardiosis, toxoplasmosis, Back-up for cholera
typhoid fever shigellosis, G- sepsis, MRSA, Listeria
Avoid in pregnancy due to absence of safety data
Limited to topical and oral use due
to nephrotoxicity, kanamycin is
most ototoxic ; Neomycin has the
hypersensitivity, nephrotoxicity (reversible), ototoxicity most skin reactions (allergic
(irreversible), neuromuscular blockade reactions, contact dermatitis)
nephrotoxicity (reversible), ototoxicity (irreversible), Ototoxcity of AG's can be increased
neuromuscular blockade by loop diuretics
For Treatment of serious infections
hypersensitivity, nephrotoxicity (reversible), ototoxicity caused by organisms resistant to
(irreversible), neuromuscular blockade other aminoglycosides
low solubility in acidic urine causing
formation of stones ; Resistance is
due to plasmin-mediated
(decreased intracellular
accumulation of the drug, increased
production of PABA by bacteria,
GI upset, mild hepatic dysfunction, acute hemolysis in G6PD decreased sensitivity of
deficiency, nephrotoxicity (precipitate in the urine at acidic pH --> dihydropteroate synthetase to
crystalluria, hematuria), hypersensitivity (cross-allergenicity with sulfas and production of
other related drugs such OHAs and diurectics), exfoliative dihydrofolate reductase that has
dermatitis, polyarteritis nodosa, SJS, hematotoxicity decreased affnity for the drug ;
(granulocytopenia, thrombocytopenia, aplactis anemia), sulfonamides are formulated in a
kernicterus ; Drug Interactions: warfarin, methotrexate, bilirubin 5:1 ratio with trimethoprim
GI upset, acute hemolysis in G6PD deficiency, nephrotoxicity, Sulfonamides are weakly acidic
hypersensitivity, hematotoxicity, kernicterus ; trimethoprim while Trimethroprim is a weak base
toxicity: antifolate effects (megaloblastic anemia, leukopenia, ; remedy for antifolate effects:
granulocytopenia) Folinic acid supplement
Page 58 of 87

i. First Generation Fluoroquinolones: Norfloxacin,
Nalidixic acid
ii. Second Generation Fluoroquinolones: Ciprofloxacin,
ofloxacin, Enoxacin Norfloxacin
Inhibits DNA replication by binding to DNA gyrase and
topoisomerase IV (G+) and Topoisomerase II (G-),
bactericidal, inhibition of Topoisomerase II results in
blockade of relaxation of supercoiled DNA that is
catalyzed by DNA gyrase while inhibition of
Topoisomerase IV interferes with the separation of
replicated chromosomal DNA during cell division ;
General use of FQs: For infections of the urogenital
and GI tract by G- (gonococci, E. coli, Klebsiela,
Campylobacter, Enterobacter, Pseudomonas,
Salmonella, Shigella), respiratory tract, skin and soft
tissue infection ; may be used against meningococcal
carrier state, for treatment of TB and prophylaxis in
neutropenic patients
Inhibits DNA replication by binding to DNA gyrase and
topoisomerase IV (G+) and Topoisomerase II (G-),
bactericidal, bactericidal ; For UTI and GIT infections
(gram rods, gonococci, gram + cocci), atypical
pneumonia (Mycoplasma, Chlamydophila),
Mycobacteria ; increased activity against G-
General SE: GI distress, skin rashes, HA, dizziness, insomnia,
increased LFT, phototoxicity, CNS effects (dizziness, headache), General properties of quinolones:
tendinitis and tendon rupture, opportunistic infection by Candida good oral bioavailability, high Vd,
and Streptococci ; CI in pregnancy and in children (damage t1/2 3-8hrs, absorption is impeded
growing cartilage --> arthropathy), enhance toxicity of by antacids, elimination is via
methylxanthines (theophylline) ; Mechanism of resistance for kidneys by tubular secretion (may
Quinolones: decreased intracellular accumulation via efflux compete with probenecid for
pumps, change in porin structure, chnages in sensitivity of target excretion) EXCEPT for
enzyme svia point mutations in the antibiotic binding region, MOXIFLOXACIN ; Norfloxacin does
mutations in the quinolone resistance determining region of the not achieve adequte plasma levels
gyrA gene that encodes for DNA gyrase for use in systemic infections
high resistance esp for C. jejuni,
gonococci, G+ cocci like MRSA,
GI distress, skin rashes, HA, dizziness, insomnia, increased LFT, Pseudomonas and Serratia ; are
phototoxicity, CNS effects (dizziness, headache), tendinitis and used as alternative to Ceftriaxone
tendon rupture, opportunistic infection by Candida and and Cefixime in gonorrhea ;
Streptococci ; CI in pregnancy and in children (damage growing Ofloxacin can be used against C.
cartilage --> arthropathy) trachomatis
Page 59 of 87

iii. Third Generation Fluoroquinolones: Levofloxacin,
Gemifloxacin, Moxifloxacin, Sparfloxacin
iv. Fourth Generation Fluoroquinolones: Trovafloxacin,
Alatrofloxacin
Inhibits DNA replication by binding to DNA gyrase and
topoisomerase IV (G+) and Topoisomerase II (G-),
bactericidal, bactericidal ; For lung infections caused
by gram + cocci, atypical pneumonia (Chlamydia,
mycoplasma) ; less G- activity compared to 2nd gen
but increased activity against G+ cocci, enterococci,
MRSA
Inhibits DNA replication by binding to DNA gyrase and
topoisomerase IV (G+) and Topoisomerase II (G-),
bactericidal, bactericidal ; has broad spectrum activity
(gram and gram +), enhanced activity against
anaerobes
"Respiratory Quinolones" ;
Moxifloxacin and Gemifloxacin are
the newest members of this family
and are condisered to have the
broadest spectrum of activity with
increased activity aginst anaerobes
ang atypical agents ; FQ elimination
is via kidneys by tubular secretion
(may compete with probenecid for
excretion) EXCEPT Moxifloxacin ;
NEVER use moxifloxacin in UTI ;
Levofloxacin is used in CAP caused
by Chlamydia, Mycoplasma and
Legionella ; Gemifloxacin,
Levofloxacin and Moxifloxacin can
prolong QT ; Levofloxacin has
superior activity against G(+)
bacteria including S. pneumoniae ;
All have relatively long t1/2
permitting once daily dosing ; Oral
absorption is impaired by cations ;
GI distress, skin rashes, HA, dizziness, insomnia, increased LFT, Gatifloxacin can cause
phototoxicity, CNS effects (dizziness, headache), tendinitis and hyperglycemia in DM Px and
tendon rupture, opportunistic infection by Candida and hypoglycemia in patients also
Streptococci ; CI in pregnancy and in children (damage growing receiving OHA and was withdrawn
cartilage --> arthropathy) from the market in 2006 (USA)
GI distress, skin rashes, HA, dizziness, insomnia, increased LFT,
phototoxicity, CNS effects (dizziness, headache), tendinitis and
tendon rupture, opportunistic infection by Candida and additional SE: diabetes
Streptococci ; CI in pregnancy and in children (damage growing (gatifloxacin), hepatotoxicity
cartilage --> arthropathy) QT prolongation (trovafloxacin)
Page 60 of 87
D. Miscellaneous agents
Reactive reduction by ferredoxin forming free radicals
that disrupt electron transport chain, bactericidal ; For
anaerobic or mixed intra-abdominal infections,
vaginitis (trichomonas, gardnerella),
pseudomembranous colitis, brain abscess, protozoal
i. Metronidazole, tinidazole infections
Forms multiple reactive intermediates when acted
upon by bacterial nitrofuran reductase, bactericidal ;
ii. Nitrofurantoin For UTI (except Proteus and Pseudomonas)
Antimycobacterial Drugs
Inhibits mycolic acid synthesis, bactericidal ; For TB,
for latent infection, given as a sole drug for
A. Isoniazid (nicotinic acid derivative) prophylaxis of close contacts and skin test converters
GI irritation, metallic taste, headache, dark urine, leukopenia, DOC for amoebiasis, giardiasis and
dizziness, ataxia, neuropathy, seizures and disulfiram reaction Pseudomembranous colitis
single OD dose can prevent
recurrent UTI ; acidification of urine
GI irritation, skin rashes, pulmonary infiltrates, phototoxicity, enhances activity ; adjust dose in
neuropathies, hemolysis in patients with G6PD deficiency renal patients
Most impt drug in TB, prevent
neurotoxicity by giving pyridoxine
(vit B6) ; structural congener of
pyridoxine ; high level resistance
due to deletion of KatG gene
whichh codes for catalase-
peroxidase enzyme involved in
bioactivation of INH, low level
resistance due to deletion og inhA
hepatotoxicity, neurotoxicity (seizures, peripheral neuritis, gene which encodes the target
insomnia, restlessness, muscle twitching), acute hemolysis in enzyme which is an acyl protein
G6PD deficiency, drug-induced lupus reductase ; Potent CYP450 inhibitor

Potent CYP450 inducer ; rapid

B. Rifamycin derivatives: Rifampicin, rifabutin, rifapentine,
rifamixin
Inhibits DNA-dependent RNA polymerase, bactericidal
; For TB, leprosy, prophylaxis for meningococcal and
staphylococcal carrier states, drug-resistant infections
(MRSA, PRSP) when given together with Vancomycin,
can be used as sole drug in the treatment of latent TB
in INH-intolerant patient or in close contact of
patients with INH-resistant strains of the organism
red-orange urine, light chain proteinuria, skin rash,
thrombocytopenia, nephritis, hepatotoxicity, flulike syndrome,
anemia, impair antibody response
development of resistance if used
alone ; resistance is due to changes
of drug sensitivity of the
polymerase enzyme; undergoes
enterohepatic recirculation ;
orange-colored metabolites ; delay
emergence of resistance to dapsone
; Rifabutin is equally effective as
anti-mycobacterial agent with less
drug interaction and it is the
preferred anti-TB for AIDS patients ;
Rifamixin is not absorbed in the GIT
and is used for traveler's diarrhea

Page 61 of 87

C. Ethambutol (butanol derivative)
D. Pyrazinamide (pyrazine derivative)
E. Streptomycin (aminoglycoside)
Drugs for Leprosy
A. Sulfones: Dapsone, acedapsone
B. Clofazimine
Antifungal Agents
A. Polyene antifungal: Amphotericin B
Inhibits arabinosyl transferases involved in the
synthesis of arabinogalactan in mycobacterial cell
wall, bacteriostatic ; For TB
Unknow MOA, bacteriostatic but can be bactericidal
on actively dividing mycobacteria, is metabolozed to
pyrazinoic acid, t 1/2 is increased in liver and kidney
disease ; For TB
for MDRTB (TB meningitis, miliary TB, severe organ
TB)
Inhibition of folic acid synthesis, bacteriostatic ; For
leprosy, alternative for PCP pneumonia
Binds to guanine bases in bacterial DNA, bactericidal ;
For leprosy
Binds to ergosterol in fungal cell membranes, forming
artificial pores, fungicidal, WIDEST antifungal
spectrum ; For systemic fungal infections (aspergillus,
blastomyces, candida, Cryptococcus, histoplasma,
mucor), for initial induction before followup
treatment with azoles, can be used topically in
mycotic corneal ulcers and keratitis
Resistance is due to mutation in
emb gene ; dose adjustment id
dose-dependent visual disturbances (decreased visual acuity, red needed in renal patients ; always
green color blindness, retrobulbar neuritis, retinal damage, optic used in combination with other
neuritis), headache, confusion, hyperuricemia, peripheral neuritis drugs for TB
Most hepatotoxic anti-TB drug, also
known as sterilizing agent ; require
metabolic conversion via
pyrazinamidases in MTb ; resistance
is via mutation in pncA gene which
hepatotoxicity, nongouty polyarhtralgia, asymptomatic codes for pyrazinamidases and
hyperuricemia, myalgia, GIT irritation, maculopapular rash, increased efflux systems ; decrease
porphyria, photosensitivity ; CI in pregnancy dose in hepatic and renal patients
see entry see entry
Most active drug against M. leprae ;
used in combination with rifampicin
and clofazimine ; Acedapsone is a
repository form of dapsone which
GI irritation, fever, skin rashes, methemoglobinemia, acute has drug action that can last for
hemolysis in G6PD deficiency patients several months
GI irritation, skin discoloration a phenazine dye
Control infusion reactions by
slowing the rate of infusion and
premedication with antihistamines,
additive nephrotoxicity with other
nephrotoxic drugs
(aminoglycosides) ; highly lipid
soluble, poorly absorbed in the GIT ;
high Vd except in the CNS with a
infusion reactions (chills, fever, muscle spasms, vomiting, t1/2 of 2weeks ; resistance is due to
hypotension), dose limiting nephrotoxicity (decreased GFR, ATN decreased level of ergosterol or
with magnesium and potassium wasting, decreased change in membrane structure ; has
erythropoietin), neurotoxicity (seizure, neuronal damage) the WIDEST antifungal spectrum
Page 62 of 87

B. Flucytosine
C. Azole Antifungals
i. Ketoconazole (Imidazole)
ii. Fluconazole (Triazole)
iii. Itraconazole (Triazole)
iv. Voriconazole (Triazole)
Accumulated in fungal cells by the action of permease decrease dose in renal patients ;
and converted by cytosine deaminase to 5-FU, which resistance is due to decreased
inhibits thimidylate synthase, pyrimidine activity of fungal permease and
antimetabolite, fungistatic ; given together with deaminase ; has synergistic effect
ampho B and Triazoles - For cryptococcal infection, when given with ampho B and
systemic candidal infections, chromoblastomycosis reversible myelosuppresion, alopecia, hepatotoxicity Triazoles.
Limited to topical use because of
systemic toxicity ; narrow antifungal
spectrum ; resistance is due to
Inhibit 14-demethylase --> decreased ergosterol chnages in the sensitivity of target
production --> increased permeability of cell enzyme ; Potent CYP450 inhibitor ;
membrane, Inhibits fungal P450-dependent enzymes Ketoconazole is rarely used due to
blocking ergosterol synthesis, fungistatic ; For chronic GI disturbances (vomiting, diarrhea), rash, hepatotoxicity, drug drug interactions and narrow
mucocutaneous candidiasis, dermatophytosis interaction, gynecomastia, menstrual irregularities and infertility spectrum
Inhibit 14-demethylase --> decreased ergosterol
production --> increased permeability of cell
membrane, Inhibits fungal P450-dependent enzymes
blocking ergosterol synthesis, fungistatic ; DOC for
candidiasis (esophageal, oropharyngeal, alternative to Ampho B in the
vulvovaginitis), coccidioidomycosis, cryptococcal treatment of C. neoformans, as
meningitis (treatment and prophylaxis) GI disturbances (vomiting, diarrhea), rash, hepatotoxicity effective as Ampho B in candidemia
Inhibit 14-demethylase --> decreased ergosterol
production --> increased permeability of cell
membrane, Inhibits fungal P450-dependent enzymes
blocking ergosterol synthesis, fungistatic ; DOC for
blastomycosis, sporotrichosis, dermatophytosis esp
onchomycosis, chromoblastomycosis ; alternative for
infections due to Aspergillus, Coccidioides,
Cryptococcus and Histoplasma , for esophageal may also be used for subcutaneous
candidiasis resistant to fluconazole GI disturbances (vomiting, diarrhea), rash, hepatotoxicity chromoblastomycosis
Inhibit 14-demethylase --> decreased ergosterol
production --> increased permeability of cell
membrane, Inhibits fungal P450-dependent enzymes
blocking ergosterol synthesis, fungistatic ; co-DOC for
invasive aspergillosis, alternative in candidemia, for
fluconazole-resistant organisms, for candidal GI disturbances (vomiting, diarrhea), rash, hepatotoxicity, blurring
esophagitis and stomatitis in AIDS patients of vision in 30% of patients, CI in pregnancy wider specturm azole
Page 63 of 87
 Inhibit 14-demethylase --> decreased ergosterol
production --> increased permeability of cell
membrane, Inhibits fungal P450-dependent enzymes
blocking ergosterol synthesis, fungistatic ; For Candida
and Aspergillus, as prophylaxis of fungal infection
during cancer chemotherapy, salvage therapy in
v. Posaconazole (Triazole) invasive aspergillosis
Inhibit 14-demethylase --> decreased ergosterol
production --> increased permeability of cell
membrane, Inhibits fungal P450-dependent enzymes
blocking ergosterol synthesis, fungistatic ; For
mucocutaneous candidiasis, dermatophytosis,
vi. Clotrimazole, miconazole, ketoconazole seborrheic dermatitis, pityriasis versicolor
Inhibit beta-glucan synthase which produces (1-->2)
glycan which is a cellwall component, thus decreasing
fungal cell wall synthesis, fungostatic ; For
disseminated and mucocutaneous candidiasis who fail
to respond to amphoB, for mucormycosis, salvage
D: Echinocandins: Caspofungin, anidulafungin, micafungin therapy for invasive aspergillosis
Interferes with microtubule function in
dermatophytes, inhibits synthesis and polymerization
E. Griseofulvin of nucleic acids, fungistatic ; For dermatophytosis
Inhibits withg ergosterol synthesis by inhibiting fungal
squalene oxidase leading to increased squalene which
interferes with ergosterol synthesis, fungicidal ; For
F. Terbinafine dermatophytosis, onchomycosis
Binds to ergosterol in fungal cell membranes, forming
artificial pores, fungicidal ; For candidiasis
((oropharyngeal, esophageal and vaginal), for GI
fungal infections in patients with impaired defense
G. Nystatin (polyene) mechanisms
BROADEST spectrum triazole ; the
only azole with activity against
Rhizopus sp. (mucormycosis) ;
GI disturbances (vomiting, diarrhea), rash, hepatotoxicity Potent CYP450 inhibitor
Limited to topical use because of
None when administered topically systemic toxicity
all are given IV ; micafungin can
headache, GI distress, rash, fever, flushing (histamine release), increase levels of cyclosporine and
elevated liver enzymes tacrolimus
given PO ; Accumulates in keratin ;
potent CYP450 inducer ; absorption
is increased by intake of fatty meal ;
headache, mental confusion, GI irritation, photosensitivity, resistance is due to decreased
hepatotoxicity, disulfiram reaction, drug interactions (decreases transport of drug into the fungal cell
bioavialability of warfarin) ; contraindicated in porphyria wall
given PO and topical, also
accumulates in keratin, more
effective than griseofulvin in
GI upset, rash, headache, taste disturbances onchomycosis
Minimal mucocutaneous
absorption, available as swish and
nephrotoxicity (severe) swallow preparation
Page 64 of 87
Antiviral Agents
A. Anti-Herpes
Activated by viral thymidine kinase (TK) to forms that
inhibit viral DNA polymerase, guanosine analog,
competitive substrate for DNA polymerase, causes
chain termination after its incorporation into the viral
DNA ; For infections due to HSV1, HSV2, VZV
(mucocutaneous and genital herpes, prophylaxis in
AIDS and in other Immunocompromised states such
i. Acyclovir, valacyclovir, penciclovir, famciclovir, as organ transplant patients, herpes encephalitis,
docosanol neonatal HSV infection etc.
Inhibits fusion between the HSV envelope and plasma
membrane, prevents viral entry and subsequent
ii. Docosanol replication
nausea, diarrhea, headache, delirium, tremor, seizures,
hypotension, nephrotoxicity
nausea, diarrhea, headache, delirium, tremor, seizures,
hypotension, nephrotoxicity
given PO, topical and IV ; dose
adjustment in renal patients ; No
activity against strains of HSV with
absent thymidine kinase activity ;
resistance is due to changes in viral
DNA polymerase ; Valacyclovir is a
prodrug that is converted to
Acyclovir and reached plams levels
3-5x (longer t1/2) more than
acyclovir ; Penciclovir does not
cause chain termination ;
Famciclovir is a prodrug which is
converted to Penciclovir in vivo
topical preparation shortens healing
time

given as IV or intraocular implant

iii. Ganciclovir, valganciclovir (anti-CMV)
iv. Cifodovir (anti-CMV)
Inhibits viral DNA polymerase causing chain
termination, guanosine derivative ; For infections due
to CMV, HSV1, HSV2, VZV ; For prohylaxis and
treatment of CMV retinitis and other CMV infections
in the immunocompromised patients
Inhibits viral DNA polymerase causing chain
termination ; For CMV retinitis, mucocutaneous HSV
infections, acyclovir-resistance, ganciclovir-resistance,
genital warts and molluscum contangiosum
(for CMV retinitis) ; No activity
against strains of HSV with absent
thymidine kinase activity ; CMV
resistance is due to mutation in viral
DNA polymerase and in the genes
that code for the activating viral
phosphotransferase ; Valganciclovir
leukopenia, thrombocytopenia, mucositis, hepatotoxicity, is a prodrug of ganciclovir with
seizures, neutropenia increased oral bioavialability
Active against strains of HSV with
absent thymidine kinase activity ;
resistance is due to mutation in
DNA polymerase ; dose adjustment
nephrotoxicity in renal patients

Page 65 of 87

Inhibits viral RNA polymerase, DNA polymerase, and
HIV reverse transcriptase, binds to pyrophosphate
binding site ; as alternative for prophylaxis and
treatment of CMV retinitis, gancyclovir-resistant
strains of CMV, HSV infection in patients with AIDS,
v. Foscarnet (anti-CMV) also used in organ transplantation
vi. Vidarabine adenine analog ; For HSV, VZV, CMV
vii. Idoxuridine, trifluridine pyrimidine analogs ; For herpes keratitis (HSV-1)
antisense oligonucleotide that binds to mRNA of CMV
causing inhibition of early protein synthesis ; For CMV
viii. Fomivirsen retinitis
B. Drugs for HIV
Inhibit HIV reverse transcriptase after
phosphorylation by cellular enzymes, acts as chain
terminators via insertion into the growing DNA chain ;
For HIV infection, prevention of maternal-fetal HIV
i. NRTI: transmission
a. Abacavir guanosine analog
b. Didanosine (ddI) NRTI
c. Emtricitabine NRTI
Active against strains of HSV with
absent thymidine kinase activity ;
does not require phosphorylation
for antiviral activity ; resistance is
due to mutations in DNA
nephrotoxicity, electrolyte abnormalities (hypocalcemia), GU polymerase gene ; dose adjusment
ulcerations, CNS effects (headache, hallucination, seizures) in renal patients
used topically only because it is
rapidly metabolized into the
GI irritation, paresthesia, tremor, convulsion, hepatic dysfunction, inactive form and because it has a
CI in pregnancy toxic potential
topical only because it is too toxic fo
irritation, blurred vision, photophobia systemic use
injected intravitreally ; concurrent
systemic use of anti-CMV in threapy
is recommended to protect against
extraocular and contralateral retinal
iritis, vitritis, increased IOP, changes in vision CMV disease
these are prodrugs converted by
host cell kinases tp triphosphates
causing competitive binding of
natural nulecotides to the dNTP-
binding site of Reverse
Transcriptase ; resistance is due to
see specific drugs below mutation in pol gene
good oral bioavailability, T1/2 is 12-
hypersensitivity reaction 24hrs, resistance is slow
oral bioavailability is decreased by
acute pancreatitis, peripheral neuropathy, diarrhea, hepatic food and chelating agents ; dose
dysfunction, hyperuricemia, CNS effects adjustment in renal patients
aesthenia, GI upset, headache, hyperpigmentation of palms of per orem once a day treatment,
soles, CI in pregnancy, children, renal and hepatic and patients dose adjustment in renal patients
Page 66 of 87
 80% oral bioavailability ;may also be
used for Hepa B infection ; HAART,
d. Lamivudine (3TC) NRTI GI upset, headache, fatigue, insomnia dose adjustment in renal patients
peripheral neuropathy esp if given together with Zalcitabine, lactic good oral bioavailability, dose
e. Stavudine (d4T) NRTI acidosis with hepatic steatosis adjustment in renal patients
a nucleotide but acts as NRTI, competitively inhibits oral bioavailabilty is 25-40% ;
RT, cause chain termination after incorporation into halflife is 60hours ; also used
f. Tenofovir DNA GI upset, asthenia, headache, Fanconi syndrome, AKI against HBV
peripheral neuropathy, pancreatitis, esophageal ulceration, increased oral bioavailability, dose
g. Zalcitabine (ddC) NRTI stomatitis, arthralgias adjustment in renal patients
BM suppression (anemia, neutropenia, thrombocytopenia), acute dose adjustment in uremic patients
cholestatic hepatitis, agitation, insomnia, myalgia, headache, GI and cirrhosis ; affected by enzymes
h. Zidovudine (ZDV) Azidothymidine or AZT upset inducers and inhibitors
Inhibits HIV reverse transcriptase, no phosphorylation Delavirdine and Nevirapine (rash, increased AST/ALT, Efavirenz binds to a different binding site ;
required, do not compete with nucleoside (teratogenicity), Etravirine (increased cholesterol and resistance is due to mutations in pol
ii. NNRTI: Delavirdine, efavirenz, etravirine, nevirapine triphosphate ; For HIV infection triglycerides) gene
metabolized by CYP3A4 and
CYP2D6, affected by enzyme
a. Delavirdine NNRTI rashes, teratogenic inducer and inhibitor
enhanced absorption by fatty
CNS dysfunction, skin rash, increased plasma cholesterol, meals, drug interactions are
b. Efavirenz NNRTI teratogenic common
nausea, vomiting, diarrhea, increased cholesterol, triglycerides
c. Etravirine NNRTI, for drug-resistant HIV and LFTs NEWEST NNRTI
used as a singledose to prevent HIV vertical
transmission at the onset of labor and also given to good oral bioavailability,t1/2 is
d. Nevirapine the neonate rash, SJS, TEN >24hours

General SE: hyperglycemia, insulin resistance, hyperlipidemia,

altered body fat distribution (buffalo hump, gynecomastia, truncal
iii. Protease Inhibitor: Atrazanavir, Darunavir, cleaves precursor polyprotein to form the final obesity, facial and peripheral lipodystrophy) due to the inhibition Resistance is due to mutation in pol
Fosamprenavir, Indinavir, Nelfinavir, Lopinavir-Ritonavir, structural protein of the mature virion core, inhibits of lipid-regulating proteins which have active sites with structural gene ; are potent CYP3A4 inhibitor
Saquinavir, Tipranavir viral protein processing ; For HIV infection homology to that of HIV protease esp Ritonavir

Page 67 of 87
 per orem absorption requires acidic
environment ; can penetrate CSF
and seminal fluid ; is not associated
with dyslipidemia, fat deposition or
peripheral neuropathy, skin rash, hyperbilirubinemia, QT metabolic syndrome ; CYP3A4 and
a. Atazanavir Protease Inhibitor prolongation 2C9 inhibitor
rash, hepatotoxicity, hypersensitivity ; CI in patients with sulfa Given together with Ritonavir in
b. Darunavir Protease Inhibitor allergy patients resistant to other PIs

GI upset, paresthesia, rash, CI in pregnant patients and children if a prodrug that is converted to the
drug uses propylene glycol as solvent ; does not have risk for active drug Amprenavir ; absorption
hyperlipidemia, fat maldistribution, hyperglycaemia and insulin is impaired by fatty food ; used with
c. Fosamprenavir Protease Inhibitor resistance lowdose Ritonavir
decreased bioavailability in the
nausea, vomiting, diarrhea, thrombocytopenia, presence of food ; affected by
d. Indinavir Protease Inhibitor hyperbilirubinemia, nephrolithiasis, insulin resistance enzyme inhibitors and inducers
there is increased compliance with
used as a combination drug: uses subtherapeutic dose this drug ; Ritonavir has boosting
of ritonavir which inhibits CYP3A4 mediated effect on other PI due to enzyme
e. Lopinavir-Ritonavir metabolism of lopinavir GI upset (well-tolerated side effects) inhibitory effect
absorption is increased by food,
short half-life ; has the most
favorable safety profile for
f. Nelfinavir Protease Inhibitor Diarrhea pregnancy
Protease Inhibitor ; subtherapeutic doses inhibit
CYP3A4-mediated metabolism of other Pis (Indnavir, good oral bioavailability esp when
Lopinavir, Saquinavir) which permits lower dose of the taken with meals ; affected by
g. Ritonavir other PI GI upset, bitter taste, paresthesia, increased LFT's enzyme inducer and inhibitors
Protease Inhibitor ; given together with low dose
Ritonavir to improve compliance and decrease GI affected by enzyme inducers and
h. Saquinavir upset nausea, vomiting, diarrhea, dyspepsia, rhinitis inhibitors
newer drug ; induces P-glycoprotein
transporters which leads to
Protease Inhibitor ; given with Ritonavir for PI- alteration of GI absorption of other
i. Tipranavir resistant HIV GI upset, rash, hepatotoxicity drugs
iv. Entry inhibitors:

Page 68 of 87

a. Fusion Inhibitor: Enfuvirtide, Docosanol
b. CCR5 receptor antagonist: Maraviroc
C. Drugs for Influenza
i. Uncoating inhibitors: Amantadine, rimantadine
ii. Neuraminidase inhibitors: Oseltamivir, Zanamivir,
Peramivir
D. Drug for HBV and HCV
i. Interferon-
Binds to gp41 subunit of viral envelope glycoprotein,
preventing fusion of viral and cellular membranes ;
For previously drug-treated patients with persistent
HIV replication despite ongoing therapy
Blocks viral attachment by blocking CCR5, a
transmembrane protein involved in the attachment of
HIV to host cell ; For HIV infection
Inhibit early step replication and prevent uncoating by
binding to M2 proton channels ; For influenza A and
rubella
Inhibits neuraminidase which cleaves sialic acid
residues from viral proteins and surface proteins of
infected cells , decrease release of progeny virus ; For
influenza A and B, shortens duration of symptoms
cytokine, increased activity of JAKS leading to
phosphorylation of signal transducers and activation
of transcription (STATS) which causes increased
formation of antiviral proteins , also increases NK cells
that destroy infected liver cells, Degrades viral RNA
via activation of host cell RNAse (ribonuclease) ; For
chronic HBV, HCV infection, Kaposi sarcoma, genital
warts, prevents dissemination of HZV in cancer
patients and decreased CMV shedding after renal
transplantation
injection site reaction, hypersensitivity reaction, increased subcutaneous and usually given
incidence of bacterial pneumonia together with other HIV agents
good tissue penetration ; affected
cough, diarrhea, muscle and joint pains, increased LFTs by enzyme inhibitors and inducers
Amantadine is also used in treating
parkinsonism ; should be given
within 48hrs of exposure ;
Rimantadine has longer halflife and
doe snot need dose-adjustment for
renally-impaired Px ; there is
GI irritation, dizziness, cerebellar dysfunction (ataxia, dysarthria), increased resistance observed with
livedo reticularis amantadine
DOC for influenza (including H1N1) ;
Oseltamivir is PO while Zanamivir is
intranasal ; Peramivir has been
given temporary emergency use
authorization by US FDA for H1N1 in
GI effects (Oseltamivir), bronchospasm in asthmatics and cough 2009 but has not yet been licensed
with throat discomfort (Zanamivir ) by the US FDA
alopecia, myalgia, severe depression, flu-like syndrome, thyroid slow absorption, given IM or SC
dysfunction, reversible hearing loss, neutropenia ; once a day 3x week but the PEG-
Contraindications include autoimmune disease, history of cardiac form is only given once a week,
arrhythmia and pregnancy given topically for genital warts
Page 69 of 87

Inhibits HBV DNA polymerase causing chain
termination after incorporation into the viral DNA ;
For lamivudine-resistant Hepatitis B infection,
suppresses HBV replication and improves liver
ii. Adefovir, Dipivoxil, Telbivudine, Tenofovir histology and fibrosis
iii. Entecavir guanosine nucleoside, inhibits DNA polymerase
see entry, also active for HBV, rapidly suppresses HBV
iii. Lamivudine (3TC) replication
Inhibits guanosine triphosphate formation, prevents
capping of viral mRNA, blocks RNA-dependent RNA
polymerase, inhibit replication of many DNA and RNA
viruses like Influenza A and B, parainfluenza,
paramyxo viruses, HCV and HIV ; For HCV infection
(with IFN-) and RSV infection, decreases mortality in
iii. Ribavirin viral hemorrhagic fevers
Antiprotozoal Drugs
A. Antimalarial drugs
accumulates in the food vacuole of plasmodia >
Prevents polymerization of heme into hemozoin >
inc heme concentration which is toxic to the parasite,
Blood schizonticide ; For malaria (non-falciparum,
chloroquine-sensitive), DOC for acute attacks of non-
Falciparum and sensitive Falciparum malaria, used as
chemoprophylaxis except in regions where P.
falciparum is resistant, for autoimmune diseases such
i. Chloroquine, hydroxychloroquine as rheumatoid arthritis, amoebic liver abscess
Dipiroxil is a prodrug of Adefovir ;
Telbivudine is a newer drug
(nucleoside analog) but
develpoment of resistance is rapid,
it is as effective as lamivudine ;
Tenofovir is an anti-RT drug that is
also effective in chronic HBV, it is
active against lamivudine and
Lactic acidosis, renal toxicity, severe hepatomegaly with steatosis entecavir-resistant strains
is as effective as lamivudine, longer
headache, dizziness, fatigue, nausea t1/2 of 12hrs
Coinfection between HBV and HIV
may increase the risk of pancreatitis
with lamivudine use ; longer t1/2 in
HBV infected cells than in HIV
(lower dose required in HBV than in
see entry HIV)
given PO, IV or aerosol, avoid
concomitant administration of
anatcids ; Early IV administration of
ribavirin decreases mortality in viral
haemolytic anemia, conjunctival and bronchial irritation, hemorrhagic fevers ; monotherapy
teratogen is NOT effective
May precipitate porphyria ;
Chloroquine is 4-aminoquinoline
derivative, can be given PO and has
high Vd, absorption is decrease by
antacids ; resistance is due to dec.
intracellular accumulation via inc
GI irritation, skin rash, headache, severe skin lesions, peripheral activation of membrane pumps, dec
neuropathies, myocardial depression, retinal damage, auditory intravacuolar accumulation via
impairment, psychosis transporter encoded by pfcrt gene
Page 70 of 87
 Complexes with double stranded DNA to prevent
strand separation > blocks DNA replication and
transcription to RNA, blood schizonticide ; For malaria
(chloroquine-resistant) and severe falciparum malaria
(quinidine), given together with Doxycycline and or
ii. Quinine, Quinidine gluconate Clindamycin to shorten duration of disease
Unknown MOA, blood schizonticide ; For
chemoprophylaxis (chloroquine-resistant areas) ; 1st
line drug (weekly administration) for prophylaxis in all
areas with Chloroquine resistance), alternative to
quinine in acute attacks and uncomplicated infections
iii. Mefloquine from falciparum malaria
8-aminoquinoline, Forms quinoline-quinone
metabolites which are electron-transferring redox
compounds that act as cellular oxidants, tissue
schizonticides, gametocides ; For malaria, eradicates
liver stages of P. vivax and P. ovale (radical cure of P.
vivax and P. ovale), alternative as primary prevention,
iv. Primaquine terminal prophylaxis (vivax, ovale), PCP pneumonia
Atovaquone disrupts mitochondrial electron
transport, blood and tissue schizonticide, proguanil
inhibits folate synthesis, sporonticide ; For treatment
and chemoprophylaxis of chloroquine-resistant
falciparum, protective vs. Mefloquine-resistant
v. Atovaquone-proguanil falciparum
Sequential blockade of folic acid synthesis
(sulfadoxine blocks Dihyrodpteroate synthetase,
Pyrimethamine blocks Dihydrofolate reductase, blood
schizonticide and sporonticide ; For malaria (for
vi. Sulfadoxine-pyrimethamine (Fansidar) Chloroquine-resistant)
Impairs progeny of malarial apicoplast genes,
resulting in abnormal cell division, blood schizonticide
vii. Doxycycline ; For chemoprophylaxis in multi-drug resistant strains
Quinine is commonly used with
doxycycline or clindamycin to limit
cinchonism (headache, tinnitus, vertigo), hemolysis in G6PD toxicities, PO and IV (in severe
deficiency, blackwater fever, blurring of vision, GI upset, infection) ; NEVER use as
disturbance n cardiac conduction ; CI in pregnancy prophylaxis
GI distress, skin rash, headache, dizziness, cardiac conduction
defects, psychiatric disorders (psychosis), neurologic symptoms,
seziures is a 4-quinoline derivatives, PO
Eradicates hypnozoites in the liver,
preventing malarial relapse, PO ,
should be used with a blood
GI distress, pruritus, headaches, methemoglobinemia, hemolysis schizonticide, 14-day course of Tx
in G6PD deficient patients ; CI in pregnancy after Tx with choloroquine
also effective against Mefloquine-
resistant Falciparum infection ;
Proguanil has a t1/2 12-16h ;
abdominal pain, nausea, vomiting, diarrhea, headache, rash, Atovaquone is an alternative for P.
increased liver enzymes jiroveci infection
GI disturbances, teratogen (enamel dysplasia and discoloration), t1/2 is usually >100h, PO, highly
hepatotoxicity, nephrotoxicity, photosensitivity, vestibulotoxicity, protein bound ; pyrimethamine is a
hemolysis sporonticide
GI disturbances, teratogen (enamel dysplasia and discoloration), Do not drink with milk (decreased
hepatotoxicity, nephrotoxicity, photosensitivity, vestibulotoxicity absorption), PO
Page 71 of 87

Unknown MOA, active vs the erythrocytic stage of all
4 strains including Chloroquine-resistant, blood
schizonticide ; For chloroquine-resistant malaria and
viii. Halofantrine , lumefantrine severe falciparum malaria
is metabolized in the food vacuole of protozoa >
Forms toxic free radicals in malarial food vacuole,
ix. Artemsinin, artesunate, artemether, blood schizonticide ; For malaria (falciparum and MDR
dihydroartemsinin strains)
MOA same as chloroquine (inhibits the digestion of
x. Amiodaquine hemoglobin) ; For chloroquine-resistant falciparum
B. Anti-amoebiasis
Unknown MOA, converted to Diloxanide freebase
(active amobecide), luminal amebicide ; DOC for
i. Diloxanide Furoate asymptomatic cyst carrier of E. histolytica
Inhibits protein synthesis by blocking ribosomal
movement along messenger RNA, tissue amebicide ;
back up drug for severe intestinal, hepatic and
ii. Emetine, dehydroemetine extraintestinal amebiasis
halogenated hydroxyquinoline, Unknown MOA,
luminal amebicide ; Alternative to Diloxanide for mild
ii. Iodoquinol to severe intestinal amebiasis
Lumefantrine used in combination
with artemether (Co-arthem) for
uncomplicated falciparum infection
; Halofantrine is never used for
prophylaxis because of
cardiotoxicity and embryogenecity,
abdominal pain, diarrhea, vomiting, cough, rash, headache, Lumefantrine has minimal
pruritus, elevated liver enzymes, cardiotoxicity, teratogen cardiotoxicity
Co-artem is the DOC for
uncomplicated falciparum malaria
in the Philippines ; Combination
therapy of artemesinins with one or
two long-acting antimalarial drugs
(amodiaquine, mefloquine,
sulfadoxine/pyrimethamine or
lumefantrine) is favored to retard
the development and progression
of drug resistance in P. falciparum ;
not given as Prophylaxis due to
short t1/2 (1-3h) ; the only reliably
effective meds vs Quinine-resistant
nausea, vomiting, diarrhea ; SAFE in pregnancy strains
low-cost, given as combination with
agranulocytosis, aplastic anemia Artesunate
converted in vivo into Diloxanide
flatulence, nausea, abdominal cramps freebase which is the amoebicide
Reserved only for situations where
metronidazole cant be used , given
GI distress, muscle weakness, CV dysfunction (arrhythmias and SC or IM , usually given together
CHF) with luminal amebicides
GI distress, thyroid enlargement, skin reactions due to iodine Usually used in combination with
toxicity, neurotoxicity (peripheral neuropathy, visual dysfunction) metronidazole, PO
Page 72 of 87

Reactive reduction by ferredoxin forming free radicals
that disrupt electron transport chain, tissue amebicide
; DOC for severe intestinal wall disease and in hepatic
abscess and other extra intestinal amebic disease,
DOC for trichomoniasis, also used for giardiasis,
bacterial vaginosis (Gardnerella vaginalis), anaerobic
iii. Metronidazole, Tinidazole, Secnidazole infections, H. pylori PUD
An aminoglycoside, Inhibits protein synthesis, binds to
16S ribosomal subunit, luminal amebicide ; For
iv. Paromomycin intestinal amebiasis, cryptosporidiosis
Reactive reductions by ferredoxin forming free
radicals that disrupt electron transport chain, tissue
amebicide ; For metronidazole-resistant amebiasis,
v. Nitazoxanide giardiasis, cryptosporidiosis (DOC)
C.Drugs for Pneumocystis and Toxoplasmosis
Sequential blockade of dihydropteroate synthase
(sulfamethoxazole) and dihydrofolate reductase
(trimethoprim), bactericidal ; DOC for prophylaxis and
treatment of Pneumocystosis, prophylaxis (T. gondii, I.
i. Co-trimoxazole belli)
Unknown MOA but may involve inhibition of glycolysis
or interference with NA metabolism of Protozoans
and Fungi ; For prophylaxis and treatment of
ii. Pentamidine pneumocystosis and trypanosomiasis
Sequential blockade of dihydropteroate synthase
(sulfadiazine) and dihydrofolate reductase
(pyrimethamine) ; DOC for prophylaxis and treatment
iii. Pyrimethamine-sulfadiazine of toxoplasmosis
Atovaquone disrupts mitochondrial electron transport
; For mild to moderate PCP, as chemoprophylaxis for
iv. Atovaquone Chloroquine resistant malaria (with Proguanil)
given PO, IV or topical,
Metronidazole t1/2 is 6-8h,
Tinidazole t1/2 is 12-14h; dose
adjustment in renal patients, well
distributed even in CSF ; active
against protozoan and bacteria
(Bacteroides and Clostridium, DOC
GI irritation, metallic taste, headache, dark urine, leukopenia, for Pseudomembranous colitis) ;
dizziness, ataxia, neuropathy, seizures, disulfiram reaction, causes potentiation of warfarin
opportunistic infections, parestheisa, CI in pregnancy action ; bets taken with meals
may be given together with
tetracycline in mild intestinal
disease ; superior to Diloxanide in
asymptomatic carries but SE limits
headaches, dizziness, rashes, arthralgia its use
may also be used in helminthic
GI distress infections
GI upset, acute hemolysis in G6PD deficiency, nephrotoxicity, Recommended at CD4 count < 200,
hypersensitivity, hematotoxicity, kernicterus given daily, PO or IV
Administered by nasal
respiratory stimulation followed by depression, hypotension, spray/aerosol, given once a month
hypoglycaemia, anemia, neutropenia, hepatitis, pancreatitis, if used for prophylaxis, IV or IM for
inhalant route has minimal SE 21 days if for Tx of active disease
an alternative drug for
Toxoplasmosis is Clindamycin ,give
gastric irritation, glossitis, neurologic symptoms (headache, daily for 3-4 weeks if for Tx of active
insomnia, tremors, seizures), hematotoxicity (megaloblastic toxoplasmosis , if for Toxoplasma
anemia, thrombocytopenia), pseudomembranous colitis encephalitis, give for at least 6
(clindamycin) weeks
abdominal pain, nausea, vomiting, diarrhea, fever, increased liver has increased absorption in the
enzymes presence of food, PO
Page 73 of 87
D. Drugs for Trypanosomiasis
i. Pentamidine
Unknown MOA but may involve inhibition of glycolysis
or interference with NA metabolism of Protozoans
and Fungi ; For hemolymphatic stage of T. gambiense
and T. rhodiense, For prophylaxis and treatment of
pneumocystosis
respiratory stimulation followed by depression, hypotension, do not use for latter stages because
hypoglycaemia, anemia, neutropenia, hepatitis, pancreatitis, it does not cross the BBB, also used
inhalant route has minimal SE for Kala-azar and PCP

Polyanionic compound, Unknown MOA ; DOC for
early hemolymphatic stages of African sleeping
ii. Suramin sickness, Alternative to Ivermectin in onchocerciasis
Suicide inhibitor of ornithine decarboxylase ; DOC for
iii. Eflornithine advanced west African sleeping sickness
Organic arsenical, inhibits enzyme sulfhydryl (-SH)
groups in trypanosomes ; DOC for African sleeping
iv. Melarsoprol sickness
Nitrofurazone derivative, Inhibits trypanothione
reductase which is unique to the parasite ; DOC for
Chagas disease / American Sleeping sickness
(Trypanosoma cruzi), alternative for African sleeping
v. Nifurtimox sickness, also for mucocutaneous leishmaniasis
Drugs for Leishmaniasis
Pentavalent antimony, Inhibits glycolysis or effects on
vi. Sodium Stibogluconate NA metabolism ; DOC for Leishmaniasis
Anthelmintics
Selectively inhibits microtubule synthesis and glucose
uptake in nematodes, ovicidal ; Whipworm infections
(drug of choice), Also a primary drug (together with
albendazole) for ascariasis, pinworm, Trichinosis,
A. Mebendazole Visceral larval migrans (backup)
fatigue, nausea, vomiting, seizures, shock fever, rash, headache, Do not cross blood brain barrier ,
paresthesia, neuropathies, renal abnormalities (proteinuria), Used in combination with
chronic diarrhea, haemolytic anemia and agranulocytosis melarsoprol
diarrhea, vomiting, anemia, thrombocytopenia, leukopenia,
seizures Crosses blood brain barrier, PO, IV
Crosses BBB, administered
parenterally because it causes GI
GI irritation, reactive encephalopathy upset
nausea, vomiting, fever, rash, restlessness, insomnia,
neuropathies, seizures Does not cross BBB
IV ; alternative for leishmaniasis are
as follows: Pentamidine or
Miltefosine (for visceral
leishmaniasis), Fluconazole or
Metronidazole (for cutaneous
GI symptoms, fever, rash, arthralgia, healdache, myalgia, sterile leishmaniasis) and Amphotericin B
abscesses, cardiotoxicity (for mucocutaneous leishmaniasis)
Greatly affected by enzyme
inducers and inhibitors ;
Contraindicated in pregnancy, Use
cautiously in patients with Cirrhosis
GI irritation, agranulocytosis, alopecia, Elevated liver enzymes and children <2y.o.

Page 74 of 87

Inhibits microtubule assembly, larvicidal and ovicidal ;
DOC for Ascariasis, Hookworm, Pinworm, Hydatid
disease ; Also used for Whipworm infections,
Cutaneous & Visceral Larva migrans, Cysticercosis
(larval stages of T. solium), Angiostrongylus
B. Albendazole cantonensis, Capillaria philippinensis
Immobilizes microfilariae by an unknown mechanism
> inc susceptibility to host defense mechanism ;
C. Diethylcarbamazine DOC for filariasis and eye worm disease (Loa-Loa)
Intensifies GABA-mediated neurotransmission in
nematodes > immobilizes parasites > removal by
reticuloendothelial system ; Used for Strongyloidiasis
(drug of choice), Onchocerciasis, Cutaneous larva
D. Ivermectin migrans, Filariasis (back up)
Stimulates nicotinic receptors at NMJ of nematodes
> depolarization-induced paralysis, Causes release
of ACh and inhibition of Cholinesterase, Kills adult
worms not eggs ; DOC for pinworm, may be used also
for Hookworm, Trichostrongylus and Ascaris
E. Pyrantel pamoate infections
Structural congener of Mebendazole, same MOA as
Mebendazole, Selectively inhibits microtubule
synthesis and glucose uptake in nematodes, Inhibits
fumarate reductase. Ovicidal, has anti-inflammatory
and immunosuppressive action in the host ; Used for
F. Thiabendazole Trichinosis (drug of choice), Strongyloidiasis (backup)
primary drug for ascariasis,
ancylostomiasis, trichuriasis ; safety
in pregnant and children is not yet
established ; Improved penetration
(> Praziquantel) of the
subarachnoid space in
Neurocysticersosis
reversible leukopenia, alopecia, elevation of liver function tests, Should not be given to patients with
bone marrow suppression Cirrhosis
headache, malaise, weakness, anorexia, filarial fever (fever, May cause mazzotti reaction when
rashes, ocular damage, joint and muscle pain, lymphangitis) used for onchocerciasis
Antidote for Mazzoti reaction:
antihistamine and NSAIDs ; CI in
pregnancy, children 5 y.o. and Avoid
Mazzotti reaction (fever, headache, dizziness, rashes, pruritus, concomitant use with other drugs
tachycardia, hypotension, pain in muscles and joints and lymph that enhance GABA activity
glands), corneal opacities (Barbituraates, BZDs etc)
Contraindicated in patients with
hepatic dysfunction (may cause an
increase in LFT) ; No study on
GI distress headache, weakness, dizziness, insomia, rash, fever, pregnant and children <2y.o.
Gastrointestinal irritation, Headache, Dizziness, Drowsiness,
Leukopenia, Hematuria, Hypersensitivity reactions (SJS),
Hepatotoxicity (intrahepatic cholestasis, liver failure), Reactions CI in renal and liver disease and in
caused by dying parasites pregnancy
Page 75 of 87
 Increases membrane permeability to calcium >
contraction of trematode and cestode muscle >
muscle paralysis, vacualization and death ; DOC for
trematodes (schistosoma, paragonimus, clonorchis,
opistorchis, Fasciolopsis, Heterophyes) and cestodes
(taenia, diphyllobothrium, Hymenopelsis) together
with Niclosamide ; for infection by small and large
intestinal flukes ; alternative to Albendazole in
G. Praziquantel Cysticerci
Uncouples oxidative phosphorylation or by activating
ATPases, scoleces and segments are killed but NOT
Ova ; alternative drug to Praziquantel for cestode
infection (Taenia, Diphyllobotrium), not effective in
cystecercosis (use Albendazole or Praziquantel
instead) or Hydatid disease (use Albendazole),
effective in the Tx of infections from small and large
H. Niclosamide intestinal flukes
GABA agonist > paralyze ascaris > expelled by
normal peristalsis , block ACh at the myoneural
junction --> expulsion via normal peristalsis ; As
I. Piperazine alternative for ascariasis
Unknown MOA ; co-DOC (with Triclabendazole) for Tx
of Fascioliasis (sheep liver fluke), as alternative for
J. Bithionol paragonimiasis
an organophosphate prodrug > Dichlorvos (AchE
inhibitor) -> muscle contraction > paralysis ; Active
K. Metrifonate vs Schistosoma haemoatobium
effective solely in Schistosoma mansion (intestinal
bilharziasis) - on male immature forms and adult
L. Oxamniquine schistosomal forms ; MOA is unknown
Used with steroid when treating
neurocysticercosis to dec swelling ,
contraindicated in ocular
cysticercosis (may cause irreparable
eye damage) ; May be used as an
headache, dizziness, nausea, malaise, Inc ICP, seizure adjunct to Albendazole in Hydatid
(neurocystecercosis) ; CI in pregnancy disease
Avoid ethanol consumption for 48
hours upon drug consumption ;
Safety in children <2y.o. and
GI distress, headache, rash, fever pregnanct not yet established
Contraindicated in pregnancy,
impaired renal or hepatic function
or with a history of epilepsy or
GI upset chronic neurologic disease
Nausea,vomiting, diarrhea, abdominal cramps, phototoxicity, rash do not use in Px <8y.o.
Excess cholinergic stimulation (DUMBBELSS) CI in pregnancy
GI upset, pruritus, eosinophilia, urticaria, pulmonary infiltrates,
fever, orange-red discoloration of urine ; CI in pregnancy and Px is not allowed to drive within
seizure disorder, proteinuria, microscopic hematuria, 24hrs after intake of Oxamniquine
Page 76 of 87
Cancer Chemotherapy
A. Alkylating agents
i. Nitrogen Mustards: Cyclophosphamide, Chlorambucil,
Mechlorethamine
ii. Platinum Analogs: Cisplatin, Carboplatin, oxaliplatin
iii. Alkyl sulfonate: Busulfan
iv. Nirtosoureas: Carmustine, lomustine
v. Others: Procarbazine, Dacarbazine
B. Antimetabolites
all are Cell-cycle non-specific ; Universal MOA: form
reactive molecular species that alkylate nucleophilic
groups on DNA bases, particularly the N-7 of guanine
leading to cross-linking of bases, abnormal base
pairing and DNA strand breakage
Forms DNA cross-links, resulting in inhibition of DNA
synthesis and function, Cell-cycle nonspecific,
Mechlorethamine has additional MOA: converts to a
reactive cytotoxic product ; For non-hodgkins
lymphoma, breast cancer, ovarian cancer,
neuroblastoma, CLL
Forms DNA cross-links, resulting in inhibition of DNA
synthesis and function, Cell-cycle nonspecific ;
component of regimen For testicular cancer, ovarian
cancer, bladder cancer and lung cancer ; Oxaliplatin is
used also for advanced colon CA
Forms DNA cross-links, resulting in inhibition of DNA
synthesis and function, Cell-cycle nonspecific ; For
CML
Forms DNA cross-links, resulting in inhibition of DNA
synthesis and function, Cell-cycle nonspecific ; For
brain tumors, melanoma, skin cancer
a reactive agent which forms hydrogen peroxide,
which generates free radicals that cause DNA strand
scission, cell cycle non-specific ; component of reigned
For Hodgkins lymphoma, non-hodgkins lymphoma,
brain tumors
all are cell-cycle specific , they also have
immunosuppressant action
bone marrow suppression, hemorrhagic cystitis, hepatotoxicity,
alopecia, SIADH, pulmonary toxicity, cardiac dysfunction ;
Mechorethamine SE include marked vesicant action, sterility,
myelosuppresion, alopecia
nausea, vomiting, nephrotoxicity, neurotoxicity (peripheral
neuritis), ototoxicity (acoustic nerve damage), hematotoxicity
pulmonary fibrosis, adrenal insufficiency, skin pigmentation
CNS toxicity (dizziness, ataxia), nausea and vomiting, bone
marrow suppression, skin flushing
bone marrow suppression, pulmonary toxicity, hemolysis,
disulfiram reaction,skin reactions, peripheral neuropathy, CNS
dysfunction
Resistance is due to increased DNA
repair, decreased drug permeability
and production of trapping agents
such as thiols
Rescue therapy is MESNA and
hydration; metabolite is acrolein
which is important for
Cyclophosphamides anti-cancer
effect and also its toxicity
IV, Rescue therapy is Amifostine,
decreased nephrotoxicity by giving
mannitol with forced hydration ;
Carboplatin is less nephrotoxic but
has more myelosuppression
Spares the bone marrow
Highly lipophilic allowing ease of
passage through BBB into the CNS
PO, can pemetrate the CSF,
LEUKEMOGENIC, CPY450 inhibitor,
Dacarbazine is phototoxic

Page 77 of 87

i. Folate antagonist: Methotrexate
ii. Purine antagonist: 6-Mercaptopurine, 6-thioguanine,
fludarabine, cladribine
iii. Pyrimidine antagonist: 5-Fluorouracil
iv. Pyrimidine antagonist: Cytarabine (ARA-C)
Inhibits dihydrofolate reductase, decreases synthesis
of thymidylate, amino acids, purine nucleotides >
interfere with NA and CHON metabolism ; cell cycle
specific ; For choriocarcinoma, acute leukemia, non-
hodgkin, primary CNS lymphoma, breast cancer, head
and neck cancer, bladder cancer ; also for psoriasis,
rheumatoid arthritis, ectopic pregnancy
are activated by hypoxanthie-guanine
phosphoribosyltransferase (HGPRT) to toxic
nucleotides which inhibit enzymes in purine
metabolism > Inhibits de novo purine nucleotide
synthesis , cell cycle specific ; For acute leukemia
(AML, ALL), CML
converted to 5-fluoro-2-deoxyuridine-5-
monophosphate (5-FdUMP) which Inhibits
thymidylate synthase, incorporation inhibits DNA
synthesis and function, cell cycle specific ; For bladder
cancer, breast cancer, colorectal cancer, anal cancer,
head and neck cancer, liver cancer and ovarian
cancer, topically for keratoses and superficial basal
cell skin cancer
a cytosine arabinoside, activated by kinases to Ara-
Cytidine Triphosphate (AraCTP) which Inhibits DNA
polymerase > inhibition of DNA synthesis and
repair, inhibits ribonucleotide reductase with reduced
formation of dNTPs, cell cycle specific ; For AML, ALL,
CML
PO, IV, Rescue therapy is Leucovorin
(Folinic acid) ; cytotoxic due to
formation of polyglutamate
derivatives ; resistance is due to
decreased drug accumulation,
changes in drug sensitivity or
activity of DHF reductase and
decreased formation of
polyglutamates ; clearance is
dependent on renal function
therefore adequate hydration is
bone marrow suppression, pulmonary infiltrates and fibrosis, important to prevent crystallization
mucositis, crystalluria, hepatotoxic into stones
6-MP metabolism inhibited by
allopurinol and febuxostat ,
Resistance is due to decreased
activity of HGPRT, increased alkaline
phosphatase activity (which
inactivates the toxic nucleotide) ,
bone marrow suppression, hepatic dysfunction (necrosis, undergo significant FPE (by xanthine
jaundice, cholestasis) oxidase)
IV, can distribute to CSF, causes
thymineless death of cells,
Resistance is due to decreased
activation of 5-FU, increase
thymidylate synthase activity and
decreased sensitivity of this enzyme
; another metabolite is 5-
florouridine-5triphosphate (FUTP)
which incorporates into RNA >
interfere with RNA processing and
bone marrow suppression, GI irritation, alopecia function
Most specific for the S-phase of the
cell cycle, Resistance is due to
decreased uptake and decreased
conversion to AraCTP, a cytosine
GI irritation, bone marrow suppression, neurotoxicity arabinoside
Page 78 of 87

v. Pyrimidine antagonist: Gemcitabine
C. Natural Anticancer Drugs
i. Vinca alkaloid: Vincristine, Vinblastine, Vinorelbine
ii. Podophyllotoxin: Etoposide, Teniposide
iii. Camptothecins: Topotecan, Irinotecan
iv. Taxanes: Paclitaxel, Docetaxel
a deoxycytidine analog, converted to Gemcitabine
diphosphate which inhibits ribonucleotide reductase
with reduced formation of deoxyribonucleotide
triphosphate required for DNA synthesis, Gemcitabine
triphosphate is incorporated into DNA causing chain
termination, cell cycle specific ; For pancreatic cancer,
bladder cancer, non-small cell lung cancer, non-
Hodgkins lymphoma bone marrow suppression, neutropenia, pulmonary toxicity a deoxycytidine analog
all are cell-cycle specific
Prevents assembly of tubulin dimers into microtubule
assembly blocking the formation of mitotic spindles,
causes cell arrest at metaphase, cell cycle specific ;
For acute leukemias, lymphomas, wilms tumor and IV, highly distributed except in CSF,
neuroblastoma ; Vinblastine For lymphomas, Acts primarily in M phase of cancer
neuroblastomas, testicular carcinoma and Kaposi cell cycle, Resistance is due to
sarcoma ; Vinorelbine For non-small cell lung cancer increased efflux of drugs via
and breast cancer Neurotixicity (areflexia, peripheral neuritis, paralytic ileus) membrane drug transporter
Induces DNA breakage by inhibiting DNA
topoisomerase II, inhibits mitochondrial electron
transport, cell cycle specific ; Combination regimen PO, high Vd ; dose adjustment in
For lung cancer, prostate cancer, testicular cancer, renal patients ; Act on the Late S
non-hodgkins lymphoma, germ cell and gastric cancer bone marrow suppression, alopecia, GI distress and early G2 phase
Inhibits DNA topoisomerase I which cute and
relegates single DNA strands during normal DNA
repair, cell cycle specific; For advanced ovarian cancer
(2nd line), small cell lung cancer, Irinotecan For Irinotecan can be used for
metastatic colorectal cancer bone marrow suppression, diarrhea metastatic colorectal cancer
Interferes with mitotic spindle synthesis by preventing
microtubule disassembly into tubulin monomers, cell
cycle specific ; For solid tumors - advanced breast and
ovarian cancer, lung cancer, gastroesophageal cancer, Paclitaxel (neutropenia, thrombocytopenia, peripheral
prostate cancer, bladder cancer, head and neck neuropathy, hypersensitivity),
cancer Docetaxel (neurotoxicity, bone marrow suppression) Act on M phase
Page 79 of 87
D. Antitumor antibiotics
Intercalates between base pairs, inhibits
topoisomerase II, generates free radicals, blocks
synthesis of RNA and DNA causing DNA strand
scission, causes membrane disruption, cell cycle non-
specific ; Doxorubicin For Hodgkins and Non-Hodgkins
lumphoma, myelomas, sarcomas, breast cancer,
endometrial cancer, lung cancer, ovarian cancer and
thyroid cancer ; Daunorubicin For acute leukemias
Idarubicin For AML, Epirubicin For breast cancer and
gastroesophageal ; Mitoxantrine For acute myeloid
i. Anthracycline: Doxorubicin, Daunorubicin, Idarubicin, leukemias, Non-Hodgkins lymphoma, breast and alopecia, nausea, vomiting, Cardiotoxicity (dilated Rescue therapy is Dexrazoxane and
Epirubicin, Mitoxantrone gastroesophageal cancer cardiomyopathy, CHF) liposomal formulation of the drug
Generated free radicals which bind to DNA and causes
DNA strand breaks leading to inhibition of DNA
synthesis, intercalates with DNA, cell cycle specific ; IV, inactivated by tissue
Component of regimens in Hodgkins lymphoma and aminopeptidases, Most specific for
testicular cancer, lymphomas and squamous cell pneumonitis, pulmonary fibrosis, alopecia, mucocutaneous the G2 phase of cell cycle, a
ii. Bleomycin cancer, head and neck cancer, skin cancer reactions, hypersensitivity reactions glycopeptide
Binds to double stranded DNA, inhibits DNA-
dependent RNA synthesis, cell cycle non-specific ; For
melanoma, wilms tumor, choriocarcinoma, Kaposi
iii. Actinomycin D sarcoma bone marrow suppression, skin reactions, GI irritation None
Metabolized into an alkylating agent that cross-links
DNA ; In combination regimens for adenocarcinoma
iv. Mitomycin C of the cervix, stomach, pancreas and lungs severe myelosuppression, toxic the heart, liver, lungs and kidneys IV, used for hypoxic tumor cells
E. Miscellaneous Anticancer Drugs
Tyrosine kinase inhibitor of the protein product of Resistance is due to mutation is bcr-
i. TK inhibitor: Imatinib, Dasatinib, Nilotinib bcr-abl oncogene in CML ; For CML, GIST diarrhea, myalgia, fluid retention, CHF abl gene
ii. Growth Factor Receptor Inhibitor
recognizes a surface protein in breast CA cells that
overexpress Her-2-neu receptors for epidermal
a. Her-2-neu inhibitor: Trastuzumab growth factor nausea, vomiting, chills, fever, headache, cardiotoxicity (CHF) None

Page 80 of 87
 EGFR (Epidermal Growth Factor Receptor) regulate
signaling involved in cellular proliferation, invasion
and metastasis and angiogenesis, it also inhibits
cytotoxic activity of some anti-cancer and radiation
treatment, Gefitinib and Erlotinib are capable of
inhibiting EGFRs Tyrosine Kinase domain ; Cetuximab
(+ Irinotecan and Oxalipatin) For metastatic colon
cancer and Head and Neck cancer ; Panitumumab For
b. EGFR inhibitor: Cetuximab, Panitumumab, Gefitinib, refractory colorectal cancer ; Gefitinib and Erlotinib as Erlotinib can also be used for
Erlotinib second-line agents for non-small cell lung cancer folliculitis, diffuse hair loss, dry skin, paronychia advanced pancreatic cancer
VEGF (Vascular Endothelial Growth Factor) has a role
in angiogenesis required for metastasis, Inhibits
binding of VEGF to VEGFR leading to inhibition of
VEGF signalling, inhibits tumor vascular permeability
but enhances tumor blood flow and drug delivery ;
Sorefenib Sunitinib and Pazopanib inhibits multiple
receptor Tyrosine Kinase including those associated to
c. VEGF Inhibitor: Bevacizumab, Sorafenib, Sunitinib, VEGF ; For metastatic colorectal cancer, breast cancer, hypertension, arterial thrombosis, impaired wound healing, may also be used in non-small cell
Pazopanib diabetic retinopathy proteinuria, GI perforation lung CA and renal CA
Binds to a surface protein in NHL cells, induces
complement-mediated lysis, direct cytotoxicity and
induction of apoptosis ; For Non-Hodgkins lymphoma
iv. Rituximab and other lymphomas hypersensitivity reaction, bone marrow suppression None
Endogenous glycoproteins with antineoplastic,
immunosuppressive and antiviral actions ; For hairy alopecia, myalgia, depression, thyroid dysfunction, hearing loss,
v. Interferon alpha cell leukemia, early CML, T-cell lymphoma bone marrow suppression None
Depletes serum asparagine ; For ALL, T-cell
auxotrophic CA (leukemia and lymphomas) that
vi. Asparaginase require asparagine for growth acute pancreatitis, bleeding, severe hypersensitivity reaction None
Allows DNA transcription and differentiation of Only vitamin that can cure cancer,
immature leukemic promyelocytes into mature retinoic acid syndrome (dyspnea, fever, weight gain, peripheral treat retinoic acid syndrome with
vii. All-Trans retinoic acid granulocytes ; For acute promyelocytic leukemia edema) dexamethasone
a reversible inhibitor of 26s proteasome in
viii. Protease Inhibitor: Bortezomib mammalian cell ; For multiple myeloma peripheral neuropathy, thrombocytoppenia
F. Hormonal Anticancer Agents
Suppresses inflammation and immune response, may
trigger apoptosis and work on nondividing cancer cells adrenal suppression, growth inhibition, muscle wasting,
i. Prednisone ; For CLL, Hodgkins lymphoma, leukemia, lymphoma osteoporosis, salt retention see entry

Page 81 of 87

ii. SERM: Tamoxifen, Toremifene
iii. Androgen antagonist: Flutamide
iv. GnRH analog: Leuprolide, Goserelin Nafarelin
v. Aromatase inhibitor: Anastrazole, Letrozole
Drugs Used in the Treatment of Gastrointestinal Diseases [Divided into 2 classes: agents that reduce intragastric acidity and agents that promote mucosal defense
A. Antacids: Magnesium-Aluminum Hydroxide, Calcium
carbonate, Sodium bicarbonate
Estrogen antagonist actions in breasts tissue and CNS,
estrogen agonist effects in uterus, liver and bone ; For
hormone-responsive breast cancer, Toremifene For
advanced breast cancer
Androgen antagonist ; For prostate cancer
Increased LH, FSH secretion with intermittent
administration, reduced LH and FSH secretion with
prolonged continuous administration ; For prostate
cancer
Reduces estrogen synthesis by inhibiting aromatase;
For advanced breast cancer
Neutralize stomach acid by reacting with protons in
the lumen ; For peptic ulcer disease, Gastroesophagal
reflux
hot flushes, thromboembolism, endometrial hyperplasia, Prevents osteoporosis and decrease
endometrial cancer risk of atherosclerosis
GnRH analogs (leuprolide) must be
co-administered to prevent acute
gynecomastia, hot flushes, impotence flare-up of prostate cancer
hot flushes, sweats, headache, osteoporosis, gynecomastia,
gynecomastia, testicular atrophy, impotence, bone pain see entry
nausea, diarrhea, hot flushes, bone and back pain, dyspnea, Effective againsts breast cancer that
peripheral edema have become resistant to tamoxifen
Impairs absorption of tetracyclines,
flouroquinolones,itraconazole and
iron --> should not be given within 2
hours with these drugs ; When used
regularly in large doses needed to
significantly raise the stomach pH,
antacids, decrease recurrence rate
of peptic ulcers ; Aluminum and
Magnesium are always given
Sodium bicarbonate: Belching, metabolic alkalosis. Calcium together to cancel out each other's
carbonate: hypercalcemia, renal insufficiency, metabolic alkalosis adverse effects ; Avoid in renally
(milk-alkali syndrome) exc for Aluminum Magnesium Hydroxide impaired patients ; DOA: 1-2 hours
Page 82 of 87

B. H2 receptor antagonist: Cimetidine, Ranitidine,
Famotidine, Nizatidine
C. Proton Pump Inhibitor: Omeprazole, Lansopraole,
Rabeprazole, Pantoprazole, Esomeprazole
D. Mucosal Protective Agent:
i. Sucralfate
ii. Bismuth Salicylate
Competitive pharmacologic block of H2 receptors ;
For peptic ulcer disease, Zollinger-Ellison syndrome,
Gastroesophagal reflux, dyspepsia
Irreversible blockade of H/K ATPase in active gastric
parietal cells, Long lasting reduction of meal
stimulated and nocturnal acid secretion ; For Peptic
ulcer disease(DOC), Zollinger-Ellison syndrome,
Gastroesophageal reflux, dyspepsia
polymerizes in acidic environmet > polymers bind to
injured tissue and forms a protective covering over
ulcer bed, Accelerates healing of peptic ulcers and
reduces recurrence rate ; For Peptic ulcer disease
forms a protective coating on ulcerated tissue,
stimulates mucosal protective mechanisms, direct
antimicrobial effects and sequestration of
enterotoxins ; For Peptic ulcer disease, Dyspepsia,
Gynecomastia (cimetidine only), Diarrhea, headache, fatigue,
Myalgias, constipation, Nosocomial pneumonia, Mental status
changes, Bradycardia, Hypotension, Blood dyscrasias
Diarrhea, headache, abdominal pain, Malabsorption syndrome
(Vit B12, Ca, Fe, Zn, Digoxin, Ketoconazole), Infections
(respiratory, enteric), Hypergastrinemia, Atrophic gastritis
constipation, dizziness, flatulence, dry mouth
Black stools, darkening of tongue, Encephalopathy (Atraxia,
headaches, confusion, seizures)
Cimetidine is a potent inhibitor of
CYP450. Highly effective in
suppressing nocturnal acid
secretion but only modest effect on
meal- stimulated secretion ; avoid
in renally and hepatically (severe)
impaired patients ; are highly
selective and does not affect H1 and
H3 receptors, may also reduce
seceretion of pepsin ; DOA: 6-10hrs
; Reduces acid secretion by 60-70%
usually enetric coated, t1/2 is 1-
2hrs but DOA of is around 24hrs,
needs 3-4 days treatment to
achieve full effectiveness ;
decreases bioavailability drugs that
require acidity for GI absorption ;
when used for PUD together with 2
antibiotics, achieve 90% cure ;
Reduces acid secretion by 90-98% ;
should be taken on an empty
stomach since food decreases its
bioavailability by 50%
Highly insoluble, requiring frequent
dosing (QID) ; chemically: Aluminum
Sucrose Sulfate
Reduces stool frequency and
liquidity in infectious diarrhea
Page 83 of 87

iii. Misoprostol
E. Prokinetics
i. Metoclopramide, Domperidone, Erythromycin,
Neostigmine
F. Laxatives
i. Bulk-forming: Psyllium, Methylcellulose, Polycarbophil
ii. Stool-softener: Docusate, Glycerine, Mineral oil
iii. Osmotic: Lactulose, Magnesium oxide, Magnesium
hydroxide, Sorbitol, Magnesium citrate, Sodium
phosphate, Polyethylene Glycol
iv. Stimulant: Bisacodyl, Aloe, Senna, Cascara, Castor oil
v. Miscellaneous: Lubiprostone, Methylnaltrexone,
Alvimopan
Infectious diarrhea
PGE1 analog, Activates EP receptors, causes increased
HCO3 and mucus secretion and inhibits acid secretion
in the stomach, causes uterine contraction ; For
Peptic ulcer disease, Prevention of NSAID-induced see entry, decreases ulcer in NSAIDs
gastric mucosal injury, Abortifacient Abdominal pain, Diarrhea, Uterine cramping, Miscarriage induced ulceration
Metoclopramide and domperidone block D2
receptors, Erythromycin stimulates motilin receptor,
Increases gastric emptying and intestinal motility ; As
Antiemetic for post operative/chemotherapy Domperidone does not cross the
vomiting, Diabetic gastroparesis (drug of choice), BBB (less toxic) ; Increases LES
Neostigmine for acute large bowel distention Parkinsonism, Extrapyramidal effects, Hyperprolactinemia pressure (helpful in GERD)
Indigestible, hydrophilic colloids that absorb water,
forming a bulky emollient gel that distends the colon
and promotes peristasis ; For constipation Diarrhea None
Soften stool material, Permitting water and lipids to Diarrhea, Aspiration,(Lipid pneumonitis), Malaabsorption of fat-
penetrate the stool ; For constipation soluble vitamins (A, D, E, K) None
Soluble but nonabsorbable compound that result in
increased stool liquidity due to an obligate increase in
fecal fluid ; For Constipation, Hepatic encephalopathy Diarrhea, Flatus, Abominal cramps, Electrolyte abnormalities
(lactulose), Preparation for endoscopy (polyethylene (hyperphosphatemia, hypocalcemia, hypernatremia, hypokalemia,
glycol) hypermagnesemia) None
Unknown. Directly stimulate enteric nervous system
and colonic electrolyte and fluid secretion Diarrhea can cause melanosis coli
Lubiprostone is a Chloride channel activator which
stimulates Cl secretion into the intestines leading to
increased fecal fluid content, Methylnaltrexone and
Alvimopan are Opioid receptor antagonist that block
intestinal mu receptors, but not the CNS mild nausea, stomach pain, mild diarrhoea, bloating, headache NONE
Page 84 of 87

G. Anti-diarrheals: Diphenoxylate, Loperamide,
Kaolin+Pectin, Colloidal Bismuth
H. Drugs for IBS
Activates opioid receptors in enteric nervous system.
Slows motility with negligible CNS effects, Kaolin
(+pectin) absorbs bacterial toxin and fluid leading to
decreased stool liquidity ; for Diarrhea (nonspecific,
noninfectious)
Do not use in children less than 4
years of age (increased chance of
causing paralytic ileus), Reverse
ileus by administering Betanechol.
Drowsiness, Nausea, Paralytic ileus, interfere with absorption of Direct m-agonist, Kaolin is hydrated
other drugs Magnesium Aluminum Silicate

i. laxatives, antidiarrheals and low-dose TCA see entry see entry see entry
see entry ; antispasmodic for abdominal pain, for IBS
ii. Anticholinergics: Dicylomine, Hyoscyamine with prominent diarrhoea see entry see entry
iii. 5HT3 antagonist: Alosteron see entry ; For IBS with severe diarrhoea severe constipation, ischemic colitis see entry
see entry ; activate type2 chloride channels in small
iv. Lubiprostone intestines ; For IBS with predominant constipation see entry see entry
I. Anti-emetics
Blocks chemoreceptor trigger zone and enteric
nervous system 5-HT3 receptors ; For Vomiting (Post Headache, Dizziness, Constipation, QRS and QT prolongation
i. Ondansetron, Granisetron, Dolasetron, Palonosetron chemothereaphy, postoperative) (Dolasetron only) see entry
antagonist of the Neurokinin-1 receptor in the areas
postrema that is activated by substance P and other
tackykinins ; For post-chemotherapy nausea and
ii. Aprepitant vomiting fatigue, dizziness, diarrhea an enzyme inhibitor
iii. Scopoloamine see entry ; For motion sickness emesis see entry see entry
J. Drugs for IBD
Unknown. Probably inhibits production of eicosanoid
inflammatory mediators (PG and LT) and interfering
i. Aminosalicylates: Mesalamine, Balsalazine, Olsalazine, with cytokines ; For Inflammatory bowel disease (mild Gastrointestinal upset,Headaches, Arthralgias, Myalgias, Bone Not useful for treating active flare
Sulfasalazine to moderate) marrow suppression, Malaise, Hypersensitivity reactions ( severe) ups of disease

ii. Other agents: Antibiotics, Immunosuppressibe see entry ; Natalizumab is a Mab that blocks intergrins
antimetabolites (Azathioprine, 6-MP, Methotrexate), anti- in circulating leukocytes, restricted to severe
TNF (Infliximab), Natalizumab refractory Crohns disease multifocal leukoencephalopathy see entry
K. Miscellaneous Agents

Page 85 of 87

i. Pancreatic lipase: Pancreatin or Pancrealipase
ii. Drugs that inhibit formation of Gallstones: Ursodiol
For pancreatic enzyme replacement, improve
digestion of fats proteins and carbohydrates ; For
pancreatic insufficiency due to Cystic Fibrosis,
pancreatitis and pancreatectomy hyperuricemia Taken with every meal
a bile acid derivative that decreases cholesterol
content of bile by decreasing hepatic cholesterol
secretion and other effects on hepatocyte canalicular
membrane ; For gallstone in patients refusing or not headache, dizziness, mild stomach pain, rhinorrhea, sore throat,
eligible for surgery rash hair loss None

Drugs Used For Cough

decrease sputum activity ; Usually derivatives of

A. Mucolytics : N-acetylcysteine, Carbocysteine, Ambroxol
cysteine; reduce disulfide bridges that bind
glycoproteins to other proteins such as albumin ; Also
act as antioxidants & may reduce airway inflammation
; Orally available drugs are well-tolerated; but of little
benefit in acute respiratory condition
Chest tightness, Disagreeable odor, Drowsiness, Fever,
Hemoptysis, Increased volume of bronchial secretions, Irritation
of tracheal or bronchial tract, Nausea, Rhinorrhea, Stomatitis, available as IV, PO, IM and
Vomiting inhalational forms

may act as an irritant to gastric vagal receptors, and Drowsiness, Incomplete or Infrequent Bowel Movements,
recruit efferent parasympathetic reflexes that cause Inducing of a Relaxed Easy State, Stomach Cramps, dizziness or Are often emetics (ipecac,
B. Expectorants: Guiafenesin glandular exocytosis of a less viscous mucus mixture. headache, a rash, or. nausea, vomiting, or stomach upset guaifenesin)

DO NOT suppress in bacterial lung

infections, asthma, bronchiectasis
(suppurating bronchial
inflammation) or chronic bronchitis
Used for dry painful cough of neoplasia or pleural where antitussives can cause
disease ; Irritative cough in inflammation of the harmful sputum thickening &
C. Antitussives respiratory tract (epiglottitis); in hemoptysis retention

Page 86 of 87

i. Centrally-acting: Opioid antitussives (codeine,
dextromethorphan)
ii. Centrally-acting: Non-opioid (butamirate citrate)
iii. Peripherally-acting: Levodropropizine
decreased sensitivity of the medullary/ CNS cough
centers to peripheral stimuli and decreased mucosal
secretion
act through receptors in the brainstem to inhibit
cough
Non-opoid drug with a peripheral action by inhibiting
the afferent pathways that generate the cough reflex
(modulates C-fibre activity)
Morphine may be effective but
indicated only in intractable cough
from bronchial carcinoma ;
Dextromethorphan has no addictive
Decreases secretions in the bronchioles, thickens sputum & potential, no analgesic effect,
inhibits ciliary activity, reducing clearance of thickened sputum, produces less constipation and
Constipation inhibition of mucociliary clearance
Centrally acting antitussive but is
neither chemically or
Somnolence, nausea, vomiting, diarrhea, dizziness and pharmacologically related to
hypotension opioids
does not cause side effects such as
constipation or respiratory
Nausea, vomiting, heartburn, diarrhea, fatigue, weakness, depression which can be produced
drowsiness, dizziness, headache, palpitations by opioid antitussives
Page 87 of 87