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Comprehensive Pharmacology Summary By: Mr Ednan and FPGEE October Group

Drug Mechanism of action Side effect Interaction Contraindications:


1 Antiepileptic: Many typical anticonvulsants Carbamazepine: NV, Carbamazepine Carbamazepine: CBC should be
Seizures: work by blocking Jaundice, abdominal pain, pale Antiepileptic drugs, monitored; can lower white blood
Anticonvulsants voltagesensitive sodium stool, darkened urine, unusual antibiotics, isoniazid, cell count.
Carbamazepine channels in the brain. bruising bleeding, fever, sore cimetidine, Therapeutic drug monitoring is
(drug of choice in Phenobarbital potentiates synaptic throat, ulcer in the mouth, propoxyphene, required Caution: in patients with
Parial inhibition through an action on dizziness, drowsiness, diltiazem, verapamil, bone marrow depression,
and tonic cloinc GABA receptor. unsteadiness. CCB, warfarin, TCAs glaucoma and elderly.
seizures) Ethosuximide inhibits calcium ion Phenytoin: NV, swollen and grapefruit juice. REM dermatological reactions,
Phenytoin influx through T type channels in gums, rash, swollen glands, Phenytoin blood dyscrasias, suicidal thoughts
Phosphenytoin the thalmic neurons. bleeding, jaundice, fever, sore Antiepileptic drugs, and behavior.
Oxcarbamazepine Gabapentin promotes the release of throat. disulfiram, isoniazid, PhenytoinMyocardial insufficiency
Clonazepam GABA. Phosphenytoin: Similar to chloramphenicol, hypotension, renal failure and
Ethosuximide (drug Absence seizures (sometimes phenytoin. propoxyphene, elderly.
of choice in referred to as petit mal seizures) Oxcarbazepine: NV, corticosteroids, Clonazepam
absence involve an interruption to dermatological reactions, digitoxin, doxycycline, Caution: Patients with psychoses,
seizures) consciousness where the person dizziness, somnolence, estrogens, furosemide, acute narrow-angle glaucoma, and
Felbamate experiencing the seizure seems to headache, ataxia, fatigue, oral contraceptives, significant liver disease.
Gabapentin become vacant and unresponsive cognitive symptoms, vertigo, quinidine, rifampin, REM: withdrawal symptoms with
Lamotrigine for a short period of time (usually abdominal pain, abnormal theophylline, vit D, abrupt discontinuation, suicidal
Phenobarbital (drug up to 30 seconds). gait, tremor, diplopia, enteral nutritional thoughts and behavior.
of choice of febrile Slight muscle twitching may occur. nystagmus, abnormal vision. therapy, coumarin, Ethosuximide Avoid exposure to
seizures and grand Tonic-clonic seizures (sometimes Hyponatremia. warfarin, TCAs,DM, sunlight and ultraviolet light and
mal seizures in referred to as grand mal seizures), Clonazepam drowsiness, arthritis drugs. alcoholic beverages
children) involve an initial contraction of the ataxia, behavior disturbances Phosphenytoin REM: Blood dyscrasias, systemic
Primidone muscles (tonic phase) which may in children, hypersalivation, Amiodarone, quinidine. lupus erythematosus, suicidal
Tiagabine involve tongue biting, urinary bronchial hypersecretion, Oxcarbazepine: thoughts and behavior. Hepatic
Topimarate incontinence and the absence of anemia, leukopenia, Phenytoin and renal toxicity.
Valproate breathing. thrombocytopenia, respiratory phenobarbital, oral Gabapentin
Sodium divalproex Myoclonic seizures involve depression, anorexia, weight contraceptive. REM: Suicidal thoughts and
Vigabatrin sporadic muscle contraction and loss. Clonazepam behavior.
Levetiractem can result in jerky movements of Ethosuximide NV, fatigue, Phenytoin, levodopa, Lamotrigine: Caution: in renal,
muscles or muscle groups. headaches, drowsiness, digoxin. hepatic, or cardiac impairment.
Atonic seizures involve the loss of eosinophilia, Ethosuximide Phenobarbital:
muscle tone, causing the person to granulocytopenia, leukopenia, Carbamazepine, Caution in patients with hepatic
fall to the ground. These are blurred vision, hiccups, valproic acid. disease and elderly
sometimes called 'drop attacks' but confusion, urticaria, SSS, renal Felbamate: Tiagabine:
should be distinguished from damage, periorbital edema. Phenytoin, To monitor: Periodic
similar looking attacks that may Felbamate: N, infection, carbamazepine. ophthalmological. REM: Suicidal
occur in narcolepsy or cataplexy. aplastic anemia, liver failure, Valproic acid. thoughts, behavior.
acne, insomnia, headache, Gabapentin Antacids, Topimarate:
anxiety, hyperactivity, fatigue, cimetidine, oral REM: Suicidal thoughts, behavior,
peripheral edema, contraceptives. teratogenic effects.
vasodilation, hypotension, Lamotrigine: Vigabatrin: REM: Vision loss,
HTN, diplopia blurred vision, Carbamazepine, suicidal thoughts and behavior.
anorexia, weight decrease, QT phenobarbital,
prolongation and torsade de primidone, valproic
pointes. acid.
Gabapentin Somnolence, Phenobarbital:
dizziness, ataxia, nystagmus, Antiepileptic drugs,
dyspepsia, dryness of mouth, acetazolamide,
constipation, increased chloramphenicol,
appetite, diplopia, blurred cimetidine,
vision, CHF, HTN / furosemide, rifampin,
hypotension, dry skin, fungal pyridoxine, ethanol.
dermatitis, herpes infection, Tiagabine:
SSS, DM. Phenobarbital,
Lamotrigine: phenytoin,
NV, dizziness, diplopia, ataxia, carbamazepine. Take
blurred vision, rash, SSS, with food.
photosensitization. Topimarate:
Phenobarbital: NV, Phenytoin,
respiratory depression, carbamazepine.
Withdrawal convulsions. Valproic acid:
Tiagabine: Confusion, Antiepileptic drugs,
dizziness, fatigue, GI upset, aspirin, warfarin,
mouth ulceration, and antacids.
anorexia, EEG abnormalities,
sudden unexpected death,
rash.
Topimarate: N, breast pain in
females, tremor, back pain,
chest pain, dyspepsia, leg
pain.
Valproic acid: NV, abdominal
pain, anoxia.
Vigabatrin:
Somnolence, fatigue, light-
headedness, peripheral
neuropathy, anemia,
depression.
Levetiracetam: Somnolence,
weakness, hostility, infection,
dizziness, depression,
nervousness, pruritis, skin
discoloration, rash, alopecia,
drowsiness, cough.
2 Antidepressants: They act within the brain to Fewer and less severe than Metabolised by CYP450
SSRIs increase the amount of the TCAs and MAOI. and CYP2D6 so drug
Fluoxetine (Prozac; neurotransmitter, serotonin (5- Insomnia, GI effects (nausea, interactions are
Sarafem) hydroxytryptamine or 5-HT), in vomiting), common
Sertraline (Zoloft) the synaptic gap by inhibiting sexual dysfunction, a nxiety
Escitalopram: its reuptake (Reuptake is the WITHDRAWL SYMPTOMS: On
(Lexapro:Cipralex) reabsorption of a neurotransmitter abrupt discontinuation
Citalopram(Celexa) by the molecular transporter of a nightmares and vivid dreams
Fluvoxamine (Luvox) pre-synaptic neuron after it has so tapered dose needed
Paroxetine (Paxil) performed its function of
transmitting a neural impulse).
3 Selective Venlafaxine is chemically unrelated Similar to SSRIs Substrates for CYP2D6
Norepinehprine to other antidepressants, and Also produce withdrawal Produce
Reuptake is categorized as a serotonin- symptoms. SEROTONIN
Inhibitor (SNRI) norepinephrine reuptake inhibitor SYNDROME if given
Venlafaxine (effexor) (SNRI). It works by blocking the with MAOIs or other
transporter "reuptake" proteins Serotonergic agents
for key neurotransmitters
affecting mood, thereby leaving
more active in the synapse.
4 TCAs; It was thought that tricylic Numerous adverse effects Substrates of CYP 450
Antidepressants antidepressants work by limit their use enzymes so many
amitriptyline (Elavil) inhibiting the re-uptake of the -Anticholinergic side effects: interactions MAO
amoxapine (Asendin) neurotransmitters Dry mouth, blurred vision, INHIBITORS,
clomipramine norepinephrine and serotonin constipation, urinary retention, ADRENERGIC AGENTS
(Anafranil) by nerve cells. However, this tachycardia
desipramine response occurs immediately, -Quinidine like arrhythmias
(Norpramin) however mood does not lift for -Weight gain
doxepin (Adapin, around two weeks. It
Sinequan) is now thought that changes
imipramine (Tofranil) occur in receptor sensitivity in
nortriptyline the cerebral cortex and
(Pamelor) hippocampus.
trimipramine
(Surmontil)
5 Tetracyclic Mirtazapine is chemically unrelated -Weight gain, increased
Antidepressant to other antidepressants. It is appetite
Remeron thought to work by blocking -Sedation
(Mirtazipine) presynaptic alpha-2 adrenergic
receptors that normally inhibit
the release of the
neurotransmitters
norepinephrine and serotonin,
thereby increasing active levels
in the synapse. Mirtazapine also
blocks post-synaptic 5-HT2 and 5-
HT3 receptors—an action which is
thought to enhance serotonergic
neurotransmission while causing a
low incidence of side effects.
6 Antipsychotic: These drugs are also referred to as Sedation, blurred vision,
Schizophrenia neuroleptic drugs, or simply constipation, dry mouth,
Typical neuroleptics. Typical antipsychotics Extrapyramidal symptoms,
Antipsychotics are sometimes referred to as major Lowered seizure threshold,
Chlorpromazine tranquilizers because some of orthostatic hypotension,
Fluphenazine them can tranquilize and sedate hyperprolactinemia, moderate
Haloperidol when taken in large doses. All weight gain, QT
Thiothixene antipsychotic drugs tend to block prolongation,photosensitivity,
Thioridazine the D2 neuroreceptors in the temperature dysregulation,
Trifluoperazine dopamine pathways in the neuroleptic malignant
Loxapine brain, so the normal effect of syndrome, sexual dysfunction,
dopamine release in the elevated liver enzymes.
relevant synapses is reduced.
It is the blockade of D2 Sedation, extrapyramidal
receptors in the mesolimbic symptoms (except Clozapine),
pathway of the brain which is anticholinergic effects, Clozapine:
Atypical thought to produce the Lowered seizure threshold, Complete blood count (CBC) must
Antipsychotics intended antipsychotic effect. orthostatic hypotension, be monitored.
Clozapine (Clozaril) hyperprolactinemia Caution in patients at risk for
Olanzapine (Zyprexa) All atypical antipsychotics are FDA (risperidal), moderate to seizures or with a history of a
Quetiapine approved for use in the treatment severe weight gain, QT seizure disorder.
(Seroquel) of schizophrenia. Some carry FDA prolongation, diabetes
Risperidone approved indications for acute mellitus,
(Risperidal) mania, bipolar mania, psychotic hypercholesterolemia,
↑DA → agitation, bipolar maintenance, and neuroleptic malignant
Schizophrenia other indications. syndrome, sexual dysfunction.
↓DA → PD Modulation of the dopamine Agranulocytosis (Clozapine).
neurotransmitter system is
necessary for antipsychotic
activity while D2 receptor
antagonism coupled with 5 –
HT2A receptor antagonism is
responsible for the atypicality
of atypical antipsychotics.
7 Mood Stabilizers Mania describes a medical Li:Early: GI upset, nausea, Increase Li levels: Lithium: Acute renal failure,
condition characterized by severely polydipsia, nocturia, dry ACEIs, ARAII, NSADs, women in their first trimester of
Lithium carbonate. elevated mood. mouth, hand tremor, thiazides, dehydration, pregnancy, pregnancy, renal
Lithium: blocks the enzyme leukocytosis, polyuria. renal dysfunction, impairment, cardiovascular
inositol 1 phosphatase which Long term: Morphological Sodium los, and disease, dehydration, seizure
Anticonvulsants: affects neurotransmitters. kidney changes, EKG changes, fluoxetine. disorder, and thyroid disease.
Valproic acid, Anticonvulsants are most mood bradycardia, weigth gain, Decrease Li levels: Consider: age, weight, and renal
Carbamazepine stabilizers too. We revised them decreased libido, Acetazolamide, function
Oxcarbazepine before #1) hypothyroidism, rash, acne. methylxanthines,
Gabapentin Toxicity: Severe drowsiness, osmotic diuretics,
Lamotrigine Other manic symptoms include coarse hand tremor, muscle pregnancy (3third
Topiramate irritability, reduced need of twitching, seizures, trimester), sodium
sleep, hypersexuality, choreoathetosis, vomiting, supplements, urine
religiosity, hyperactivity, confusion, vertigo. alkalinizers.
talkativeness, flight-of-ideas, Others: Antipsychotics,
and grandiose plans. benzodiazepines,
8 Alzheimer’s Acetylcholinesterase (AChE) Nausea, diarrhea, vomiting, Are substrates for
Disease; Dementia inhibition was thought to be anorexia, tremors, cytochrome P450
donepezil (Aricept) important because there is bradycardia, and muscle (except Rivastigmine).
galantamine selective loss of forebrain cramps.
(Reminyl) cholinergic neurons as a result of
rivastigmine (Exelon) Alzheimer's. AChE-inhibitors
reduce the rate at which
acetylcholine (ACh) is broken
down and hence increase the
concentration of ACh in the
brain. Acetylcholinesterase-
inhibitors seemed to modestly
Mematine (NMDA moderate symptoms but do not
receptor prevent disease progression
Antagonist) A including cell death.
novel drug The NMDA receptor (NMDAR) is Confusion, agitation,
an ionotropic receptor for restlessness.
glutamate (NMDA is a name of its
selective specific agonist).
NMDARs play a critical role in
synaptic plasticity mechanisms and
thus are necessary for several
types of learning and memory.
9 5-HT3 receptor 5-HT3 receptor blockers Headache.
blockers principally used as an antiemetic
Antiemetic (cancer). The 5-HT3 receptor is a Dolasetron:
Granisetron ligand-gated Na+ and K+ cation Electrocardiographic changes
Ondansetron (zofran) channel, resulting in a direct (prolonged QT interval).
Dolasetron (anzemet) plasma membrane depolarization.
Antidopaminergic: Sedation,
Metoclopramide (GIT Metoclopramide is a diarrhea, and extrapyramidal
motility inhibitor; parasympa-thomimetic, and is symptoms
Prokinetic) also a potent dopamine
antagonist that enters the central
nervous system. It is used for
gastric emptying in patients with
gastric motor failure (gastro-
paresis).
1 Anti Migraine; 5 HT Triptans are a family of tryptamine Paresthesias, flushing, feeling Monoamine oxidase Avoid in familial hemiplegic migraine,
0 Receptors drugs used in the treatment of of pressure, tightness or pain inhibitors (MAOIs): basilar migraine, ischemic stroke,
Agonists migraine and cluster headaches. in the chest, neck, and jaw (excluding eletriptan, uncontrolled hypertension, ischemic
heart disease, prinzmetal angina,
(Triptans) Their action is attributed to their and headache (Naratriptan frovatriptan, and
ischemic complications,
Sumatriptan (Imitrex) binding to serotonin 5-HT1B and 5- lower). naratriptan).
cerebrovascular or peripheral vascular
5HTD1 HT1D receptors in cranial Eletriptan: disease, renal or hepatic disease, near-
Rizatriptan (Maxalt) blood vessels (causing their ketoconazole, term prior exposure to ergots alkaloid
Naratriptan (Amerge) constriction) and subsequent itraconazole, or other 5-HT agonists.
Zolmitriptan (Zomig) nefazodone,
5HTB1/D1 troleandomycin,
clarithromycin,
nelfinavir, and
ritonavir.
1 Antiarrrhythmics Antiarrhythmic agents are a group Quinidine, Torsades des
1 Class Ia agents of drugs that are used to pointes, Cinchonism,
include quinidine, suppress fast rhythms of the thrombocytopenic purpura,
procainamide and heart (cardiac arrhythmias), such NVD (nausea, vomiting,
disopyramide. as atrial fibrillation, atrial flutter, diarrhea).
Class Ib agents ventricular tachycardia, and Procainamide: Lupus like
include lidocaine, ventricular fibrillation. syndrome and hypersensitivity
mexiletine, tocainide, Class I agents interfere with reactions.
and phenytoin. the sodium (Na+) channel, Disopyramide. Potent
Class Ic agents which anticholinergic effects, NVD.
include encainide, prolongs the action potential Lidocaine:
flecainide, duration by slowing conduction CNS: Paresthesias, drowsiness,
moricizine, and Class II agents are anti- confusion, restlessness at low
propafenone. sympathetic nervous system dose.
Class II agents agents. All agents in this class are Seizures and disorientation at
include esmolol, beta blockers. They act by high dose. Cardiac depression
propranolol, and slowing conduction through the arrhythmias if given by rapid
metoprolol. AV node. IV.
Class III agents Class III agents affect potassium Flecainide: May worsen
include amiodarone, (K+) influx. They prolong arrhythmias.
azimilide, bretylium, repolarization. Propranolol: Heart failure.
clofilium, dofetilide, Class IV agents affect the AV Depressed AV conduction.
ibutilide, sematilide, node. They decrease Bronchospasm. Hypotension.
and sotalol. conduction through the AV Amiodarone: Corneal
Class IV agents node. deposits (reversible)
include verapamil Class V agents work by other or Hypo or hyperthyroidism.
and diltiazem. unknown mechanisms. Photosensitivity.
Class V agents Pulmonary fibrosis.
include adenosine Sotalol: Arrhythmias.
and digoxin. Verapamil: Sinus
bradycardia.
AV block. GI upset.
1 Calcium Channel Calcium channel blockers work by Verapamil: Constipation,
2 Blockers blocking voltage-sensitive hypotension, bradycardia,
Dihydropyridine calcium channels in the heart edema, CHF, GI upset.
calcium channel and in the blood vessels. This Diltiazen: Edema, headache,
blockers prevents calcium levels from dizziness, asthenia, Rash.
Amlodipine besylate increasing as much in the cells Nifedipine: MI, peripheral
(Norvasc) when stimulated, leading to less edema, reflex tachycardia,
Nicardipine (Cardene, contraction. This decreases total Headache, flushing, edema.
Carden SR) peripheral resistance by dilating
Nifedipine (Procardia, the blood vessels, and decreases
Adalat) cardiac output by lowering the
Nitrendipine (Cardif, force of contraction.
Nitrepin) Because resistance and output
Nimodipine drop, so does blood pressure.
(Nimotop) Unlike with beta-blockers, the heart
Phenylalkylamine is still responsive to
calcium channel sympathetic nervous system
blockers stimulation, so blood pressure can
Verapamil be
hydrochloride (Calan) maintained more effectively
Diltiazem
hydrochloride
(Cardizem)
1 Fibrates;Hyperchol The fibrates are a class of Fibrates:
3 esterolemia amphipathic carboxylic acids. Muscle damage when fibrate
Clofibrate (largely Fibrates increase the activity of added with statin.
obsolete due to side- lipoprotein lipase, a plasma Gallstone formation.
effect enzyme that degrades NVD.
profile, e.g. chylomicrons and VLDL.
gallstones) Fibrates are structurally and
Gemfibrozil (e.g. pharmacologically related to the
Lopid) thiazolidinediones, a novel class of
Fenofibrate anti-diabetic drugs that also act
Bezafibrate (e.g. on PPARs .Although less effective in
Bezalip) lowering LDL, fibrates
improve HDL and triglyceride
levels, and seem to improve
insulin resistance when the
dyslipidemia is associated with
other features of Syndrome X
(hypertension and diabetes
mellitus type 2).

Statins are the most potent Statins: Myositis, CPK


cholesterol-lowering agents, elevation, rhabdomyolysis,
Statins lowering LDL-cholesterol (so-called memory loss, high BP.
atorvastatin "bad cholesterol") by 30–50%.
(Lipitor®) However, they are less effective
fluvastatin (Lescol®) than the fibrates in reducing
lovastatin triglycerides and raising HDL-
(Mevacor®, cholesterol. Statins act by
Altocor®, not competitively inhibiting 3-
marketed in the UK) hydroxy-3-methylglutaryl
pravastatin coenzyme
(Pravachol®, A (HMG CoA) reductase, an
rosuvastatin enzyme of the HMG-CoA
(Crestor®) reductase pathway, the body's
simvastatin (Zocor®) metabolic pathway for the
synthesis of cholesterol.
1 Diuretics Diuretic is any drug that tends to Osmotic Diuretics:
4 Osmotic diuretics increase the flow of urine from Headache, NV, Chills,
(e.g., mannitol) the body (diuresis). They also dizziness, polydipsia.
Carbonic decrease the extracellular fluid
anhydrase volume, and are primarily used to Carbonic Anhydrase
inhibitors (e.g., produce a negative extracellular Inhibitors: Acidosis.
acetazolamide, fluid balance. Diuretics are used to
dorzolamide) treat heart failure, liver THIAZIDE DIURETICS:
cirrhosis, hypertension and certain Chlorothiazide: hypokalemia,
kidney diseases. Some common hyponatremia, hyperglycemia,
diuretics are caffeine, cranberry hiperuricemia,
juice and alcohol. hypercalcemia, oliguria,
Thiazides (e.g., anuria, decreased placental
hydrochlorothiazide, flow.
bendroflumethiazide) Thiazides are a class of drug that
promote water loss from the body Loop Diuretics:
((diuretics)). They inhibit Na+/Cl- Furosemide: Ototoxicity,
reabsorption from the hypovolemia,
distal convoluted tubules in the hypomagnesemia.
kidneys. Thiazides also cause hypokalemia
loss of potassium and an hyponatremia, hyperglycemia,
Loop diuretics increase in serum uric acid. sulfonamide allergy.
(e.g., furosemide,
bumetanide, Loop diuretics act on the Ethacrynic acid:Most
ethacrynic acid) Na+/K+/Cl- cotransporter in the ototoxic.
ascending loop of Henle to
inhibit sodium and chloride
reabsorption. Because
magnesium and calcium
reabsorption in the thick ascending
Potassium-sparing loop is dependent on sodium and
diuretics (e.g., chloride concentrations, loop POTASSIUM SPARING
spironolactone, diuretics also inhibit their DIURETICS:
amiloride, reabsorption. This raises the Hyperkalemia, sodium or
triamtrene) osmotic pressure inside the loop, water depletion, patients with
driving more water into the filtrate DM may develop glucose
causing increased urine volume. intolerance, endocrine
Potassium sparing diuretics work disturbances. Triamterene
by inhibiting sodium will turn urine blue.
reabsorption in the distal
convoluted tubules and
collecting ducts in the kidneys.
This promotes the loss of sodium
and water from the body, but
without depleting potassium.
1 Alpha Adrenergic In BPH, the prostate grows larger Postural hypotension on first
5 Receptor Blockers and presses against the urethra dose is sudden and severe,
Alfuzosin and bladder, interfering with the sodium depletion, edema, dry
Doxazosin normal flow of urine. It leads to mouth, headaches,
Terazosin symptoms of urinary hesitancy, nightmares, sexual
Prazosin frequent urination, increased risk of dysfunction,lethargy.
Tamsulosin urinary tract infections and urinary
retention. Alpha blockers are used
to block alpha 1 receptors that
mediate muscular activity in
the bladder neck, prostate and
prostatic capsule.
1 Anti Diabetic, Type Thiazolidinediones are selective Not indicated for use in type 1
6 2 agonists for nuclear peroxisome diabetes, exacerbate CHF,
Thiazolidinediones proliferator-activated receptor- edema, weight gain, increased
Rosiglitazone gamma (PPAR). These drugs bind LFT.
(Avandia) to PPAR, which activates insulin-
Pioglitazone (Actos) responsive genes that regulate
carbohydrate and lipid metabolism.
Thiazolidinediones require
insulin to be present for their
action. Thiazolidinediones exert
their principal effects by increasing
insulin sensitivity in peripheral
tissue but also may lower glucose
production by the liver.
1 Sulfonylurea; Sulfonylureas bind to an ATP- Hypoglycemia, weight gain, GI
7 Antidiabetic dependent K+ channel on the upset, headache, teratogenic.
First generation: cell membrane of pancreatic beta
Chlorpropamide cells. This inhibits a tonic,
Tolbutamide hyperpolarizing outflux of
Tolazamide potassium, which causes the
Second electric potential over the
generation: membrane to become more
Glipizide , Gliclazide positive. This depolarization opens
Glibenclamide , voltage-gated Ca2+ channels. The
Glimepiride rise in intracellular calcium
Glyburide leads to increased fusion of
insulin granulae with the cell
membrane, and therefore increased
secretion of proinsulin.
1 Cancer Alkylating agents are so named Alkylating Agents Alkylating agents:
8 Alkylating Agents because of their ability to add Cisplatin: Nephrotoxicity, Pregnancy, patients with bone
Cisplatin, alkyl groups to many nausea and vomiting, marrow suppression, Renal
Carboplatin, electronegative groups peripheral neuropathy, disease(with cisplatin)
Ifosfamide, undervconditions present in myelosuppression, ototoxicity. Platinum Analogs:
Chlorambucil, cells. They stop tumor growth Carboplatin: Hypersensitivity to
Busulfan, Thiotepa. by crosslinking guanine Myelosuppression, nausea and cisplatin/platinum products or
Cyclophosphamide nucleobases in DNA double- vomiting, peripheral mannitol
helix strands - directly neuropathy, ototoxicity. Severe
attacking DNA. This makes the Ifosfamide: myelosuppression/significant
Cancer; strands unable to uncoil and Myelosuppression, bleeding
Antimetabolites separate. hemorrhagic cystitis,
5 Fluoro Uracil (5 FU) somnolence, confusion.
Methotrexate, Anti-metabolites masquerade as Chlorambucil:
Fludarabine purine or pyrimidine – which Myelosuppression, pulmonary
become the building blocks of DNA. fi brosis, hiperuricemia.
They prevent these Busulfan:
substances becoming incorporated Myelosuppression, pulmonary
in to DNA during the "S" fi brosis, aplastic anemia, skin
phase (of the cell cycle), Hyperpigmentation. Thiotepa:
stopping normal development and Myelosuppression, nausea and
division. An important example is 5- vomiting, mucositis, skin Antimetabolites:
Fluoro Uracil (5FU), which inhibits rashes. Cyclophosphamide: Ampicillin, aspirin,
thymidylate synthase. Myelosuppression, Nsaids,
Fludarabine inhibits function of hemorrhagic cystitis, Cephalosporins.
multiple DNA polymerases, DNA immunosuppression, alopecia,
primase, DNA ligase I and is stomatitis, SIADH
S phase-specific. Methotrexate Antimetabolites: Plant Alkaloids: Demyelinating
Caner; Plant (being folate antagosnist) inhibits 5 FU: Stomatitis, form of Charcot–Marie–Tooth
alkaloids dihidrofolate reductase, enzyme myelosuppression, diarrhea, syndrome, pregnancy, significant
Vincristine essential for purines and nausea and vomiting, granulocytopenia, bacterial
Plant alkaloids:
Vinblastine pyrimidines synthesis. cerebellar ataxia. infections.
Drugs known to inhibit
Methotrexate: Mucositis,
drug metabolism by
These alkaloids are derived from myelosuppression, pulmonary
hepatic CYP 3A
plants and block cell division fi brosis, hepatotoxicity,
subfamily. Vincristine
by preventing microtubule nephrotoxicity, diarrhea, skin
sulfate: Itraconazole.
synthesis and mitotic spindle erythema.
formation. These are vital for cell Fludarabine: Antibiotics: Hypersensitivity,
division and without them it can Myelosuppression, nausea and Children < 12 years, myeloid
not occur. The main examples are vomiting, fever, malaise, malignancies, heart failure, atrial
vinca alkaloids such as pulmonary infi ltrates. arrhythmias, thromboembolic
vincristine, and vinblastine which Plant alkaloids: disorders.
Antibiotics:
Cancer; Anti tumor bind to specific sites on tubulin, Vincristine: Peripheral Caution: Major organ dysfunction.
Cyclophosphamide -
Antibiotics inhibiting the assembly of tubulin neuropathy, paralytic ileus, Plicamycin: Breast feeding.
doxorubicin.
Doxorubicin into microtubules SIADH
Daunorubicin Vinblastine: Myelosuppression,
Bleomycin They prevent cell division by paralytic ileus, alopecia,
Actinomycin several ways: (1) binding to DNA nausea, stomatitis.
plicamycin (Safe use through intercalation between Antibiotics:
in pregnancy) two adjacent nucleotide bases Daunorubicin:
and making it unable to Myelosuppression,
separate, (2) inhibiting cardiotoxicity, stomatitis,
ribonucleic alopecia, nausea and
acid (RNA), preventing enzyme vomiting.
synthesis, (3) interfering with Bleomycin: Pneumonitis,
cell replication. Bleomycin acts in pulmonary fibrosis, fever,
unique way through oxidation anaphylaxis,
of a DNA-bleomycin-Fe(II) complex hyperpigmentation,
and forming free radicals, which alopecia
induce damage and chromosomal Actinomycin: Bone marrow, a
aberrations. cough, sore throat, pain,
passing urine or may feel cold
and shivery, anemia, bruising,
hair loss, skin changes.
Plicamycin: headache, NV,
vesicant, hepatic injury,
Coagulation factors II, V, VII
and X. Azotemia, GIT
problems.
1 Immunosuppressa Tacrolimus s a macrolide antibiotic. Tacrolimus: Nephrotoxicity, Tacrolimus: Avoid Grape fruit
9 nt, Eczema It acts by reducing peptidylprolyl neurotoxicity post transplant, Antiepileptic drugs,
Organ Transplant isomerase activity by binding diabetes, hair loss. rifampin isoniazid,
Tacrolimus (Prograf, to the immunophilin Cyclosporine: Nephrotoxicity, azole antifungal
Protopic) FKBP-12, creating a new complex. neurotoxicity hepatotoxicity, agents , macrolide
Mycophenolate This inhibits both Tlymphocyte hirsutism and gingival antibiotics,
mofetil (Cellcept) signal transduction and IL-2 hyperplasia. calcium-channel
Cyclosporine transcription. blockers, antiviral
Cellcept is metabolised in the liver agents
to mycophenolic acid which
inhibits inosine
mononophosphate
dehydrogenase, the
enzyme which controls the rate
of synthesis of guanine
monophosphate in the de novo
pathway of purine synthesis
used in the proliferation of
lymphocytes.
Cyclocporine has same action as
Tacrolimus.
2 Immunosuppressiv Azathioprine is used for Azathioprine: Bone marrow Xanthine oxidase
0 e immunosuppression in organ suppression. inhibitor, allopurinol,
Azathioprine transplantation and
autoimmune disease such as
rheumatoid arthritis or Crohn's
disease. It is converted in the body
to 6-
mercaptopurine. Azathioprine acts
to inhibit purine synthesis
necessary for the proliferation
of cells, especially leukocytes and
lymphocytes.
2 DMARD Disease-modifying antirheumatic Methotrexate: Bone marrow
1 gold salts (sodium drugs (DMARDs) are a category of suppression, diarrhea,
aurothiomalate, drugs used in many autoimmune mucositis.
auranofin) disorders to slow down disease
D-penicillamine progression. They are used in
chloroquine and diseases such as Crohn's disease
hydroxychloroquine and ulcerative colitis, lupus
(antimalarials) erythematosus (SLE), idiopathic
sulfasalazine (SSZ) thrombocytopenic purpura (ITP),
methotrexate (MTX) myasthenia gravis and various
azathioprine others.
cyclosporin A Methotrexate inhibits
dihydrofolate reductase, an
enzyme that is part of the
folate synthesis metabolic
pathway. Dihydrofolate reductase
catalyses the conversion of
dihydrofolate to the active
tetrahydrofolate. Methotrexate,
therefore, inhibits the synthesis
of DNA, RNA, thymidylates, and
Leflunomide (Arava) proteins. Methotrexate is cell
cycle S-phase selective, and has a
greater negative effect on rapidly
dividing cells, which are replicating
their DNA, and thus inhibits the
growth and proliferation of these
cells.
Arava inhibits pyrimide
sysnthesis.
2 Proton Pump PPIs act by irreversibly blocking Diarrhea, GI pain, headache. Inhibit CYP2C19
2 Inhibitors (PPIs) the K/H – ATPase or more
Omeprazole, commonly just proton pump of Diazepam, warfarin,
Lansoprazole, the gastric parietal cell. The phenytoin, clopidogrel,
Esomeprazole, proton pump is the terminal stage theophylline
Pantoprazole, in gastric acid secretion, being
Rabeprazole directly responsible for secreting
H+ ions into the gastric lumen,
making it an ideal target for
inhibiting acid secretion.
2 Antithyroids Both agents inhibit iodide NV, dermatologic reactions, To monitor: Serum thyroid levels
3 PTU oxidation and iodorhiouracil headache, drowsiness, and the FTI.FDA black box
(propylthyouracil) coupling but PTU only diminishes paresthesia, vertigo, neuritis, warning: Severe liver injury and
Tepazole peripheral deiodonation of T4 to loss of taste, arthralgia, acute liver failure (PTU)
(methimazole) T3. myalgia. Severe:
Agranulocytosis,
granulocytopenia,
thrombocytopenia, drug fever,
hepatitis,
hypoprothrombinemia.
2 Corticosteroids Corticosteroids have potent anti- Suppress pituitary–adrenal Estrogens, oral Caution: Diabetes, adrenal
4 Prednisone inflammatory and axis, peptic ulcer, GI contraceptives, suppression, CHF, osteoporosis,
Methylprednisone immunosuppressive hemorrhage, ulcerative itraconazole, macrolide myasthenia gravis, psychiatric
Dexamethasone properties.They bind to esophagitis, acute antibiotics, diseases.
glucocorticoid pancreatitis, weight gain, cyclosporine,
receptors altering DNA and osteoporosis, hyperglycemia, potassium-depleting
RNA translation causing drop in acne, increased susceptibility diuretics, digitalis
circulating T lymphocytes. As a to infection, cushingoid “moon glycosides.
consequence, corticosteroids face”, “buffalo hump”,
are widely used as drugs to treat headache, vertigo, increased
inflammatory conditions such as intraocular, glaucoma,
arthritis or dermatitis, and as cataracts intracranial
adjunction therapy for pressures, muscle weakness,
conditions such as autoimmune psychological disturbances,
diseases. edema, HTN.
2 Anti – obesity It works by inhibiting pancreatic GI (soft or liquid stools), Fish oil.
5 Orlistat (Xenical) lipase, an enzyme that breaks increased defecation, fecal
down fat in the intestine. urgency, abdominal pain,
Without this enzyme, fat from the decreased absorption of
diet is excreted undigested, and not vitamins A, D, E, K, and beta-
absorbed by the body. carotene.
2 OCPs The Pill works by preventing Relatively low: Most due to Cerebrovascular, thromboembolic
6 Birth Control Pills ovulation, as well as making estrogen component. disease, estrogen dependent
the uterus less likely to accept Cardiovascular both. Breast neoplasms, liver disease, and
implantation of an embryo if fullness, depression, fluid pregnancy. Age of 35 who are
one is created, and thickens retention, headache, NV. heavy smokers.
the mucus in the cervix making Carcinogenicity: Increased
it more difficult for sperm to incidence of cervical cancer,
reach any egg. Taken correctly, it induce other neoplasms.
is the Production of benign tumors,
single most reliable form of hemorrhage, abnormal
reversible contraception. Most glucose tolerance, weight gain
brands use 20 to 40 micrograms of (nortestosterone) (less weight
ethinyloestradiol as the gain drospirenone). Changes in
estrogen component and either a the serum lipoprotein profile.
fixed or varying (the bi and
triphasic pills) amount of
progestogen as the
progesterone analogue. Most
progestagens are used for their
antiestrogenic properties in oral
contraceptives to avoid over
stimulation of the endometrium
which could lead to endometriosis.
2 Inflammatory Ulcerative colitis is an inflammatory Mesalamine (5 ASA): Mesalamine Mesalamine Caution: rarely
7 Bowel Disease disease of the bowel, that usually Diarrhea, headache, Mercaptopurine, exacerbation of IBD
(IBD) affects the distal end of the large abdominal pain, cramps, antacids or acid
Ulcerative Colitis and intestine and rectum. The main flatulence, skin rash. Rarely lowering agents.
Crohn’s Disease difference between the two is the hepatotoxicity or acute or
location and nature of the chronic renal injury.
inflammatory changes in the gut.
Crohn's can affect any part of
the gastrointestinal tract, from
mouth to anus. Ulcerative
Mesalamine (5 colitis, in contrast, is restricted
ASA) (Pentasa, to the colon, and spares the
Asacol) anus.
Olsalazine Mesalamine, also known as 5- Sulfasalazine Sulfasalazine
olsalazine, aminosalicylic acid (5-ASA), is an Fever, dizziness, headache, folic acid
balsalazide anti-inflammatory drug used to itching, rash, photosensitivity,
treat inflammation of the GI upset, nausea, vomiting,
rectum, mild to moderate diarrhea, reversible
ulcerative colitis and oligospermia
inflammation of the lower
colon.
Sulfasalazine
Sulfasalazine is a sulfa drug used
primarily in the treatment of
inflammatory bowel disease. It is a
5-acetylsalicyclic acid
derivative. It is also used for
rheumatoid arthritis.
2 Leukotriene Leukotrienes are autocrine and Zafirlukast: Headache, Zafirlukast: Aspirin, To monitor: for vasculitic rash,
8 receptors paracrine eicosanoid lipid dizziness, nausea, diarrhea erythromycin, eosinophilia, increasing
antagonists mediators derived from theophylline, pulmonary, cardiac, and
(LTRA); Asthma arachidonic acid by 5- terfenadine, warfarin, neuropathic symptoms.
lipoxygenase. dofetilide.
Zafirlukast Zafirlukast is an oral leukotriene
(Accolade) receptor antagonist (LTRA) for the
maintenance treatment of asthma. Montelukast: Avoid in patients
Available as a tablet, it with phenylketonuria.
blocks the action of leukotriene
C4 on its receptors, thus reducing Montelukast: Headache, Montelukast: Hepatic
constriction of the airways, dizziness, and dyspepsia. enzyme inducers (e.g.,
build-up of mucus in the lungs and rifampin,
Montelukast inflammation of the breathing phenobarbital).
(Singulair) passages.

Montelukast blocks the action


of leukotriene D4 on the
cysteinyl leukotriene receptor
CysLT1, thus inhibiting
bronchoconstriction.
2 Bisphosphonates Bisphosphonates inhibit Well tolerated. GI irritation, Contraindicated in women with a
9 Alendronate osteoclastic activity. They reduce heartburn, esophageal creatinine clearance less than 30
Risedidronte both the resorption and irritation. diarrhea, abdominal mL/min.
etidronate formation of hydroxyapetite pain, musculoskeletal pain.
crystals. Unusual jaw necrosis, atypical
fractures of the femur.
3 Influenza A and B Oseltamivir is a neuraminidase NV, self-injury, delirium Oseltamivir To monitor: Abnormal
0 Tamiflu (Oseltamivir) inhibitor used in the treatment of (pediatric). behavior.
and prophylaxis of both influenza A Caution: impaired renal function.
Zanamivir and influenza B. Oseltamivir is Zanamivir: Severe reactive
a prodrug, usually administered as asthma or COPD
oseltamivir phosphate, with
the drug being converted heptically
to the active metabolite.
3 Influenza A (Flu) Influenza (or as it is commonly Ataxia, nightmares, insomnia, Caution: Elderly patients,
1 Amantadine known, the flu or the grippe) is a depression, confusion, impaired renal function.
contagious disease caused by an dizziness, fatigue, anxiety, To monitor: History of seizures or
RNA virus of the orthomyxoviridae headache. Anticholinergic psychiatric disorders.
family. Amantadine inhibits reactions.
replication of the influenza A
virus by interfering with viral
attachment and
uncoating.
3 Anticoagulants The oral anticoagulants are a class Warfarin: Warfarin: Numerous: Warfarin:
2 Warfarin of pharmaceuticals that act by Hemorrhage, skin lesions, Inhibition of Pregnancy (X)
Phenindione antagonizing the effects of necrosis, purple toe syndrome, metabolism: Acute Black box warning for bleeding
vitamin K. It is important to alopecia. alcoholintoxication, risk.
note that they take at least 48 cimetidine, Monitor and adjust the
to 72 hours for the chloramphenicol, anticoagulant effect.
anticoagulant effect to develop cotrimoxazole, To monitor: if necessary:
fully. Vitamin K is converted to disulfiram, response with prothrombin
vitamin K epoxide in the liver. This metronidazole. time/INR measurements.
epoxide is then reduced by the Stimulation : Chronic
enzyme epoxide reductase. The alcohol, ingestion,
reduced form of vitamin K barbiturates,
epoxide is necessary for the glutethimide,
synthesis of many coagulation griseofulvin, rifampin Heparin:
factors (II, VII, IX and X, as well Antagonist: Spinach, Hypersensitive, bleeding disorders;
as protein C and protein S). broccoli. alcoholics; having or have had
Warfarin inhibits the enzyme Additive effect: recent surgery of the brain, eye,
epoxide reductase in the liver, Garlic. spinal cord.
Heparin thereby inhibiting coagulation. To monitor:
Common indications for warfarin Heparin: Hemorrhage, Heparin: The bleeding time.
use are atrial fibrillation, Hypersensitivity reactions Protamine sulfate
artificial heart valves, deep (chills, fever, urticaria, (neutralization).
venous thrombosis and anaphylactic shock),
pulmonary embolism. thrombosis,
Heparin works by potentiating thrombocytopenia,
the action of antithrombin III, as osteoporosis, abnormal liver
it is similar to the heparan sulfate function tests.
proteoglycans which are naturally
present on the cell membrane of
the endothelium.
Because antithrombin III
inactivates many coagulation
proteins, the process of
coagulation will slow down.
3 Beta Blockers Beta blockers or beta-adrenergic Propanolol: Propanolol: Propanolol: Asthma, COP.
3 Cardioselective blocking agents are a class of drugs Bronchoconstriction, sexual Cimetidine, fluoxetine,
Acebutolol, Atenolol, used to treat a variety of impairment, disturbance in paroxetine, ritonavir,
Betaxolol Bisoprolol, cardiovascular conditions and some metabolism, fasting barbiturates,
Esmolol, Metoprolol other diseases. Beta blockers block hypoglycemia. phenytoin, rifampin
Nebivolol the action of epinephrine and
norepinephrine on the β-
Nonselective adrenergic receptors in the
Nadolol, propanolol, body (primarily in the heart,
Sotalol, Pindolol, peripheral blood vessels, bronchi,
pancreas, and liver). The hormones
and neurotransmitters stimulate
the sympathetic nervous system by
acting on these receptors.
Propanolol is used for social phobia.
3 Biguanide; Metformin is antihyperglycemic, Potential fatal lactic acidosis Vitamin B12, Renal and/or hepatic disease,
4 Glucophage not hypoglycemic. It does not cause (rarely). intravenous acute myocardial infarction, severe
insulin release from the pancreas radiographic contrast infection, or diabetic ketoacidosis.
and generally does not cause agents. Caution >80 years, history of
hypoglycemia, even in large doses. CHF, alcohol abuse.
Metformin has no significant effects
on the secretion of glucagon,
cortisol, growth hormone, or
somatostatin. Metformin reduces
glucose levels primarily by
decreasing hepatic glucose
production and by increasing insulin
action in muscle and fat.
3 Digitalis: Cardiac Digoxin inhibits the Na+-K+ N, headache, fatigue, Quinidine, verapamil, Caution: Hypothyroidism, hypoxia,
5 Glycoside ATPase pump in the confusion, color perception amiodarone, K renal failure, myocarditis.
Digoxin membranes of the heart cells alteration, halos in dark depleting diuretics, To monitor: renal insufficiency and
(myocytes). This causes an objects. Hypercalcemia and corticosteroids. dosage adjustment.
increase in the hypomagnesemia. Ventricular
level of sodium ions in the tachycardia.
myocytes, which then leads to a
rise in the level of calcium ions.
This increased level of calcium
increases the contractility of the
myocardium (muscle of the heart).
Digoxin also decreases the
conduction of electrical
impulses through the AV node,
making it a commonly used drug in
controlling the heart rate during
atrial fibrillation or atrial flutter.
3 Selective Estrogen Selective estrogen receptor Clomiphene: Headach,
6 Receptor modulator (SERMs) is a class of nausea, vasomotor flushes,
Modulator medication that acts on the visual disturbances, ovarian
(SERM) estrogen receptor. A enlargement.
clomifene (an characteristic Toremifene: Endometrial
ovulation) that distinguishes these substances hyperplasia. Raloxifene: women who will be
raloxifene from receptor agonists and Raloxifene: Hot flashes, leg pregnant, history of
(osteoporosis) antagonists is that their action is cramps, deep vein thrombosis, thromboembolic events.
tamoxifen (breast different for various tissues, pulmonary embolism, retinal
cancer) thereby granting the possibility to vein thrombosis.
toremifine (breast selectively inhibit or stimulate
cancer) estrogen-like action in various
tissues. There are three types of
estrogen receptors, which are
intracellular: α (α homodimer), β
(β homodimer) and αβ (α- and β-
receptor heterodimer). The α-
receptor is generally stimulatory,
but the β-receptor may inhibit
the α-isoform as well as
suppressing transcription
independently
3 Antiretroviral Protease inhibitors are a class of PIs: PIs: PIs: Simvastatin, lovastatin,
7 Drugs; HIV medication used in viral infections. Saquinavir: Prolongs PR and Warfarin. rifampin, cisapride, pimozide,
Protease inhibitors They act by inhibiting specific QT interval, torsades de Ritonavir: midazolam, triazolam, ergots,
(PIs); HIV viral enzymes that are pointes. inhibits many P450 alfuzosin, salmeterol, St. John’s
Saquinavir, Ritonavir, essential to the viral life cycle by Ritonavir: GI intolerance, isoenzymes wort.
Indinavir, Nelfinavir cleaving viral proteins. Protease circumoral paresthesias, Indinavir: Atazanavir, Caution antiepileptic drugs,
inhibitors are molecules that hyperlipidemia, Vitamin C. erectile dysfunction drugs,
inhibit the function of hyperglycemia, fat Nelfinavir Methadone. colchicine, azole antifungals.
peptidases maldistribution, ↑ liver Saquinavir: Trazodone.
and In medicine, protease inhibitor function tests, taste RTIs RTIs
is often used interchangeably with perversion. Zidovudine: Dose adjustment in renal
Reverse alpha 1-antitrypsin. Indinavir: Nephrolithiasis, Cotrimoxazole, dysfunction (except abacavir).
Transcriptase indirect hyperbilirubinemia, atovaquone, valproic Black box warning: Potential
Inhibitors (RTIs) Reverse Transcriptase Inhibitors hyperglycemia, acid, methadone, lactic acidosis and severe
Nucleoside Analog inhibit activity of reverse hyperlipidemia, fat probenecid, cytotoxic hepatomegaly with steatosis.
Reverse transcriptase, a viral enzyme maldistribution, drugs ganciclovir, Didanosine:
Transcriptase HIV needs to reproduce. Lack of headache, GI intolerance. dapsone, ribavirin, Zalcitabine:
Inhibitors (NARTIs) or this enzyme prevents HIV from Nelfinavir: D, GI intolerance, interferonalpha,Rifabut Lamivudine:
(NRTIs). building DNA based on its RNA. hyperlipidemia, in, rifampin. Black box warning: acute
(Zidovudine, hyperglycemia, fat Didanosine: exacerbations of hepatitis B.
didanosine, maldistribution, pancreatitis, Zalcitabine: Abacavir:
Zalcitabine, PR interval prolongation. Stavudine: Black box warning:
Stavudine, RTIs Zidovudine. hypersensitivity.
Lamivudine, Zidovudine: Bone marrow Lamivudine: NNRTIs
Abacavir) suppression, macrocytic Cotrimoxazole, Nevirapine: OCPs, efavirenz,
Non-Nucleoside anemia, neutropenia, emtricitabine. atazanavir, ritonavir, ketoconazole,
Reverse headache, malaise, seizures, rifampin, St. John’s wort. Black
Transcriptase anxiety, fever, rash, Abacavir: Alcohol box warning: hepatic necrosis
Inhibitors (NNRTIs) symptomatic myopathy. NNRTIs Efavirenz: 1 trimester of
(nevirapine: Didanosine: Reversible Rash, hepatotoxicity. pregnancy, childbearing, unreliable
Viramune, efavirenz: peripheral neuropathy, Nevirapine: contraception, cisapride,
Sustiva®, pancreatitis. Methadone midazolam, triazolam, ergot
delavirdine: Stavudine: Reversible Efavirenz: St. John’s derivatives.
Rescriptor®) peripheral neuropathy, wort, levonorgestrel.
headache, rash, NVD. Fatal Delavirdine:
episodes of pancreatitis. Alprazolam,
Lamivudine: Minor. midazolam, triazolam,
Headache, fatigue, GI simvastatin, lovastatin,
reactions (NVD), dizziness, rifabutin, cisapride.
neuropathy, insomnia. PPIs and H2-receptor
NNRTIs antagonists, St. John’s
Nevirapine: SSS, N, wort, carbamazepine,
symptomatic hepatitis, fever, phenobarbital,
headache. phenytoin, rifampin.
Efavirenz: Insomnia,
dizziness, drowsiness,
nightmares, hallucinations,
rash, ↑ transaminases, GI
disturbances.
Delavirdine: N, rash, SSS,
headache.

3 Antituberculosis Rifampicin inhibits DNA- Rifampin: Serious Rifampin: CS, WARF, Rifampin:
8 Rifampin dependent RNA polymerase in hepatotoxicity, skin rash, OCPs, quinidine, To monitor: Liver function tests.
bacterial cells by binding its beta drowsiness, headache, fatigue, digitoxin, PIs, NNRTIs,
Rifabutin & subunit, thus preventing confusion, NV, abdominal pain. KCZ, verapamil, Isoniazid:
rifapentine. (Newer) transcription of messenger RNA Colors urine, sweat, tears, methadone, OADs, Monitor: CBC, liver function.
(mRNA) and subsequent saliva, feces orange-red. CYA, dapsone, Cam, Caution: Age, diabetes, HIV,
translation to proteins. Influenza-like syndrome. BARB. Probenecid. uremia, alcoholism, malnutrition,
ASA. pregnancy, seizure disorder
Isoniazid Isoniazid inhibits the mycolic Isoniazid: Skin rash, fever, Isoniazid: PHT,
acid cell wall synthesis via jaundice, peripheral neuritis, Antacids (Aluminum),
oxygen-dependent pathways, Blood dyscrasias, GI (NV, CBZ, cycloserine,
such as the catalase-peroxidase epigastric distress). SSRIs, ethionamide,
reaction. CNS toxicity (insomnia, meperidine.
restlessness, hyperreflexia,
convulsions. Hepatitis).

3 Vancomycin Vancomycin is an antibiotic used in Fever, chills, phlebitis, red man Amino glycosides:
9 (Vancocin) the prophylaxis and treatment of syndrome (flushing), shock, ototoxicity and
The drug of choice infections caused by Gram- hearing loss, renal failure. nephrotoxicity
and last resort where positive bacteria. Vancomycin
other antibiotics are acts
not effective. by inhibiting proper cell wall
synthesis in Gram-positive
bacteria. Vancomycin needs to be
given intravenously (IV) for
systemic therapy since it does not
cross through the intestinal lining. It
is a large hydrophilic molecule
which partitions poorly
across the gastrointestinal mucosa.
The only indication for oral
vancomycin therapy is in the
treatment of pseudomembranous
colitis, where it must be given
orally to get to reach the site of
infection in the colon.
4 Metronidazole Metronidazole is an antibiotic and GIT(NAUSEA,VOMITING,ABDO WITH ALCOHOL
0 (Flagyl) antiparasitic drug classified as a MINAL CRAMP) ~FROM DISULFIRAM
nitroimidazole. It inhibits METALIC TESTE,ORAL LIKE EFFECT
nucleic acid synthesis and is YEAST INFECTION
used for the treatment of infections (MONILIASIS)
involving anaerobic bacteria as ,NEUROTOXICOLOGIC
well as protozoal infections. PROBLEM
Conditions it is useful in include: (DIZZINESS,VERTIGO AND
giardiasis, amoebiasis, NUMBNESS)
Trichomonas vaginalis
infections, bacterial vaginosis,
pseudomembranous colitis,
Helicobacter pylori infections,
and acne rosacea.
4 Polyene Antibiotics The polyenes bind with sterols in ALLERGY,GIT DISTURBANCE ,
1 Imidazole the fungal cell wall, principally GYNECOMASTIA AND
(Miconazole,Ketocona ergosterol. This causes the cell's IMPOTANCE.
zole contents to leak out and the HEPATIC DYSFUNCTION AND
Clotrimazole cell dies. Human (and other LIVER MICROSOMAL ENZYME
,Econazole, animal) cells contain cholesterol INHIBITOR
Mebendazole rather than ergosterol so are much OTHER AZOLES~ LESS SIDE
,Oxiconazole less susceptible. EFFECT
Thiabendazole The imidazole and triazole FLUCONAZOLE~ NO
,Tiaconazole) groups of antifungal drugs ENDOCRINE SIDE EFFECT
Triazole inhibit
(Fluconazole the enzyme cytochrome P450
,Itraconazole) 14α-demethylase. This enzyme
Allyalamine converts lanosterol to ergosterol,
(Terbinafine; Lamisil) and is required in fungal cell wall
synthesis. These drugs also block
steroid synthesis in humans.
Allylamines inhibit the enzyme
squalene epoxidase, another
enzyme required for ergosterol
synthesis

4 Quniolones and Quinolones and fluoroquinolones GIT(NAUSEA,VOMITING,DIARR THEOPHYLLINE~


2 Fluoroquinolones form a group of broad-spectrum HEA) INCREASE
Antibiotics antibiotics. They are derived from CNS(DIZZINESS,HEADACHE,SE CIPROFLOXACINE
Ciprofloxacin (Cipro) nalidixic acid. IZURE) CONCENTRATION
Levofloxacin Quinolones act by inhibiting the PHOTOTOXICITY DECREASE CATIONS
(Levaquin) bacterial DNA gyrase enzyme. GATIFLOXACIN~ DIABETES ( AL,Mg,Ca,Zn,Fe)
Norfloxacin (Noroxin) This way they inhibit nucleic acid GREPAFLOXACIN~ ABSORPTION
Ofloxacin (Floxin) synthesis and act PROLONGED QTINTERVAL
Moxifloxacin (Avelox) bacteriocidically. TROVAFLOXACIN~ FETAL
Gatifloxacin (tequin) LIVER DAMAG

4 Macrolides The mechanism of action of the GIT:(NAUSEA,VOMITING MICROSOMAL


3 Antibiotics macrolides is inhibition of ,DIARRHIEA) ENZYME INHIBITER
(erythromycin bacterial protein synthesis by LIVER: CHOLESTATIC ~INCREASE
,clarithromycin binding reversibly to the JAUNDICE WARFARINE TOXICITY
azithromycin subunit 50S of the bacterial OTOTOXCIT
roxithromycin) ribosome, thereby inhibiting
The macrolides are a translocation of peptidyl-tRNA.
group of drugs This action is mainly bacteriostatic,
(typically antibiotics) but can also be bactericidal in high
whose activity stems concentrations.
from the presence of Macrolides tend to accumulate
a macrolide ring, a within leukocytes, and are therefore
large lactone ring actually transported into the site of
to which one or infection.
more Macrolides are used to treat
deoxy sugars, infections such as respiratory
usually cladinose and tract infections and soft tissue
desosamine, are infections. Beta-hemolytic
attached. The streptococci, pneumococci,
lactone ring can be staphylococci and enterococci are
either 14, 15 or 16- usually susceptible to macrolides.
membered. Unlike penicillin, macrolides
Macrolides belong to have shown effective against
the polyketide class mycoplasma, mycobacteria, some
of rickettsia and chlamydia.
natural products.

4 Aminoglycosides Aminoglycosides are a group of OTOTOXICITY CEPHALOSPORINS,


4 Amikacin, antibiotics that are effective against ,NEPHROTOXICITY ,SKELETAL POLYMYXINS AND
gentamicin, certain types of bacteria. MUSCLE RELAXANT ,ALLERGIC FUROSAMDE.
kanamycin, Aminoglycosides work by REACTION
neomycin, binding to the bacterial 30S
streptomycin, and ribosomal subunit, causing
tobramycin. misreading of t-RNA, leaving
the bacterium unable to
synthesize proteins vital to its
growth. Aminoglycosides are
useful primarily in infections
involving aerobic, Gram-negative
bacteria, such as Pseudomonas,
Acinetobacter, and Enterobacter.
4 Finasteride Finasteride acts by inhibiting 5- allergic reaction, male breast
5 (Propecia): alpha reductase, the enzyme cancer, Less serious side
Antiandrogen the converts testosterone to effects (impotence, abnormal
5 – alpha reductase dihydrotestosterone. It is used in ejaculation, swelling in hands
inhibitor benign prostate hyperplasia (BPH) or feet,
Flutamide in low doses, and in prostate cancer swelling or tenderness in
Bicalutamide in higher doses. It is registered in breasts, dizziness)
(Casodex) many countries for malepattern
Nilutamide baldness.
(Anandron)
4 Tetracyclines Tetracyclines bind to 30S subunit GIT(ANOREXIA,EPIGASTRIC
6 Doxycylcine of bacterial ribosome, blocking PAIN, ABDOMINAL DISTENTION
Demeclomycin aminosyl transfer RNA on the ,PERIANAL
Minocycline receptor site on the m RNA IRRITATION),CLACIFIED
ribosomal complex TISSUE,FETAL HEPATOTOXICITY
PHOTOSENSITIVTY,
AZOTEMIA,FAN-CNI
SYNDROME(TETRACYCLINE~E
PITETRACYCLINE~ LEADE TO
NAUSEA ,VOMITING,POLYURIA,
POLYDIPSIA,PROTEINEURIA
,ACIDOSIS AND GLYCOSURIA
4 Βeta Lactam β-lactam antibiotics are a broad Penicillins: Hypersensitivity Penicillins: Penicillins:
7 Antibiotics class of antibiotics including reactions (urticarial, vesicular, Probenecid. A positive history for reactions
Penicillins penicillin derivatives, bullous, scarlatiniform, Antagonism: Renal impairment.
Cephalosporins cephalosporins, monobactams, maculopapular. Thrombopenic Erythromycins, Procaine hypersensitivity is a
First generation carbapenems and β-lactamase purpura, fever, eosinophilia, tetracyclines, or contraindication to the use of
cephalosporins inhibitors; basically anyantibiotic angioedema, serum sickness). chloramphenicol. procaine penicillin G.
cephalexin agent which contains a β-lactam Anaphylaxis: (severe Parenteral products
,cephalothin nucleus in its molecular structure. hypotension, contain either Cephalosporins:
cephazolin β-lactam antibiotics were mainly bronchoconstriction, nausea, potassium, sodium. Ceftriaxone: Newborns receiving
Second generation active only against vomiting, abdominal pain, and Cephalosporins: concurrent administration of
cephalosporins Gram-positive bacteria, the extreme weakness).GI Cross-sensitivity with calcium containing solutions.
cefaclor ,cefuroxime development of broad-spectrum β- distress, bone marrow penicillin.Probenecid IV calcium-containing solutions.
cefamandole lactam antibiotics active against suppression, superinfection. (except ceftazidime).
Second generation various Gram-negative organisms Cephalosporins: Alcohol consumption:
cephamycins has increased the usefulness of the Hypersensitivity (See for cefmetazole,
Moderate β-lactam antibiotics. All β- lactam penicillins), NVD, cefotetan,
spectrum with antibiotics are bactericidal, and act superinfection, nephrotoxicity, cefoperazone. Carbapenems:
anti-anaerobic by inhibiting the synthesis of Clostridium difficile–induced Antacids Cefaclor Cross-sensitivity reactions those
activity. the peptidoglycan layer of colitis. extended-release are allergic to penicillin or
cefotetan , cefoxitin bacterial cell walls. tablets, cefdinir, cephalosporins
Third generation The peptidoglycan layer is Cefoperazone, cefmetazole, cefpodoxime.
cephalosporins important for cell wall cefotetan: bleeding diatheses. H2-antagonists:
Broad spectrum. structural cefpodoxime &
ceftriaxone , integrity, especially in Gram- cefuroxime.
cefotaxime positive organisms. The final Iron supplements and
Broad spectrum transpeptidation step in the iron-fortified foods:
with anti- synthesis of the peptidoglycan is cefdinir
Pseudomonas facilitated by transpeptidases Cephalosporins: may
activity. known as penicillin binding proteins Carbapenems: NVD, cause false-positive
ceftazidime (PBPs). Inhibition of PBPs may also pseudomembranous colitis, glycosuria results.
Fourth generation lead to the activation of autolytic seizures, dizziness,
cephalosporins enzymes in the bacterial cell wall. hypotension.
cefepime β-lactam antibiotics are indicated
Carbapenems for the prophylaxis and treatment
of bacterial infections caused by
susceptible organisms.
4 Analgesics: An opioid is any agent that binds to NV, constipation (e.g., CNS depressants (e.g., To monitor: Respiratory rate,
8 Narcotics opioid receptors found principally in codeine), sedation, respiratory alcohol, anesthetics, warned about driving or operating
Endogenous the central nervous system and depression, anticholinergic antidepressants, machinery.
opioids gastrointestinal tract. There are effects (dry mouth and urinary antihistamines,
Opioid-peptides that four broad classes of opioids: retention), hypersensitivity, barbiturates,
are produced in the endogenous opioid peptides, CNS excitation. benzodiazepines,
body:endorphins produced in the body; opium Tolerance (increase doses), phenothiazines). MAO
dynorphins alkaloids, such as morphine dependence (physical inhibitors.
enkephalins (the prototypical opioid) and dependence), withdrawal
Opium alkaloids codeine; semi-synthetic opioids symptoms.
Phenanthrenes such as heroin and oxycodone; and
naturally occurring in fully synthetic opioids such as
opium:morphine pethidine and methadone that have
,codeine structures unrelated to the opium
thebaine alkaloids.
Semisynthetic There are at least three major
derivatives classes of opioid receptors: μ, κ
diamorphine and
(heroin) , oxycodone δ. These are all G-protein
hydrocodone coupled receptors acting on
,dihydrocodeine GABAergic neurotransmission.
hydromorphone The μ receptor (the μ represents
,oxymorphone morphine) is perhaps the most
Synthetic opioids important – being responsible for
Phenylheptylamine most of the analgesic and other
s major pharmacological effects
methadone as well as many of the adverse
levomethadyl effects of opioids.
acetate Opioid overdose can be rapidly
hydrochloride reversed with any of several opioid
Phenylpiperidines antagonists such as naloxone.
pethidine These competitive antagonists are
(meperidine) drugs that bind to the μ-opioid
fentanyl , alfentanil receptors with higher affinity than
sufentanil agonists but do not activate them.
Diphenylpropylami The main clinical indications of
ne derivatives opioids include; moderate-to-
propoxyphene severe acute pain and chronic
dextropropoxyphene pain cough (mainly codeine)
Benzomorphan diarrhea (mainly loperamide and
derivatives diphenoxylate used therapeutically)
pentazocine , relief of severe dyspnoea (e.g.
phenazocine lung cancer, terminal COPD)
Oripavine
derivatives
buprenorphine
Morphinan
derivatives
butorphanol,
nalbufine
tramadol, loperamide
diphenoxylate
Opioid antagonists
naloxone , naltrexone
4 Gout Colchicine inhibits the Colchicine: Pregnancy.
9 Colchicine cytoskeleton by binding to NVD, abdominal pain, Caution: hepatic, renal, or
tubulin, one of the main myopathy, neutropenia, cardiovascular disease.
constituents of microtubules. aplastic anemia, alopecia.
Allopurinol is used for long term
treatment. Allopurinol treatment
Allopurinol should not be initiated during an Allopurinol: Hypersensitivity
attack of gout, as it can then runs in skin. Acute attacks of Allopurinol
worsen the attack. In humans, gout. Colchicine and NSAIDS: 6-mercaptopurine,
xanthine oxidase is normally NV. azathioprine.
found
in the liver and not free in the
blood. Because xanthine oxidase is
a metabolic pathway for uric acid
formation, the xanthine oxidase
inhibitor allopurinol is used in
the treatment of gout.