USMLE PHARMACOLGY WORKSHEETS

Drug
ANS
Cholinergic agonists
Direct acting

Indirect acting

Cholinergic antagonists
Muscarinic antags

NMJ blockers

Ganglionic blockers
Parasympathetic
Agonists

acetylcholine
bethanechol
carbachol
pilocarpine
methacholine
nicotine
edrophonium
physostigmine
neostigmine

mechanism of action

stims bladder and bowel

miosis and contraction of ciliary mm

side effects
DUMBELS
D iarrhea and Decr BP
U rination
M iosis
B ronchoconstriction
E xcitation of skeletal mm
L acrimation
S alivation and Sweating

dx of myasthenia gravis
tertiary amine - can enter CNS
quaternary amine no CNS
opposite of DUMBELS

atropine
scopolamine
ipratropium
Non-depolarizing
tubocurarine
vecuronium
atracurium
Depolarizing - succinylcholine

eye and face first, respiratory last

nicotine

depolarizing no clinical uses

Synthetic choline esters

carbachol
bethanechol
methacholine

no hydrolysis by AChE
no hydrolysis by AChE
small hydrolysis by AChE

bronchoconstrict and hypotension

metabd by plasma cholinesterase

tachy, vasodilate, mydriasis, GI

Drug
Muscarinic agonists
muscarine
pilocarpine
Nicotinic agonists nicotine
Indirect agonists
edrophonium
neostigmine
physostigmine
pyridostigmine
organophosphates
Antagonists

Sympathetic
Adrenergic receptors

Muscarinic antags
atropine
scopolamine
homotropine
ipratropium bromide
Nicotinic antags
hexamethonium
D-tubocurarine
succinylcholine
decamethonium
Indirect antagonists
hemicholimium

Agonists
NE
phenylephrine
methoxamine
metaraminol
clonidine
guanabenz, guanfacine

mechanism of action

side effects

inhib AChE
short acting, reversible
medium acting, reversible
medium acting, reversible
long acting, reversible
irreversible

non-depolarizing, ganglia and NMJ

non-depolarizing, NMJ only
depolarizing, NMJ only, short acting
depolarizing, NMJ only
blocks vesicular uptake of choline

not used clinically

has both direct and indirect effects

2-selective partial agonist
2-selective

effects of stimulation:
vasoconstriction
mydiasis radial mm in eye
ejaculation
stim of pilomotor mm

Drug
Antagonists
ergot alkaloids
phentolamine
phenoxybenzamine
prazosin
terazosin
receptor agonists

receptor antagonists

1 selective agonists
dobutamine
2 selective agonists
albuterol
salmeterol
terbutaline
metaproterenol
1, 2 nonselective agonists
isoproterenol
Mixed agonists ( and )
epi
ephedrine
mephantermine
1 selective antagonists
metoprolol
atenolol
esmolol
acebutolol
1, 2 nonselective antagonists
propranolol
nadolol
timolol
pindolol
Adrergic neuron blockers
reserpine
guanethidine

mechanism of action

side effects

reversible
irreversible
1-selective
1-selective

CTY without heart rate or SVR

asthma

effects of stim: HR, CTY,

AV node condctn, CO
effects of stim:
bronchodilation
relaxation of viscera

pressor agent
1
2
1
2

Epi > NE >> Iso

Epi > NE >> Iso
Iso > Epi = NE
Iso > Epi >> NE

anti-HTN

blocks vesicular uptake of NE

blocks NE release

Drug

mechanism of action

Levdopa
Carbidopa
Entacapone

prodrug
inhib LevDA conversion in periphery
COMT inhib (prolongs DA life)

dopamine agonists

Bromocriptine
Apomorphine
Pramipexole
Ropinarole

D2 agonist not very effective

D2 agonist very effective
D2/D3
D2/D3

ACh neuron inhibitors

Trihexyphenidyl
Benzotropine
Diphenhydramine

helps sialorrhea, not bradykinesia

Adjuvants

Amantadine
Diprenyl

treats Levdopa side effects

allows lower dose of Levdopa

CNS/Neurologic
Antiparkinson
drugs that replete dopamine

Stimulants
drugs affecting catechol
neurons

Alzheimers

other stimulants

side effects

amphetamine
methamphetamine
ephedrine
methylphenidate (Ritalin)
cocaine
AChE inhibitors
Donezapil
Rivastigmine
memantine

low therapeutic index

non-competitive antag of NMDA

low therapeutic index

caffeine
theobromine
modafinil

ETOH

Anti-epileptics
Na channel inactivators

Drug
naltrexone
acamprosate
disulfiram

mechanism of action
opioid antag
glutamate antag
aldehyde dehydrogenase inhib

side effects

phenytoin
fosphenytoin
carbamazepine
lamotrigine
tobrimate
valproate

inactivates rapid firing Na channel

prodrug of phenytoin, less toxic
prolongs inactivation of Na

arrhythmias

Ca channel blockers

valproate
ethosuxamide

GABA potentiators

tigapine
phenobarbitol
felbamate

Unknown

GABApentin

Status epilepticus

diazepam
lorazapam
phenytoin

Psychiatric
Anti-psychotics
typical

reserpine
chlorpromazine
thioridazine
haloperidol
domperidone
thiothixine
benzotropine
trihexyphenidyl

diplopia

liver, GI, no use w/phenobarb

prevents GABA reuptake

post-synaptic GABA agonist
post-synaptic GABA agonist

aplastic anemia

parkinsonism, tardive dyskinesia

(after prolonged use), sedation,
anti-cholinergic

atypical

Anxiolytics
Anxiety

Insomnia

Drug
clozapine
olanzapine
risperidone
aripiprazole

mechanism of action

side effects
not as many extra-pyramidal
effects, weight gain

Benzodiazepines
alprazolam
diazepam
lorazapam
triazolam
5HT/NE uptake inhibs
SSRI
SNRI
imimpramine
venalfixine
Buspirone
Herbal
kava kava
valerian

GABA inhibs, can not OD

short acting
intermediate acting
long acting

dependence

Benzodiazepines
Flurazepam
Temazepam
Non-benzos
zolpidem (ambien)
Barbituates
pentobarbital
phenobarbitol

+ diazepam = coma

sedative
life 18-48h
life 4 days

Drug
Anti-depressants
Depression

mechanism of action

side effects

inhibit 5HT uptake, muscarinic &

-1 antags

low therapeutic index, dry mouth,

dizziness, constipation, tachy,
orthostatic HTN

TCAs
Tertiary amines
Imipramine
Amitryptiline
Secondary amines
Desipramine
Nortryptiline

inhibit NE uptake, muscarinic &

-1 antags

MAOIs
Phenalzine
Tranylcypromide
deprenyl

SSRIs

non-selective MAOI

MAO-A NE and DA neurons,

involved in tyramine metab in gut
MAO-B 5HT neurons

MAO-B but non-selective at dose

5 HT uptake inhib
Fluoxetine
Sertraline
Paroxetine

Other
Trazadone
Nefazadone
Venalfixine
Buproprion
Mirtazapine
Bi-polar

Lithium
Valproate
Lamotrigine
Olanzapine

NE and DA uptake inhib

low therapeutic index

Drug

mechanism of action

side effects

Lovastatin
Fluvastatin
Atorvastatin
Pravastatin
Simvastatin

HMG Co-A reductase inhib which upregs

LDL receptors

GI upset, muscle ache, hepatitis

Bile acid binding resins

Cholestyramine
Colestipol

prevent reabsorp of bile

bloating

Niacin

Nicotinic acid
Vitamin B3

inhibit mobilization or peripheral FFAs

flushing

Fibrates

Gemfibrozil
Clofibrate
Fenofibrate

enhanced oxidation of FFAs

potentiates warfarin

heparin

stims antithrombin III which binds

thrombin
binds to ATIII selective inhib of FX/Xa
vitK analog competive inhibitor

Cardiovascular
Atherosclerosis
Statins

Antithrombosis
Anticoagulants

fondaparinaux sulfate
warfarin (coumadin)
Anti-platelets

inhibs of platelet signaling

aspirin
clopidigrel
ticlopidine
dipyridamole
glycoprotein IIb/IIIa antags
abmixicab
eptifibitide
tirofiban

irreversibly inhib cyclooxygenase

irreversibly blocks platelet P2Y12 ADP
interferes w/platelet aggegation
platelet cAMP platelet activation

neutropenia and TTP

cardiac death

Drug
streptokinase
TPA (alteplase & retaplase)
urokinase
anistrplase

mechanism of action
convert plasminogen plasmin

Prothrombotics

aprotinin

inhibs lakikrein-kinin inhibs

fibrinolysis

Anti-arrhythmics
Class I Na channel

Class Ia

incr ARP and AP

sudden death arrhythmias

quinidine
procainamide
Class Ib lidocaine
Class Ic flecainide

raise threshold and prolong RRP

raise threshold and slow conduction

pro-arrhythmic (not as bad)

sudden death arrythmias

Thrombolytics

Class II blockers

propanolol

Class III K channel

amiodarone
soltalol

Class IV Ca channel

verapamil
diltiazem

other

adenosine
digitalis

Cardiac glycosides
Digitalis glycosides

side effects
contraindicated in pxs w/strep inf

contraindicated w/asthma
block DRK channels + Class I, II, and IV
block DRK channels + Class II

torsades de pointed (ventr tachy)

temporary asystole

digoxin
digitoxin
digoxin immune Fab

Bipyridines

milnirone

select non-selec blocker

carvidilol

1 agonist
Anti-hypertensives
Central acting

Drug
dobutamine

mechanism of action

clonidine
guanbenz
methyldopa

stimulates central 2

Noradrenergic blockers

guanethidine

Adrenreceptor antags

Beta blockers
propranolol
pindalol
labetolol
metoprolol
atenolol
Alpha blockers
prazosin
phentolamine

Diuretics

see below

Ca channel blocker

see below

ACE inhibitors

see below

ARBs

see below

Diuretics
Osmotic

side effects

mannitol
urea

Carbonic anhydrase inhibs

acetazolamide

block HCO3 reabsorption

Loop

furosemide
bumetanide

block Na/K/2 Cl

10

Thiazides

K sparing

Vasodilators & antianginal

K channel openers

Drug
HCTZ
metolazone

mechanism of action
block Na/Cl

spironolactone
amiloride
triamterene

blocks upreg of Na channel

blocks Na channel
block Na channel

side effects

minoxidil

Ca channel blockers

verapamil
diltiazem
nifedipine
nimodapine

Nitrodilators

nitroglycerin
isosorbide dinitrate
nitric oxide
nitroprusside

ACE inhibs

captopril
enalapril
ramipril

ARBs

losartan

cGMP PDE Type 5 inhibs

sildenafil

Natiuretic factors

nesiritide

11

Drug

mechanism of action

side effects

omeprazole
lansoprazole
labeprazole
pantoprazole
esomeprazole

irreversible proton pump inhibs

nausea and diarrhea

H2R antagonists

cimetidine
ranitidine
famotidine
nizatidine

inhibs GS protein needed to activate pump

p450 inhib, nausea, prolactin

Prostaglandin analog

misoprostol

stims Gi which inhibs proton pump

diarrhea, uterine contractions

GI Drugs
Control of gastric acidity
PPIs

Anti-emetics
5HT3R antagonists

Dopamine R antagonists

odansetron
granisetron
dolasetron
thenothiazine
metaclopramide
domperidone

Antihistamines

cyclizine
hydroxyzine
promethazine
diphenhydramine

Anticholinergics

scopolamine

antag the DA R on the Chemoreceptor TZ

CNS effects
No CNS effects

dronabinol
Glucocorticoids & NSAIDs

12

Prokinetics
Cholinergic agonists

Drug

mechanism of action

side effects

carbechol
bethanechol

ACh is main NT for GI motility

lots of global side effects

AChE inhibitor

neostigmine

Dopamine D2R antags

metaclopramide
domperidone

dopamine inhibs gastric motility

Serotonin R modulators

metaclopramide
cisparide
tegaserod

5HT4R agonist (stimulatory receptor)

Somatostatin analog

octreotide

enhances gastric emptying

Motilin R agonist

erythromycin

Motilin is a potent contractile hormone

IBS
5HT4R agonist

tegaserod

Diarrhea
Intraluminal

fiber

Opiates

loperamide
dipenoxylate
difenoxen

Somatostatin analog

octreotide

blocks DRKs in heart-arrhythmia

anti-secretory and anti-motility

cholestyramine

binds bile acids

bismuth

antisecretory, -inflammatory, -microbial

can bind and inactivate drugs

13

Drug

mechanism of action

IBD
5 aminosalicylates

sulfasalazine

COX/lipoox pthwy inhibs

mesalamine

Immunosuppression

6-mercaptopurine
methotrexate
cyclosporine

inhibs DHFR

Inflliximab

Monoclonal Ab to TNF

albuterol
salmeterol

short acting
long acting

Monoclonal antibody
Respiratory
Asthma
2 agonists

side effects

tachy and tremor

Corticosteroids

beclomethasone
fluticasone

all the probs with steroids

Anticholinergics

ipratropium

few due to poor systemic absorp

Leukotriene inhibs

zileuton
zafirlukast

inhib Arach Acid Leuko 5-lipox inhib

LTD4 R antag

not for acute

Methylxanthines

theophylline

cAMP bronchodilation

seizures and arrythmias

cromolyn sodium

prophylactic - stabilize mast cells

laryngeal edema

nedocromil

prophylactic - stabilize mast cells

bad taste

14

Drug

mechanism of action

raloxifene
tamoxifen

agonist on bones, antag on breasts

etidronate
pamidronate
alendronate
risendronate

long term inhibs of bone resorption

calcitonin

decr osteoclast activity

anabolic agents

teriparatide

stims bone formation

Insulin and anti-diabetics

Biguanides

metformin

gluconeogenesis in liver, insulin dep

lactic acidosis

Thiazolidinediones

pioglitazone
rioglitazone

glucose uptake peripherally via PPAR

activation, gluconeo in liver

edema and weight gain

Sulfonylureas and glinides

nateglinide
repaglinide
meglitinide
glipizide

insulin secretagogues, stimulate beta cell

production of insulin

hypoglycemia

Alpha-glucosidase inhibs

acarbose
miglitol

delay absorption of carbs and so moderate

post prandial spike

flatulence and incr LFTs

Insulin

glargine
lispro and aspart
regular
NPH

slow absorp and sustained release

fast acting moderate post prandial spike
fast acting but give 30 mins before meal
long acting but not as long as glargine

Endocrine
Osteoporosis
Ca and Vit D supplements
ERT
SERM

Bisphosphonates

side effects

15

Drug

mechanism of action

see above

lower LDL

Bile acid sequestrants

cholestyramine
colestipol
colesevalam

lower LDL

Cholesterol absorp inhibs

ezetimibe
plant stanol and sterol esters

lower LDL

Niacin

see above

lower TGs

Fibrates

see above

lower TGs and incr HDL

Hyperlipidemia
Statins

Omega 3 fatty acids

Anti-obesity
Adrenergic

side effects

+ statin = rhabdomyalisis

lower TGs

dexamphetamine
phentermine

Serotonergic

sibutramine
fenfluramine dexfenfluramine

nutrient absorption blockers

orlistat

reuptake inhibitor
serotonin releasers

Antibiotics
Nucleic acid inhibs

Fluoroquinolones

sulfamethoxazole

bacteriostatic PABA analog

trimethoprim

bacteriostatic DHFR inhib, can cross BBB

nitrofurantoin

uncomplicated UTI

ciprofloxacin
ofloxacin

DNA gyrase inhib

kernicterus,p450 inhib,crystalluria

cartilage dmg

16

-lactams
Penicillins

Cephalosporins

Protein synthesis inhibitors

Aminoglycosides

Drug

mechanism of action

penG
penV
penicillinase resistant
oxacillin
nafcillin
ampicillin
ampicillin + sulbactam
amoxicillin
amoxicillin + clavulante
ticaracillin
ticaracillin + clavulante
piparcillin
piparacillin + tazobactam
aztreonam
imipenem
-lactamase inhibs
sulbactam
clavulante
tazobactam

inhib bacterial cell wall transpeptidation

side effects

-lactamase producing S. aureus

broad spectrum but not MRSA

1st generation cephalexin

2nd generation cefuroxime
3rd generation
ceftriaxone
cefotaxime
ceftazadime

gram pos
gram neg like HIB, Neisseria, S. pneumo
gram neg

vancomycin

inhib bacterial cell wall transglycosylation

gentamicin
amikacin
trobramicin
streptamicin

bactericidal; aerobic; 30s subunit

ototoxicity and nephrotoxicity

17

Drug
doxycycline
minocycline

mechanism of action
30s, chlamydia, cholera, lyme

side effects
hepatotox, dep in bones and teeth

erythromycin
azithromycin
clarithromycin

50s,legionella,mycoplas,chlamdia,anthrax

GI irrit, hepatotox, p450 inhib

does NOT inhib p450

chloamphenicol

50s, serious infections, incl CNS

aplastic anemia and p450 inhib

clindamycin

50s; anaerobic, S.aureus, PCP

psuedomemb colitis, hepatotox

Oxazolidinones

linezoilid

50s, VRSE, MRSA, PRSP

MAO inhib, superinfections

Streptogramins

dalfopristin
quinupristin

50s, bactericidal when given together,

VRSE, MRSA, PRSP

metronudazole

anaerobes

Tetracyclines

Macrolides

TB drugs
isoniazid
rifampin
ethambutol
pyrazinamide

bactericidal except Ethambutol

mycolic acid synth inhib;
Tb DNA dep RNA pol inhib
only dividing mycobacs;for MAC + clarith

periph neuritis,slow/fast acetyl

GI, hepatotox, p450 induce
retrobulbar neuritis,periph neuritis
hepatotox, gout-like sx

Anti-fungals

Azole family

Amphoteracin B

complex w/sterols results in apoptosis

nephro, cardio, and neurotoxic

Flucytosine

fungal uracil analog; chain termin

bone marrw suppr, alopecia, GItox

Imidizole ketoconazole
Triazoles
fluconazole
itraconazole

CSF

18

Drug

mechanism of action

side effects

chloroquine
primaquine
mefloquine

erythrocytic cidal
exoerythrocytic cidal;

leukopenia, hemlytic crisis (G6PD

Trypanosomiasis

saramin

tx pre-CNS

neurotox

Worms

Round mebendazole
Flat
Flukes - praziquantal
Tapeworms
niclosamide
praziquantal

poor GI absorb so intraluminal effect

amantadine
neuramidase inhibs
zanamivir
oseltamavir

flu A by blocking M2 so no uncoating

prevent cleave of sialic acid-virus no exit
inhaled
oral

Herpes

trifluorothymadine
acyclovir

thymidine analog, topical

guanine analog; 100x affinity of viral TK

AIDS

RT inhib azidothymadine
Protease inhibitor combo
lopinavir-ritonavir
Fusion inhib - enfuvirtide

inhib viral replic

blocks HIV attachment to cells

Anti-parasitics
Entamoeba, giardia, trich
Malaria

Anti-virals
Influenza

metronidazole

Ca++ perm of worm cell membrane

T. solium

paranoia, depression
can be prob for asthmatics

19

Analgesics and Anesthetics

Opioids
Endogenous

Drug

mechanism of action

endorphins
enkephalins
dynorphins

opioid work on three receptors in CNS:

analges,euphor,resp depr,miosis,constp
analges, sedation, dysphoria, miosis
- analgesia

side effects

Alkaloids

morphine
codeine
heroin

Synthetic

fentanyl
methadone
pentazacine
hydrocodone
meperidine

agonist antag

long life(resp dep after 2-3days)

+ MAOIs = severe resp depression

naloxone
naltrexone

comp antag for

comp antag for

Antagonists

Chronic pain
Non-opioid
Opioid

NSAIDs
Full agonist
fentanyl
hydromorphone
heroin
morphine
methadone
meperidine
Partial agonist
buprenorphine
oxycodone
hydrocodone
codeine
propoxyphene

20

Adjuvant

Local anesthetics
Ester linked

Amide linked

General anesthetics
Inhalational

Injectable/IV

Drug
Muscle relaxants
cyclobenaprine
methocarbamol
diazepam
baclofen
anti-convulsants see above
local anesthetics see below
anti-depressants see above

mechanism of action

side effects

cocaine
procaine
benzocaine
tetracaine

metabolized by blood = short life; if

administer w/epi, vasoconstr prevents
blood from reaching site and incr life

arrythmias, euphoria

lidocaine
etidocaine
mepvicaine
bupivacaine
(S)-ropivacaine

metabolized by liver = longer life

hepatitis, malign hyperthermia

halothane
enflurane
isoflurane
desflurane
sevoflurane
nitrous oxide
propofol
ketamine
barbiturates thiopental
benzodiazapenes
midazolam
diazepam

NMDA-R antag, dissociative anesthesia

bad dreams

21

Drug

mechanism of action

side effects

lorazepam
Immunosuppression
Prototype mediators

NSAIDs
Non-specific

thromboxanes
prostacyclin (PGI2)
prostaglandin E2
leukotrienes
histamine
IL-1
IL-2
TNF

aspirin
acetaminophen
ibuprofen
naproxen
piroxicam
etodolac
nabumetone
endomethacin

COX-2

celecoxib

Leukotriene inhibitors

zileuton
zafirlukast

Anti-rheumatics

Disease modifying
entanercept
infliximab
Slow acting
methotrexate
gold salts
penicillamine
hydroxychloroquine

decoy TNF-receptor
anti-TNF monoclonal antibody

22

Anti-gout

Anti-histamine

Immunosuppressive
Cytotoxic

Drug
indomethacin
colchicine
allopurinol
uricosuric agents

mechanism of action
NSAID
acute attack inhib MTs
Inhib xanthine oxidase - uric acid synth
reduce resorbtion of urate from the urine

penetrate CNS - sedation

penetrate CNS - sedation

dimenhydrinate
diphenhydramine
loratidine
cetirizine
fexfenadine

methotrexate
azathioprine
cyclophosphamide

side effects

Inhibit prod of immune system cells

Corticosteroids

hydrocortisone
dexamethasone
methylprednisone

interrupt of adren-pituit axis, Na &

H2O retention, cushingoid effects,
general immunosup, osteoporosis

Selective

cyclosporine
tacrolimus
sirolimus
mycophenolate mofetil
anti-CD3
anti-IL-2
daclizumab
basiliximab

inhibition of clonal expansion of T cells

iInhibition of clonal expansion of T cells
inhibition of clonal expansion of T cells
inhibits nucleoside synthesis in T cells
monoclonal Ab against T cell receptor
monoclonal Ab against IL-2

Immunostimulant

GM-CSF
G-CSF

increase the production of hematopoietic

cells

23

Chemotherapy
Cell cycle nonspecific
Alkylating agents

Antibiotics (except bleo)

Cell cycle specific

Antimetabolites

Plant deriviatives

Drug

mechanism of action

side effects

cyclophosphamide
nitrourea
cisplatin

alkylate DNA, cause DNA cross-linking

carcinogenic

anthracyclines
doxorubicin
daunorubicin
dactinomycin

intercalate DNA, breaks via Topo II

Folate analogs - methotrexate

Purine analogs
6-mercaptopurine
6-thioguanine
Pyrimidine analogs
5-fluorouracil
cytosine arabinoside- ara-C

renal
cardiac, carcinogenic

intercalate DNA, inhib RNA synth

inhibs DHFR
antag HGPRT

leucovorin reduces myelosuppres

inhib thymidilate synthase

inhib DNA pol

Vinca alkaloids
vinblastine
vincristine
Podophyllotoxins
etoposide
tenoposide
Taxanes - paclitaxel

bind tubulin depol so no MTs form

bind to tubulin pol & overstabilization

Antibiotics

bleomycin

DNA breaks via free radicals

Hormones

Anti-estrogen - tamoxifen
GnRH agonists
leuprolide
goserelin
Steroids - prednisone

estrogen antag
initially agonists but cause recep downreg

peripheral neuropathy
inhib Topo II religation

pulmonary

24

Miscellaneous

Drug
hydroxyurea
L-asparaginase

mechanism of action
inhib RNA reductase inhib DNA synth
uses up asparagine (essntl aa for tumors)

side effects
hypersensitivity

25