Pharmacology Drugs From First Aid For The Usmle Step 1, 2009 Ed.

Front 1

What do alpha 1 receptors do?

Back 1

increase vascular smooth muscle contraction, increase pupillary dilator muscle contraction (mydriasis)

Front 2

What do alpha 2 receptors do?

Back 2

decrease sympathetic outflow, decrease insulin release

Front 3

What do beta 1 receptors do?

Back 3

increase HR, increase contractility, increase lipolysis, increase renin release

Front 4

What do beta 2 receptors do?

Back 4

increase HR, increase contractility, increase lipolysis, increase glucagon release.
decrease uterine tone
cause vasodilation, bronchodilation

Front 5

What do M1, M2, and M3 receptors do?

Back 5

M1: CNS and ENS
M2: decrease HR and contractility of atria
M3: increase exocrine gland secretions, increase gut peristalsis, increase bladder contraction, bronchoconstriction, increase pupillary sphincter mus cle contraction (miosis), ciliary muscle contraction (accommodation)

Front 6

What do D1 and D2 receptors do?

Back 6

D1: relaxes renal vascular smooth muscle
D2: modulates NT release, especially in brain

Front 7

What do H1 and H2 receptors do?

Back 7

H1: increase nasal and bronchial mucus production, contraction of bronchioles, pruritis, pain
H2: increase gastric acid secretion

Front 8

What do V1 and V2 receptors do?

Back 8

V1: increase vascular smooth muscle contraction
V2: increase water permeability and reabsorption in the collecting tubules of the kidney

Front 9

What do H1, alpha 1, V1, M1, M3 (HAVe 1 M&M) have in common?

Back 9

All use Gq --> phospholipase C --> PIP2 --> IP3 and DAG --> increased calcium and protein kinase C

Front 10

What do B1, B2, D1, H2, V2 (Bubble Boy Don't Have Virus) have in common?

Back 10

All use Gs --> adenylate cyclase --> increased cAMP --> increased PK A.

Front 11

What do M2, alpha2, and D2 (MAD 2's) have in common?

Back 11

All use Gi, which blocks adenylyl cyclase --> decreased cAMP --> decreased PK A.

Front 12

Bethanechol

Back 12

Direct cholinergic agonist, used for post-op and neurogenic ileus and urinary retention. (activates bowels and bladder)

Front 13

Carbachol

Back 13

Direct cholinergic agonist, used for glaucoma, pupillary contraction, and release of intraocular pressure

Front 14

Pilocarpine

Back 14

Direct cholinergic agonist, used for xeropthalmia, as an antidote for scopalamine (or atropine or hyoscyamine) poisoning, narrow angle glaucoma (contracts pupillary sphincter), wide angle glaucoma (contracts ciliary muscle). Potent stimulator of sweat, tears, saliva.
Resistant to AChE.

Front 15

Methacholine

Back 15

Direct cholinergic agonist, used in challenge test for dx of asthma b/c stiulates muscarinic receptors in airway when inhaled.

Front 16

neostigmine

Back 16

Indirect cholinergic agonst (acetylcholinesterase inhibitor); used for post-op and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade (post-op). No CNS penetration.

Front 17

Pyridostigmine

Back 17

Indirect cholinergic agonist (AChE inhibitor); used for myasthenia gravis (long acting), does not penetrate CNS

Front 18

Edrophonium

Back 18

Indirect cholinergic agonist (AChE inhibitor); used for dx myasthenia gravis

Front 19

Physostigmine

Back 19

Indirect cholinergic agonist (AChE inhibitor); used for glaucoma and atropine OD.

Front 20

Echothiophate

Back 20

Indirect cholinergic agonist (AChE inhibitor); used for glaucoma.

Front 21

Symptoms of Cholinesterase Inhibitor Poisoning (e.g. parathion and other organophosphates, which are irreversible inhibitors) --> too much acetylcholine!

Back 21

DUMBBELSS
Diarrhea
Urination
Miosis
Bronchospasm, Bradycardia
Excitation of skeletal muscle and CNS
Lacrimation
Sweating and Salivation (also abdominal cramping)

Treatment: atropine (muscarinic antagonist) plus pralidoxime (chemical antagonist binds to organophosphate, removing it from AChE and regenerating the latter).

Front 22

Atropine (bella donna alkaloid)

Back 22

Muscarinic antagonist.
Blocks DUMBBELLS
increased pupil dilation and cycloplegia
decrease secretions
acid secretion
decreased motility
decreased urgency in cystitis
TOXICITY: increased body temp, rapid pulse, dry mouth, dry flushed skin; cycloplegia, constipation, disorientation.(Hot as a hare, dry as a bone, red as a beet, blind as a bat, mad as a hatter).
ELDERLY: acute angle-closure glaucoma and urinary retention in men w/ BPH
INFANTS: hyperthermia

Front 23

Hexamethonium

Back 23

nicotinic antagonist
ganglionic blocker used in experimental models to prevent vagal reflex responses to changes in BP; e.g. prevents reflex bradycardia caused by NE.
TOXICITY: severe orthostatic hypotension, blurred vision, constipation, sexual dysfunction.

Front 24

Epinephrine

Back 24

alpha 1 and 2, beta 1 and 2 AGONIST!! low doses selective for beta 1.
APPLICATIONS: anaphylaxis, open angle glaucoma, asthma, hypotension

Front 25

NE

Back 25

alpha 1 and 2 > beta 1
USE: hypotension (but decrease renal perfusion)

Front 26

Isoproterenol

Back 26

beta 1 = beta 2
USE: AV block

Front 27

Dopamine

Back 27

D1 = D2 > beta > alpha (agonist)
inotropic AND chronotropic
USE: shock (increase renal perfusion), heart failure

Front 28

Dobutamine

Back 28

beta 1>beta2 (agonist)
only inotropic
shock, heart failure, cardiac stress testing

Front 29

phenylephrine

Back 29

alpha 1>alpha 2 (agonist)
USE: pupillary dilation, vasoconstriction, nasal decongestion

Front 30

albuterol
terbutaline

Back 30

beta 2>beta 1 (agonist)
albuterol for acute asthma
terbutaline reduces premature uterine contractions

Front 31

ritodrine

Back 31

beta 2 (agonist)
reduces premature uterine contractions

Front 32

Dopamine

Back 32

D1 = D2 > beta > alpha (agonist)
inotropic AND chronotropic
USE: shock (increase renal perfusion), heart failure

Front 33

Dobutamine

Back 33

beta 1>beta2 (agonist)
only inotropic
shock, heart failure, cardiac stress testing

Front 34

phenylephrine

Back 34

alpha 1>alpha 2 (agonist)
USE: pupillary dilation, vasoconstriction, nasal decongestion

Front 35

albuterol
terbutaline

Back 35

beta 2>beta 1 (agonist)
albuterol for acute asthma
terbutaline reduces premature uterine contractions

Front 36

ritodrine

Back 36

beta 2 (agonist)
reduces premature uterine contractions

Front 37

amphetamine

Back 37

indirect general sympathomimetic agonist, releases stored catecholamines.
USE: narcolepsy, obesity, ADD

Front 38

ephedrine

Back 38

indirect general sympathomimetic agonist, releases stored catecholamines
USE: nasal decongestion, urinary incontinence, hypotension

Front 39

cocaine

Back 39

indirect general sympathomimetic agonist; inhibits uptake.
CAUSES: vasoconstriction and local anesthesia

Front 40

clonidine
alpha-methyldopa

Back 40

centrally acting alpha-2 agonist, decrease central adrenergic outflow.
USE: HTN, especially w/ renal dz (no decrease in blood flow to kidney)

Front 41

selective beta 2 agonists

Back 41

metaproterenol (for asthma)
albuterol
salmeterol (long acting, for asthma prophylaxis)
terbutaline
ritodrine (reduces premature uterine contractions)

Front 42

phenoxybenzamine
phentolamine

Back 42

nonselective alpha blockers
phenoxyenzamine is irreversible, phentolamine is reversible.
USE: pheochromocytoma (use phenoxybenzamine before removing tumor, since high levels of released catecholamines will not be able to overcome blockage
TOXICITY: orthostatic hypotension, reflex tachycardia

Front 43

prazosin, terazosin, doxazosin

Back 43

alpha 1 selective blockers
USE: HTN, urinary retention in BPH
TOXICITY: 1st dose orthostatic hypotension, dizziness, HA

Front 44

mirtazapine

Back 44

alpha 2 selective blocker
USE: DEPRESSION
TOXICITY: sedation, increased serum chol, increased appetite

Front 45

What are beta blockers used for, and how do they exert their effects?

Back 45

HTN - (decreased CO, decreased renin secretion)
ANGINA PECTORIS - (esp. propranolol) --> decreased HR and contractility --> decreased O2 consumption
MI - beta blockers decrease mortality
ARRHYTHMIA PROPHYLAXIS AFTER MI (propranolol, metoprolol, timolol) - reduced automaticity of all cardiac pacemakers
SVT (propranolol, esmolol, acebutolol) - decreased AV conduction velocity (class II antiarrhythmic)
CHF - slows progression of chronic failure
GLAUCOMA (timolol) - decreases secretion of aqueous humor.
HYPERTROPHIC CARDIOMYOPATHY: (propranolol) - slowed rate contraction
MIGRAINE PROPHYLAXIS - propranolol
FAMILIAL TREMOR - propranolol
Thyroid storm, thyrotoxicosis (propranolol, esmolol) -

Front 46

TOXICITY OF BETA BLOCKERS?

Back 46

impotence, exacerbation of asthma, CV adverse effects (bradycardia, AV block, CHF), CNS adverse effects (sedation, sleep alterations); use w/ caution in diabetics.

Front 47

Non-selective beta blockers

Back 47

propranolol, timolol, nadolol, pindolol, labetolol

Front 48

beta-1 selective antagonists (beta 1 > beta 2)

Back 48

acebutol (partial agonist), betaxolol, esmolol (short acting), atenolol, metoprolol.

Front 49

non-selective alpha and beta antagonists

Back 49

carvedilol, labetalol - decrease mortality in heart failure

Front 50

partial beta agonists

Back 50

pindolol, acebutolol
these may be better choices (esp. acebutolol) for a pt w/ Asthma or COPD, b/c they have some intrinsic sympathomimetic activity.