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51 Cards in this Set

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Isoproterenol
isuprel
non-selective Beta-AR agonist
extremely potent Beta-AR
potent vasodilator
positive chronotropy
Adverse reactions: isoproterenol
tachycardia, BP, arrhythmias
Phenylephrine

(neosynephrine)
alpha-1 AR agonist
Phenylephrine
relatively pure alpha-AR agonist
potent constrictor
similar but less potent than NE
not inactivated by COMT (increase the bioavailability)
nasal decongestion, mydriatic (dilation of pupil), hypertensive
Clonidine
catapress

alpha-2 AR agonist
Clonidine
alpha-2 agonist
orally prolonged hypotensive response (CNS)

IV, acute hypertensive response followed by hypotension
Clinical uses for Clonidine
hypertension, menopausal flushing, and migraines
Adverse effects of Clonidine
remember, Clonidine is an alpha-2 agonist

dry mouth, sedation, and contact dermatitis
Dobutamine
Dobutrex

Beta-1 AR agonist
Dobutamine

Dobutrex
Beta-1 AR agonist

acts directly on B1-AR in the heart

force > rate

cardiogenic shock
Dobutamine

Dobutrex

(non-heart related things)
dilates renal and mesenteric vessels

IV infusion for (+) inotropic effect in cardiac decompensation
Dobutamine

Adverse reactions
tachycardia, hypertension, hypotension, ectopic activity
Albuterol
Ventolin

Beta-2 AR agonist
Albuterol

(Ventolin)
bronchodilator: oral, inhalation, and IV

adverse reactions: tachycardia, tremor, tolerance
Ephedrine
indirect acting agonist

alkaloid from plant

increases NE release, direct agonism

prolonged action duration, potent CNS stimulant

nasal decongestant, treatment hypotension
adverse reactions of Ephedrine
hypertension, insomnia, tachyphylaxis
Amphetamine
indirect acting agonist

release of biogenic amines from storage

has no hydroxyl groups and is therefore hydrophobic...can easily get into the CNS
Amphetamine activites
potent CNS stimulant

prolonged action duration

treatment of obesity, narcolepsy, attention deficit disorder
Adverse reactions of amphetamine
restlessness, tremor, irritability, insomnia, dependency, and tolerance
Tyramine
indirect acting agonist

release of biogenic amines from storage (like NE and epi)

byproduct of tyrosine metabolism

high concentration in fermented blood

metabolized by liver MAO

caution MAO inhibitors, severe hypertension
Cocaine
indirect acting agonist

inhibition of NE and dopamine reuptake

local anesthetic effect also potent CNS stimulant

shorter lasting, but more intense, than amphetamine

hypertension, AMI, arrhythmias, seizures
activation of alpha-1 AR causes...
contraction and constriction
activation of alpha-2 AR causes...
inhibition of NE release
activation of Beta-1 AR causes...
increase in heart rate and contractility
activation of beta-2 AR causes...
relaxation of smooth muscle airways and uterus
sympatholytic
blocks sympathetic activity
3 mechanisms to block sympathetic activity
1. decrease sympathetic outflow from brain
2. suppress nerve terminal NE (inhibit synthesis, deplete granules, and suppress release of NE)
3. block postsynaptic receptors (best way)
bretylium and guanethidine
inhibits the release of NE from the nerve terminal
alpha-AR blockers
vasodilation, decreases BP
Phentolamine

(Regitine)
Regitine

a nonselective alpha-AR blocker

reversible

rarely used
Phenoxybenzamine

(Dibenzyline)
Dibenzyline

alpha-AR blocker

irreversible

use in peripheral vasospasm
adverse reactions to alpha-AR blockers
hypotension, tachycardia
alpha-1 selective blockers
vasodilation and reduction in arterial pressure

no reflex tachycardia

useful for hypertension and BPH

no decrease cardiac function
alpha-2 selective blockers
are not clinically useful
Prazosin
Minipress

antihypertensive

used alone or in combination

alpha-1 AR selective blockers
Adverse reactions of prazosin (minipress)
"first dose" effect

postural hypotension
Beta-1 AR blockade reactions
CV effects:

reduce HR, delay AV conduction, decrease rate of depolarization, decrease force of contraction, decrease O2 consumption, decrease BP, inhibit renin release, and peripheral edema
Beta-2 AR blockade reactions
vasoconstriction in arterioles, increased airways resistance, decreased glycogenolysis and gluconeogenesis, and inhibition of insulin release

(MUST be careful in diabetic and asthmatic patients...for diabetics, you can really cause severe hypoglycemia)
Propranolol
Inderal

beta-AR non selective blocker
Propranolol

Inderal
beta-AR non selective blocker

degree of antagonism is dependent on the prevailing sympathetic tone

exhibits equal affinity for beta 1 and beta 2

highly lipophilic, readily enters CNS

membrane stabilizing effect observed at higher concentrations
Uses of propranolol (Inderal)
used in treatment of hypertension and IHD

IV for life-threatening arrhythmias

IV and oral formulations
Serious reactions of Propranolol (Inderal)
severe bradycardia, CCF, bronchoconstriction, hypoglycemia, and aggravated PVD
Timolol
Blocadren

beta-AR non selective blocker
Timolol (Blocadren)
no intrinsic sympathomimetic activity

no membrane stabilizing

low lipophilicity

used to treat open angle glaucoma

adverse reactions: bronchoconstriction
Pindolol
Visken

has intrinsic sympathomimetic activity

partial agonist activity

low degree of membrane stabilization

adverse reaction: bronchoconstriction, bradycardia
the partial agonist activity of Pindolol is important because...
1. maintains some degree of beta-1 AR activation while blunting the cardiac response to increased SANS

2. produces smaller reductions in resting HR

3. useful in patients dependent on sympathetic drive because of poor cardiac reserve

4. preferred in patients subject to bradycardia
Sotalol
Betapace

beta-AR non-selective blocker

prolongs cardiac action potential

blocks K+ channels

used for atrial and ventricular tachyarrhythmias
Metoprolol
Lopressor

Beta-1 AR selective blocker

no ISA

hepatic biotransformation (can give to patients with renal insufficiency)

used for hypertension, ischemic HD

adverse reactions: bronchoconstriction and bradycardia
Atenolol
Tenormin

Beta-1 selective blocker

hypertension

renal excretion (use with patients who have liver problems)

ischemic heart disease

adverse reaction: bronchoconstriction, bradycardia
Labetolol
Normodyne, trandate

Beta-non selective blocker and alpha-1 AR blocking

Beta-1 = beta 2 > alpha 1 > alpha 2

hypertension and pheochromocytoma

adverse reactions: hypotension, tachycardia
Carvedilol
Coreg

beta-AR non selective blocker and alpha-AR blocking

Beta-1 = Beta-2 > alpha1 > alpha2

antioxidant effects

improves survival with heart failure