Adrenergic Agonist Lecture

Front 1

Isoproterenol

Back 1

isuprel
non-selective Beta-AR agonist
extremely potent Beta-AR
potent vasodilator
positive chronotropy

Front 2

Adverse reactions: isoproterenol

Back 2

tachycardia, BP, arrhythmias

Front 3

Phenylephrine

(neosynephrine)

Back 3

alpha-1 AR agonist

Front 4

Phenylephrine

Back 4

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

Front 5

Clonidine

Back 5

catapress

alpha-2 AR agonist

Front 6

Clonidine

Back 6

alpha-2 agonist
orally prolonged hypotensive response (CNS)

IV, acute hypertensive response followed by hypotension

Front 7

Clinical uses for Clonidine

Back 7

hypertension, menopausal flushing, and migraines

Front 8

Adverse effects of Clonidine

Back 8

remember, Clonidine is an alpha-2 agonist

dry mouth, sedation, and contact dermatitis

Front 9

Dobutamine

Back 9

Dobutrex

Beta-1 AR agonist

Front 10

Dobutamine

Dobutrex

Back 10

Beta-1 AR agonist

acts directly on B1-AR in the heart

force > rate

cardiogenic shock

Front 11

Dobutamine

Dobutrex

(non-heart related things)

Back 11

dilates renal and mesenteric vessels

IV infusion for (+) inotropic effect in cardiac decompensation

Front 12

Dobutamine

Adverse reactions

Back 12

tachycardia, hypertension, hypotension, ectopic activity

Front 13

Albuterol

Back 13

Ventolin

Beta-2 AR agonist

Front 14

Albuterol

(Ventolin)

Back 14

bronchodilator: oral, inhalation, and IV

adverse reactions: tachycardia, tremor, tolerance

Front 15

Ephedrine

Back 15

indirect acting agonist

alkaloid from plant

increases NE release, direct agonism

prolonged action duration, potent CNS stimulant

nasal decongestant, treatment hypotension

Front 16

adverse reactions of Ephedrine

Back 16

hypertension, insomnia, tachyphylaxis

Front 17

Amphetamine

Back 17

indirect acting agonist

release of biogenic amines from storage

has no hydroxyl groups and is therefore hydrophobic...can easily get into the CNS

Front 18

Amphetamine activites

Back 18

potent CNS stimulant

prolonged action duration

treatment of obesity, narcolepsy, attention deficit disorder

Front 19

Adverse reactions of amphetamine

Back 19

restlessness, tremor, irritability, insomnia, dependency, and tolerance

Front 20

Tyramine

Back 20

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

Front 21

Cocaine

Back 21

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

Front 22

activation of alpha-1 AR causes...

Back 22

contraction and constriction

Front 23

activation of alpha-2 AR causes...

Back 23

inhibition of NE release

Front 24

activation of Beta-1 AR causes...

Back 24

increase in heart rate and contractility

Front 25

activation of beta-2 AR causes...

Back 25

relaxation of smooth muscle airways and uterus

Front 26

sympatholytic

Back 26

blocks sympathetic activity

Front 27

3 mechanisms to block sympathetic activity

Back 27

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)

Front 28

bretylium and guanethidine

Back 28

inhibits the release of NE from the nerve terminal

Front 29

alpha-AR blockers

Back 29

vasodilation, decreases BP

Front 30

Phentolamine

(Regitine)

Back 30

Regitine

a nonselective alpha-AR blocker

reversible

rarely used

Front 31

Phenoxybenzamine

(Dibenzyline)

Back 31

Dibenzyline

alpha-AR blocker

irreversible

use in peripheral vasospasm

Front 32

adverse reactions to alpha-AR blockers

Back 32

hypotension, tachycardia

Front 33

alpha-1 selective blockers

Back 33

vasodilation and reduction in arterial pressure

no reflex tachycardia

useful for hypertension and BPH

no decrease cardiac function

Front 34

alpha-2 selective blockers

Back 34

are not clinically useful

Front 35

Prazosin

Back 35

Minipress

antihypertensive

used alone or in combination

alpha-1 AR selective blockers

Front 36

Adverse reactions of prazosin (minipress)

Back 36

"first dose" effect

postural hypotension

Front 37

Beta-1 AR blockade reactions

Back 37

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

Front 38

Beta-2 AR blockade reactions

Back 38

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)

Front 39

Propranolol

Back 39

Inderal

beta-AR non selective blocker

Front 40

Propranolol

Inderal

Back 40

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

Front 41

Uses of propranolol (Inderal)

Back 41

used in treatment of hypertension and IHD

IV for life-threatening arrhythmias

IV and oral formulations

Front 42

Serious reactions of Propranolol (Inderal)

Back 42

severe bradycardia, CCF, bronchoconstriction, hypoglycemia, and aggravated PVD

Front 43

Timolol

Back 43

Blocadren

beta-AR non selective blocker

Front 44

Timolol (Blocadren)

Back 44

no intrinsic sympathomimetic activity

no membrane stabilizing

low lipophilicity

used to treat open angle glaucoma

adverse reactions: bronchoconstriction

Front 45

Pindolol

Back 45

Visken

has intrinsic sympathomimetic activity

partial agonist activity

low degree of membrane stabilization

adverse reaction: bronchoconstriction, bradycardia

Front 46

the partial agonist activity of Pindolol is important because...

Back 46

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

Front 47

Sotalol

Back 47

Betapace

beta-AR non-selective blocker

prolongs cardiac action potential

blocks K+ channels

used for atrial and ventricular tachyarrhythmias

Front 48

Metoprolol

Back 48

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

Front 49

Atenolol

Back 49

Tenormin

Beta-1 selective blocker

hypertension

renal excretion (use with patients who have liver problems)

ischemic heart disease

adverse reaction: bronchoconstriction, bradycardia

Front 50

Labetolol

Back 50

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

Front 51

Carvedilol

Back 51

Coreg

beta-AR non selective blocker and alpha-AR blocking

Beta-1 = Beta-2 > alpha1 > alpha2

antioxidant effects

improves survival with heart failure