Drug List 3: Adrenergic Antagonists

Question 0

Phentolamine

Answer 0

Reversible alpha antagonist (non-selective),
Ind: pheochromocytoma, reverse vasoconstriction from alpha antagonists
Mech: decrease PVR, reflex increase CO
Admin: injection, FAST onset & short duration of action
SE: orthostatic hypotension, nasal congestion, miosis, tachycardia/angina, nausea/vomiting

Question 1

Phenoxybenzamine

Answer 1

Irreversible (!) alpha R antagonist,
Ind: pheochromocytoma, Raynaud’s disease
Mech: decrease PVR –> reflex increase CO (+ contractility & HR)
Admin: oral.
* 2-3 hr onset delay (prodrug), long duration (Irreversible)
SE: orthostatic hypotension, nail congestion, miosis, tachycardia/angina, nausea/vomiting

Question 2

Doxazosin

Answer 2

Alpha-1 antagonist,
Ind: hypertension, BPH, Raynauld’s disease
Mech: decrease PVR, no reflex CO change
SE: orthostatic hypotension, dizziness/vertigo, tachycardia, general hypotension

Question 3

Prazosin

Answer 3

Alpha-1 antagonist,
Ind: HTN, Raynauld’s disease
Mech: decrease PVR –> reflex increase HR & contractility, no CO reflex change
*heart increase = attenuated bc alpha-2 Rs spared (less reflex response)
SE: orthostatic hypotension, dizziness/vertigo, tachycardia, hypotension

Question 4

Terazosin

Answer 4

Alpha-1 antagonist,
Ind: HTN, BPH, Raynauld’s disease
Mech: decrease PVR, no reflex CO change
SE: orthostatic hypotension, dizziness/tachycardia, hypotension

Question 5

Atenolol

Answer 5

beta-1 antagonist
Ind: HTN in pts w/ increased risk (asthma, COPD, DM…), angina
Mech: decrease CO and BP, little change to PVR/pulmonary f(x)/metabolism
SE: cardiac failure, bradycardia, hypotension, fatigue

Question 6

Esmolol

Answer 6

Beta-1 antagonist
Ind: arrhythmia/hypertension (short acting, parenteral)
Mech: decrease CO & BP, little change PVR, pulm. f(x), or metabolism
SE: Cardiac failure, bradycardia, arrhythmia

Question 7

metoprolol

Answer 7

beta-1 antagonist
Ind: HTN for special pts (asthma/COPD/DM), angina, increase survival post-MI
Mech: decrease CO & BP, little change PVR, pulm. f(x), or metabolism
note: metablized by P450s in Liver!!
SE: cardiac failure, bradycardia, hypotension/fatigue

Question 8

Propanolol

Answer 8

beta-1 & beta-2 antagonist
Ind: HTN, migraine, hyperthyroidism, angina, increase survival post-MI, arrhythmias, performance anxiety
Mech: decrease HR &contractility (B1), block reflex effects (slowly decrease BP), increase PVR, bronchoconstriction, metabolic effects
SE: cardiac failure, arrhythmias, bronchoconstriction, hypotension/fatigue, hypoglycemia if insulin-dep. DM!
** should taper off to avoid rebound effects!**

Question 9

timolol

Answer 9

beta-1 & beta-2 antagonist
Ind: HTN, open-angle glaucoma, increase survival post-MI
mech: decrease CO & BP, bronchoconstrict, decrease intraocular pressure
SE: visual disturbances, cardiac failure, arrhythmias, bronchoconstriction, hypotension/fatigue, hypoglycemia in insulin-dep. DM!

Question 10

Nadolol

Answer 10

beta-1 & beta-2 antagonist
Ind: HTN, angina
Mech: decrease CO & BP, bronchoconstriction
* long duration of action!*
SE: cardiac failure, arrhythmias, bronchoconstriction, hypotension/fatigue, hypoglycemia in insulin-dep. DM!

Question 11

Acebutolol

Answer 11

beta-1 antagonist w/ ISA
Ind: HTN for special pts (asthma, COPD, DM, bradycardia)
Mech: mild decrease CO & BP, little change to PVR/pulm. f(x)/metabolism
SE: cardiac failure, bradycardia, hypotension/fatigue

Question 12

Pindolol

Answer 12

beta-1 & beta-2 antagonist w/ ISA
Ind: HTN for special pts (asthma, COPD, DM, bradycardia)
Mech: mild decrease CO & BP, little effect on PVR/pulm f(x)/metabolism
SE: cardiac failure, bradycardia, hypotension/fatigue

Question 13

LabetAlol

Answer 13

alpha-1 & beta-1 antagonist, beta-2 partial agonist (ISA)
Ind: pheochromocytoma, HTN emergencies
Mech: decrease PVR and CO
SE: orthostatic hypotension, cardiac failure, bradycardia, hypotension/fatigue

Question 14

Reserpine

Answer 14

indirect: blocks NE/DOPA/5-HT uptake into vesicles
Ind: mild-moderate HTN not used in USA
Mech: gradually reduce BP & CO
SE: MANY: nausea, GI, cramps, weight gain, nasal congestion, depression, etc. (too many to be good med.)

Question 15

Guanethidine

Answer 15

indirect: blocks AP-dep. release of NE
Ind: mild-moderate HTN not used in USA
Mech: gradually reduce BP & CO
SE: MANY: nausea, GI, cramps, weight gain, nasal congestion, depression, etc. (too many to be good med.)