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Chapter 18
Adrenergic Antagonists
15
Medical
Graduate
09/11/2014

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Term
-What kind of blockades do most adrenergic antagonists produce?

-Which is more selective: adrenergic antagonists or agonists?

-What are the 2 groups?
Definition
-competitive (reversible)

-most adrenergic antagonists are more selective

-Alpha-adrenergic blocking agents and beta-adrenergic blocking agents
Term
Phenoxybenzamine and Phentolamine block what adrenergic receptors?
Definition
-a1 and a2
-nonspecific
-watch out for reflex tachycardia w a2 blockades!
Term
Alfuzosin, Doxazosin, Prazosin, Silodosin, Tamsulosin, Terazosin block what adrenergic receptors?
Definition
-a1 (a1-selective agents)
Term
Carteolol, Nadolol, Penbutolol, Pindolol, PROPRANOLOL, Sotalol, Timolol, block what adrenergic receptors?

how is Labetalol different?
Definition
-b1 and b2
-labetalol and carvidilol block b1, b2, and a1
Term
Acebutolol, Atenolol, Betaxolol, Bisoprolol, Esmolol, METOPROLOL, Nebivolol block what adrenergic receptors?
Definition
-b1 (b1-selective agents)
Term
How do adrenergic antagonists help with BPH? and HTN?
Definition
-reduce contraction of smooth muscle in bladder neck and prostatic capsule by giving a1 antagonist
-vasodilation
Term
What adrenergic drugs help with Pheochromocytoma and Raynauds?
Definition
-catecholamine secreting tumor in adrenal medulla
-principal cause of HTN is activation of a1 receptors (sometimes b1 too)
-need a1 adrenergic antagonist to help with surgery
Term
Effects of a1 blockade?
-on bp?
-on HR?
-mucous?
-ejaculation?
-Na?
Definition
-orthostatic hypotension
-reflex tachycardia (via ANS response)**MOST SIGNIF on a2 blockade!!
-nasal congestion
-inhibition of ejaculation (reversible)
-Reduced BP promotes renal retention of Na and H20 (usually combined w/ diuretic when used for HTN)
Term
What do you give when there is a phentolamine OD?
Definition
-NE to increase BP!
-Why not epinephrine? bc it activates b2 receptor which will cause vasodilation which can drop BP even more
Term
Why not use a a2 blockade on MI or angina pts?
Definition
-bc tachycardia will make problem worse so pt will need CCB or BB to prevent reflex tachycardia
Term
Adverse effects of b1 blockade?
Definition
-bradychardia
-reduced CO
-precipitation of HF
-AV heart block
-Rebound cardiac excitation
Term
Adverse effects of b2 blockade?
Definition
-bronchoconstriction
-inhibition of glycogenolysis *life threatening w/ DM
Term
Why is DM a contraindication of properanolol?
Definition
-bc it blocks b1 and b2 which inhibits glycogenolysis and therefore decreases BS
Term
Beta blockers:
1 generation?
2 generation?
3 generation?
Definition
-non selective (propranolol)
-cardioselective (metoprolol)
-vasodilating (carvidolol, labetalol)
Term
-What are nonselective beta blockers?
-adverse effects? (including CNS effects)
-drug interactions?
Definition
-1st generation BB (propranolol)
-bradycardia, AV heart block, HF, rebound cardiac excitation, bronchoconstriction, inhibition of glycogenolysis
-CNS: lipid soluble can cross BBB, insomnia, depression, nightmares, hallucinations, can cross placenta

-CCA (bc have same MOA and can lower HR and impair contractility), insulin
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