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Pharm L10
Adenoreceptor Antagonists
9
Medical
Graduate
05/07/2009

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Term
phentolamine
Definition
a1 and a2 pure competitive antagonist, reversible. decrease in bp (a1). reflex tachycardia (a2). Adverse: tachycardia, nasal congestion, headache. Uses: pheochromocytoma and male erectile dysfxn (not anymore).
Term
prazosin
Definition
a1 antagonist, reversible. high first pass metabolism. Lacks reflex tachycardia. Uses: HTN, BPH.
Term
phenoxybenzamine
Definition
irreversible a antagonist. 14-48 hrs duration. also blocks NE reuptake. reduces bp, baroreceptor reflex may increase CO. Enters CNS. Adverse: ortostatic hypotension, tachycardia, nasal stuffiness, inhibition of ejaculation, fatigue, sedation, nausea. Uses: pheochromocytoma.
Term
propranolol
Definition
Protoype non selective b1 and b2 antagonist. pure competitive antagonist. no ISA. high first pass, large Vd. Uses: HTN, angina, tachaycardia and arrythmia, ventricular contractions, MI, pheochromocytoma, migrane prophylaxis. Adverse: bardycardia, less contractility, decresed CO, bronchoconstriction, exercise intolerance, fatigue, sleep probs. Contraindications: diabetes mellitus.
Membrane stabilizing, so cant use in glaucoma.
Term
pindolol
Definition
partial agonist b1 and b2. ISA. Uses: HTN, angina.
Also: membrane stabilizing.?
Term
metoprolol
Definition
pure b1 selective antagonist, competitive. No ISA, no membrane stabilizing. Uses: stable angia, CHF. Contraindications: acute MI, higher order heart block.
Term
atenolol
Definition
pure competitive b1 antagonist. no ISA or membrane stabilizing. Uses: HTN.
Term
labetalol
Definition
competitive b1 and b2 antagonist and also a1 antagonist. ISA at b receptors. Uses: HTN. Rare Adverse: liver failure.! Contraindicated: CHF
Term
carvedilol
Definition
new generation of b1, b2, and a1 blockers. antioxidant. antiproliferative effects (prevent heart remodeling). No ISA. Membrane Stabilizing. Vasodilates. Uses: CHF.
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