Alpha

blocker

ØNonselective α-blocker
• Irreversible : Phenoxybenzamine
• Reversible : Phentolamine

ØSelective α-blocker
• selective α1-blocker
Ex.Prazoin,doxazoin , terazoin
• selective α2-blocker
Ex.Yohimbine
Katzung BG, Trevor A. PharmacologyExamination & Board Review 10th ed, 2013
Relative selectivity of antagonists for adrenoceptors

Katzung BG. Basic & Clinical

Pharmacology 14th ed ,2018
Alpha blocker

• Cardiovascular effects
-decrease TPR , BP
-reflex tachycardia : increase HR, CO, fluid retention
• Eye : Miosis
• Respiratory : Nasal congestion
• GI : increase intestinal motility
Nonselective α-blocker

Phenoxybenzamine
• Noncompetitive irreversible blocker : long-acting
• dilation both arterioles & veins —>decrease TPR , BP
• reflex tachycardia
• Inhibit reuptake of NE

Richard A.Harvey ,Lippincott’s Illustrated Reviews:Pharmacology 5th ed ,2012

Nonselective α-blocker
Phentolamine
• Competitive reversible blocker : short-acting
• dilation both arterioles & veins —>decrease TPR , BP
• reflex tachycardia
selective α1-blocker
Prazosin
• Prototype for selective α1-blocker
• Affinity binding to α1 ~1000folds than α2 receptor
• Relax smooth muscle of both arterioles & veins
—> decrease TPR , BP
• Less tachycardia
Therapeutic uses of α-blocker

• Hypertension
• Benign Prostatic Hypertrophy (BPH)
• Pheochromocytoma : high level of NE and Epi released from adrenal
medulla
-Phenoxybenzamine, Phentolamine
Adverse effect
• Orthostatic hypotension
• Reflex tachycardia
• Sexual dysfunction
• Nasal congestion

Richard A.Harvey ,Lippincott’s Illustrated Reviews:Pharmacology 5th ed ,2012

Katzung BG, Trevor A. PharmacologyExamination & Board Review 10th ed, 2013
References
• Brunton LL, Chabner BA, Knollmann BC. Goodman & Gliman’s The
Pharmacological Basis of Therapeutics 12th ed, 2013
• Katzung BG, Trevor A. Basic & Clinical Pharmacology 14th ed, 2018
• Katzung BG, Trevor A. PharmacologyExamination & Board Review
10th ed, 2013