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Hypertension Drugs

Mechanism of action for the major categories of antihypertensives

DrugMechanism of Action
ACE inhibitors (captopril, enalapril) Inhibition of ACE leads to reduced angiotensin II (vasodilation) and aldosterone (reduced Na+ retention) levels and increased bradykinin (--> vasodilation) levels.
Angiotensin antagonists (losartan and EXP3174) Inhibition of angiotensin II receptor (--> vasodilation)
Ca++ antagonists (verapamil, diltiazem) Block Ca++ channels. Decreased intracellular Ca++ leads to reduced contractility and vasodilatation.
α1-antagonists (prazosin, doxazocin) Inhibition of α1-mediated vasoconstriction reduces peripheral resistance and venous pressure. Also improves lipid profile to decrease risk of CAD.
Sodium nitroprusside Decomposes to NO, which activate guanylyl cyclase, thus increasing cGMP levels, and causing vasodilatation
Thiazide diuretics (hydrochlorothiazide, polythiazide) Reduction of blood volume/indirect vasodilatation
Centrally acting drugs (clonidine, α-methyldopa) α2-agonists. False transmitter activates central inhibitory neurons, causing inhibition of NA release and vasodilatation.
β-antagonists (nonselective - propranolol, selective - atenolol) Block β1-receptors in heart, causing decreased rate, systolic BP, cardiac contractility, and myocardial O2 demand. Work in heart, kidney (RAS), and CNS
Created by: golfspy



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