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Classes of Antihypertensive Drugs Aldosterone receptor antagonists (blockers) Angiotensin II antagonists Angiotensin-converting enzyme inhibitors -Blockers 1-Selective Nonselective -Blockers -1/-2 -1 predominant / Intrinsic sympathomimetic activity Calcium channel antagonists Nondihydropyridine Dihydropyridine Central 2 agonists Direct renin inhibitors Direct vasodilators Diuretics Thiazide-type Loop-type Potassium-sparing Ganglionic blockers Classes of Antihypertensive Drugs There are currently 11 classes and more than 200 different drugs or combinations of drugs approved by the United States Food and Drug Administration to treat hypertension. This slide outlines the different classes of antihypertensive drugs and highlights the major pharmacological differences among drugs within each class when there is important heterogeneity within the class. On average, most antihypertensive drugs decrease systolic and diastolic blood pressures by about 10 mm Hg and 5 mm Hg, respectively, when administered as monotherapy. 2

Antihypertensive Drug Classes: Action Sites Cardiac Output  Blood Pressure Total Peripheral Resistance = -Blockers Non-DHP CCBs Diuretics -Blockers ACE Inhibitors AT1 Blockers Direct renin inhibitors 1-Blockers 2-Agonists All CCBs Diuretics Sympatholytics Vasodilators Antihypertensive Drug Classes Antihypertensive Drug Classes: Action Sites β-Blockers decrease blood pressure primarily by reducing cardiac output. They also decrease renal renin output and, thereby, angiotensin II-mediated vasoconstriction. Angiotensin-converting enzyme inhibitors, angiotensin type-1 blockers, direct renin inhibitors, 1-blockers, 2-agonists, sympatholytics, and vasodilators decrease blood pressure by reducing total peripheral resistance through various mechanisms. Calcium channel blockers can either affect total peripheral resistance (dihydropyridines) or can reduce both cardiac output and total peripheral resistance (nondihydropyridines). Diuretics initially reduce cardiac output by decreasing intravascular fluid volume; with continued therapy, however, they also reduce total peripheral resistance via vasodilation. ACE = angiotensin-converting enzyme; AT1 = angiotensin type 1; CCBs = calcium channel blockers; DHP = dihydropyridine 3

Summary Drugs from 11 major classes have been approved by the United States Food and Drug Administration to treat hypertension Many of these drugs have complementary effects to reduce blood pressure and prevent target organ damage The goal of antihypertensive therapy is to use doses of drugs that effectively lower blood pressure while minimizing adverse effects Combinations of drugs that have complementary actions – or allow the actions of one drug to offset the adverse effects of a second drug – are often required to achieve this goal The dose-response relationship for a single drug may vary with the target organ-protective effect for which that drug is being prescribed Summary 4