THE ANGIOTENSIN-II TYPE-1 RECEPTOR ANTAGONISTS - A NEW CLASS OF ANTIHYPERTENSIVE DRUGS

he angiotensin II (AII) type 1 receptor antagonists represent a new ph armacologic class of drugs that are specifically designed to displace AII from its type 1 receptor subtype. These drugs antagonize AII-induc ed biologic actions, including smooth-muscle contraction, sympathetic presser mechanisms, and aldosterone release. Initial clinical trials s uggest that these drugs are effective in the treatment of essential hy pertension and hypertensive patients with intrinsic renal disease. Thu s, they are the newest addition to the therapeutic armamentarium for t he treatment of hypertensive diseases. We review the developmental his tory and pharmacology of the AII type 1 receptor antagonists. We speci fically discuss the following factors: mechanism(s) of action; members under clinical investigation; effects on renal function, salt and wat er excretion, and plasma renin activity, plasma AII type 1, and plasma aldosterone concentrations; and efficacy and safety. Given the demons trable benefits of AII type 1 receptor blockade, these drugs should ac hieve broad utility in the treatment of hypertensive diseases.