title: The angiotensin II type 1 receptor antagonists. A new class of antihypertensive drugs.
abstract: The angiotensin II (AII) type 1 receptor antagonists represent a new pharmacologic class of drugs that are specifically designed to displace AII from its type 1 receptor subtype. These drugs antagonize AII-induced biologic actions, including smooth-muscle contraction, sympathetic pressor mechanisms, and aldosterone release. Initial clinical trials suggest that these drugs are effective in the treatment of essential hypertension and hypertensive patients with intrinsic renal disease. Thus, they are the newest addition to the therapeutic armamentarium for the treatment of hypertensive diseases. We review the developmental history and pharmacology of the AII type 1 receptor antagonists. We specifically discuss the following factors: mechanism(s) of action; members under clinical investigation; effects on renal function, salt and water excretion, and plasma renin activity, plasma AII type 1, and plasma aldosterone concentrations; and efficacy and safety. Given the demonstrable benefits of AII type 1 receptor blockade, these drugs should achieve broad utility in the treatment of hypertensive diseases.
authors.affiliation: Department of Internal Medicine, University of Missouri School of Medicine, Columbia, USA.
authors.forename: J H
authors.initials: JH
authors.lastname: Bauer
authors.forename: G P
authors.initials: GP
authors.lastname: Reams
mesh_terms: D000179:Acrylates / Q000494:pharmacology; D057911:Angiotensin Receptor Antagonists; D000818:Animals; D000959:Antihypertensive Agents / Q000009:adverse effects / Q000494:pharmacology*; D001562:Benzimidazoles / Q000494:pharmacology; D001565:Benzoates / Q000494:pharmacology; D001713:Biphenyl Compounds / Q000494:pharmacology; D006801:Humans; D007093:Imidazoles / Q000494:pharmacology; D000077405:Irbesartan; D019808:Losartan; D011725:Pyridines / Q000494:pharmacology; D011804:Quinolines / Q000494:pharmacology; D000077333:Telmisartan; D013777:Tetrazoles / Q000494:pharmacology; D013876:Thiophenes; D014633:Valine / Q000031:analogs & derivatives / Q000494:pharmacology; D000068756:Valsartan; D005466:Fluorocarbons
chemical_list: D000179:Acrylates; D057911:Angiotensin Receptor Antagonists; D000959:Antihypertensive Agents; D001562:Benzimidazoles; D001565:Benzoates; D001713:Biphenyl Compounds; D007093:Imidazoles; D000077405:Irbesartan; D019808:Losartan; D011725:Pyridines; D011804:Quinolines; D000077333:Telmisartan; D013777:Tetrazoles; D013876:Thiophenes; D014633:Valine; D000068756:Valsartan; C085920:2-butyl-3-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-3H-imidazo(4,5-b)pyridine; C084927:forasartan; C069045:DuP 532; D005466:Fluorocarbons; C081112:ICI D8731; C068373:eprosartan; C070967:L 158809; C066026:losartan carboxylic acid; C077793:candesartan cilexetil