PMID: 9532516Apr 9, 1998Paper

Human pharmacokinetic/pharmacodynamic profile of irbesartan: a new potent angiotensin II receptor antagonist

Journal of Hypertension. Supplement : Official Journal of the International Society of Hypertension
L M Ruilope

Abstract

Inhibition of the renin-angiotensin system has been the focus of considerable research as the enzymatic pathway resulting in the production of angiotensin II is implicated in the development of hypertension and cardiovascular disease. Blocking the renin-angiotensin system with angiotensin converting enzyme (ACE) inhibitors is an effective blood pressure control measure, but is less than ideal due to incomplete blockade and the effects of concomitant blockade of kinase II. Angiotensin II receptor antagonists block the renin-angiotensin system at the receptor level, and thus impede the system regardless of the pathway responsible for the formation of ACE. Irbesartan is a new, unique angiotensin II receptor antagonist with favorable pharmacokinetic/pharmacodynamic properties that are close to ideal for an antihypertensive agent. Irbesartan is a specific AT1 receptor antagonist with rapid oral bioavailability (peak plasma concentrations occurring at 1.5-2 h after administration) and a long half-life (11-15 h) that provides 24-h blood pressure control with a single daily dose. The maximal blood pressure fall occurs between 3 and 6 h after the dose. Unlike other angiotensin II receptor antagonists, irbesartan is relatively unaffected...Continue Reading

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