HUMAN PHARMACOKINETIC PHARMACODYNAMIC PROFILE OF IRBESARTAN - A NEW POTENT ANGIOTENSIN-II RECEPTOR ANTAGONIST/

Background Inhibition of the renin-angiotensin system has been the foc us of considerable research as the enzymatic pathway resulting in the production of angiotensin II is implicated in the development of hyper tension and cardiovascular disease. Angiotensin converting enzyme inhi bitors Blocking the renin-angiotensin system with angiotensin converti ng enzyme (ACE) inhibitors is an effective blood pressure control meas ure, but is less than ideal due to incomplete blockade and the effects of concomitant blockade of kinase II. Angiotensin II receptor antagon ists Angiotensin II receptor antagonists block the renin-angiotensin s ystem 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 pharmacokine tic/pharmacodynamic properties that are close to ideal for an antihype rtensive agent, Irbesartan is a specific AT(1) receptor antagonist wit h rapid oral bioavailability (peak plasma concentrations occurring at 1.5-2 h after administration) and a long half-life (11-15 h) that prov ides 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 o ther angiotensin II receptor antagonists, irbesartan is relatively una ffected by food or drugs. Conclusions The pharmacokinetic/pharmacodyna mic properties of irbesartan have been demonstrated to provide superio r blood pressure control and tolerability in all classes of hypertensi on and patient populations.