Pharmacology of the angiotensin II receptor antagonist, eprosartan

Authors: Edwards R.M.; Ruffolo R.R.

Source: Expert Opinion on Investigational Drugs, Volume 7, Number 3, March 1998 , pp. 463-469(7)

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Abstract:

The non-peptide angiotensin II receptor antagonists represent a new class of drugs with demonstrated efficacy in the treatment of hypertension. Eprosartan is a potent, orally active AT₁ receptor antagonist which is chemically distinct from losartan and other non-peptide angiotensin II receptor antagonists. Eprosartan has a high affinity for the angiotensin II AT₁ receptor, but does not interact with the AT₂ receptor, adrenergic receptors or other receptors involved in cardiovascular regulation. In contrast to most other angiotensin II antagonists, eprosartan is a true competitive antagonist of the AT₁ receptor. Eprosartan is effective in antagonising the cardiovascular and renal effects of exogenous angiotensin II in both experimental animals and humans. Furthermore, it is an effective antihypertensive agent when administered to renin-dependent hypertension animal models, and in patients with mild to severe hypertension. The antihypertensive effect of eprosartan is maintained over a 24-h interval following a single dose with no reported dose-dependent adverse side-effects.

Keywords: angiotensin; angiotensin II receptor; eprosartan; hypertension; renin-angiotensin system

Document Type: Miscellaneous

Affiliations: 1: SmithKline Beecham Pharmaceuticals, Department of Renal Pharmacology, UW2521, 709 Swedeland Road, Box 1539, King of Prussia, PA 19406-0939, USA(Tel: +1 610 270 6184; Fax: +1 610 270 5681)

Publication date: 1998-03-01

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