Journal article
Antagonizing the angiotensin II subtype 1 receptor: a focus on olmesartan medoxomil.
- Nussberger J Division of Hypertension and Vascular Medicine, Centre Hospitalier Universitaire Vaudois, Lausanne, Switzerland. Juerg.Nussberger@chuv.hospvd.ch
- Koike H
- 2004-08-05
Published in:
- Clinical therapeutics. - 2004
Angioedema
Angiotensin II Type 1 Receptor Blockers
Angiotensin-Converting Enzyme Inhibitors
Animals
Antihypertensive Agents
Clinical Trials as Topic
Cough
Humans
Imidazoles
Olmesartan Medoxomil
Receptor, Angiotensin, Type 1
Renin-Angiotensin System
Tetrazoles
English
BACKGROUND
The orally active, nonpeptide antagonists of the angiotensin II subtype 1 (AT1) receptor represent a recent class of antihypertensive drugs that selectively block the renin-angiotensin system. Olmesartan medoxomil is the newest member of this class.
OBJECTIVE
This article reviews the renin-angiotensin system and how this system can be pharmacologically inhibited by the selective antagonists of the AT1 receptor, with a main focus on the AT1 receptor antagonist olmesartan.
METHODS
Key studies were selected from previous work to illustrate the antihypertensive, cardioprotective, and renoprotective effects of olmesartan, and to compare class effects of AT1 receptor antagonists and angiotensin-converting enzyme (ACE) inhibitors.
RESULTS
Olmesartan, the active metabolite of olmesartan medoxomil, is a highly potent antagonist of the AT1 receptor. It inhibits the contractile responses to angiotensin II in guinea pig aorta, inhibits the pressor responses to angiotensin II in rats and dogs, and exhibits dose-dependent antihypertensive effects in spontaneously hypertensive rats. In addition to its antihypertensive effects, olmesartan medoxomil provides protection against cardiac and renal damage in animal models. AT1 receptor antagonists are more specific inhibitors of the renin-angiotensin system compared with ACE inhibitors. They are well tolerated and have an excellent safety profile. Unlike angiotensin-converting enzyme inhibitors, AT1 receptor antagonists lack the nonangiotensin-related side effects such as cough and angioedema.
CONCLUSIONS
AT1 receptor antagonists such as olmesartan represent a valid therapeutic option for the treatment of hypertension and other cardiovascular and renal diseases.
The orally active, nonpeptide antagonists of the angiotensin II subtype 1 (AT1) receptor represent a recent class of antihypertensive drugs that selectively block the renin-angiotensin system. Olmesartan medoxomil is the newest member of this class.
OBJECTIVE
This article reviews the renin-angiotensin system and how this system can be pharmacologically inhibited by the selective antagonists of the AT1 receptor, with a main focus on the AT1 receptor antagonist olmesartan.
METHODS
Key studies were selected from previous work to illustrate the antihypertensive, cardioprotective, and renoprotective effects of olmesartan, and to compare class effects of AT1 receptor antagonists and angiotensin-converting enzyme (ACE) inhibitors.
RESULTS
Olmesartan, the active metabolite of olmesartan medoxomil, is a highly potent antagonist of the AT1 receptor. It inhibits the contractile responses to angiotensin II in guinea pig aorta, inhibits the pressor responses to angiotensin II in rats and dogs, and exhibits dose-dependent antihypertensive effects in spontaneously hypertensive rats. In addition to its antihypertensive effects, olmesartan medoxomil provides protection against cardiac and renal damage in animal models. AT1 receptor antagonists are more specific inhibitors of the renin-angiotensin system compared with ACE inhibitors. They are well tolerated and have an excellent safety profile. Unlike angiotensin-converting enzyme inhibitors, AT1 receptor antagonists lack the nonangiotensin-related side effects such as cough and angioedema.
CONCLUSIONS
AT1 receptor antagonists such as olmesartan represent a valid therapeutic option for the treatment of hypertension and other cardiovascular and renal diseases.
- Language
-
- English
- Open access status
- closed
- Identifiers
-
- DOI 10.1016/s0149-2918(04)90141-5
- PMID 15291375
- Persistent URL
- https://sonar.ch/global/documents/277943
Statistics
Document views: 63
File downloads: