(Circulation. 2001;103:904.)
© 2001 American Heart Association, Inc.
Cardiovascular Drugs |
Angiotensin II Type 1 Receptor Blockers
From the Division of Hypertension and Vascular Medicine, CHUV, Lausanne, Switzerland.
Correspondence to Prof M. Burnier, Division of Hypertension and Vascular Medicine, Hôpital Nestlé, Av P. Decker, Centre Hospitalier Universitaire Vaudois, 1011 Lausanne/Switzerland. E-mail Michel.Burnier@chuv.hospvd.ch
Key Words: angiotensin • hypertension • heart failure • antihypertensive agents
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Introduction |
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In the 1970s, a series of observations demonstrated that angiotensin II has deleterious effects on the heart and kidney and that patients with high levels of plasma renin activity are at a higher risk of developing stroke or myocardial infarction than those with low plasma renin activity.1 2 Thereafter, the development of pharmacological probes that block the renin-angiotensin system helped define the contribution of this system to blood pressure control and to the pathogenesis of diseases such as hypertension, congestive heart failure, and chronic renal failure. Thus, the concept of treating hypertension and congestive heart failure by a specific blockade of the renin-angiotensin system was first established with the use of saralasin, a nonselective peptidic antagonist of angiotensin II receptors.3 4 5 6 7 8 9 With saralasin, it became possible to demonstrate that angiotensin II receptor blockade, alone or in combination with salt depletion, lowers blood pressure in hypertensive patients and improves systemic hemodynamics in patients with congestive heart failure.3 4 5 6 7 8 9 10 However, saralasin had many drawbacks. Because it is a peptide, it had to be administered intravenously. This characteristic limited its use to hours or a few days at maximum. In addition, at higher doses, saralasin had some partial agonist, angiotensin II–like effects.
The next major breakthrough in the understanding of the
renin-angiotensin system was triggered by the development of orally
active angiotensin-converting enzyme (ACE)
inhibitors.10 11 12 13 14 15
Studies performed with these agents rapidly confirmed and reinforced
the seminal clinical observations made with saralasin. ACE inhibitors
are now recognized as an important therapeutic step to control blood
pressure in
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