PMID: 2483429Jan 1, 1989Paper

The renin-angiotensin system and ramipril, a new converting enzyme inhibitor.

Journal of Cardiovascular Pharmacology
D Vasmant, N Bender

Abstract

Angiotensin converting enzyme (ACE) inhibitors have offered new perspectives in the treatment of hypertension. The development of new ACE inhibitors such as ramipril provides an opportunity to improve the knowledge on this class of drug, and to optimize the benefit/risk ratio for the patient. Ramipril was selected among several analogs because of its unique physicochemical properties. It is a nonsulfhydryl ACE inhibitor, and after oral absorption it is transformed in the liver into its active metabolite ramiprilat, which is at least 23 times more lipophilic than enalaprilat. Furthermore, the in vitro affinity of ramiprilat for the enzyme is 7 times higher than for enalaprilat and 47 times higher than for captopril. The ramiprilat-ACE complex is therefore very stable and dissociates 6 times more slowly than the enalaprilat-ACE complex and 22 times more slowly than the captopril-ACE complex. Ramipril possesses a favorable pharmacokinetic profile as a consequence of its physicochemical properties: its high potency allows the use of very low doses, and the slow dissociation of the ramipril-ACE complex explains the long duration of its action, permitting a once-daily treatment. Dose-finding studies have confirmed that very low doses...Continue Reading

Related Concepts

Related Feeds

Antihypertensive Agents: Mechanisms of Action

Antihypertensive drugs are used to treat hypertension (high blood pressure) which aims to prevent the complications of high blood pressure, such as stroke and myocardial infarction. Discover the latest research on antihypertensive drugs and their mechanism of action here.