Acute effects of the new oral angiotensin converting enzyme inhibitor 1- (D-3-acetylthio-2-methylpropanoyl) -L-prolyl-L-phenylalanine (Alacepril) in essential hypertension
Mizuno, K.; Hashimoto, S.; Kunii, N.; Tani, M.; Niimura, S.; Yabe, R.; Watari, H.; Fukuchi, S.
Research Communications in Chemical Pathology and Pharmacology 49(2): 175-187
1985
ISSN/ISBN: 0034-5164 PMID: 2997886 Document Number: 242819
In 15 patients with mild-to-moderate essential hypertension a new orally active angiotensin converting enzyme inhibitor, 1-(D-3-acetylthio-2-methylpropanoyl)-L-prolyl-L-phenylalanine (Alacepril), was administered with a single oral dose of 50 mg to evaluate its antihypertensive effect. Following Alacepril plasma angiotensin converting enzyme (ACE) activity was inhibited by approximately 75% within 2 h. Plasma renin activity increased slightly whereas plasma levels of aldosterone decreased significantly. Blood pressure fell markedly not only in patients with high renin levels but also in those with low renin levels. Nevertheless, the magnitude of blood pressure reduction was correlated with the pre-treatment plasma renin values (r = -0.602, p less than 0.05 systolic, r = -0.667, p less than 0.01 diastolic). No relevant changes in pulse rate was observed. These findings demonstrate that in essential hypertension the novel orally active ACE inhibitor Alacepril exerts marked antihypertensive effect, which may offer a new effective approach to treatment of hypertension.