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Single and repeated dosing of the converting enzyme inhibitor perindopril to normal subjects
Author(s) -
Bussien Jeanpaul,
d'Amore Tancredi Fasanella,
Perret Laurent,
Porchet Marinette,
Nussberger Jürg,
Waeber Bernard,
Brunner Hans R
Publication year - 1986
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1986.95
Subject(s) - perindopril , plasma renin activity , angiotensin converting enzyme , blood pressure , renin–angiotensin system , endocrinology , medicine , aldosterone , oral administration , pharmacology , essential hypertension , morning , enzyme inhibitor , ace inhibitor , angiotensin ii , clinical pharmacology , chemistry , enzyme , biochemistry
The new orally active angiotensin converting enzyme (ACE) inhibitor perindopril (S9490‐3) was evaluated in 18 normotensive men. In three subjects the pressor response to exogenous angiotensin I was tested. A 8 mg oral dose reduced the pressor response by >80%. Single oral perindopril doses of 2, 4, 8, and 16 mg were given to groups of five subjects each. Eight and 16 mg decreased plasma ACE activity within 4 hours to <10% of control; 72 hours later, plasma ACE activity was still reduced by at least 40%. Doses of 4 and 8 mg po once a day were then given for 8 days to two groups of six subjects. Four hours after the first and the last morning doses, plasma angiotensin II, aldosterone, and plasma ACE activity fell significantly, whereas blood angiotensin I and plasma renin activity rose. There was no evidence of drug accumulation. No significant change in blood pressure or heart rate was observed. Thus in normotensive subjects, perindopril seems an effective, orally active, long‐lasting ACE inhibitor. Clinical Pharmacology and Therapeutics (1986) 39, 554–558; doi: 10.1038/clpt.1986.95