Influence of food on the clinical effect of angiotensin I converting enzyme inhibitor (SQ 14,225).

Abstract

To clarify the influence of food on the clinical effect of angiotensin I converting enzyme inhibitor (SQ 14,225, captopril), 25 mg of the drug was administered to patients with hypertension in a 2 way crossover study design. In the 1st study (study I), each subject received the drug 30 min after breakfast, and changes in blood pressure (BP), blood concentration of captopril (BCC), plasma renin activity (PRA), plasma aldosterone (PA) and plasma angiotensin I converting enzyme activity (ACE-A) were determined for 3 h. BP was recorded for 6 h. Four days after study I, the same subjects received the drug 2 h after breakfast, and each parameter was again determined (study II), similarly to study I. No significant difference in the hypotensive responses to captopril was observed between both studies during 6 h of observation. Maximum hypotensive effects were found within 90 min of the treatments in study I and study II, and BP returned almost to baseline levels at 6 h in both studies. Maximum BCC levels were found 60 and 90 min after the drug administration in studies I and II, respectively, and these approximated to half of each maximum level at 180 min. There were no statistically significant differences in the biological half-life (T1/2), maximum concentration (C max), maximum concentration time (T max), and area under the blood concentration curve (AUC)03 between both studies. The peak in PRA occurred at 60 and 90 min after the administration of the drug in studies I and II, respectively. In study I, a slightly greater reduction of PA levels was found, but there was no significant difference in the magnitude of the reduction between both studies. Evidently food did not exert any significant influence on the clinical effect of captopril.