The influence of food on the pharmacokinetics and ACE inhibition of cilazapril.
1. The influence of food on the pharmacokinetics and angiotensin-converting enzyme (ACE) inhibitory effects of oral 5 mg doses of cilazapril was investigated in a two-way crossover study in 16 volunteers. 2. Plasma and urine concentrations of cilazaprilat, the active diacid metabolite of cilazapril, and plasma ACE activity were determined by a radio-enzymatic method. 3. Cmax decreased by 30% (P less than 0.05) with a delay in (t)max of 1 h (P less than 0.05) and area under curve (AUC) was decreased by 14% (P less than 0.05). The elimination rate was unaltered. 4. Onset of ACE inhibition was delayed by approximately 30 min but degree and duration were unaffected. 5. The effect of food on the bioavailability of cilazapril at this dose would not be expected to be clinically significant.
Massarella
J W
JW
Hoffmann-La Roche Inc., Nutley, New Jersey 07110.
DeFeo
T M
TM
Brown
A N
AN
Lin
A
A
Wills
R J
RJ
D000293:Adolescent; D000328:Adult; D000806:Angiotensin-Converting Enzyme Inhibitors / Q000493:pharmacokinetics* / Q000494:pharmacology; D001682:Biological Availability; D017315:Cilazapril / Q000031:analogs & derivatives; D005502:Food; D006801:Humans; D011724:Pyridazines / Q000097:blood / Q000493:pharmacokinetics* / Q000494:pharmacology / Q000652:urine
D000806:Angiotensin-Converting Enzyme Inhibitors; D011724:Pyridazines; D017315:Cilazapril; C045980:cilazaprilat