Pharmacokinetic alterations of quinapril during repeated treatment in elderly subjects.
OBJECTIVE
To examine whether the pharmacokinetics of quinaprilat, an active metabolite, change during repeated treatment with quinapril, an ACE inhibitor, in elderly subjects.


METHODS
Quinapril (10 mg) was given once daily for 8 days in eight elderly hypertensive subjects (76 years old). Blood samples were obtained for a 24-h period after the first and eighth doses.


RESULTS
Plasma concentrations of quinaprilat after the eighth dose significantly higher than those after the first dose. The maximum plasma concentration (Cmax) tended to be greater, and the area under the plasma concentration-time curve (AUC) was significantly greater after the eighth dose.


CONCLUSIONS
The study showed an increase in quinaprilat concentrations and subsequent increase in AUC, during repeated treatment with quinapril in elderly subjects. However, the differences observed were very small and of no clinical significance.
Sasaki
M
M
Department of Clinical Pharmacology, Jichi Medical School, Tochigi, Japan.
Maeda
A
A
Fujimura
A
A
D000368:Aged; D000806:Angiotensin-Converting Enzyme Inhibitors / Q000097:blood / Q000493:pharmacokinetics*; D001794:Blood Pressure / Q000187:drug effects; D005260:Female; D006801:Humans; D007546:Isoquinolines / Q000097:blood / Q000493:pharmacokinetics*; D008297:Male; D000077583:Quinapril; D044005:Tetrahydroisoquinolines
D000806:Angiotensin-Converting Enzyme Inhibitors; D007546:Isoquinolines; D044005:Tetrahydroisoquinolines; D000077583:Quinapril