Abstract
Angiotensin-converting enzyme (ACE) inhibitors, temocapril and enalapril, are prodrugs that are converted to the active metabolites, temocaprilat and enalaprilat, respectively. Temocaprilat is eliminated by renal and biliary routes, while enalaprilat is mainly excreted in urine [1, 2]. This difference explains a 2-fold increase in plasma temocaprilat and a 13-fold increase in plasma enalaprilat in patients with renal insufficiency [3]. Because renal function is physiologically decreased with age, it is hypothesized that, compared with temocaprilat, accumulation of enalaprilat during repeated dosing is greater and blood pressure (BP)-lowering effect is enhanced in elderly hypertensive patients. In this study, temocapril or enalapril was given once daily for 14 days to elderly hypertensive patients. Pharmacokinetic profiles and BP-lowering effects after single and repeated dosings of these drugs were determined.
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