Enalapril pharmacokinetics and ACE inhibition, following single and chronic oral dosing
Edeki, T.; Johnston, A.; Li Kam Wa, E.; Turner, P.
International Journal of Clinical Pharmacology and Therapeutics 32(3): 142-146
1994
ISSN/ISBN: 0946-1965 PMID: 8205376 Document Number: 433163
Twelve normal volunteers were given 10 mg enalapril maleate by single and 2 weeks multiple dose administration, and blood samples were collected for the determination of enalaprilat concentration and angiotensin converting enzyme (ACE) activity. The mean terminal elimination half-life following a single administration of 10 mg enalapril, was 27 hours. The inhibition of ACE activity paralleled enalaprilat concentrations following both single and multiple dosing and the time of maximum inhibition of ACE activity was associated on both occasions with maximum concentration of enalaprilat. E-max modelling of enalaprilat concentration and ACE activity gave comparable values of E-max for both methods of administration. An accumulation factor of 1.7 was calculated from the area under the concentration time curve (AUC) of enalaprilat within a dosing interval at steady-state and the total AUC following single administration of enalapril. There were no significant differences between males and females in the accumulation factor, half-life and AUC-inf.