Clinical pharmacology of enalapril

Enalapril is administered as the ethyl ester of the potent angiotensin converting enzyme (ACE) inhibitor enalaprilat. As such, it is 60% absorbed and 40% bioavailable as the active species. Absorption is not affected by food. Serum concentrations are proportional to dose, less a small drug residue apparently bound to the enzyme. The half-life for accumulation is approximately 11 h. The drug is eliminated by the kidney without further metabolism. Maximum inhibition of plasma ACE occurs 2-4 h after administration and persists for more than 24 h with clinical doses. ACE inhibition is associated with increases in plasma renin and angiotensin I levels, decreases in angiotensin II and aldosterone concentrations and reduction in blood pressure. All of these events are closely correlated when analysed statistically. The clinical and haemodynamic effects of these actions are addressed in other papers.