Description
Mechanism of Action
Enalapril, a prodrug of enalaprilat, competitively inhibits ACE from converting angiotensin I to angiotensin II (a potent vasoconstrictor) resulting in increased plasma renin activity and reduced aldosterone (a hormone that causes water and Na retention) secretion. This promotes vasodilation and BP reduction.
Onset: Approx 1 hr.
Duration: 12-24 hr.
Absorption: Well absorbed from the GI tract (approx 60%). Time to peak plasma concentration: Oral: Enalapril: Approx 1 hr; enalaprilat: 3-4 hr.
Distribution: Distributed into milk (trace amounts), crosses the placenta and appears to cross the blood-brain barrier poorly. Plasma protein binding: 50-60% (enalaprilat).
Metabolism: Extensively hydrolysed to enalaprilat in the liver via esterases.
Excretion: Via urine (43% as enalaprilat and 18% as enalapril); faeces (27% as enalaprilat and 6% as enalapril). Elimination half-life: Approx 11 hr.
MIMS Class
ACE Inhibitors/Direct Renin Inhibitors
ATC Classification
C09AA02 – enalapril; Belongs to the class of ACE inhibitors. Used in the treatment of cardiovascular disease.;
