The clinical pharmacology of lisinopril.

Structurally, lisinopril differs from captopril in that it does not contain a sulphydryl group and it differs from enalapril and related compounds in that it is not an ester prodrug. Published data on the clinical pharmacology of lisinopril are reviewed and data from new studies are presented. A radioimmunoassay has been used to study the clinical pharmacokinetics of lisinopril and 14C-lisinopril has been used in metabolism studies in man. Following oral administration, lisinopril is absorbed slowly but the absorbed drug is immediately available without any requirement for biotransformation by the liver. The plasma half-life controlling accumulation during chronic administration is 12-13 h and the absorbed drug is eliminated via glomerular filtration. These properties are consistent with once-daily dosing and uncomplicated clinical use in the treatment of hypertension and congestive heart failure.