No sex-related pharmacokinetic and pharmacodynamic differences of captopril

Captopril is an angiotensin-converting enzyme inhibitor (ACEI) used in the treatment of hypertension and congestive heart failure and has demonstrated its cardiovascular effects in experimental animal models, healthy volunteers and patients. The aim of this study was to find out whether or not differences in the pharmacokinetic profile and the haemodynamic response of a 100-mg single oral dose of captopril appeared between subjects of both sexes. Twenty-four young healthy volunteers (12 males and 12 females) took part in the trial. Blood samples to assess captopril plasma concentrations, determined by reverse phase high performance liquid chromatography (HPLC), as well as haemodynamic variables, were obtained before and at different times following drug intake. Pharmacokinetic parameters did not show significant sex differences. Systolic and diastolic blood pressure exhibited a statistically significant decrease between 0.5 and 8 h in both sexes. No significant sex-related differences were found. The drug exhibited a good tolerability.