Pharmacokinetic properties of captopril after acute and chronic administration to hypertensive subjects.

The pharmacokinetic properties of captopril were studied in two groups of hypertensive patients; (1) those who had never taken captopril (acute group), and (2) those who had been taking captopril for at least 6 months (chronic group). It was found that after 100 mg of captopril orally, the mean peak plasma level in the chronic group was three times higher than that in the acute group while the area under the curve was twice as high in the chronic group. These data suggest that bioavailability increases with chronic administration, and thus it may be possible to reduce the dosage of captopril and still maintain blood pressure control while reducing side effects.