We studied blood pressure response, plasma renin activity (PRA) and captopril pharmacokinetics in 8 children receiving orally 0.7 mg/kg of the drug. The drug increased PRA in all patients, in 5 to abnormally high levels. Peak captopril concentrations were achieved between half an hour and 2 h, and ranged between 100 and 547 ng/ml. Mean elimination half-time (T1/2) was 1.5 h, ranging between 0.98 and 2.3 h. There was a significant positive correlation between the area under the curve (AUC) and elimination T1/2 of the drug. There was a significant inverse correlation between AUC or elimination T1/2 and percent change in diastolic blood pressure; the 2 children who had no change in diastolic blood pressure had the largest AUC and the lowest apparent clearance of captopril. The kidney is the major site of captopril's pharmacological action. It is possible that longer retention of captopril in the plasma, evidence by larger AUC, may reflect less captopril available to modulate renin activity in the kidney.