Acute hemodynamic effects of intravenous captopril were measured, and left ventricular function was analyzed by radionuclide angiography in 11 patients with moderate to severe hypertension. All subjects received 1 mg captopril bolus injection initially, and followed in 10 minutes intervals by 2 mg or 5 mg injections according to their blood pressure response. Eight patients experienced an acute reduction of blood pressure; three patients remained unresponsive. The onset of action occurred within 5 minutes with peak effect at 5 to 10 minutes and a duration of action of 20 to 30 minutes. The hemodynamic effects were characterized by arteriolar dilation (reduced systemic vascular resistance P less than 0.01), and apparent venous dilatation (reduced right atrial, pulmonary wedge pressure P less than 0.05 & 0.01 respectively). Pulmonary vascular resistance was not altered. Ejection fraction remained unchanged. Isovolumic relaxation period lengthened (109 +/- 20.1 vs 137.39 +/- 21.15 msec, P less than 0.05) and coronary perfusion pressure gradients dropped (113.8 +/- 5.6 vs 101.1 +/- 11.3 mmHg P less than 0.001) following intravenously administered captopril. Intravenous captopril may reduce arterial pressure by inducing arterial dilatation with minimal adverse effect. The prolongation of isovolumic relaxation period should mainly attribute to the decrease of coronary filling load.