Ketanserin, a selective S2-serotonin receptor blocker with alpha 1-adrenergic blocking effects, may be a suitable antihypertensive medication after coronary artery surgery and lacks side effects seen with other vasodilators. Fifty patients with systolic blood pressures greater than 150 mmHg after coronary artery surgery were given, in a randomized double-blind fashion, either ketanserin (K) or saline (S). Each patient received six successive boluses of 1 mL of S or 1 mL of K (5 mg) at 2-minute intervals. After the last injection, sodium nitroprusside was started whenever the systolic blood pressure exceeded 150 mmHg. In the K group, the following significant (P < 0.05) changes occurred: systolic and diastolic arterial pressure -12% and -11%, respectively; heart rate -3%; systolic and diastolic pulmonary artery pressure -5% and -6%; central venous pressure -5%; pulmonary capillary wedge pressure -5%; systemic vascular resistance -16%; pulmonary vascular resistance -8%; stroke index +6%. None of these parameters changed significantly in the S group. There was no change in pulmonary shunt fraction in either group. In the K group, five patients did not require any further antihypertensive therapy during the 120 minutes following the last bolus injection. Twenty patients needed sodium nitroprusside during this period. This occurred 37 minutes (+/- 17 min) after the last bolus. In conclusion, after coronary artery bypass surgery, K is an effective antihypertensive medication, which does not cause reflex tachycardia or an increase in pulmonary shunt fraction. Exceeding the recommended dose of 10 (or 20) mg, as done in this study, does not seem to improve effectiveness or prolong the duration of action.