Ketanserin, hypertension, and chronic alcoholism: double-blind study in forty patients.

In a randomized double-blind trial involving 40 alcoholic hypertensive patients, the antihypertensive activity of ketanserin, a serotonin antagonist with high affinity for S2 serotonergic receptors, was compared with a placebo. Patients in both groups were matched for age, body weight, blood pressure, alcoholic consumption, and length of alcoholism. The administration of ketanserin significantly reduced (p less than 0.001) mean supine blood pressure from 167/106 mmHg (22.3/14.1 kPa) at baseline to 145/87 mmHg (19.3/11.6 kPa) after 90 days of treatment versus a slight non-significant reduction with the placebo. No significant changes in heart rate, body weight, or laboratory parameters occurred. The incidence of side-effects was low in both groups. The results of this study suggest the possible role of serotonin in the pathogenesis of alcohol-related hypertension and the potential treatment of the disease using S2-receptor antagonists such as ketanserin.

Ketanserin (S2-receptor blocking agent), platelet activity and chronic alcoholism.

Ketanserin is a pure and selective antagonist of serotonin S2-receptors in blood vessels, platelets and bronchial tissue. It antagonizes serotonin-induced vasoconstriction, bronchoconstriction and platelet aggregation, and indirectly it blocks platelet release reaction. Ketanserin has little or no effect on healthy subjects. Serotonin-induced or serotonin-potentiated platelet aggregation is inhibited in blood drawn from ketanserin-treated healthy volunteers. Oral or parenteral ketanserin treatment did not cause major changes in beta-thromboglobulin (beta-TG) and platelet factor 4 (PF4) plasma concentrations, when basic values were normal. Increased microaggregate formation was found in alcoholics and heavy drinkers. It was also found that beta-TG and PF4 levels were higher in these patients than in the controls. Ketanserin treatment tended to normalize these protein levels in such patients.