Ketanserin, a novel 5-hydroxytryptamine antagonist: monotherapy in essential hypertension.

Blood pressure and heart rate, supine and standing, were studied in patients with essential hypertension during 8 weeks of oral therapy with two dosage schedules of ketanserin, 40 mg once and twice daily. Ketanserin caused significant reductions in both supine and standing blood pressure but no significant alterations in heart rate in both groups of patients. Measurements of blood pressure and heart rate over a 24 h period during steady state conditions revealed that maximal blood pressure reduction was correlated with time to peak plasma concentrations. Steady state plasma concentrations of ketanserin were significantly higher in the patients receiving 40 mg twice daily compared to 40 mg once daily. In the group with once daily treatment, tmax was 1.2 +/- 0.17 h, Css 13 +/- 4.3 ng/ml, Cmax 137 +/- 19.6 ng/ml and t1/2, z h. 9.6 +/- 1.27 h.