Ketanserin in combination with beta-adrenergic receptor blocking agents in the treatment of essential hypertension.

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Abstract
The antihypertensive properties of ketanserin, a 5‐HT2 receptor antagonist, was investigated in combination with beta‐adrenoceptor blockade. Ketanserin was given 40 mg twice daily to 10 hypertensive patients during 4 weeks in a double‐blind placebo‐controlled trial. Ketanserin significantly reduced supine and erect blood pressure compared to double‐blind placebo, while no changes in heart rate were seen. When the blood pressure was assessed during 24 h at steady state conditions, the blood pressure reduction was maximal 1‐2 h after tablet intake, corresponding to peak plasma concentrations of ketanserin. The blood pressure remained significantly reduced until next tablet intake (12 h). At steady state, on a 40 mg twice daily regimen, Css was 41.6 +/‐ 4.22, 36.9 +/‐ 5.19 and 39.8 +/‐ 4.81 ng/ml, Cmax 102.4 +/‐ 15.64 ng/ml and tmax 1.6 +/‐ 0.32 h. A slight sedation was observed in six patients. This side effect occurred 1‐2 h after tablet intake and tended to subside with continued treatment.