Ketanserin in combination with beta-adrenergic receptor blocking agents in the treatment of essential hypertension.
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.
D000319:Adrenergic beta-Antagonists / Q000008:administration & dosage*; D000368:Aged; D000959:Antihypertensive Agents / Q000008:administration & dosage*; D001794:Blood Pressure / Q000187:drug effects; D004359:Drug Therapy, Combination; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D006973:Hypertension / Q000188:drug therapy*; D007650:Ketanserin; D008297:Male; D008875:Middle Aged; D010880:Piperidines / Q000008:administration & dosage* / Q000009:adverse effects / Q000097:blood
D000319:Adrenergic beta-Antagonists; D000959:Antihypertensive Agents; D010880:Piperidines; D007650:Ketanserin