Chronic effect of ketanserin in mild to moderate essential hypertension.

Abstract

Ketanserin, an antagonist highly selective for 5-hydroxytryptamine (serotonin) type 2 (S2) receptors, was given as monotherapy in a dose of 40 mg b.i.d. to 24 subjects with mild to moderate essential hypertension. Its effects were evaluated in a placebo-controlled double-blind crossover study. The effect on blood pressure in 18 subjects was monitored by 24-hour ambulatory intra-arterial measurements. Systolic and diastolic intra-arterial pressures were significantly lowered by ketanserin both during the day and at night, whereas heart rate was unchanged. Cuff pressure readings (triplicate measurements) with the London School of Hygiene sphygmomanometer and an automatic device (12 measurements in 1 hour) in the outpatient clinic also showed a significant effect on both supine and standing pressures. No postural hypotension was noted. Ketanserin had no effect on endogenous creatinine clearance, serum cholesterol levels, and the plasma levels of norepinephrine, renin, and aldosterone. The only side effect that was significantly more common with ketanserin than with placebo treatment was an increase in body weight. Ketanserin may have a place in the treatment of mild to moderate essential hypertension.

Ketanserin: A novel cardiovascular drug

“…Orthostatic hypotension was not a feature of ketanserin treatment. Ketanserin had no adverse effects on the peripheral circulation, in spite of a reduction in blood pressure De Leeuw et al, 1983;Hosie and Gould, 1985;Omvik and Lund-Johansen, 1983;Persson et al, 1983;Woittiez et al, 1986;and unpublished data].…”

“…There was no concomitant stimulation of aldosterone production [Wenting et al, 19841. There was no evidence that ketanserin influenced the sympathetic or the renin-angiotensin-aldosterone system during chronic oral treatment Woittiez et al, 1986;and unpublished data]. Ketanserin had no effect on the release of pituitary hormones (PRL, GH, LH, ACTH, ADH), on thyroid function, or on plasma cortisol levels (unpublished data).…”

Is beta 1-antagonism essential for the antihypertensive action of beta-blockers?

“…3 Then a series of blood pressure measurements was made every 5 minutes for 1 hour using an automatic oscillometric device (Accutorr, Datascope, Paramus, NJ, USA). 4 At the end of each week of placebo or active treatment, blood pressure was also measured intra-arterially. All blood pressure measurements were made 2 to 4 hours after the last dose of placebo or active drug.…”

Hemodynamic and hormonal adaptations to beta-adrenoceptor blockade. A 24-hour study of acebutolol, atenolol, pindolol, and propranolol in hypertensive patients.

“…Blood pressure was measured in triplicate with a blind sphygmomanometer (London School of Hygiene Sphygmomanometer, Cinetronics, Middenhall, UK). 17 After this washout period, the patients were given placebos for 2 weeks. The placebo tablets were matched with the active medication with regard to appearance and number of tablets taken each day.…”