The Effect of Ketanserin on Blood Pressure and Biochemical Parameters in Treated Patients with Essential Hypertension

Abstract

17 subjects with essential hypertension (14 male, 3 female - ages: 40-69 years), 13 of whom continued their previous anti-hypertensive therapy, completed a double-blind cross-over trial of ketanserin 40 mg twice daily versus placebo tablets twice daily - each treatment phase was six weeks in duration. For the group as a whole, blood pressure (BP) was reduced in the ketanserin phase compared with the placebo phase; supine mean BP decrease: 4 +/- 1 mm Hg (p less than 0.05); standing mean BP decrease: 7 +/- 1 mm Hg (p less than 0.001). Heart rate (HR) was also significantly decreased in the ketanserin phase by 5 +/- 1 beats/minute (p less than 0.001). When individual subgroups were analysed the reductions in BP and HR were greater in subjects already receiving anti-hypertensives, diuretic and/or beta blockers. Changes were observed in 24 hour urine sodium and potassium excretion - sodium (mmol/day): placebo 137 +/- 17, ketanserin 174 +/- 19 (p less than 0.05); potassium (mmol/day): placebo 74 +/- 8, ketanserin 57 +/- 5. For the group as a whole there were no significant adverse effects during the ketanserin phase, although two subjects had a dose reduction of ketanserin because of drowsiness and dizziness. Two additional subjects withdrew from the study due to adverse effects, one in the placebo phase. In conclusion ketanserin in the dose administered has a modest hypotensive effect which is best seen in subjects already receiving other anti-hypertensive agents.

Ketanserin: A novel cardiovascular drug

“…4). The magnitude of the blood pressure reduction by ketanserin in combination with these agents again was proportional to the initial blood pressure [Hedner and Persson, 1984;Wing et al, 1984;and unpublished data].…”

“…Creatinine clearance remained unchanged, and urinalysis did not reveal abnormalities Wing et al, 1984;Woittiez et al, 19861. During 1-year treatment with ketanserin in hypertensive patients with renal impairment, proteinuria decreased significantly [Dzurik et al, 19851.…”

“…The therapeutic dose of 2 0 4 0 mg twice daily controlled blood pressure over 24 hr, as measured intra-arterially ( Fig. 2) and by ambulatory monitoring Andren et al, 1983;Cameron and Ramsay, 1985;De Lorenzo et al, 1986;Hedner et al, 1983Hedner et al, , 1985Strano et al, 1986;Waal-Manning et al, 1984Wing et al, 1984;and unpublished data].…”

A pharmacological analysis of the rat mast cell 5‐HT gastric lesion test and the effects of ketanserin

“…Ketanserin is a potent S2-antagonist with very high oral effectiveness, and this antagonism at the level of the vessel wall [Van Nueten et al, 1981, 19831, andof platelets [De Clerck et al, 1982;De Clerck and Van Nueten, 19821 is generally considered to be of primary importance in its therapeutic antihypertensive effects Anderson et al, 1983;Andren et al. 1983;De Cree et al, 1981;Fagard et al, 1984;Hedner et al, 1984;Omvik and Liind-Johansen, 1983;Persson et al, 1983;Saraste et al, 1984;Wenting et al, 1984;Wing et al, 1984;Zabludowski et al, 19841.…”

Ketanserin

“…22). Ketanserin does not reduce blood pressure below the normal level in normotensive individuals (for published data see 1, 4,26,57,66,289,291).…”