Mechanism of action of ketanserin: studies on cardiovascular reactivity in essential and diabetes-associated hypertension.
Ketanserin is a selective serotonin-S2 receptor antagonist with alpha 1-adrenoceptor inhibiting activity. The relative contribution of the latter mechanism to antihypertensive efficacy was studied in a group comprising eight normal subjects, 10 patients with essential hypertension and eight diabetics with arterial hypertension. Ketanserin treatment administered over a period of 8 weeks, decreased arterial pressure in patients with essential hypertension and, to a lesser extent, in diabetics, but not in normal subjects. In all three groups, exchangeable sodium, blood volume, the activity of the adrenergic and renin-angiotensin-aldosterone systems and the pressor responsiveness to norepinephrine (NE) or angiotensin II (Ang II) were unaltered, while the pressor reactivity to phenylephrine showed a significant decrease in normal subjects only. This suggests that the antihypertensive mechanism of ketanserin does not involve a modification of the physiological relationship between endogenous noradrenergic and pressor reactivity to NE. Moreover, ketanserin does not interfere with Ang II-dependent mechanisms.
Waser
M
M
Ospedale Italiano, Viganello, Switzerland.
Ziegler
W H
WH
Beretta-Piccoli
C
C
D000328:Adult; D001794:Blood Pressure / Q000187:drug effects*; D003925:Diabetic Angiopathies / Q000188:drug therapy*; D005260:Female; D006801:Humans; D006973:Hypertension / Q000188:drug therapy*; D007650:Ketanserin / Q000627:therapeutic use*; D008297:Male; D008875:Middle Aged; D009638:Norepinephrine / Q000502:physiology; D012084:Renin-Angiotensin System; D013997:Time Factors
D007650:Ketanserin; D009638:Norepinephrine