Fagard R, Fiocchi R, Lijnen P, Staessen J, Moerman E, de Schaepdryver A, Amery A
Br Heart J. 1984 Feb;51(2):149-56. doi: 10.1136/hrt.51.2.149.
Ketanserin (120 mg/day) or placebo was given orally to 14 patients with mild to moderate essential hypertension according to a double blind crossover protocol, each treatment period lasting six weeks. Resting intra-arterial pressure in the recumbent position was reduced from 150/84 to 141/77 mm Hg; the hypotensive effect persisted throughout an uninterrupted graded exercise test to the point of exhaustion. The haemodynamic effects were similar at rest and during exercise. Overall, systemic vascular resistance decreased by 14%, heart rate fell by 5%, but stroke volume and cardiac output increased. Mean pulmonary arterial pressure and capillary wedge pressure were not significantly affected, but pulmonary vascular resistance decreased by 15%. The pressor response to methoxamine was significantly reduced by ketanserin. Both plasma noradrenaline and adrenaline concentrations increased, plasma renin activity and angiotensin II concentration decreased, and plasma aldosterone concentration was unchanged. The data indicate that ketanserin induces arteriolar dilatation, possibly related to an alpha-1-antagonistic action and to a reduced circulating angiotensin II concentration. The haemodynamic response is complex, and an increase in cardiac output limits the hypotensive effect. There is no firm evidence of an effect on venous tone as cardiac filling pressures do not change.
按照双盲交叉试验方案,对14例轻至中度原发性高血压患者口服酮色林(120毫克/天)或安慰剂,每个治疗期持续6周。卧位时的静息动脉内压从150/84毫米汞柱降至141/77毫米汞柱;在不间断的分级运动试验直至疲劳时,降压效果持续存在。静息和运动时的血流动力学效应相似。总体而言,全身血管阻力降低14%,心率下降5%,但每搏输出量和心输出量增加。平均肺动脉压和毛细血管楔压未受显著影响,但肺血管阻力降低15%。酮色林显著降低了对甲氧明的升压反应。血浆去甲肾上腺素和肾上腺素浓度均升高,血浆肾素活性和血管紧张素II浓度降低,血浆醛固酮浓度未变。数据表明,酮色林可诱导小动脉扩张,可能与α-1拮抗作用及循环中血管紧张素II浓度降低有关。血流动力学反应较为复杂,心输出量增加限制了降压效果。由于心脏充盈压未改变,尚无确凿证据表明其对静脉张力有影响。