De Luca N, Rosiello G, Crispino M, Volpe M, Galletti P, Buzzetti G, Trimarco B
Clinica Medica, Facoltá di Medicina, University of Naples, Italy.
J Clin Pharmacol. 1988 Apr;28(4):332-8. doi: 10.1002/j.1552-4604.1988.tb03154.x.
The antihypertensive efficacy of a serotonin-receptor antagonist, ketanserin, was compared with that of a well-established antihypertensive drug, metoprolol, and their cardiac and forearm hemodynamic effects were investigated using echocardiography and bidimensional pulsed Doppler flowmetry, respectively. Twenty hypertensive subjects completed a double-blind, cross-over, randomized study using ketanserin and metoprolol. Two 5-week courses with ketanserin or metoprolol were preceded by a placebo period; the total duration of the study was 15 weeks. Despite a comparable efficacy in reducing systolic and diastolic blood pressure (about 10% of the basal value), the two drugs showed quite different effects on forearm hemodynamics. Ketanserin increased forearm blood flow and induced a significant decrease in forearm vascular resistance (from 141 +/- 16 to 75 +/- 11 mm Hg/mL/sec, P less than .01). Furthermore, this treatment was able to improve brachial artery compliance (from 1.89 +/- .3 to 3.2 +/- .3 cm4/dyne 10(-7), P less than .01). On the contrary, metoprolol did not modify forearm hemodynamics. Both drugs did not significantly modify cardiac performance, as evaluated by left ventricle circumferential fiber shortening. Cardiac output was increased by ketanserin (from 5.9 +/- .3 to 6.6 +/- .5 L/min, P less than .05) and fell during treatment with metoprolol (from 5.9 +/- .4 to 4.9 +/- .3 L/min P less than .01). Thus, the two drugs reduce blood pressure through different hemodynamic mechanisms and the effects of ketanserin on systemic and peripheral circulation seem more favorable.
将血清素受体拮抗剂酮色林的降压疗效与一种成熟的降压药物美托洛尔进行了比较,并分别使用超声心动图和二维脉冲多普勒血流仪研究了它们对心脏和前臂血流动力学的影响。20名高血压患者完成了一项使用酮色林和美托洛尔的双盲、交叉、随机研究。在使用酮色林或美托洛尔进行两个为期5周的疗程之前有一个安慰剂期;研究的总持续时间为15周。尽管在降低收缩压和舒张压方面疗效相当(约为基础值的10%),但这两种药物对前臂血流动力学的影响却大不相同。酮色林增加了前臂血流量,并导致前臂血管阻力显著降低(从141±16降至75±11mmHg/mL/sec,P<0.01)。此外,这种治疗能够改善肱动脉顺应性(从1.89±0.3提高到3.2±0.3cm4/dyne 10(-7),P<0.01)。相反,美托洛尔并未改变前臂血流动力学。通过左心室圆周纤维缩短评估,两种药物均未显著改变心脏功能。酮色林使心输出量增加(从5.9±0.3升至6.6±0.5L/min,P<0.05),而在美托洛尔治疗期间心输出量下降(从5.9±0.4降至4.9±0.3L/min,P<0.01)。因此,这两种药物通过不同的血流动力学机制降低血压,并且酮色林对全身和外周循环的影响似乎更有利。