Chrysant S G
Am Heart J. 1983 Nov;106(5 Pt 2):1243-50. doi: 10.1016/0002-8703(83)90183-7.
The acute and chronic autonomic, systemic, and renal hemodynamic effects of trimazosin and placebo were studied in patients with uncomplicated essential hypertension of mild to moderate severity. In these studies, trimazosin effectively reduced arterial pressure through a decrease in peripheral vascular resistance. In the acute studies the cardiac output increased, whereas in the chronic studies it remained unchanged. Acutely, trimazosin selectively increased renal blood flow, which was out of proportion to the increase in cardiac output. No significant effects on autonomic function, metabolic function, or renin and aldosterone release were observed with trimazosin after acute or chronic administration. No tolerance to the action of the drug developed. No significant hemodynamic or metabolic changes were observed when compared with placebo either acutely or chronically. Our conclusions are as follows: (1) trimazosin is an effective and safe antihypertensive agent given in single daily doses; (2) it exerts its effects mainly through direct arteriolar dilatation and less through autonomic inhibition; (3) its antihypertensive effectiveness is not compromised by the development of tolerance; (4) it exerts a selective beneficial effect on renal circulation that is unrelated to systemic hemodynamic changes; and (5) these properties of trimazosin may make it a desirable drug for the treatment of hypertension complicated by renal failure.
研究了曲马唑嗪和安慰剂对轻度至中度单纯性原发性高血压患者的急性和慢性自主神经、全身及肾脏血流动力学的影响。在这些研究中，曲马唑嗪通过降低外周血管阻力有效降低动脉血压。急性研究中的心输出量增加，而慢性研究中的心输出量保持不变。急性给药时，曲马唑嗪选择性增加肾血流量，其增加幅度与心输出量的增加不成比例。急性或慢性给药后，未观察到曲马唑嗪对自主神经功能、代谢功能或肾素及醛固酮释放有显著影响。未出现对该药物作用的耐受性。与安慰剂相比，急性或慢性给药时均未观察到显著的血流动力学或代谢变化。我们的结论如下：（1）曲马唑嗪是一种每日单次给药有效且安全的抗高血压药物；（2）其作用主要通过直接小动脉扩张，而非通过自主神经抑制；（3）其抗高血压效果不会因耐受性的产生而受损；（4）它对肾循环有选择性有益作用，与全身血流动力学变化无关；（5）曲马唑嗪的这些特性可能使其成为治疗合并肾衰竭的高血压的理想药物。
