Nelson G I, Hussain M, Forsyth D, Wilson J, Silke B, Taylor S H
J Cardiovasc Pharmacol. 1984 Jan-Feb;6(1):176-81.
As a preliminary to a larger clinical trial, the haemodynamic effects of the selective alpha 1-adrenoceptor antagonist trimazosin were studied at rest and during bicycle exercise in the upright position in 14 patients with uncomplicated, stable essential hypertension. Rest and exercise studies before the drug was given revealed no evidence of left ventricular pumping deficiency. A single intravenous bolus of trimazosin (2 mg/kg) resulted in a plasma concentration of 13.1 +/- 1.0 mg/ml 30 min after injection. This plasma concentration of trimazosin was associated with a reduction in the systemic vascular resistance (p less than 0.01); in the absence of any increase in the cardiac output, this resulted in a fall in the systemic blood pressure (p less than 0.01) at rest. Heart rate and left heart filling pressure were unchanged. During 4 min of upright dynamic exercise after drug, the increment in systemic blood pressure was similar to that in the control study; i.e., the absolute level of pressure was reduced (p less than 0.01). The increases in heart rate, cardiac output, and left heart filling pressure during exercise were also unchanged after drug compared with those measured in the control study. The left heart filling pressure and cardiac output were slower to increase at the onset of exercise after trimazosin, which may imply a degree of venodilatation. There were no hypotensive symptoms or large falls in blood pressure after trimazosin at rest, but following 4 min of submaximal upright bicycle exercise, three of the 14 patients developed postural hypotension.(ABSTRACT TRUNCATED AT 250 WORDS)
作为一项更大规模临床试验的前期研究,在14例无并发症的稳定原发性高血压患者中,研究了选择性α1肾上腺素能受体拮抗剂曲马唑嗪在静息状态及直立位自行车运动期间的血流动力学效应。给药前的静息和运动研究未发现左心室泵血功能不足的证据。单次静脉推注曲马唑嗪(2mg/kg)后,注射30分钟时血浆浓度为13.1±1.0mg/ml。曲马唑嗪的这一血浆浓度与全身血管阻力降低相关(p<0.01);在心输出量未增加的情况下,这导致静息时全身血压下降(p<0.01)。心率和左心充盈压未改变。给药后进行4分钟直立动态运动期间,全身血压的升高幅度与对照研究相似;即压力的绝对值降低了(p<0.01)。与对照研究中测得的相比,给药后运动期间心率、心输出量和左心充盈压的增加也未改变。曲马唑嗪给药后运动开始时左心充盈压和心输出量的增加较慢,这可能意味着存在一定程度的静脉扩张。曲马唑嗪静息时无低血压症状或血压大幅下降,但在进行4分钟次最大强度直立位自行车运动后,14例患者中有3例出现体位性低血压。(摘要截短于250字)