Velasco M, Gilbert C A, Rutledge C O, McNay J L
Clin Pharmacol Ther. 1975 Aug;18(2):145-53. doi: 10.1002/cpt1975182145.
The cardiovascular effects of a new antihypertensive drug, bupicomide, were compared with those of hydralazine in 6 patients with mild to moderate hypertension. The mean supine arterial pressure of patients was reduced 15.2 mm Hg by bupicomide (900 to 2,000 mg/day) and 15.7 mm Hg by hydralazine (300 to 600 mg/day). Heart rate increased an average of 11.3 bpm during bupicomide and 14.5 bpm by hydralazine. Neither drug was associated with a postural decrease in mean arterial pressure. The heart rate response during maximum tolerated treadmill exercise was not diminished by either drug. Cardiac index was increased during administration of both drugs. Bupicomide and hydralazine reduced forearm vascular resistance, while renal blood flow and renal vascular resistance were not significantly modified. Evidence of equivalent augmentation of sympathetic nervous activity during administration of both drugs consisted of equal and significant increases in heart rate and urinary norepinephrine excretion, and decreases in duration of the pre-ejection period. The absolute values of these parameters were correlated with mean arterial pressure, which may indicate that the increase in sympathetic nervous activity was mediated by baroreceptor reflexes. Although bupicomide inhibits dopamine beta-hydroxylase, our results suggest that it is acting as a direct vasodilator.
在6例轻至中度高血压患者中,对一种新型抗高血压药物布匹米胺与肼屈嗪的心血管效应进行了比较。布匹米胺(900至2000毫克/天)使患者仰卧位平均动脉压降低15.2毫米汞柱,肼屈嗪(300至600毫克/天)使其降低15.7毫米汞柱。服用布匹米胺期间心率平均增加11.3次/分钟,服用肼屈嗪时增加14.5次/分钟。两种药物均未导致平均动脉压出现体位性下降。两种药物均未减弱最大耐受跑步机运动期间的心率反应。两种药物给药期间心脏指数均升高。布匹米胺和肼屈嗪均降低了前臂血管阻力,而肾血流量和肾血管阻力未发生显著改变。两种药物给药期间交感神经活动等效增强的证据包括心率和尿去甲肾上腺素排泄量同等且显著增加,以及射血前期持续时间缩短。这些参数的绝对值与平均动脉压相关,这可能表明交感神经活动的增加是由压力感受器反射介导的。尽管布匹米胺抑制多巴胺β-羟化酶,但我们的结果表明它起直接血管扩张剂的作用。