De Vita C, Triulzi E, Devizzi S, Colombo G, Palvarini M, Pocchiari F, Pataccini R
Arzneimittelforschung. 1986 Feb;36(2A):349-54.
The aim of the present investigation was to evaluate the acute hemodynamic effects of a single oral dose of 200 mg ibopamine (SB-7505), the 3,4-diisobutyryl ester of N-methyldopamine (epinine) in 11 patients with congestive heart failure (CHF) and to compare the influence of dopamine infusion and oral ibopamine on left ventricular function. Free and conjugated epinine plasma levels were also investigated in these patients and in a group of healthy volunteers to evaluate the correlation between epinine plasma levels and hemodynamic effects. The oral administration of 200 mg ibopamine to patients with CHF, increased cardiac index (+35%) and reduced peripheral and pulmonary vascular resistance (-29% and -26%) without modifying heart rate and systemic or pulmonary arterial pressure. The hemodynamic effect reached its maximum at about 90 min and was still present at 240 min. Ibopamine at a dose of 200 mg elicited similar effects to those observed with dopamine, 2-4 micrograms/kg/min. The pharmacokinetic behaviour of ibopamine in these patients was similar to that observed in a group of healthy volunteers. Free epinine plasma levels peaked at 30-60 min and decreased rapidly, thus showing a shorter time course than the hemodynamic effects.
本研究的目的是评估单次口服200毫克异波帕明(SB - 7505),即N - 甲基多巴胺(依匹宁)的3,4 - 二异丁酯,对11例充血性心力衰竭(CHF)患者的急性血流动力学影响,并比较多巴胺输注和口服异波帕明对左心室功能的影响。还对这些患者和一组健康志愿者的游离和结合型依匹宁血浆水平进行了研究,以评估依匹宁血浆水平与血流动力学效应之间的相关性。对CHF患者口服200毫克异波帕明后,心脏指数增加(+35%),外周和肺血管阻力降低(-29%和-26%),而心率、体循环或肺动脉压未发生改变。血流动力学效应在约90分钟时达到最大值,在240分钟时仍存在。200毫克剂量的异波帕明产生的效应与2 - 4微克/千克/分钟的多巴胺所观察到的效应相似。异波帕明在这些患者中的药代动力学行为与在一组健康志愿者中观察到的相似。游离依匹宁血浆水平在30 - 60分钟时达到峰值并迅速下降,因此显示出比血流动力学效应更短的时间进程。