Silke B, Verma S P, Sharma S K, Frais M A, Reynolds G, Taylor S H
University Department of Cardiovascular Studies, General Infirmary, Leeds, England.
J Cardiovasc Pharmacol. 1989 Jan;13(1):155-61.
Cicloprolol is a new cardioselective beta-blocking agent with partial agonist activity (intrinsic sympathomimetic activity, ISA). Its haemodynamic profile was compared with that of atenolol (cardioselective; no ISA) in a comparative dose-response study of 24 ischaemic patients with diminished cardiac reserve. Following a stable control period, equivalent intravenous (i.v.) beta-blocking boluses of atenolol (1, 1, 2, and 4 mg) or cicloprolol (0.025, 0.025, 0.05, and 0.1 mg/kg) were randomly administered and haemodynamics and left ventricular ejection fraction were determined at rest and during bicycle exercise. At rest, atenolol reduced heart rate (HR) and cardiac index; diastolic blood pressure (DBP), systemic vascular resistance index (SVRI), and pulmonary artery occluded pressure (PAOP) increased without change in mean arterial pressure (MAP). Cicloprolol increased left ventricular ejection fraction, reduced its end-diastolic volume, and tended to reduce filling pressure without change in other variables. During exercise, atenolol reduced ejection fraction and increased SVRI; in contrast, cicloprolol did not significantly alter these parameters. Attenuation of exercise tachycardia and cardiac index increase was similar after each agent. Thus, the cardiac performance assessed from left ventricular stroke index or ejection fraction/filling pressure relationships was less depressed after cicloprolol as compared with atenolol. The relevance of such haemodynamic differences to exercise ability or quality of life during sustained therapy warrants examination.
环丙洛尔是一种具有部分激动剂活性(内在拟交感神经活性,ISA)的新型心脏选择性β受体阻滞剂。在一项对24例心脏储备功能减退的缺血性患者进行的比较剂量反应研究中,将其血流动力学特征与阿替洛尔(心脏选择性;无ISA)的进行了比较。在一个稳定的对照期之后,随机给予阿替洛尔(1、1、2和4毫克)或环丙洛尔(0.025、0.025、0.05和0.1毫克/千克)等效的静脉注射β受体阻滞剂推注剂量,并在静息和自行车运动期间测定血流动力学和左心室射血分数。静息时,阿替洛尔降低心率(HR)和心脏指数;舒张压(DBP)、全身血管阻力指数(SVRI)和肺动脉闭塞压(PAOP)升高,平均动脉压(MAP)无变化。环丙洛尔增加左心室射血分数,减少其舒张末期容积,并倾向于降低充盈压,其他变量无变化。运动期间,阿替洛尔降低射血分数并增加SVRI;相比之下,环丙洛尔并未显著改变这些参数。每种药物后运动性心动过速和心脏指数增加的减弱相似。因此,与阿替洛尔相比,根据左心室每搏指数或射血分数/充盈压关系评估的心脏功能在使用环丙洛尔后受到的抑制较小。这种血流动力学差异与持续治疗期间运动能力或生活质量的相关性值得研究。