Maury M, Berdeaux A, Kher A, Duhaze P, Giudicelli J F
Eur J Clin Pharmacol. 1985;27(6):649-56. doi: 10.1007/BF00547043.
The beta-adrenoceptor blocking properties and pharmacokinetics of bucindolol 150 mg were compared to those of propranolol 80 mg and a placebo in a double-blind trial in 6 healthy volunteers. Heart rate (HR), systolic (SBP) and diastolic (DBP) blood pressures and peak expiratory flow rate (PEFR) at rest and during vigorous exercise, and plasma renin activity (PRA) at rest, were measured before and at intervals up to 24 h after oral administration of the drugs. Bucindolol reduced exercise tachycardia and decreased exercise PEFR, thus behaving as a non-selective beta-adrenoceptor blocking drug. In contrast to propranolol, bucindolol did not reduce resting HR and PRA, probably because of its intrinsic sympathomimetic activity. It decreased resting DBP in relation to its peripheral vasodilator properties. The effects of bucindolol developed as early as 30 min after administration and lasted up to 24 h, whereas its Tmax and T 1/2 were 1.6 and 3.6 h respectively. Comparison of the time courses of plasma bucindolol and the cardiac beta-adrenoceptor blockade strongly suggests that in man bucindolol undergoes an extensive first-pass effect, leading to the formation of one or more active metabolites.
在一项针对6名健康志愿者的双盲试验中，比较了150毫克布新洛尔与80毫克普萘洛尔及安慰剂的β-肾上腺素能受体阻断特性和药代动力学。在口服药物前及给药后长达24小时的间隔时间测量静息及剧烈运动时的心率（HR）、收缩压（SBP）和舒张压（DBP）以及呼气峰值流速（PEFR），并测量静息时的血浆肾素活性（PRA）。布新洛尔可减轻运动性心动过速并降低运动时的PEFR，因此表现为非选择性β-肾上腺素能受体阻断药物。与普萘洛尔不同，布新洛尔不会降低静息时的HR和PRA，这可能是由于其内在拟交感活性。因其外周血管舒张特性，它可降低静息时的DBP。布新洛尔的作用在给药后30分钟就开始出现，并持续长达24小时，而其达峰时间（Tmax）和半衰期（T 1/2）分别为1.6小时和3.6小时。血浆布新洛尔与心脏β-肾上腺素能受体阻断的时间过程比较强烈表明，在人体内布新洛尔会经历广泛的首过效应，导致形成一种或多种活性代谢产物。
