Singh B N, Thoden W R, Wahl J
Pharmacotherapy. 1986 Mar-Apr;6(2):45-63. doi: 10.1002/j.1875-9114.1986.tb03451.x.
Acebutolol is a new hydrophilic, cardioselective beta-adrenergic-blocking agent that possesses partial agonist and membrane-stabilizing activities. In the treatment of mild to moderate essential hypertension, once-daily acebutolol as monotherapy provides effective control in a large majority of patients and produces a further reduction in blood pressure when used concomitantly with diuretics. Acebutolol is as effective as other beta-blocking agents, and in a large, double-blind, parallel study against propranolol was found to cause less reduction in heart rate, and fewer neurologic side effects and patient withdrawals due to adverse effects. Oral acebutolol is also effective in suppressing premature ventricular contractions, and in small numbers of patients generally beneficial results were obtained in supraventricular and ventricular arrhythmias with intravenous administration. These salutary effects are attributable to beta blockade. Controlled clinical trials documented the antianginal actions of oral acebutolol in chronic stable angina pectoris; its efficacy in this regard is comparable to that of other beta-blocking agents. The drug produces smaller decreases in heart rate and cardiac output and alterations in peripheral vascular hemodynamics than beta-blocking drugs without partial agonist activity, and because of its cardioselectivity, it may be used cautiously in patients with bronchospastic disease. Acebutolol has minimal metabolic effects and does not elevate levels of blood lipids during long-term therapy; high-density-lipoprotein cholesterol increased with acebutolol in a small number of patients.
醋丁洛尔是一种新型的亲水性、心脏选择性β肾上腺素能阻滞剂,具有部分激动剂和膜稳定活性。在治疗轻至中度原发性高血压时,每日一次使用醋丁洛尔作为单一疗法可使大多数患者得到有效控制,与利尿剂合用时可进一步降低血压。醋丁洛尔与其他β阻滞剂一样有效,在一项针对普萘洛尔的大型双盲平行研究中发现,它导致心率降低较少,神经副作用和因不良反应导致的患者退出治疗的情况也较少。口服醋丁洛尔在抑制室性早搏方面也有效,少数患者静脉给药治疗室上性和室性心律失常通常取得有益效果。这些有益作用归因于β受体阻滞。对照临床试验证明口服醋丁洛尔对慢性稳定型心绞痛有抗心绞痛作用;其在这方面的疗效与其他β阻滞剂相当。与无部分激动剂活性的β阻滞剂相比,该药使心率和心输出量降低幅度较小,对外周血管血流动力学的改变也较小,并且由于其心脏选择性,可谨慎用于患有支气管痉挛性疾病的患者。醋丁洛尔的代谢作用极小,长期治疗期间不会升高血脂水平;少数患者使用醋丁洛尔后高密度脂蛋白胆固醇升高。