Singh B N, Thoden W R, Ward A
Drugs. 1985 Jun;29(6):531-69. doi: 10.2165/00003495-198529060-00003.
Acebutolol is a cardioselective beta-adrenoceptor blocking drug possessing both partial agonist (intrinsic sympathomimetic) and membrane stabilising activity. In hypertension, it can be administered once or twice daily with equal effectiveness, and has been as effective at lowering blood pressure as propranolol, diuretics, and other beta-blocking drugs (metoprolol, labetalol and atenolol) and more effective than methyldopa. Acebutolol has a significantly smaller effect on resting heart rate than propranolol, metoprolol and atenolol, although direct comparisons with drugs with intrinsic sympathomimetic activity have yet to be undertaken. In both angina and arrhythmia, when administered twice daily it has been as effective as standard therapeutic agents. The side effect profile of acebutolol appears to be comparable to that of other cardioselective beta-blockers. Its relative cardio-selectivity, partial agonist and membrane stabilising activity, hydrophilicity, and considerable extrarenal excretion may offer advantages over some beta-blocking drugs in specific patients. Choosing a beta-blocking agent, however, should be made with a knowledge of pharmacodynamic and pharmacokinetic properties of the various agents and careful consideration of how such properties may be of benefit to an individual patient.
醋丁洛尔是一种具有心脏选择性的β-肾上腺素受体阻断药，兼具部分激动剂（内在拟交感活性）和膜稳定活性。在高血压治疗中，每日给药一次或两次疗效相同，其降压效果与普萘洛尔、利尿剂及其他β受体阻断药（美托洛尔、拉贝洛尔和阿替洛尔）相当，且优于甲基多巴。醋丁洛尔对静息心率的影响明显小于普萘洛尔、美托洛尔和阿替洛尔，不过与具有内在拟交感活性的药物的直接比较尚未进行。在心绞痛和心律失常的治疗中，每日给药两次时其疗效与标准治疗药物相当。醋丁洛尔的副作用谱似乎与其他心脏选择性β受体阻断剂相当。其相对的心脏选择性、部分激动剂和膜稳定活性、亲水性以及大量的肾外排泄，在特定患者中可能比某些β受体阻断药具有优势。然而，选择β受体阻断剂时，应了解各种药物的药效学和药代动力学特性，并仔细考虑这些特性如何可能对个体患者有益。
