Carboni G P, Scardovi A B, D'Ermo M, Prati P L
Divisione Cardiologia A, Ospedale S. Camillo, Roma.
Br J Clin Pharmacol. 1991 Dec;32(6):755-7.
The effects of bopindolol, a new beta-adrenoceptor blocker, on the exercise tolerance of 12 in-patients, mean age 57 (5 years), with stable angina pectoris and documented coronary artery disease were evaluated. All patients received on 4 different days a single oral dose of bopindolol 0.5 mg, bopindolol 1.0 mg, bopindolol 2.0 mg and placebo according to a double-blind latin square design. Treadmill symptoms-limited exercise tests were performed using a Bruce protocol, 3, 12 and 24 h after dosing. Bipindolol improved (P less than 0.05) exercise tolerance in comparison with placebo (by a maximum of 33%, 52% and 26% after the 2.0 mg dose) with no adverse effect on ischaemia. The primary action of bopindolol appeared to be to reduce myocardial oxygen consumption (mainly by its negative chronotropic effect) for up to the 24th hour after oral administration. Eight (66%) patients were angina free at the 3rd, 12th and 24th h exercise test. The effects of bopindolol were not dose-related. A short period of inactivity due to hospitalization may have influenced the exercise performance and led us to underestimate the presence of a dose-response. The results of this report suggest that bopindolol has a long lasting effect in the treatment of patients with chronic stable angina pectoris.
对12例平均年龄57岁(5岁)、患有稳定型心绞痛且有冠状动脉疾病记录的住院患者,评估了新型β肾上腺素受体阻滞剂波吲洛尔对其运动耐量的影响。根据双盲拉丁方设计,所有患者在4个不同日期分别单次口服0.5毫克波吲洛尔、1.0毫克波吲洛尔、2.0毫克波吲洛尔和安慰剂。给药后3小时、12小时和24小时,使用布鲁斯方案进行跑步机症状限制运动试验。与安慰剂相比,波吲洛尔改善了(P<0.05)运动耐量(2.0毫克剂量后最大改善33%、52%和26%),且对缺血无不良影响。波吲洛尔的主要作用似乎是在口服给药后长达24小时内降低心肌耗氧量(主要通过其负性变时作用)。8例(66%)患者在第3小时、12小时和24小时运动试验时无心绞痛发作。波吲洛尔的作用与剂量无关。因住院导致的短期不活动可能影响了运动表现,使我们低估了剂量反应的存在。本报告结果表明,波吲洛尔在治疗慢性稳定型心绞痛患者方面具有持久疗效。