de Muinck E, Wagner G, vd Ven L L, Lie K I
Akademisch Ziekenhuis, Groningen, The Netherlands.
Eur Heart J. 1987 Dec;8 Suppl M:31-5. doi: 10.1093/eurheartj/8.suppl_m.31.
Recently, bisoprolol has been investigated regarding its effects on exercise tolerance and the duration of action in patients with coronary heart disease (CHD) following single oral administration. It appears, however, that the extent of effects of 5 mg bisoprolol is not fully established yet. Therefore, the effects of 5 and 10 mg bisoprolol and the duration of action were assessed in 12 patients (10 male, 2 female; mean age 60.2 years) with stable angina pectoris due to CHD after repeated administration. Patients were given 5 or 10 mg bisoprolol once daily for 2 weeks according to a double-blind, randomized cross-over design. At entry one exercise tolerance test (ETT) served as baseline measurement and following each treatment period ETTs were performed before (24-hour value) and 3 hours after tablet intake. Exercise capacity (in W X min) was calculated until the onset of angina, 0.1 mV ST-segment depression and at peak exercise. Compared to baseline all workload values during active therapy were significantly improved (P less than or equal to 0.05) except for the workload till onset of angina with bisoprolol 5 mg at 24 hours. The effects at 3 hours were significantly stronger than those after 24 hours for both dosages. Significantly stronger effects were observed 3 hours as well as 24 hours after intake during treatment with 10 mg compared to 5 mg: at peak exercise on heart rate (P less than or equal to 0.05) and exercise capacity (P less than or equal to 0.01), at identical workload on heart rate (P less than or equal to 0.01) and rate-pressure product (P less than or equal to 0.01). It was found that bisoprolol 5 mg once daily leads to therapeutic effects with a clearly maintained duration of action over 24 hours, but further increase of peak exercise capacity may be achieved with 10 mg.
最近，人们对比索洛尔单次口服给药后对冠心病（CHD）患者运动耐量和作用持续时间的影响进行了研究。然而，5mg比索洛尔的作用程度似乎尚未完全明确。因此，在12例（10例男性，2例女性；平均年龄60.2岁）因CHD导致稳定型心绞痛的患者中，评估了5mg和10mg比索洛尔的作用及作用持续时间，这些患者均经过多次给药。根据双盲、随机交叉设计，患者每天服用一次5mg或10mg比索洛尔，持续2周。入组时进行一次运动耐量测试（ETT）作为基线测量，在每个治疗期结束后，于服药前（24小时值）和服药后3小时进行ETT。计算直至心绞痛发作、ST段压低0.1mV和运动峰值时的运动能力（以W×min计）。与基线相比，积极治疗期间的所有工作量值均显著改善（P≤0.05），但24小时时服用5mg比索洛尔直至心绞痛发作的工作量除外。两种剂量在3小时时的作用均明显强于24小时时。与5mg相比，10mg治疗期间服药后3小时和24小时均观察到明显更强的作用：运动峰值时的心率（P≤0.05）和运动能力（P≤0.01），相同工作量时的心率（P≤0.01）和速率压力乘积（P≤0.01）。研究发现，每天一次服用5mg比索洛尔可产生治疗作用，作用持续时间在24小时内明显维持，但10mg可进一步提高运动峰值能力。
