Aellig W H
Br J Clin Pharmacol. 1985 Jun;19(6):775-81. doi: 10.1111/j.1365-2125.1985.tb02713.x.
Bopindolol is a potent and specific beta-adrenoceptor antagonist with partial agonist activity. In animal experiments it blocks both beta 1- and beta 2-adrenoceptors and possesses a long duration of action. In the present study in healthy volunteers bopindolol was about ten times more potent than pindolol in reducing isoprenaline-induced and exercise-induced tachycardia. In experiments on exercise-induced tachycardia an oral dose of 2 mg produced a near maximum reduction of exercise heart rate, occurring within 2 to 3 h of administration. With higher doses (up to 12 mg) the maximum effect was reached earlier (between 1 and 2 h). The long duration of action of bopindolol observed in animal studies was confirmed in man. Twenty-four hours after 4 and 10 mg bopindolol more than 2/3 of the maximum effect was still present. After 48 h 38% of the maximum effect of 4 mg and 50% of that of 12 mg remained. Even at 72 and 96 h exercise-induced tachycardia was still significantly lowered after both doses of the drug. When bopindolol was administered once daily for 5 days there was a slight increase in the maximum reduction of exercise-induced tachycardia during treatment with 1 mg/day but not with 4 mg/day, which produced a near maximum effect.
波吲洛尔是一种强效且具有部分激动剂活性的特异性β-肾上腺素能受体拮抗剂。在动物实验中，它能阻断β1和β2肾上腺素能受体，且作用持续时间长。在本项针对健康志愿者的研究中，波吲洛尔在降低异丙肾上腺素诱发的和运动诱发的心动过速方面，效力约为吲哚洛尔的10倍。在运动诱发心动过速的实验中，口服2毫克剂量可使运动心率接近最大程度降低，在给药后2至3小时内出现。使用更高剂量（高达12毫克）时，最大效应出现得更早（在1至2小时之间）。在动物研究中观察到的波吲洛尔的长效作用在人体中得到了证实。服用4毫克和10毫克波吲洛尔24小时后，仍有超过2/3的最大效应存在。48小时后，4毫克剂量的最大效应仍保留38%，12毫克剂量的保留50%。即使在72小时和96小时，两种剂量的药物给药后运动诱发的心动过速仍显著降低。当波吲洛尔每日给药一次，持续5天时，每天1毫克剂量治疗期间运动诱发心动过速的最大降低幅度略有增加，但每天4毫克剂量时未出现这种情况，4毫克剂量已产生接近最大效应。
