First Medical Service, Department of Allergology, Sahlgrens Hospital, University of Göteborg, Göteborg, Sweden.
Br J Clin Pharmacol. 1976 Dec;3(6):1007-14. doi: 10.1111/j.1365-2125.1976.tb00350.x.
The effect of metoprolol, a new beta1-adrenoceptor blocking agent, was compared to practolol in the treatment of hypertension in seventeen asthmatics during concurrent optimum bronchodilator therapy with a selective beta2-adrenoceptor-stimulant. The two beta-adrenoceptor antagonists were given at two dose levels, practolol (200 mg and 400 mg) daily, and metoprolol (100 mg and 200 mg) daily, in a twice-daily dosage schedule, at 12 h intervals, for 17 days. The comparison was made double-blind and a crossover design was used. The drugs were given in randomized order. The study started with a run-in placebo period and there was a washout period on placebo between the treatment periods. Spirometry, blood pressures and heart rates were recorded in a standardized manner. At the lower dose levels no influence on FEV1 was noted, and no difference was found between the two active drugs. At the higher dose level FEV1 was reduced by both beta-adrenoceptor-blocking drugs. Four out of twelve patients given the higher dose experienced exacerbation of their asthma. The heart rate fell with both drugs and at both dose levels. During the placebo period a marked increase of heart rate was noted. The blood pressure fell at both dose levels compared to placebo, no difference being recorded between the two drugs. Metoprolol and practolol are equally effective beta1-adrenoceptor blocking drugs. In this study it was found that metoprolol could be used in asthmatics who had indications for beta-adrenoceptor blockade, provided that the total daily dose did not exceed 100 mg. Optimal bronchodilator treatment with a bronchoselective beta-adrenoceptor agonist is an absolute prerequisite in order to avoid the risk of aggravation of asthma.
美托洛尔,一种新型的β1-肾上腺素受体阻滞剂,在 17 例同时接受选择性β2-肾上腺素能受体兴奋剂最佳支气管扩张治疗的哮喘患者中,与普萘洛尔进行了比较,以治疗高血压。两种β-肾上腺素能受体拮抗剂以两种剂量水平给药,普萘洛尔(200mg 和 400mg)每日一次,美托洛尔(100mg 和 200mg)每日两次,在 12 小时的间隔内,每日两次,共 17 天。该比较采用双盲和交叉设计。药物以随机顺序给予。该研究从一个导入安慰剂期开始,在治疗期之间有一个安慰剂洗脱期。采用标准化方法记录肺活量、血压和心率。在较低剂量水平下,对 FEV1 没有影响,两种活性药物之间没有差异。在较高剂量水平下,两种β-肾上腺素能受体阻滞剂均可降低 FEV1。在接受较高剂量的 12 名患者中,有 4 名出现哮喘恶化。两种药物均降低心率,且在两种剂量水平下均降低。在安慰剂期,心率明显增加。与安慰剂相比,两种药物在两个剂量水平下血压均下降,两种药物之间没有差异。美托洛尔和普萘洛尔是同样有效的β1-肾上腺素能受体阻滞剂。在这项研究中发现,美托洛尔可用于有β-肾上腺素能受体阻断指征的哮喘患者,只要总日剂量不超过 100mg。使用具有支气管选择性的β-肾上腺素能受体激动剂进行最佳支气管扩张治疗是避免哮喘恶化风险的绝对前提。