Lammers J W, Folgering H T, van Herwaarden C L
Clin Pharmacol Ther. 1985 Oct;38(4):428-33. doi: 10.1038/clpt.1985.199.
The cardioequipotency of 400 mg bevantolol and 100 mg atenolol was determined by measuring the exercise heart rate in healthy subjects. The beta-blockers were then used in these doses to investigate their ventilatory effects in patients with asthma. The effects of both drugs on forced expiratory flow parameters for large and small airways were assessed at rest and during and after exercise. A dose-response curve was then plotted after inhalation of the beta 2-adrenoceptor agonist terbutaline. Bevantolol significantly decreased the forced expiratory volume in 1 second (FEV1) and the peak expiratory flow rate (PEFR) at rest, while there was no such change with placebo or atenolol. Both beta-blockers decreased the maximal expiratory flow rates at 50% of forced vital capacity (MEF50) and after expiration of 75% of the forced vital capacity (MEF25) at rest; the decrease was larger after bevantolol than after atenolol. During atenolol there was a decrease in FEV1 and in PEFR (P less than 0.01) 15 minutes after exercise in comparison with preexercise values. There was no significant difference between pre- and postexercise values of MEF50 and MEF25 during atenolol dosing. After bevantolol there was only a small change in PEFR after exercise, probably because of the low preexercise values of the ventilatory indices with this drug. Inhalation of terbutaline up to a dose of 2 mg significantly improved all ventilatory indices measured, but with bevantolol the values after 2 mg inhaled terbutaline were lower than the initial values.(ABSTRACT TRUNCATED AT 250 WORDS)
通过测量健康受试者的运动心率,确定了400毫克倍凡洛尔与100毫克阿替洛尔的心脏等效性。随后以这些剂量使用β受体阻滞剂,研究其对哮喘患者的通气作用。在静息状态、运动期间及运动后,评估了两种药物对大小气道用力呼气流量参数的影响。然后在吸入β2肾上腺素能激动剂特布他林后绘制剂量反应曲线。倍凡洛尔在静息时显著降低了1秒用力呼气量(FEV1)和呼气峰值流速(PEFR),而安慰剂或阿替洛尔则无此变化。两种β受体阻滞剂在静息时均降低了用力肺活量50%时的最大呼气流量(MEF50)和用力肺活量呼出75%后的最大呼气流量(MEF25);倍凡洛尔后的降低幅度大于阿替洛尔。在服用阿替洛尔期间,运动后15分钟的FEV1和PEFR较运动前值降低(P<0.01)。在服用阿替洛尔期间,MEF50和MEF25的运动前和运动后值之间无显著差异。服用倍凡洛尔后,运动后PEFR仅有微小变化,可能是因为该药物通气指标的运动前值较低。吸入高达2毫克的特布他林可显著改善所有测量的通气指标,但吸入2毫克特布他林后,倍凡洛尔组的值低于初始值。(摘要截取自250字)