Bremner P, Woodman K, Burgess C, Crane J, Purdie G, Pearce N, Beasley R
Dept of Medicine, Wellington School of Medicine, New Zealand.
Eur Respir J. 1993 Feb;6(2):204-10.
The cardiovascular and metabolic effects of the long-acting beta 2-agonist formoterol were compared with those of salbutamol, fenoterol and placebo in 12 healthy volunteers, using a randomised, double-blind, cross-over design. On the study days, the subjects inhaled either formoterol (24 micrograms), salbutamol (400 micrograms), fenoterol (400 micrograms) or placebo, at 30 min intervals for five doses. Heart rate (HR) total electromechanical systole (Q-S2I) (a measure of inotropy), the corrected QT interval (QTc), systolic and diastolic blood pressure, plasma glucose and plasma potassium (K+) were measured prior to drug administration, 10 min after each inhalation and at 30 min intervals for 3 h after the last inhalation. All of the active agents significantly increased HR, QTc and plasma glucose, and decreased Q-S2I, diastolic blood pressure and plasma K+ compared to placebo. Fenoterol had a significantly greater maximum effect on HR, QTc and Q-S2I than either salbutamol or formoterol. Formoterol and fenoterol caused a similar maximum reduction in plasma K+, greater than that due to salbutamol. We conclude that formoterol is a more selective beta 2-agonist than fenoterol, and has similar cardiovascular effects to salbutamol when inhaled repeatedly by normal volunteers.
采用随机、双盲、交叉设计，在12名健康志愿者中比较了长效β2受体激动剂福莫特罗与沙丁胺醇、非诺特罗及安慰剂对心血管和代谢的影响。在研究日，受试者每隔30分钟吸入一次福莫特罗（24微克）、沙丁胺醇（400微克）、非诺特罗（400微克）或安慰剂，共吸入五剂。在给药前、每次吸入后10分钟以及最后一次吸入后3小时内每隔30分钟测量心率（HR）、总电机械收缩期（Q-S2I）（心肌收缩力的一种测量指标）、校正QT间期（QTc）、收缩压和舒张压、血浆葡萄糖及血浆钾（K+）。与安慰剂相比，所有活性药物均显著增加HR、QTc及血浆葡萄糖，并降低Q-S2I、舒张压及血浆K+。非诺特罗对HR、QTc及Q-S2I的最大效应显著大于沙丁胺醇或福莫特罗。福莫特罗和非诺特罗使血浆K+的最大降幅相似，且大于沙丁胺醇所致降幅。我们得出结论，福莫特罗是一种比非诺特罗更具选择性的β2受体激动剂，正常志愿者反复吸入时，其心血管效应与沙丁胺醇相似。
