Ramsdale E H, Otis J, Kline P A, Gontovnick L S, Hargreave F E, O'Byrne P M
Department of Medicine, St. Joseph's Hospital, Hamilton, Ontario, Canada.
Am Rev Respir Dis. 1991 May;143(5 Pt 1):998-1001. doi: 10.1164/ajrccm/143.5_Pt_1.998.
Formoterol fumarate is a new, high-affinity, beta 2-adrenergic receptor agonist that causes bronchodilation for at least 12 h. The purpose of this study was to compare the magnitude and duration of the effect of inhalation of formoterol (12 and 24 micrograms), albuterol (200 micrograms), and placebo in terms of protection against methacholine-induced bronchoconstriction. The 16 stable adult asthmatic subjects were studied on four separate study days. On each study day the subjects inhaled 2 puffs of the study medication, and methacholine tests were performed at 30 min and 4, 8, and 12 h later. Results were expressed as the provocative concentration of methacholine required to cause a 20% fall in FEV1 (PC20). At 30 min, 12 and 24 micrograms formoterol caused a mean 14- to 20-fold decrease in responsiveness, and albuterol a 12-fold decrease. However, albuterol had no significant protective effect at 4 h or thereafter, whereas there was still an 8-fold decrease in responsiveness for 24 micrograms formoterol and a 6-fold decrease for 12 micrograms formoterol at 12 h. This study has shown that both doses of formoterol were still actively protective against induced bronchoconstriction 12 h after inhalation, with minimal side effects. This suggests that formoterol may prove to be a very useful bronchodilator for the treatment of patients with asthma who have significant airway hyperresponsiveness or nocturnal symptoms and who require inhaled beta 2-agonists at least twice daily.
富马酸福莫特罗是一种新型、高亲和力的β2肾上腺素能受体激动剂，可引起至少12小时的支气管扩张。本研究的目的是比较吸入福莫特罗（12微克和24微克）、沙丁胺醇（200微克）和安慰剂在预防乙酰甲胆碱诱发的支气管收缩方面的作用强度和持续时间。16名病情稳定的成年哮喘患者在4个不同的研究日接受研究。在每个研究日，受试者吸入2喷研究药物，并在30分钟以及4、8和12小时后进行乙酰甲胆碱试验。结果以引起第一秒用力呼气量（FEV1）下降20%所需的乙酰甲胆碱激发浓度（PC20）表示。在30分钟时，12微克和24微克福莫特罗使反应性平均降低14至20倍，沙丁胺醇使反应性降低12倍。然而，沙丁胺醇在4小时及之后没有显著的保护作用，而24微克福莫特罗在12小时时反应性仍降低8倍，12微克福莫特罗降低6倍。本研究表明，两种剂量的福莫特罗在吸入12小时后对诱发的支气管收缩仍有积极的保护作用，且副作用最小。这表明福莫特罗可能被证明是一种非常有用的支气管扩张剂，可用于治疗气道反应性显著增高或有夜间症状且每天至少需要吸入两次β2激动剂的哮喘患者。
