Tattersfield A E
Division of Respiratory Medicine, City Hospital, Nottingham, England.
Life Sci. 1993;52(26):2161-9. doi: 10.1016/0024-3205(93)90730-q.
The longer-acting beta-receptor agonists salmeterol and formoterol are effective bronchodilators for at least 12 hours and this should be clinically useful, particularly for nocturnal asthma. Formoterol has a more rapid onset than salmeterol. There are limited dose response data on the two drugs in man but the evidence so far suggests that both drugs have roughly similar beta 2-selectivity to salbutamol and that both are about ten times as potent as salbutamol. Salmeterol may therefore have been marketed at a relatively high dose compared to salbutamol. There is no good clinical evidence to suggest that the drugs have effects other than would be expected from a beta 2-agonist with a prolonged duration of action. Medium-term studies have shown that benefit was maintained in comparison to salbutamol and, in one instance, with salmeterol when compared to placebo. Studies to date have not found any reduction in the bronchodilator response to salbutamol following regular treatment with salmeterol or formoterol, though one study has found reduced protection by salmeterol against methacholine challenge after one and two months' treatment. Longer-term safety has not been assessed.
长效β受体激动剂沙美特罗和福莫特罗作为支气管扩张剂的作用时间至少长达12小时，这在临床上应具有实用价值，尤其适用于夜间哮喘。福莫特罗的起效比沙美特罗更快。关于这两种药物在人体中的剂量反应数据有限，但目前的证据表明，这两种药物对β2的选择性与沙丁胺醇大致相似，且效力均约为沙丁胺醇的十倍。因此，与沙丁胺醇相比，沙美特罗的上市剂量可能相对较高。没有充分的临床证据表明这些药物除了具有长效β2激动剂所预期的作用外还存在其他作用。中期研究表明，与沙丁胺醇相比，疗效得以维持，并且在一项研究中，与安慰剂相比，使用沙美特罗时疗效也得以维持。迄今为止的研究尚未发现，在长期使用沙美特罗或福莫特罗治疗后，对沙丁胺醇的支气管扩张反应有所降低，不过有一项研究发现，在治疗一两个月后，沙美特罗对乙酰甲胆碱激发试验的保护作用有所减弱。尚未评估其长期安全性。
