Faulds D, Hollingshead L M, Goa K L
Adis International Limited, Auckland, New Zealand.
Drugs. 1991 Jul;42(1):115-37. doi: 10.2165/00003495-199142010-00007.
Formoterol, a long-acting beta 2-selective adrenoceptor agonist, produces dose-proportional bronchodilation in patients with obstructive airways disease with a reversible component. A significant effect occurs within minutes of inhalation of a therapeutic formoterol dose and persists for approximately 12 hours. Oral formoterol has a slower onset of action than the inhaled formulations, but also produces prolonged bronchodilatory effects. Inhaled formoterol has shown a therapeutic efficacy equivalent to or better than comparable dosages of the conventional beta 2-agonists salbutamol, fenoterol and terbutaline in short and long term trials, in both adults and children with asthma. Its prolonged duration of action permits a twice-daily dosage regimen and results in improved control of nocturnal symptoms by reducing the 'morning dip'. Formoterol also compares well with oral slow release theophylline. In addition, significantly more patients with chronic obstructive airways disease (COAD) had an improvement in symptoms when treated with formoterol compared with salbutamol or fenoterol. Noncomparative studies indicate formoterol also provides effective prophylaxis of exercise-induced asthma. Development of tachyphylaxis has not been observed. Formoterol is generally well tolerated. Adverse effects observed represent predictable extensions of its pharmacology. Tremor and palpitations are most frequently reported. The incidence of adverse events is dose-proportional and therefore related to the route of administration, being more frequent following oral than inhalation therapy. The long-acting beta 2-agonists, including formoterol, represent a significant advance over current maintenance or prophylactic bronchodilator therapy with intermediate-acting beta 2-agonists such as salbutamol, fenoterol and terbutaline, predominantly because of the twice daily administration regimen. However, comparisons with other long-acting beta 2-agonists, such as salmeterol, evaluation of its role in improving symptom control in patients failing to respond to prophylactic therapy, and clarification of the optimal role of beta 2-agonists in asthma maintenance therapy are required to fully determine the value of formoterol in the management of obstructive airways disease.
福莫特罗是一种长效β2选择性肾上腺素能受体激动剂，在患有具有可逆成分的阻塞性气道疾病的患者中可产生剂量成正比的支气管扩张作用。吸入治疗剂量的福莫特罗后数分钟内即可产生显著效果，并持续约12小时。口服福莫特罗的起效时间比吸入制剂慢，但也能产生持久的支气管扩张作用。在成人和儿童哮喘患者的短期和长期试验中，吸入福莫特罗显示出与常规β2激动剂沙丁胺醇、非诺特罗和特布他林相当剂量的治疗效果相同或更好。其作用持续时间延长，允许每日两次给药方案，并通过减少“清晨低谷”改善对夜间症状的控制。福莫特罗与口服缓释茶碱相比也表现良好。此外，与沙丁胺醇或非诺特罗相比，慢性阻塞性气道疾病（COAD）患者使用福莫特罗治疗时症状改善的患者明显更多。非对照研究表明，福莫特罗还能有效预防运动诱发的哮喘。尚未观察到快速耐受性形成。福莫特罗一般耐受性良好。观察到的不良反应是其药理学作用可预测的延伸。震颤和心悸是最常报告的不良反应。不良事件的发生率与剂量成正比，因此与给药途径有关，口服治疗比吸入治疗更频繁。包括福莫特罗在内的长效β2激动剂比目前使用如沙丁胺醇、非诺特罗和特布他林等中效β2激动剂进行的维持或预防性支气管扩张治疗有显著进展，主要是因为每日两次给药方案。然而，需要与其他长效β2激动剂如沙美特罗进行比较，评估其在对预防性治疗无反应的患者中改善症状控制的作用，并阐明β2激动剂在哮喘维持治疗中的最佳作用，以充分确定福莫特罗在阻塞性气道疾病管理中的价值。
