Cazzola M, Donner C F
A. Cardarelli Hospital, Division of Pneumology and Allergology, Naples, Italy.
Drugs. 2000 Aug;60(2):307-20. doi: 10.2165/00003495-200060020-00005.
Long-acting beta2 agonist bronchodilators (e.g. formoterol, salmeterol) are a new interesting therapeutic option for patients with chronic obstructive pulmonary disease (COPD). In the short term, both salmeterol and formoterol appear to be more effective than short-acting beta2 agonists, and in patients with stable COPD they are more effective than anticholinergic agents and theophylline. Regular treatment of patients with COPD with long-acting beta2 agonists can induce an improvement in the respiratory function and certain aspects of quality of life. Moreover, salmeterol seems to be better than ipratropium and theophylline in improving lung function at the recommended doses after a long term treatment. Use of combination therapy of a long-acting inhaled beta2 agonist and an anticholinergic agent or theophylline in patients with COPD has not been sufficiently studied. Combination of usual doses of ipratropium or oxitropium with usual doses of salmeterol or formoterol does not appear to improve pulmonary function, but this lack of improvement with the combination should not, in itself, prevent implementation of further therapeutic steps in patients responsive to an anticholinergic agent and/or salmeterol or formoterol administered singly. Neither formoterol nor salmeterol elicit significant cardiovascular effects in healthy individuals and patients with reversible airway obstruction. However, adverse cardiac events might occur in patients with COPD with pre-existing cardiac arrhythmias and hypoxaemia if they use long-acting 12 agonists, although the recommended single dose of salmeterol 50 microg or formoterol 12 microg ensures a relatively higher safety margin than formoterol 24 microg. The bronchodilatory effect of long-acting beta2 agonists seems to be fairly stable after regular treatment with these bronchodilators. Moreover, pre-treatment with a conventional dose of formoterol or salmeterol does not preclude the possibility of inducing further bronchodilation with salbutamol in patients with partially reversible COPD. All these findings support the use of long-acting beta2 agonist bronchodilators as first-line bronchodilator therapy for the long term treatment of airflow obstruction in patients with COPD. However, since physicians must always choose a drug that is highly efficacious, well tolerated and inexpensive, the cost-effectiveness analysis in relation to other bronchodilators will determine the proper place of long-acting beta2 agonists in the long term therapy of stable COPD.
长效β2受体激动剂支气管扩张剂（如福莫特罗、沙美特罗）对于慢性阻塞性肺疾病（COPD）患者而言是一种新的、有趣的治疗选择。短期内，沙美特罗和福莫特罗似乎都比短效β2受体激动剂更有效，并且在稳定期COPD患者中，它们比抗胆碱能药物和茶碱更有效。使用长效β2受体激动剂对COPD患者进行常规治疗可改善呼吸功能和生活质量的某些方面。此外，长期治疗后，在推荐剂量下，沙美特罗在改善肺功能方面似乎优于异丙托溴铵和茶碱。对于COPD患者使用长效吸入β2受体激动剂与抗胆碱能药物或茶碱的联合治疗尚未进行充分研究。异丙托溴铵或氧托溴铵的常用剂量与沙美特罗或福莫特罗的常用剂量联合使用似乎并不能改善肺功能，但联合使用时缺乏改善本身不应妨碍对单独使用抗胆碱能药物和/或沙美特罗或福莫特罗有反应的患者采取进一步的治疗措施。福莫特罗和沙美特罗在健康个体和可逆性气道阻塞患者中均不会引起显著的心血管效应。然而，患有COPD且已有心律失常和低氧血症的患者如果使用长效β2受体激动剂，可能会发生不良心脏事件，尽管推荐的沙美特罗单剂量50微克或福莫特罗12微克比福莫特罗24微克确保了相对更高的安全边际。在用这些支气管扩张剂进行常规治疗后，长效β2受体激动剂的支气管扩张作用似乎相当稳定。此外，对于部分可逆性COPD患者，用常规剂量的福莫特罗或沙美特罗进行预处理并不排除用沙丁胺醇进一步诱导支气管扩张的可能性。所有这些发现都支持将长效β2受体激动剂支气管扩张剂作为COPD患者气流阻塞长期治疗的一线支气管扩张剂疗法。然而，由于医生必须始终选择一种高效、耐受性好且价格低廉的药物，因此与其他支气管扩张剂相关的成本效益分析将决定长效β2受体激动剂在稳定期COPD长期治疗中的合适地位。
