Beeh K-M, Welte T, Buhl R
Schwerpunkt Pneumologie, III. Medizinische Klinik und Poliklinik, Klinikum der Johannes Gutenberg-Universität, Mainz, Germany.
Pneumologie. 2003 Sep;57(9):519-25. doi: 10.1055/s-2003-42216.
Anticholinergics are agents of first choice for the symptomatic treatment of patients with COPD. Tiotropium (Ba 679 BR, Spiriva) is a long-acting inhaled anticholinergic designed for once-daily bronchodilator treatment of COPD. Tiotropium is a selective antagonist of pulmonary M1 and M3 muscarinic receptor subtypes, that produces a long-lasting (24 hours), dose-dependent bronchodilation and bronchoprotection against constrictive stimuli, e. g. methacholine, following inhalation of single doses. Clinical trials with tiotropium in COPD patients over a maximum treatment duration of one year have confirmed a persisting bronchodilator effect of tiotropium compared with placebo and ipratropium, as well as meaningful clinical improvements in lung function, hyperinflation, exercise tolerance, symptom control and quality of life. Moreover, recent trials indicate that treatment with tiotropium also reduces the frequency of COPD exacerbations and hospitalizations. Comparative trials further suggest that the bronchodilator potency of tiotropium may be superior to those of available COPD treatments. Besides a higher incidence of dry mouth, the side effect profile was comparable to ipratropium bromide. In conclusion, present clinical data suggest that tiotropium has the potential of a first-line treatment for patients with COPD.
抗胆碱能药物是慢性阻塞性肺疾病(COPD)患者症状治疗的首选药物。噻托溴铵(Ba 679 BR,思力华)是一种长效吸入性抗胆碱能药物,设计用于COPD患者的每日一次支气管扩张治疗。噻托溴铵是肺部M1和M3毒蕈碱受体亚型的选择性拮抗剂,单次吸入后可产生持久(24小时)、剂量依赖性的支气管扩张作用,并对诸如乙酰甲胆碱等收缩性刺激具有支气管保护作用。在COPD患者中进行的最长治疗时间为一年的噻托溴铵临床试验证实,与安慰剂和异丙托溴铵相比,噻托溴铵具有持续的支气管扩张作用,并且在肺功能、肺过度充气、运动耐量、症状控制和生活质量方面有显著的临床改善。此外,最近的试验表明,噻托溴铵治疗还可降低COPD急性加重和住院的频率。比较试验进一步表明,噻托溴铵的支气管扩张效力可能优于现有的COPD治疗药物。除口干发生率较高外,其副作用与异丙托溴铵相当。总之目前的临床数据表明,噻托溴铵有潜力成为COPD患者的一线治疗药物。