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噻托溴铵:最新进展

Tiotropium bromide: an update.

作者信息

Heredia Josep Lluis

机构信息

S. Pneumologia, Hospital Mutua de Terrassa, c/ Dr. Robert 5, 08221 Terrassa, Barcelona, Spain.

出版信息

Open Respir Med J. 2009 Apr 14;3:43-52. doi: 10.2174/1874306400903010043.

Abstract

Tiotropium bromide is a once-daily inhaled anticholinergic bronchodilator. It works by blocking the muscarinic receptors in airway smooth muscle. Tiotropium has a wide therapeutic margin, due to its poor gastrointestinal absorption and its very low systemic bioavailability. The drug is mainly indicated in COPD patients. Clinically relevant outcomes such as significant improvements in spirometry, hyperinflation, dyspnea, heath status, acute exacerbations and mortality have been consistently observed in tiotropium clinical trials, and the drug has been shown to reduce the risk of mortality due to cardiac-vascular disease and respiratory failure. The main side effect reported is dryness of the mouth. Some subgroups of asthmatics also seem to respond to anticholinergic drugs: among them, those with the Arg/Arg genotype for the beta2-adrenergic receptor and those with a high percentage of neutrophils in sputum.

摘要

噻托溴铵是一种每日一次吸入的抗胆碱能支气管扩张剂。它通过阻断气道平滑肌中的毒蕈碱受体发挥作用。由于其胃肠道吸收差且全身生物利用度极低,噻托溴铵具有广泛的治疗窗。该药物主要用于慢性阻塞性肺疾病(COPD)患者。在噻托溴铵的临床试验中,一直观察到诸如肺功能测定、肺过度充气、呼吸困难、健康状况、急性加重和死亡率等临床相关结局有显著改善,并且该药物已被证明可降低心血管疾病和呼吸衰竭导致的死亡风险。报告的主要副作用是口干。一些哮喘患者亚组似乎也对抗胆碱能药物有反应:其中包括β2肾上腺素能受体具有Arg/Arg基因型的患者以及痰液中嗜中性粒细胞百分比高的患者。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b023/2684714/7a175d59c076/TORMJ-3-43_F1.jpg

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