吸入噻托溴铵治疗哮喘的药理学原理。

Q4 Medicine
Pneumologia Pub Date : 2015-01-01
Florin-Dan Popescu
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引用次数: 0

摘要

噻托溴铵是一种吸入性长效抗胆碱能药,具有较高的M3受体亚型(M3R)结合亲和力,M3R半衰期极长,功能选择性强。分子机制解释了与毒蕈碱受体的结合,作用持续时间长,动力学选择性及其作为逆激动剂的作用。噻托溴铵抑制气道平滑肌M3Rs导致支气管扩张。毒蕈碱调节气道平滑肌张力的细胞内信号转导途径是复杂的。将这种吸入抗胆碱能药物与β -2激动剂联合使用有许多分子药理学原因,并描述了噻托溴铵潜在的非支气管扩张剂作用。Respimat SoftMist吸入器(SMI)是一种无推进剂的口服吸入装置,基于单块喷嘴系统,碰撞液体射流,产生非常精细,缓慢移动,持久的液体气溶胶。这种独特的SMI被批准用于治疗控制不良的哮喘患者噻托溴铵。讨论了许多药物技术和药物教育的优势,并提到了哮喘患者有利的成本效益方面。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
The pharmacological rationale for the use of inhaled tiotropium in asthma.

Tiotropium is an inhaled long-acting anticholinergic, with high M3 receptor subtype (M3R) binding affinity, exceedingly half-life at M3R, and functional selectivity. Molecular mechanisms explain binding to muscarinic receptors, long duration of action, kinetic selectivity, and its role as inverse agonist. Tiotropium inhibit airway smooth muscle M3Rs leading to bronchodilation. The intracellular signal transduction pathways for the muscarinic regulation of airway smooth muscle tone are complex. There are many molecular pharmacological reasons for combining this inhaled anticholinergic with beta-2-agonists, and potential non-bronchodilator actions of tiotropium were described. The Respimat SoftMist Inhaler (SMI) is a propellant-free, oral inhalation device, based on an uniblock nozzle system with colliding liquid jets, generating a very fine, slow-moving, long-lasting liquid aerosol. This unique SMI is approved to administer tiotropium bromide in poorly controlled asthma patients. Many pharmacotechnological and pharmacoeducational advantages are discussed, and favourable cost-effectiveness aspects in patients with asthma are mentioned.

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来源期刊
Pneumologia
Pneumologia Medicine-Pulmonary and Respiratory Medicine
CiteScore
0.20
自引率
0.00%
发文量
10
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