比较药理学、生物利用度、药物动力学和药效学的吸入糖皮质激素。

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大M, Hochhaus G, Derendorf H

比较药理学、生物利用度、药物动力学和药效学的吸入糖皮质激素。

Immunol过敏中国北部。2005年8月,25 (3):469 - 88。doi: 10.1016 / j.iac.2005.05.004。

PubMed ID

16054538 (在PubMed

]

文摘

比较的药效学和药动学的吸入型皮质类固醇激素的评估是必要的。良好的知识这两个方面可以优化的有效性和安全性。当前可用的吸入糖皮质激素(PK / PD)已经显示一些所需的参数。当地的不利影响是减少一旦吸入皮质类固醇管理作为一个活动前药或显示一个好肺沉积。HFA-MDI二丙酸倍氯米松(BDP)和ciclesonide说明这两个代理。口服生物利用度低,快速系统性间隙和高血浆蛋白结合可以减少系统性不良反应。Mometasone糠酸盐、ciclesonide和丙酸具有这些特征。肺功效最大化是高肺沉积和长时间肺住所。这种效应可以通过缓慢溶解在肺部,丙酸或脂质结合一样,已被证明对布地奈德和ciclesonide。此外,肺沉积取决于吸入装置,颗粒大小,吸入技术。 Therefore,improvement in the design of MDIs, DPIs, and nebulizers, and the development of more effective drug particles will lead to an optimized pulmonary targeting. Much progress has been made in the treatment of asthma. The available inhaled corticosteroids show a high safety profile and a good pulmonary selectivity. Development of newer compounds showed that improvement is possible as the result of a complete understanding of the PK/PD concepts. However,the introduction of further improved formulations with a better efficacy/safety profile will be difficult and protracted because the existing drugs are already highly efficient.

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药物

Mometasone糠酸盐