吸入糖皮质激素的比较药理学、生物利用度、药代动力学和药效学。
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胡伯纳，何赫豪斯，胡德伦夫
吸入糖皮质激素的比较药理学、生物利用度、药代动力学和药效学。
免疫过敏临床。2005年8月;25(3):469-88。doi: 10.1016 / j.iac.2005.05.004。
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16054538 (PubMed视图］
- 摘要
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吸入糖皮质激素的药效学和药代动力学的比较是必要的评估。充分了解这两个方面可以优化疗效和安全性。目前可用的吸入糖皮质激素已经显示出一些所需的PK/PD参数。一旦吸入皮质类固醇作为非活性前药施用或表现出更好的肺沉积，局部不良反应就会减少。HFA-MDI二丙酸倍氯米松(BDP)和环奈德就是说明这一点的两种药物。低口服生物利用度、快速全身清除和高血浆蛋白结合可以最大限度地减少全身不良反应。糠酸莫米松、环奈德和丙酸氟替卡松具有这些特征。高肺沉积和长肺停留时间使肺疗效最大化。如丙酸氟替卡松或脂质偶联，可通过在肺部缓慢溶解来达到这一效果，布地奈德和环索奈德的情况也已证明。此外，肺沉积取决于吸入装置、颗粒大小和吸入技术。 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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