Developing the ideal inhaled corticosteroid
Developing the ideal inhaled corticosteroid
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DOI：
10.1378/chest.130.1_suppl.54s
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发表时间：
2006-07-01
期刊：
影响因子：
9.6
通讯作者：
Cerasoli, Franklin, Jr.
中科院分区：
文献类型：
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作者：
Cerasoli, Franklin, Jr.
吸入性皮质类固醇（ICS）被认为是最有效的哮喘治疗方法，但副作用仍令人担忧。理想的ICS比目前可用的药物具有更大的治疗比率，允许增加剂量，但不会大大增加不良事件的频率或严重程度。理想的ICS将具有以下药代动力学特性以最大化功效并最小化副作用：高肺沉积、转化为活性代谢物、高受体效力、高肺保留、低口服生物利用度、广泛代谢和快速消除。新的ICS环索奈德已被证明具有许多这些特征。环索奈德也被证明可以改善肺功能，治疗潜在的炎症，作为持续性哮喘患者的单药治疗有效，与其他ICS相比副作用减少，并且易于每日一次给药。然而，与所有新产品一样，在临床试验中观察到的优势仍然需要证明在一般临床使用中长期有益。ICS治疗指数改善可能有可能增加患者依从性，加强ICS单药治疗在初级保健环境中的使用，并增加ICS单药治疗适用的患者范围。
Inhaled corticosteroids (ICS) are considered the most effective asthma therapy, but concerns remain about side effects. The ideal ICS would have a larger therapeutic ratio than currently available agents, allowing doses to be increased but without greatly increasing the frequency or severity of adverse events. The ideal ICS would possess the following pharmacokinetic properties to maximize efficacy and minimize side effects: high pulmonary deposition, conversion to an active metabolite, high receptor potency, high pulmonary retention, low oral bioavailability, extensive metabolism, and rapid elimination. The new ICS ciclesonide has been shown to possess many of these characteristics. Ciclesonide has also been shown to improve lung function, to treat the underlying inflammation, to be effective as monotherapy in patients with persistent asthma, to have reduced side effects compared with other ICS, and to be easy to use with once-daily dosing. However, as with all new products, the advantages witnessed in clinical trials still have to be demonstrated to be beneficial long-term in general clinical use. ICS with an improved therapeutic index may have the potential to increase patient adherence, enhance the use of ICS monotherapy in the primary care setting, and increase the range of patients for whom ICS monotherapy would be appropriate.