North Shore University Hospital, NS-LIJ Health System, New York, NY, USA.
Ther Clin Risk Manag. 2011;7:351-8. doi: 10.2147/TCRM.S5433. Epub 2011 Aug 19.
Ciclesonide is a nonhalogenated synthetic inhaled corticosteroid (ICS) that has been approved by the US Food and Drug Administration for the treatment of all severities of persistent asthma. It is available as a hydrofluroalkane pressurized metered-dose inhaler in two strengths, 80 mcg/activation and 160 mcg/activation, with the recommenced dosage being two inhalations twice-daily. It is a prodrug that is converted in the lung to its active form, which possesses 100-fold greater glucocorticoid-receptor-binding affinity than the parent compound. Its relative receptor affinity is similar to budesonide. In clinical studies, ciclesonide was effective in improving pulmonary function, reducing asthma symptoms, and reducing or eliminating the need for oral corticosteroids (OCSs). Patients with severe asthma dependent on OCSs and high doses of ICSs were able to achieve greater asthma control and reduce or even eliminate the use of OCSs when switched to ciclesonide. In comparison with fluticasone propionate and budesonide, ciclesonide was demonstrated to be at least as effective in maintaining pulmonary function and asthma control. In clinical trials, ciclesonide was well tolerated, with the majority of adverse events considered mild or moderate in intensity. It had low systemic bioavailability and no clinically significant hypothalamic-pituitary-adrenal axis suppression at therapeutic doses. Its safety profile establishes ciclesonide as an important addition to the currently available ICSs.
环索奈德是一种非卤化合成吸入性皮质类固醇（ICS），已被美国食品和药物管理局批准用于治疗所有严重程度的持续性哮喘。它有两种规格的氢氟烷烃压力定量吸入器，分别为 80 mcg/次和 160 mcg/次，推荐剂量为每天两次，每次两吸。它是一种前药，在肺部转化为其活性形式，与母体化合物相比，其活性形式具有 100 倍更高的糖皮质激素受体结合亲和力。其相对受体亲和力与布地奈德相似。在临床研究中，环索奈德在改善肺功能、减轻哮喘症状和减少或消除口服皮质类固醇（OCS）的需求方面是有效的。依赖 OCS 和高剂量 ICS 的重度哮喘患者在改用环索奈德后，能够实现更好的哮喘控制并减少甚至消除 OCS 的使用。与丙酸氟替卡松和布地奈德相比，环索奈德在维持肺功能和哮喘控制方面至少同样有效。在临床试验中，环索奈德耐受性良好，大多数不良事件被认为是轻度或中度的。它具有较低的全身生物利用度，在治疗剂量下对下丘脑-垂体-肾上腺轴没有明显的抑制作用。其安全性特征使环索奈德成为目前可用的 ICS 的重要补充。
