Washington University School of Medicine, The Clinical Research Center, LLC, 1040 N Mason Road, Suite 112, St Louis, Missouri 63141, USA.
Expert Opin Pharmacother. 2010 Feb;11(3):463-79. doi: 10.1517/14656560903575647.
Asthma is a chronic disease characterized by airway inflammation and hyper-responsiveness. Inhaled corticosteroids (ICSs) constitute the guideline-recommended first-line therapy for persistent asthma. However, concerns regarding ICS-related adverse events may contribute to their underutilization by physicians and patients.
The currently available published data on the pharmacokinetic and pharmacodynamic properties, safety and efficacy of the ICS, ciclesonide, is described. Peer-reviewed publications (1996 - 2009) on the pharmacodynamic and pharmacokinetic profile, safety and efficacy of ciclesonide were reviewed.
Ciclesonide is delivered as an inactive prodrug, which is cleaved to the active molecule by intracellular esterases located in the lungs. This and other pharmacodynamic and pharmacokinetic properties may limit the amount of active molecule outside the lung and may reduce the incidence of side effects. Randomized placebo-controlled studies found that ciclesonide can initiate and maintain disease control in subjects with persistent asthma of all disease severities. Moreover, studies have found that ciclesonide is as effective as other ICSs in establishing and controlling disease symptoms. Controlled clinical trials also showed that ciclesonide is associated with minimal systemic and local treatment-related adverse events.
Published findings indicate that ciclesonide is effective at initiating and maintaining asthma control and is well tolerated, with a positive safety profile.
哮喘是一种慢性疾病,其特征是气道炎症和高反应性。吸入皮质类固醇(ICS)构成了指南推荐的持续性哮喘的一线治疗。然而,由于对 ICS 相关不良反应的担忧,可能导致医生和患者对其的应用不足。
目前已发表的关于 ICS、环索奈德的药代动力学和药效学特性、安全性和疗效的可用数据。对环索奈德的药效学和药代动力学特征、安全性和疗效的同行评审出版物(1996-2009 年)进行了回顾。
环索奈德作为一种无活性的前药给药,在肺部的细胞内酯酶的作用下被裂解为活性分子。这种和其他药代动力学和药效学特性可能限制了肺外活性分子的数量,并可能减少副作用的发生。随机安慰剂对照研究发现,环索奈德可以在所有疾病严重程度的持续性哮喘患者中启动和维持疾病控制。此外,研究发现,环索奈德在建立和控制疾病症状方面与其他 ICS 一样有效。对照临床试验还表明,环索奈德与最小的全身和局部治疗相关不良事件相关。
已发表的研究结果表明,环索奈德在启动和维持哮喘控制方面是有效的,并且具有良好的耐受性,安全性良好。