Christie Pandora
Division of Allergy, University of Washington, Seattle, Washington 98104, USA.
Drugs Today (Barc). 2005 Oct;41(10):667-75. doi: 10.1358/dot.2005.41.10.920428.
Roflumilast is a selective phosphodiesterase (PDE) 4 inhibitor with a range of anti-inflammatory properties and potential for treatment of inflammatory disease. The therapeutic effects of roflumilast are thought to be mediated via increased levels of cellular 3',5'-cyclic adenosine monophosphate (cAMP) and include inhibition of microvascular leakage, inhibition of trafficking, release of cytokines and chemokines from inflammatory cells, and bronchodilation. The anti-inflammatory and bronchodilator properties of roflumilast have resulted in clinical studies to investigate the effects of roflumilast in inflammatory airway diseases such as asthma and chronic obstructive pulmonary disease. In asthma, roflumilast taken as a once-daily oral dose of 500 ug has been shown to improve clinical symptoms and airway function, reduce exercise-induced asthma and decrease bronchial airway hyperresponsiveness. In chronic obstructive pulmonary disease, roflumilast taken as a once-daily oral dose of 500 ug has been shown to reduce the frequency of exacerbations with small effects on improving lung function. Side effects of roflumilast appear to be mild and short lasting. It is likely that this new class of selective PDE4 inhibitor may provide a therapeutic option for patients with inflammatory airway disease.
罗氟司特是一种具有多种抗炎特性且有治疗炎症性疾病潜力的选择性磷酸二酯酶（PDE）4抑制剂。罗氟司特的治疗作用被认为是通过提高细胞内环磷腺苷（cAMP）水平来介导的，包括抑制微血管渗漏、抑制炎性细胞的转运、炎性细胞因子和趋化因子的释放以及支气管扩张。罗氟司特的抗炎和支气管扩张特性已促使开展临床研究，以探究罗氟司特在哮喘和慢性阻塞性肺疾病等炎性气道疾病中的作用。在哮喘中，每日口服一次500微克的罗氟司特已被证明可改善临床症状和气道功能、减轻运动诱发的哮喘并降低支气管气道高反应性。在慢性阻塞性肺疾病中，每日口服一次500微克的罗氟司特已被证明可减少病情加重的频率，对改善肺功能的作用较小。罗氟司特的副作用似乎较轻且持续时间较短。这类新型选择性PDE4抑制剂很可能可为炎性气道疾病患者提供一种治疗选择。
