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Roflumilast: a selective phosphodiesterase 4 inhibitor.

机译：罗氟司特：一种选择性磷酸二酯酶4抑制剂。

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摘要

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 shownto 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.
机译：罗氟司特是一种选择性磷酸二酯酶（PDE）4抑制剂，具有一系列的抗炎特性，并具有治疗炎性疾病的潜力。罗氟司特的治疗作用被认为是通过增加细胞3'，5'-环腺苷单磷酸（cAMP）的水平介导的，包括抑制微血管渗漏，抑制运输，从炎症细胞释放细胞因子和趋化因子以及支气管扩张。罗氟司特的抗炎和支气管扩张剂性质已导致临床研究，以研究罗氟司特对炎症性气道疾病（如哮喘和慢性阻塞性肺疾病）的影响。在哮喘中，罗氟司特每日口服一次500 ug已显示可改善临床症状和气道功能，减少运动引起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，罗氟司特以每日一次500 ug的口服剂量服用已显示出减少加重的频率，而对改善肺功能的影响很小。罗氟司特的副作用似乎是轻度且持续时间短。这种新型的选择性PDE4抑制剂可能会为炎性气道疾病患者提供治疗选择。

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