University of Medicine and Pharmacy, Pulmonary Disease Division, Pulmonary Disease University Hospital, Iasi, Romania.
Int J Chron Obstruct Pulmon Dis. 2011;6:147-55. doi: 10.2147/COPD.S7336. Epub 2011 Feb 17.
In chronic obstructive pulmonary disease (COPD) the inflammation occurring in the airways and in other lung tissues is complex and is orchestrated by various mediators including the isoenzyme 4 of the phosphodiesterases family (PDE4), which contributes to bronchoconstriction and inflammation. Various PDE4 inhibitors have been evaluated as potential therapies in asthma or COPD but among these only roflumilast have been authorized in Europe to be used in patients with severe COPD as an add-on to the bronchodilator therapy. This review discusses the existing preclinical and clinical data supporting the use of roflumilast for this therapeutic indication and tackles some of the pending issues related to PDE4 in general and to roflumilast in particular.
在慢性阻塞性肺疾病(COPD)中,气道和其他肺组织中发生的炎症复杂,由多种介质协调,包括磷酸二酯酶家族同工酶 4(PDE4),其导致支气管收缩和炎症。已经评估了各种 PDE4 抑制剂作为哮喘或 COPD 的潜在治疗方法,但其中只有罗氟司特在欧洲被授权用于严重 COPD 患者,作为支气管扩张剂治疗的附加药物。这篇综述讨论了支持将罗氟司特用于该治疗适应症的现有临床前和临床数据,并解决了与 PDE4 一般和罗氟司特具体相关的一些待解决问题。