磷酸二酯酶抑制药——罗氟司特在慢性阻塞性肺疾病治疗中的应用

Application of phosphodiesterase inhibitor—roflumilast in chronic obstructive pulmonary disease

炎症是慢性阻塞性肺疾病(COPD)发病机制的核心,抗炎治疗在COPD管理中具有重要地位。磷酸二酯酶4(PDE4)表达于炎症细胞和平滑肌细胞,是抗炎治疗的靶目标。PDE4抑制药能有效拮抗气道炎症,但早期的PDE4抑制药效能低、不良反应多,致使应用受限。新上市的选择性PDE4抑制药——罗氟司特与PDE4有更强的亲和力,能够改善肺功能,减少COPD急性加重,且不良反应轻微,已被2010年COPD防治全球创议推荐用于重度COPD患者的治疗。

Inflammation is the central mechanism of chronic obstructive pulmonary disease （COPD）.Anti-inflammaory treatment plays an important role in COPD management. Phosphodiesterase 4 （PDE4） was identified as a therapeutic target for anti-inflammatory agents many years ago, since it is expressed in many inflammatory cells and smooth muscle cells. The application of early PDE4 inhibitors were limited by low potency and hampered by its serious adverse reactions. Current PDE4 inhibitors such as roflumilast have fewer adverse reactions and greater affinity for PDE4, and can improve the lung function, reduce exacerbation rates, make a wide application prospect. GOLD 2010 guideline had recommended its use in the treatment of severe COPD patients.