司来帕格在肺动脉高压治疗中的应用  

Application of selexipag in the treatment of pulmonary hypertension

作　　者：王志伟[1] 韩宇 程江涛 WANG Zhiwei;HAN Yu;CHENG Jiangtao(Dept.of Cardiology,Henan University People’s Hospital/Henan Provincial People’s Hospital,Zhengzhou 450003,China;Dept.of Cardiology,Fuwai Central China Cardiovascular Hospital,Zhengzhou 451464,China)

机构地区：[1]河南大学人民医院/河南省人民医院心内科,郑州450003 [2]阜外华中心血管病医院心内科,郑州451464

出　　处：《中国药房》2022年第16期2040-2043,2048,共5页China Pharmacy

基　　金：国家自然科学基金资助项目(No.81800287)。

摘　　要：司来帕格是一种口服的高选择性前列环素受体激动剂,具有抑制肺动脉平滑肌细胞收缩、增殖的作用。因其具有患者依从性好、受体亲和力高等优点,目前在肺动脉高压(PH)治疗中应用广泛。本文对司来帕格在PH治疗中的作用机制、药动学/药效学、临床应用等方面进行了综述。结果表明,司来帕格单独使用或与内皮素受体拮抗剂和(或)磷酸二酯酶抑制剂联合使用治疗世界卫生组织(WHO)心功能Ⅱ~Ⅲ级成人动脉性肺动脉高压(PAH)患者,均可降低恶化/死亡事件风险、延缓疾病进展、改善患者PAH危险分层。但其在儿童PAH、慢性血栓栓塞性PH等患者中的应用仍需进一步探索。Selexipag is a kind of oral highly selective prostacyclin(IP)receptor agonist,which can inhibit the contraction and proliferation of pulmonary artery smooth muscle cells.Because of its good patient compliance and high receptor affinity,it is currently used in the treatment of pulmonary hypertension(PH).This article reviews the mechanism of action,pharmacokinetics/pharmacodynamics and application of selexipag in the treatment of PH.The results show that selexipag alone or in combination with endothelin receptor antagonists and(or)phosphodiesterase inhibitors can effectively reduce the risk of worsening/death events,delay disease progression,and improve patients’life quality in patients with adult pulmonary arterial hypertension(PAH)of WHO cardiac functionⅡ-Ⅲgrade.However,its application in children with PAH and patients with chronic thromboembolic PH needs further exploration.

关 键 词：司来帕格 肺动脉高压 前列环素受体激动剂 

分 类 号：R972.4[医药卫生—药品]