痛风治疗新药——选择性尿酸重吸收抑制剂lesinurad
2016-11-09刘磊杨雪梁敏锐朱小霞张炯邹和建
刘磊+杨雪+梁敏锐+朱小霞+张炯+邹和建+薛愉
摘 要 痛风治疗药物又添新成员。lesinurad新近分别被美国和欧盟药政当局批准上市,用于治疗痛风相关的高尿酸血症。lesinurad是迄今第一个被批准上市的选择性尿酸重吸收抑制剂。长期、持续的血尿酸水平达标治疗是治愈痛风的关键。但是,很多患者使用1种降血尿酸药物并不能使自己的血尿酸水平降至目标值以下或长期控制于目标值以下。在这种情况下,就需联合用药治疗。lesinurad正适用于这些患者,与黄嘌呤氧化酶抑制剂合用可同时达到增加尿酸排泄和减少尿酸生成的作用。
关键词 痛风 高尿酸血症 选择性尿酸重吸收抑制剂 lesinurad
中图分类号:R971.1 文献标识码:A 文章编号:1006-1533(2016)19-0076-04
A new drug for gout — lesinurad, a selective uric acid reabsorption inhibitor*
LIU Lei, YANG Xue, LIANG Minrui, ZHU Xiaoxia, ZHANG Jiong, ZOU Hejian, XUE Yu**(Department of Rheumatology, Huashan Hospital; Institute of Rheumatology, Immunology and Allergy, Fudan University, Shanghai 200040, China)
ABSTRACT The US Food and Drug Administration and European Commission have recently approved lesinurad to treat gout-associated hyperuricemia in combination with a xanthine oxidase inhibitor (XOI). Lesinurad is the first selective uric acid reabsorption inhibitor. The long-term management of gout entails controlling hyperuricemia, which addresses the underlying pathology of the disease. Large amount of gout patients on urate-lowering therapy remain inadequate control of uric acid. For patients who can not reach the target on an XOI alone, adding an agent that can increase uric acid excretion is recommended. Lesinurad in combination with an XOI may help those reach the normal range and improve symptoms long-term.
KEY WORDS gout; hyperuricemia; selective uric acid reabsorption inhibitor; lesinurad
痛风性关节炎是由单钠尿酸盐晶体在受累关节及其周围软组织中沉积所诱发的急性炎症反应。高尿酸血症是痛风的前期疾病,血尿酸水平长期高于其饱和浓度(约为7 mg/dl)就易在关节及其周围软组织中析出并沉积尿酸盐,后者会在某些特定条件下形成单钠尿酸盐晶体,从而诱发炎症反应。有关研究显示,长期控制血尿酸水平<5 ~ 6 mg/dl可使沉积于关节内的尿酸盐重新溶解并逐步清除,最终达到彻底治愈痛风的目的。
降血尿酸药物原主要包括以下三类:①抑制尿酸生成药物,如黄嘌呤氧化酶抑制剂(xanthine oxidase inhibitor, XOI)别嘌醇、奥昔嘌醇、非布司他;②促尿酸排泄药物,如丙磺舒、苯溴马隆;③尿酸氧化酶类药物,如聚乙二醇化重组尿酸氧化酶。新近,降血尿酸药物又增添了一个新成员——口服选择性尿酸重吸收抑制剂lesinurad。……
