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非布司他在高尿酸血症和慢性痛风治疗中的应用:综述。

Febuxostat in the management of hyperuricemia and chronic gout: a review.

机构信息

Division of Clinical Pharmacology, Department of Medicine and Therapeutics, The Chinese University of Hong Kong, Prince of Wales Hospital, Shatin, New Territories, Hong Kong SAR, China.

出版信息

Ther Clin Risk Manag. 2008 Dec;4(6):1209-20. doi: 10.2147/tcrm.s3310.

Abstract

Febuxostat is a novel, potent, non-purine selective xanthine oxidase inhibitor, which in clinical trials demonstrated superior ability to lower and maintain serum urate levels below 6 mg/dL compared with conventionally used doses of allopurinol. Febuxostat was well tolerated in long term treatment in patients with hyperuricemia including those experiencing hypersensitity/intolerance to allopurinol. Dose adjustment appears unnecessary in patients with mild to moderate renal or liver insufficiency or advanced age. The most common adverse reactions reported were abnormal liver function tests, headache, and gastrointestinal symptoms, which were usually mild and transient. However, whether hepatotoxicity becomes a limitation in the use of febuxostat needs to be determined in further studies. An increased frequency of gout flares occurs for a prolonged period after treatment initiation, as with any aggressive lowering of serum urate, and prolonged prophylaxis with colchicine or NSAIDs is usually required. Febuxostat has been granted marketing authorization by the European Commission in early 2008 for the treatment of chronic hyperuricemia and gout. Febuxostat is the first major treatment alternative for gout in more than 40 years and is a promising alternative to allopurinol, although continued long-term surveillance on safety and efficacy is required.

摘要

非布司他是一种新型、强效、非嘌呤类黄嘌呤氧化酶抑制剂,临床试验表明其降尿酸能力优于别嘌醇常规剂量,能更好地将血清尿酸水平维持在 6mg/dL 以下。在高尿酸血症患者的长期治疗中,非布司他耐受性良好,包括对别嘌醇过敏/不耐受的患者。对于轻至中度肾功能或肝功能不全或高龄患者,似乎无需调整剂量。报告的最常见不良反应是肝功能检查异常、头痛和胃肠道症状,通常为轻度和短暂的。然而,肝毒性是否会成为非布司他使用的限制,需要在进一步的研究中确定。与任何积极降低血清尿酸一样,起始治疗后会出现长时间的痛风发作频率增加,通常需要长期使用秋水仙碱或 NSAIDs 预防。2008 年初,欧盟委员会批准非布司他用于治疗慢性高尿酸血症和痛风。非布司他是 40 多年来治疗痛风的首个主要替代药物,是别嘌醇的一个有前途的替代药物,尽管需要持续进行长期的安全性和疗效监测。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/847c/2643102/ad957c238e5f/tcrm-4-1209f1.jpg

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