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萘丁美酮。对其在风湿性疾病中的药理学及治疗应用的重新评估。

Nabumetone. A reappraisal of its pharmacology and therapeutic use in rheumatic diseases.

作者信息

Friedel H A, Langtry H D, Buckley M M

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 1993 Jan;45(1):131-56. doi: 10.2165/00003495-199345010-00009.

Abstract

Nabumetone is a nonsteroidal anti-inflammatory drug (NSAID) used to treat rheumatic and inflammatory conditions. It is absorbed as a nonacidic prodrug and is rapidly converted in the liver to an active metabolite which is responsible for its anti-inflammatory and analgesic effects. Published data from earlier comparative studies indicate that nabumetone, administered in a single dose of 1 to 2g daily, is as effective as aspirin, diclofenac, ibuprofen, indomethacin, naproxen and sulindac for the symptomatic treatment of rheumatoid arthritis, osteoarthritis, various nonarticular rheumatic conditions and acute soft tissue injury. Adverse events with nabumetone occur less frequently than with aspirin, and the incidence of gastrointestinal adverse events with nabumetone compares favourably with that of other NSAIDs. Rates of gastrointestinal ulceration and bleeding with nabumetone are low, apparently less than 1% annually. More recently, data from large-scale clinical trials and postmarketing surveillance studies have further confirmed the efficacy and tolerability of nabumetone. Thus, the drug should now be considered a well established member of this group of agents for the treatment of painful rheumatic and inflammatory conditions.

摘要

萘丁美酮是一种用于治疗风湿性和炎症性疾病的非甾体抗炎药(NSAID)。它作为一种非酸性前药被吸收,并在肝脏中迅速转化为一种活性代谢物,该代谢物负责其抗炎和镇痛作用。早期比较研究发表的数据表明,萘丁美酮每日单剂量服用1至2克,在类风湿性关节炎、骨关节炎、各种非关节性风湿性疾病和急性软组织损伤的症状治疗方面,与阿司匹林、双氯芬酸、布洛芬、吲哚美辛、萘普生和舒林酸一样有效。萘丁美酮的不良事件发生频率低于阿司匹林,其胃肠道不良事件的发生率与其他NSAID相比具有优势。萘丁美酮引起胃肠道溃疡和出血的发生率较低,每年明显低于1%。最近,大规模临床试验和上市后监测研究的数据进一步证实了萘丁美酮的疗效和耐受性。因此,现在该药物应被视为这一类药物中用于治疗疼痛性风湿性和炎症性疾病的成熟药物。

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