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ARE ROFECOXIB AND CELECOXIB SAFER NSAIDS?

机译:罗非昔布和塞来昔布是否可以治疗NSAIDS?

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NSAIDs work by inhibiting the enzyme cyclo-oxygenase (COX), responsible for prostaglandin synthesis. This enzyme exists in two isoforms, COX-1 and COX-2. Inhibition of COX-1 is thought to be the main cause of the gastrointestinal unwanted effects of NSAIDs, whilst inhibition of COX-2 results in anti-inflammatory effects. Rofecoxib (Vioxx - MSD) and celecoxib (Celebrex - Searle) have been developed as selective inhibitors of COX-2. Rofecoxib is licensed for the symptomatic treatment of osteoarthritis, but not for rheumatoid arthritis. The manufacturer claims that "in clinical studies rofecoxib inhibits COX-2 but not COX-1", has "the power of high-dose NSAIDs — diclofenac and ibuprofen" and "superior GI safety profile compared to conventional NSAIDs". Celecoxib is licensed for symptom relief in osteoarthritis and rheumatoid arthritis. The manufacturer claims that celecoxib has "comparable efficacy and superior GI tolerability when compared to diclofenac or naproxen". Here, we review rofecoxib and celecoxib and consider whether they are safer than conventional NSAIDs.
机译:NSAID通过抑制负责前列腺素合成的环氧化酶(COX)起作用。该酶以两种同工型存在,即COX-1和COX-2。人们认为抑制COX-1是NSAIDs胃肠道不良作用的主要原因,而抑制COX-2会导致抗炎作用。罗非昔布(Vioxx-MSD)和塞来昔布(Celebrex-Searle)已被开发为COX-2的选择性抑制剂。罗非昔布被许可用于骨关节炎的对症治疗,但不适用于类风湿性关节炎。制造商声称“在临床研究中,罗非考昔抑制COX-2,但不抑制COX-1”,具有“大剂量NSAID的功效-双氯芬酸和布洛芬”和“与常规NSAID相比具有优越的GI安全性”。塞来昔布被许可用于骨关节炎和类风湿关节炎的症状缓解。制造商声称塞来昔布“与双氯芬酸或萘普生相比具有相同的功效和优异的胃肠道耐受性”。在这里,我们回顾罗非考昔和塞来昔布,并考虑它们是否比常规的NSAID安全。

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  • 来源
    《Drug and Therapeutics Bulletin》 |2000年第11期|p.81-86|共6页
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  • 收录信息 美国《化学文摘》(CA);
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 药学;
  • 关键词

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