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[环氧化酶-2抑制剂非甾体抗炎药,神话还是现实?]

[COX-2 inhibitor non-steroidal anti-inflammatory drugs, myth or reality?].

作者信息

Peretz A

机构信息

Clinique de Rhumatologie, Département de Médecine Interne, C.H.U. Brugmann, U.L.B.

出版信息

Rev Med Brux. 2001 Sep;22(4):A377-80.

Abstract

The discovery of two isoforms of cyclooxygenase, Cox-1 constitutive and Cox-2 inducible, has prompted the development of new molecules with high Cox-2 selectivity. These new NSAIDs belong to the coxib class and have theoretically a better digestive tolerability than classical NSAID have. In Belgium, rofecoxib ((Vioxx) and celecoxib (Celebrex) are commercialized. Rofecoxib is indicated in the symptomatic treatment of osteoarthritis (12.5 to 25 mg/d) and celecoxib is indicated in osteoarthritis (200 mg/d) and in rheumatoid arthritis (200 to 400 mg/d). Several studies have demonstrated their efficacy, similarly to classical NSAID as diclofenac (Voltaren), naproxen (Naprosyne), ibuprofen (Brufen) and their superiority compared to placebo. Their safety profile for gastrointestinal events is proven in patients without ulcer history compared to classical NSAID. However, the concomitant use of aspirin decreases the benefit as demonstrated for celecoxib at 400 mg/d but not investigated for rofecoxib. The selective inhibition of Cox-2 with no effect on Cox-1 favors cardiovascular events in patients at risk. Other side effects are similar to classical NSAID. Thus Cox-2 inhibitors NSAID are interesting molecules for their sparing gastrointestinal activity. They must be used with caution in patients with ulcer history, in the elderly and in patients requiring aspirin for cardiovascular prophylaxis.

摘要

环氧化酶两种同工型(即组成型的Cox-1和诱导型的Cox-2)的发现,促使了具有高Cox-2选择性的新分子的研发。这些新型非甾体抗炎药属于昔布类,理论上比传统非甾体抗炎药具有更好的消化耐受性。在比利时,罗非昔布(万络)和塞来昔布(西乐葆)已上市。罗非昔布适用于骨关节炎的症状性治疗(12.5至25毫克/天),塞来昔布适用于骨关节炎(200毫克/天)和类风湿关节炎(200至400毫克/天)。多项研究已证明它们的疗效与双氯芬酸(扶他林)、萘普生(萘普生)、布洛芬(布洛芬)等传统非甾体抗炎药相似,且与安慰剂相比具有优势。与传统非甾体抗炎药相比,在无溃疡病史的患者中已证实它们在胃肠道事件方面的安全性。然而,阿司匹林的同时使用会降低获益,如400毫克/天的塞来昔布所示,但罗非昔布未进行此项研究。对Cox-2的选择性抑制而对Cox-1无影响,会使有风险的患者发生心血管事件。其他副作用与传统非甾体抗炎药相似。因此,Cox-2抑制剂类非甾体抗炎药因其对胃肠道的保护作用而成为有趣的分子。有溃疡病史的患者、老年人以及需要使用阿司匹林进行心血管预防的患者必须谨慎使用。

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