COX-2 inhibitors
COX-2 inhibitors
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DOI：
10.1016/s0140-6736(98)12154-2
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发表时间：
1999-01-23
期刊：
影响因子：
168.9
通讯作者：
Hawkey, CJ
中科院分区：
文献类型：
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作者：
Hawkey, CJ
在过去的100年里，阿司匹林已经证明了它作为止痛剂、抗炎剂和抗血栓剂的价值。然而，到了1938年，阿司匹林显然具有胃毒性。自20世纪60年代以来开发的非甾体抗炎药（NSAIDs）未能实现“更安全的阿司匹林”的目标。通过环加氧酶（COX）抑制前列腺素合成是阿司匹林和非阿司匹林类非甾体抗炎药治疗和毒性作用的核心，这一证明似乎确立了无痛无获的原则。这种联系可能被选择性抑制诱导型COX-2酶的药物所破坏。COX酶现在是对抗炎症过程的药物干预的目标。“安全的阿司匹林”终于出现了吗？
In the past 100 years aspirin has demonstrated its value as an analgesic, anti-inflammatory, and antithrombotic agent. However, by 1938, it was clear that aspirin was gastrotoxic. Non-steroidal anti-inflammatory drugs (NSAIDs), developed since the 1960s, failed to achieve the goal of "a safer aspirin". The demonstration that inhibition of prostaglandin synthesis via a cyclo-oxygenase (COX) enzyme was central to both the therapeutic and toxic effects of aspirin and non-aspirin NSAIDs appeared to establish the principle of no gain without pain. This link may have been broken by drugs that selectively inhibit the inducible COX-2 enzyme. The COX enzyme is now a target of drug interventions against the inflammatory process. Might the "safe aspirin" be here at last?