Suleyman H, Cadirci E, Albayrak A, Halici Z
Ataturk University, Faculty of Medicine, Department of Pharmacology, 25240 Erzurum, Turkey.
Curr Med Chem. 2008;15(3):278-83. doi: 10.2174/092986708783497247.
In this review it is shown that nimesulide, a selective cyclooxigenase-2 (COX-2) inhibitor, is different from other selective COX-2 inhibitors and classical non-steroidal anti-inflammatory drugs (NSAIDs). The anti-inflammatory effect mechanism of nimesulide (inhibition of inflammatory mediators) is similar to other classic NSAIDs, but the protective effect of nimesulide on classic NSAID-induced ulcers elucidates the difference between nimesulide and these other drugs. It is known that the selective COX-2 inhibitor nimesulide prevents NSAID-induced ulcers, while celecoxib and rofecoxib, which are more selective to COX-2, failed to prevent these ulcers. Nimesulide produces gastro-protective effects via a completely different mechanism. In addition, while selective COX-2 inhibitors increase the risk for cardiovascular diseases, nimesulide does not exert significant cardiotoxicity. This data suggests that gastrointestinal side effects of classic NSAIDs cannot be related to the COX-1 inhibition alone and also suggest that nimesulide is an atypical NSAID, which is different from both non-selective and selective COX-2 inhibitors.
本综述表明，尼美舒利作为一种选择性环氧化酶-2（COX-2）抑制剂，不同于其他选择性COX-2抑制剂和传统非甾体抗炎药（NSAIDs）。尼美舒利的抗炎作用机制（抑制炎症介质）与其他传统NSAIDs相似，但尼美舒利对传统NSAIDs诱导的溃疡的保护作用阐明了其与其他药物的差异。已知选择性COX-2抑制剂尼美舒利可预防NSAIDs诱导的溃疡，而对COX-2选择性更高的塞来昔布和罗非昔布则未能预防这些溃疡。尼美舒利通过完全不同的机制产生胃保护作用。此外，虽然选择性COX-2抑制剂会增加心血管疾病风险，但尼美舒利不会产生显著的心脏毒性。这些数据表明，传统NSAIDs的胃肠道副作用不能仅归因于COX-1抑制，也表明尼美舒利是一种非典型NSAID，不同于非选择性和选择性COX-Ⅱ抑制剂。
