Stefano Fiorucci, Distrutti Eleonora
Dipartimento di Medicina Clinica e Sperimentale, Policlinico Monteluce, Via E. dal Pozzo, 06100 Perugia, Italy.
Curr Top Med Chem. 2007;7(3):277-82. doi: 10.2174/156802607779941350.
Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used drugs but their use is hampered by gastrointestinal side effects. Cyclo-oxygenase Inhibitor Nitric Oxide Donors (CINODs) are a new class of anti-inflammatory and analgesic drugs generated by adding a nitric oxide generating moiety to the parent NSAID via an ester linkage. The combination of balanced inhibition of the two main COX isoforms with release of NO confers to CINODs a reduced gastrointestinal toxicity and a potent anti-inflammatory activity. It is suggested that the NO, which is released by the metabolism of nitrate as the compounds are broken down, may counteract the consequences of the NSAID-induced decrease in gastric mucosal prostaglandins. Recent clinical trials with CINODs (previously termed NO-NSAIDs) have provided data consistent with pre-clinical observations.
非甾体抗炎药(NSAIDs)是广泛使用的药物,但其使用受到胃肠道副作用的限制。环氧化酶抑制剂一氧化氮供体(CINODs)是一类新型抗炎和镇痛药,通过酯键将一氧化氮生成部分添加到母体NSAID上而产生。对两种主要COX同工型的平衡抑制与NO释放的结合赋予CINODs降低的胃肠道毒性和强大的抗炎活性。有人认为,随着化合物分解,硝酸盐代谢释放的NO可能抵消NSAID诱导的胃黏膜前列腺素减少的后果。最近关于CINODs(以前称为NO-NSAIDs)的临床试验提供的数据与临床前观察结果一致。