非甾体抗炎药(NSAIDs)是目前最广泛的处方药之一,胃肠道(GI)的毒性仍然是NSAIDs类药物最大的问题。其中,选择性COX-2抑制剂的发展是由于选择性抑制COX-2可能会减少胃肠道副作用。然而,由于长期使用非甾体抗炎药可能导致副作用,目前对于选择性COX-2抑制剂的研发热情已经减少。近年来,出现了一些新的方法来开发适合胃肠道的NSAIDs,并且取得了一些非常有前景的结果。发表于2015年3月的《药物研究综述》(Medicinal Research Reviews)杂志的一篇文章,对过去的二十年中开发非甾体抗炎药的方法和策略进行了综述,同时对目前设计和开发更安全的非甾体类抗炎药的方法进行了总结。
参考文献:Suthar, SK et al. Medicinal Research Reviews 2015;35(2):341–407.
英文链接:Recent Developments in Chimeric NSAIDs as Safer Anti-Inflammatory Agents.
http://onlinelibrary.wiley.com/doi/10.1002/med.21331/full
Recent Developments in Chimeric NSAIDs as Safer Anti-Inflammatory Agents
原文摘要:
NSAIDs are among the most widely prescribed medications across the world, but the gastrointestinal (GI) toxicity still remains the biggest problem and the challenge for current NSAIDs-based therapeutics. The development of selective COX-2 inhibitors was driven by the assumption that selective inhibition of COX-2 would reduce the GI side effects. However, the initial enthusiasm for selective COX-2 inhibitors has faded away due to the emergence of serious side effects associated with the long-term use of these NSAIDs. In the recent years, a number of novel approaches to develop gastrosparing NSAIDs have been explored with the promising results. This review deals with such approaches and strategies that have been employed in the last two decades and are being used currently in the design and development of safer NSAIDs.