Nandakishore Ravindran, Yalavarthi Prasanna R, Kiran Yengala R, Rajapranathi Malepati
Department of Pharmaceutics, Sree Vidyanikethan College of Pharmacy, Andhra Pradesh 517102, India.
Curr Drug Discov Technol. 2014 Jun;11(2):127-32. doi: 10.2174/1570163811666140127123717.
For ages aspirin has established its value as an analgesic, anti-inflammatory drug, but in 1938, it was found to be a causative factor of gastric inflammation (ulcer). Later discovered non-steroidal anti-inflammatory drugs (NSAIDs) were found effective as aspirin but failed to overcome the goal of safer aspirin. As the method of prostaglandin inhibition through COX is a common mechanism to both the wanted and unwanted effects of aspirin and non-aspirin NSAIDs, the COX enzyme becomes a target for drug designers for the development of the "safe aspirin". In the late 1990s, a new class of drug molecules collectively known as selective inhibitors of cyclooxygenase-2(Coxibs) was developed for the treatment of pain and inflammation. Coxibs developed were as efficacious as the common NSAIDs, but they are devoid of major side effect, the gastrointestinal bleeding. This review presents an overview on all the discovered COX-2 inhibitors, their physiological role, side effects and reasons of their withdrawal.
长期以来，阿司匹林已确立其作为镇痛药和抗炎药的价值，但在1938年，它被发现是胃炎症（溃疡）的一个致病因素。后来发现的非甾体抗炎药（NSAIDs）与阿司匹林一样有效，但未能实现比阿司匹林更安全的目标。由于通过COX抑制前列腺素的方法是阿司匹林和非阿司匹林NSAIDs的有益和有害作用的共同机制，COX酶成为药物设计师开发“安全阿司匹林”的靶点。在20世纪90年代后期，开发了一类新的药物分子，统称为环氧化酶-2（Coxibs）选择性抑制剂，用于治疗疼痛和炎症。所开发的Coxibs与普通NSAIDs一样有效，但它们没有主要副作用，即胃肠道出血。本综述概述了所有已发现的COX-2抑制剂、它们的生理作用、副作用以及它们被撤市的原因。
