Buttgereit F, Burmester G R, Simon L S
Department of Rheumatology and Clinical Immunology, Charité University Hospital, Humboldt University, (FB, GRB), Berlin, Germany.
Am J Med. 2001 Feb 19;110 Suppl 3A:13S-9S. doi: 10.1016/s0002-9343(00)00728-2.
Conventional nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used to treat pain and inflammation but are frequently associated with gastrointestinal side effects, including life-threatening bleeding or perforation of gastroduodenal ulcers. Conventional NSAIDs are nonselective inhibitors of two isoforms of cyclooxygenase (COX): COX-1 and COX-2. The inhibition of COX-1 is believed to be responsible for inducing mucosal injury primarily by impairing prostaglandin-dependent mucosal protective mechanisms. The latest development in reducing the incidence of ulcers and ulcer complications associated with conventional NSAIDs is the use of recently approved COX-2-specific inhibitors (CSIs). This article critically reviews the data on gastrointestinal toxic side effects for conventional NSAIDs without as well as with prevention therapy. In addition, we compare these data with those for the CSIs, namely, celecoxib and rofecoxib. Finally, we offer recommendations on the clinical use of these drugs, emphasizing the need to balance clinical effectiveness with the avoidance of potential gastrointestinal side effects.
传统非甾体抗炎药（NSAIDs）常用于治疗疼痛和炎症，但常伴有胃肠道副作用，包括危及生命的胃十二指肠溃疡出血或穿孔。传统NSAIDs是环氧化酶（COX）两种同工酶COX-1和COX-2的非选择性抑制剂。抑制COX-1被认为主要通过损害前列腺素依赖性黏膜保护机制而导致黏膜损伤。降低与传统NSAIDs相关的溃疡和溃疡并发症发生率的最新进展是使用最近获批的COX-2特异性抑制剂（CSIs）。本文批判性地回顾了有关传统NSAIDs在无预防治疗以及有预防治疗情况下胃肠道毒性副作用的数据。此外，我们将这些数据与CSIs（即塞来昔布和罗非昔布）的数据进行比较。最后，我们对这些药物的临床应用提出建议，强调在避免潜在胃肠道副作用的同时平衡临床疗效的必要性。
