Skelly M M, Hawkey C J
Division of Gastroenterology, University Hospital, Queen's Medical Centre, Nottingham NG7 2UH, UK.
Int J Clin Pract. 2003 May;57(4):301-4.
Safe and effective drug treatment is an important objective of all doctors. In the treatment of arthritis, non-steroidal anti-inflammatory drugs offer effective treatment but safety is significantly limited, largely due to gastrointestinal toxicity. Attention has recently focused on exploiting increased knowledge of metabolism of arachidonic acid to allow the development of safer anti-inflammatory drugs. Dual inhibitors of cyclo-oxygenase and lipoxygenase are planned. These drugs may inhibit formation of both prostaglandins and leukotrienes. This review outlines the salient features of cyclo-oxygenase and lipoxygenase metabolism of arachidonic acid. The role of the eicosanoids in mediating inflammation and gastrointestinal integrity is delineated. Evidence is presented regarding action of licofelone, one COX/LOX inhibitor that is currently in advanced stages of clinical trials. This review examines the hypothesis that licofelone is an effective anti-inflammatory agent that does not cause peptic damage.
安全有效的药物治疗是所有医生的重要目标。在关节炎治疗中,非甾体抗炎药能提供有效的治疗,但安全性受到显著限制,这主要是由于胃肠道毒性。最近,人们的注意力集中在利用对花生四烯酸代谢的更多了解来开发更安全的抗炎药物。环氧化酶和脂氧合酶的双重抑制剂正在研发中。这些药物可能会抑制前列腺素和白三烯的形成。这篇综述概述了花生四烯酸的环氧化酶和脂氧合酶代谢的显著特征。阐述了类花生酸在介导炎症和胃肠道完整性方面的作用。文中提供了有关利考昔(一种目前正处于临床试验后期的COX/LOX抑制剂)作用的证据。这篇综述探讨了利考昔是一种不会导致消化性损伤的有效抗炎剂这一假说。