非甾体类抗炎药物的研究进展

PROGRESS IN THE STUDY OF NON STEROIDAL ANTI IMFLAMMATORY DRUGS

阿司匹林类的非甾体类抗炎药是治疗关节炎和风湿病的主要药物，其作用机制系通过抑制环氧化酶（ Ｃ Ｏ Ｘ） 而减少前列腺素合成。已发现 Ｃ Ｏ Ｘ１ 和 Ｃ Ｏ Ｘ２ 为同功酶，并认为抗炎药物对 Ｃ Ｏ Ｘ１ 的抑制与产生不良反应有关，而对 Ｃ Ｏ Ｘ２ 的抑制则带来治疗效果。因此，国外已研制出新的选择性 Ｃ Ｏ Ｘ２ 抑制剂。

Aspirin and other NSAIDs have been the main agents for treatment of pain and inflammation associated with arthritis and rheumatism. Sir John Vane suggested that these agents exerted their effects by inhibition of cyclooxygenase(COX) and resulted in reducing prostaglandins production. Following the discovery of twoisoenzymes of COX in 1991, COX 1 and COX 2,it is now believed that the GI and renal side effects of NSAIDs are induced by COX 1 inhibition ,whilst theirtherapeutic effects are produced by COX 2 inhibition. Now some highly selective COX 2 inhibitors have been marketed but whether their GI side effects were improved need to be confirmed.