A General Pharmacological properties D 5. COX-1/C0X-2 and selectivity of the drugs u COX-1: constructive; involved in physiologic regulatory functions in GI tract, kidney, etc. i 0 inhibition of cox-i is related to the adverse effects I COX-2: inducible; involved in pathological responses such as inflammation, and pregnancy; D inhibition of COX-2 is related to the therapeutic effects
5. COX-1 / COX-2 and selectivity of the drugs COX-1: constructive; involved in physiologic regulatory functions in GI tract, kidney, etc.; inhibition of COX-1 is related to the adverse effects. COX-2: inducible; involved in pathological responses such as inflammation, and pregnancy; inhibition of COX-2 is related to the therapeutic effects. A. General Pharmacological properties
膜磷脂 皮质 PLA2 激素 IT下[0x上[花生四烯酸(+炎性刺激 生理刺激}cox1ox2 非甾体 (+) 抗炎药 中间体 PGE2 PGI2 炎症介质 TXA2
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表2010Ox1和COX2的特性比较 C0X-1 COX-2 生成 固有的 需经诱导 功能 生理学 生理学:妊娠时PG生成增加 保护捍肠 病理学;生成蛋白酶PG及其他致炎介 调节血小板聚集(TXA2) 质引起炎症 调节外周血管阻力(PGI2) 调节肾血流量分布(PCⅠ、PGE) 抑制剂 选择性哚美辛阿司匹林吡罗昔康美洛昔康尼美舒利、萘丁美酮 非选择性 萘普生、布洛芬、双氯芬酸钠