对乙酰氨基酚和水杨酸盐对阿司匹林诱导的人血小板环氧化酶抑制作用的影响。

Effect of acetaminophen and salicylate on aspirin-induced inhibition of human platelet cyclo-oxygenase.

作者信息

Rao G H, Reddy K R, White J G

出版信息

Prostaglandins Leukot Med. 1982 Jul;9(1):109-15. doi: 10.1016/0262-1746(82)90076-2.

Abstract

Recent studies have shown that salicylic acid, a metabolite of aspirin, effectively competes for the same site on the platelet cyclo-oxygenase enzyme. In the present investigation we have evaluated the effect of salicylate and acetaminophen on aspirin induced inhibition of cyclo-oxygenase and platelet function. Results of our studies show that both drugs at equimolar concentrations had no inhibitory effect on aspirin induced blockage of cyclo-oxygenase or platelet function. Even at higher concentrations acetaminophen failed to protect cyclo-oxygenase or prevent inhibition of platelet function by aspirin. Salicylate at concentrations above 5 mM effectively blocked the inhibition of cyclo-oxygenase activity and platelet aggregation in response to arachidonate.

摘要

近期研究表明，阿司匹林的代谢产物水杨酸可有效竞争血小板环氧化酶上的同一位点。在本研究中，我们评估了水杨酸盐和对乙酰氨基酚对阿司匹林诱导的环氧化酶抑制及血小板功能的影响。我们的研究结果显示，两种药物在等摩尔浓度下对阿司匹林诱导的环氧化酶阻断或血小板功能均无抑制作用。即使在更高浓度下，对乙酰氨基酚也无法保护环氧化酶或防止阿司匹林对血小板功能的抑制。浓度高于5 mM的水杨酸盐可有效阻断花生四烯酸诱导的环氧化酶活性抑制和血小板聚集。