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柳氮磺吡啶(非乙酰化水杨酸酯)和阿司匹林对人体血清前列腺素的影响。

Effects of salsalate (nonacetylated salicylate) and aspirin on serum prostaglandins in humans.

作者信息

Morris H G, Sherman N A, McQuain C, Goldlust M B, Chang S F, Harrison L I

出版信息

Ther Drug Monit. 1985;7(4):435-8. doi: 10.1097/00007691-198512000-00012.

Abstract

Prostaglandin E2 (PGE2), thromboxane B2 (TXB2), and salicylic acid were measured in blood samples from 10 healthy men after administration of antiinflammatory doses of aspirin (3.9 g/day) or salsalate (3.0 g/day). Each medication was given for 3 days, followed by an observation period of 13 days. Plasma salicylate concentrations were slightly, but generally insignificantly, higher during aspirin dosing, although both drugs produced salicylic acid levels in the antiinflammatory range. Serum levels of PGE2 and TXB2, which reflected synthesis of cyclo-oxygenase products by platelets, were minimally affected by salsalate but profoundly suppressed by aspirin. When medication was discontinued, the effects of salsalate on serum PGE2 and TXB2 were readily reversible within 36 h, whereas the recovery from aspirin was still incomplete after 13 days of observation. These results indicate that the two orally administered salicylates have differential effects on prostaglandin synthesis in platelets and may also differ in their therapeutic and adverse effects.

摘要

对10名健康男性给予抗炎剂量的阿司匹林(3.9克/天)或双水杨酸酯(3.0克/天)后,检测其血液样本中的前列腺素E2(PGE2)、血栓素B2(TXB2)和水杨酸。每种药物给药3天,随后观察13天。在服用阿司匹林期间,血浆水杨酸浓度略高,但一般无显著差异,尽管两种药物产生的水杨酸水平均在抗炎范围内。反映血小板环氧化酶产物合成的血清PGE2和TXB2水平受双水杨酸酯影响极小,但被阿司匹林显著抑制。停药后,双水杨酸酯对血清PGE2和TXB2的影响在36小时内即可迅速逆转,而在观察13天后,阿司匹林的恢复仍不完全。这些结果表明,两种口服水杨酸盐对血小板中前列腺素合成的影响不同,其治疗作用和不良反应可能也有所不同。

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