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萘普生在人体内的代谢

Naproxen metabolism in man.

作者信息

Segre E J

出版信息

J Clin Pharmacol. 1975 Apr;15(4 Pt. 2):316-23. doi: 10.1002/j.1552-4604.1975.tb01458.x.

Abstract

In summary, naproxen is an acidic, highly albumin-bound drug. After oral administration, it is promptly and fully absorbed. The mean half-life of the drug in man is 13 hours, close to ideal for twice-daily administration. The only metabolite detected in man is the 6-desmethyl compound. Both it and naproxen itself are excreted in the urine, primarily as conjugates. The kinetics of naproxen binding to serum albumin tend to limit attainable plasma levels. They increase little if the dose is increased beyond 500 mg twice daily, since greater concentrations are rapidly cleared. Albumin binding and competitive displacement are also responsible for potential interactions of naproxen with drugs such as warfarin, sulfonylureas, and aspirin. Experience thus far does not indicate that any of the potential interactions are clinically meaningful.

摘要

总之,萘普生是一种酸性、与白蛋白高度结合的药物。口服后,它能迅速且完全被吸收。该药物在人体内的平均半衰期为13小时,非常适合每日服用两次。在人体中检测到的唯一代谢物是6 - 去甲基化合物。它和萘普生本身都通过尿液排泄,主要以结合物形式排出。萘普生与血清白蛋白结合的动力学往往会限制可达到的血浆水平。如果每日剂量超过500毫克两次,血浆水平增加很少,因为更高的浓度会迅速被清除。白蛋白结合和竞争性置换也是萘普生与华法林、磺酰脲类药物和阿司匹林等药物发生潜在相互作用的原因。迄今为止的经验表明,任何潜在的相互作用在临床上都没有意义。

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