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血浆半衰期长短不同的受试者中苯妥英的代谢

Phenytoin metabolism in subjects with long and short plasma half-lives.

作者信息

Glazko A J, Peterson F E, Chang T, Dill W A, Smith T C, Buchanan R A

出版信息

Ther Drug Monit. 1982;4(3):281-92. doi: 10.1097/00007691-198208000-00006.

DOI:10.1097/00007691-198208000-00006
PMID:7135458
Abstract

Normal adult men with long and short phenytoin plasma half-lives were given 300-mg oral doses of phenytoin once daily for 15 days. Plasma levels of phenytoin (DPH) and its major metabolite (p-HPPH) were measured during the period of drug administration and for 5 days thereafter. Average steady-state plasma levels of DPH rose to 13.4 micrograms/ml in the long half-life group, compared with 3.6 micrograms/ml in the short half-life group. HPPH levels in the long half-life group were about one half of those observed in the short half-life group. The DPH/HPPH ratios in plasma specimens showed excellent correlation with the plasma half-lives of DPH and average steady-state levels, suggesting that this ratio could provide guidance in the selection of optimum dosage regimens for problem patients.

摘要

将苯妥英血浆半衰期长和短的正常成年男性每天口服300毫克苯妥英,持续15天。在给药期间及之后5天测量苯妥英(DPH)及其主要代谢物(p-HPPH)的血浆水平。在长半衰期组中,DPH的平均稳态血浆水平升至13.4微克/毫升,而短半衰期组为3.6微克/毫升。长半衰期组中的HPPH水平约为短半衰期组中观察到的水平的一半。血浆标本中的DPH/HPPH比值与DPH的血浆半衰期和平均稳态水平显示出极好的相关性,这表明该比值可为问题患者选择最佳给药方案提供指导。

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Phenytoin metabolism in subjects with long and short plasma half-lives.血浆半衰期长短不同的受试者中苯妥英的代谢
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引用本文的文献

1
Piperine in food: interference in the pharmacokinetics of phenytoin.食物中的胡椒碱:对苯妥英钠药代动力学的干扰。
Eur J Drug Metab Pharmacokinet. 2001 Oct-Dec;26(4):241-7. doi: 10.1007/BF03226378.
2
Inability of ibuprofen to alter single dose phenytoin disposition.布洛芬不能改变苯妥英单次给药的处置。
Br J Clin Pharmacol. 1986 Feb;21(2):165-9. doi: 10.1111/j.1365-2125.1986.tb05171.x.
3
Lack of effect of erythromycin on the pharmacokinetics of single oral doses of phenytoin.红霉素对单次口服苯妥英钠药代动力学无影响。
Br J Clin Pharmacol. 1988 Sep;26(3):330-3. doi: 10.1111/j.1365-2125.1988.tb05285.x.
4
Lack of pharmacokinetic interaction between nifedipine, sparteine and phenytoin in man.硝苯地平、司巴丁和苯妥英在人体内不存在药代动力学相互作用。
Br J Clin Pharmacol. 1991 Feb;31(2):175-8. doi: 10.1111/j.1365-2125.1991.tb05508.x.