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佐美酸在人和动物体内的药代动力学及代谢研究综述。

Review of the pharmacokinetics and metabolism of zomepirac in man and animals.

作者信息

Muschek L D, Grindel J M

出版信息

J Clin Pharmacol. 1980 Apr;20(4):223-9. doi: 10.1002/j.1552-4604.1980.tb01702.x.

DOI:10.1002/j.1552-4604.1980.tb01702.x
PMID:6769977
Abstract

Zomepirac has been shown to be rapidly and completely absorbed after oral administration to man. Urinary excretion is the principal route for removal of zomepirac and its metabolites in man and in animals. Zomepirac is highly bound to plasma protein. The pharmacokinetics of zomepirac after single and multiple doses in man can be adequately described by a two-compartment oral absorption model. There is a linear relationship between dose and peak plasma concentration, AUC, and urinary excretion of zomepirac. The bioavailability of zomepirac was unaffected by single or repeated doses of antacid. The rhesus monkey has been shown to be a good predictive animal model for zomepirac's metabolism and pharmacokinetics in man, with glucuronidation found to be the principal route of metabolism in both species.

摘要

佐美酸经口服给药后,在人体内能迅速且完全地被吸收。在人和动物体内,尿液排泄是佐美酸及其代谢产物排出体外的主要途径。佐美酸与血浆蛋白高度结合。单剂量和多剂量给药后,人体内佐美酸的药代动力学可用双室口服吸收模型进行充分描述。佐美酸的剂量与血浆峰浓度、曲线下面积(AUC)以及尿液排泄量之间呈线性关系。抗酸剂单次或重复给药对佐美酸的生物利用度没有影响。恒河猴已被证明是预测佐美酸在人体内代谢和药代动力学的良好动物模型,在这两个物种中,葡萄糖醛酸化都是主要的代谢途径。

相似文献

1
Review of the pharmacokinetics and metabolism of zomepirac in man and animals.佐美酸在人和动物体内的药代动力学及代谢研究综述。
J Clin Pharmacol. 1980 Apr;20(4):223-9. doi: 10.1002/j.1552-4604.1980.tb01702.x.
2
Disposition of zomepirac sodium in man.佐美酸纳在人体中的处置情况。
J Clin Pharmacol. 1982 Oct;22(10):470-6. doi: 10.1002/j.1552-4604.1982.tb02637.x.
3
Zomepirac kinetics in healthy males.健康男性体内唑美昔康的动力学
Clin Pharmacol Ther. 1980 Mar;27(3):395-401. doi: 10.1038/clpt.1980.53.
4
The metabolism of zomepirac sodium. I. Disposition in laboratory animals and man.氯胺吡酸的代谢。I. 在实验动物和人体中的处置情况
Drug Metab Dispos. 1980 Sep-Oct;8(5):343-8.
5
Dose-dependent pharmacokinetics and renal handling of zomepirac in rhesus monkeys.猴体内佐美酸的剂量依赖性药代动力学及肾脏处理情况
J Pharmacol Exp Ther. 1981 Dec;219(3):665-8.
6
Absorption and excretion of tolemetin in man.托美丁在人体中的吸收与排泄。
Clin Pharmacol Ther. 1976 Feb;19(2):224-33. doi: 10.1002/cpt1976192224.
7
Abnormal glucuronidation of zomepirac in patients with cirrhosis of the liver.在肝硬化患者中,佐美酸的葡萄糖醛酸化异常。
Hepatology. 1983 May-Jun;3(3):415-22. doi: 10.1002/hep.1840030322.
8
Effect of probenecid on the formation and elimination of acyl glucuronides: studies with zomepirac.丙磺舒对酰基葡萄糖醛酸苷形成和消除的影响:以佐美酸进行的研究
Clin Pharmacol Ther. 1985 Aug;38(2):121-7. doi: 10.1038/clpt.1985.146.
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The metabolism of zomepirac sodium. II. Isolation and identification of the urinary metabolites in rat, mouse, rhesus monkey, and man.佐美酸纳的代谢。II. 大鼠、小鼠、恒河猴及人体尿液代谢物的分离与鉴定。
Drug Metab Dispos. 1980 Sep-Oct;8(5):349-52.
10
Zomepirac--aspirin interactions in man.
J Clin Pharmacol. 1984 Aug-Sep;24(8-9):371-80. doi: 10.1002/j.1552-4604.1984.tb02789.x.

引用本文的文献

1
Zomepirac: a review of its pharmacological properties and analgesic efficacy.佐美酸:其药理特性与镇痛效果综述
Drugs. 1982 Apr;23(4):250-75. doi: 10.2165/00003495-198223040-00002.