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代谢物药代动力学:肾清除和肝清除药物及代谢物经不同给药途径给药后代谢物的曲线下面积和药物代谢分数率。

Metabolite pharmacokinetics: the area under the curve of metabolite and the fractional rate of metabolism of a drug after different routes of administration for renally and hepatically cleared drugs and metabolites.

作者信息

Pang K S

出版信息

J Pharmacokinet Biopharm. 1981 Aug;9(4):477-87. doi: 10.1007/BF01060890.

DOI:10.1007/BF01060890
PMID:7310645
Abstract

A model comprised of four compartments, a central and liver compartment for a drug, and a central and liver compartment for a metabolite, is presented to describe the interrelationships between the area under the curve of the metabolite and physiological parameters after intravenous and intraportal administration of the drug. The model includes renal and hepatic eliminatory mechanisms for both drug and metabolite as long as the metabolite is formed only by the liver. It is found that when competing renal eliminatory pathways exist for a drug, the area under the curve for the metabolite will change according to the route of drug administration. Also, the fractional rate of metabolism of a drug to form the metabolite will be underestimated by the normal use of the ratio areas under the curve of the metabolite. Other properties of the model are also discussed.

摘要

提出了一个由四个隔室组成的模型,一个用于药物的中央隔室和肝脏隔室,以及一个用于代谢物的中央隔室和肝脏隔室,以描述静脉内和门静脉内给药后代谢物曲线下面积与生理参数之间的相互关系。只要代谢物仅由肝脏形成,该模型就包括药物和代谢物的肾脏和肝脏消除机制。研究发现,当药物存在竞争性肾脏消除途径时,代谢物的曲线下面积将根据药物给药途径而变化。此外,通过正常使用代谢物曲线下面积的比值,将低估药物形成代谢物的代谢分数率。还讨论了该模型的其他特性。

相似文献

1
Metabolite pharmacokinetics: the area under the curve of metabolite and the fractional rate of metabolism of a drug after different routes of administration for renally and hepatically cleared drugs and metabolites.代谢物药代动力学:肾清除和肝清除药物及代谢物经不同给药途径给药后代谢物的曲线下面积和药物代谢分数率。
J Pharmacokinet Biopharm. 1981 Aug;9(4):477-87. doi: 10.1007/BF01060890.
2
The area under the curve of metabolites for drugs and metabolites cleared by the liver and extrahepatic organs. Its dependence on the administration route of precursor drug.肝脏和肝外器官清除的药物及代谢物的代谢物曲线下面积。其对前体药物给药途径的依赖性。
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Drug Metab Dispos. 1995 Feb;23(2):166-77.
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Primary, secondary, and tertiary metabolite kinetics.初级、次级和三级代谢物动力学。
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本文引用的文献

1
Prediction of steady-state behavior of metabolite from dosing of parent drug.根据母体药物给药情况预测代谢物的稳态行为。
J Pharm Sci. 1980 May;69(5):610-2. doi: 10.1002/jps.2600690541.
2
Metabolite pharmacokinetics: methods for simultaneous estimates of elimination rate constants of a drug and its metabolite. A commentary.代谢物药代动力学:同时估算药物及其代谢物消除速率常数的方法。一篇评论
Drug Metab Dispos. 1980 Jan-Feb;8(1):39-43.
3
Kinetic considerations relating to the accrual and elimination of drug metabolites.与药物代谢物的累积和消除相关的动力学考量。
A phase I clinical and pharmacokinetic study of the oral and the oral/intravenous administration of menogaril.
美诺加明口服及口服/静脉给药的I期临床和药代动力学研究。
Invest New Drugs. 1993 Feb;11(1):17-27. doi: 10.1007/BF00873906.
4
Drug metabolite concentration-time profiles: influence of route of drug administration.药物代谢物浓度-时间曲线:给药途径的影响
Br J Clin Pharmacol. 1984 Apr;17(4):385-94. doi: 10.1111/j.1365-2125.1984.tb02362.x.
5
Fractions metabolized in a triangular metabolic system: cinromide and two metabolites in the rhesus monkey.在三角代谢系统中代谢的组分:恒河猴体内的西溴米特及其两种代谢物。
J Pharmacokinet Biopharm. 1985 Aug;13(4):373-86. doi: 10.1007/BF01061475.
6
Drug metabolite kinetics: noncompartmental analysis.药物代谢物动力学:非房室分析。
Br J Clin Pharmacol. 1985 Jun;19(6):855-6. doi: 10.1111/j.1365-2125.1985.tb02730.x.
7
A review of metabolite kinetics.代谢物动力学综述。
J Pharmacokinet Biopharm. 1985 Dec;13(6):633-62. doi: 10.1007/BF01058905.
8
Pharmacokinetics of methysergide and its metabolite methylergometrine in man.甲基麦角新碱及其代谢产物甲基麦角新碱在人体中的药代动力学。
Eur J Clin Pharmacol. 1986;30(1):75-7. doi: 10.1007/BF00614199.
9
Primary, secondary, and tertiary metabolite kinetics.初级、次级和三级代谢物动力学。
J Pharmacokinet Biopharm. 1988 Oct;16(5):493-527. doi: 10.1007/BF01062382.
10
Mephenytoin stereoselective elimination in the rat: II. Comparison of mephenytoin stereoselective clearance during chronic intravenous and hepatic portal vein administration.美芬妥英在大鼠体内的立体选择性消除:II. 慢性静脉注射和肝门静脉给药期间美芬妥英立体选择性清除率的比较。
Eur J Drug Metab Pharmacokinet. 1989 Oct-Dec;14(4):269-78. doi: 10.1007/BF03190110.
Br J Pharmacol Chemother. 1967 Feb;29(2):136-49. doi: 10.1111/j.1476-5381.1967.tb01947.x.
4
Pharmacokinetic model for chlordiazepoxide--HCl in the dog.狗体内氯氮䓬盐酸盐的药代动力学模型。
J Pharm Sci. 1970 Nov;59(11):1569-74. doi: 10.1002/jps.2600591105.
5
Two-compartment model for a drug and its metabolite: application to acetylsalicylic acid pharmacokinetics.药物及其代谢物的二室模型:在乙酰水杨酸药代动力学中的应用。
J Pharm Sci. 1970 Mar;59(3):364-7. doi: 10.1002/jps.2600590319.
6
Pharmacokinetics of isoniazid and some metabolites in man.异烟肼及其某些代谢产物在人体中的药代动力学。
J Pharmacokinet Biopharm. 1976 Aug;4(4):287-325. doi: 10.1007/BF01063121.
7
A theoretical examination of the effects of gut wall metabolism, hepatic elimination, and enterohepatic recycling on estimates of bioavailability and of hepatic blood flow.
J Pharmacokinet Biopharm. 1978 Oct;6(5):355-67. doi: 10.1007/BF01062719.
8
Hepatic clearance of drugs. III. Additional experimental evidence supporting the "well-stirred" model, using metabolite (MEGX) generated from lidocaine under varying hepatic blood flow rates and linear conditions in the perfused rat liver in situ preparation.药物的肝清除率。III. 额外的实验证据支持“充分搅拌”模型,该证据来自于在不同肝血流速率及灌注大鼠原位肝制备的线性条件下,由利多卡因产生的代谢物(MEGX)。
J Pharmacokinet Biopharm. 1977 Dec;5(6):681-99. doi: 10.1007/BF01059690.
9
Sequential first-pass elimination of a metabolite derived from a precursor.
J Pharmacokinet Biopharm. 1979 Jun;7(3):275-90. doi: 10.1007/BF01060018.
10
Disposition kinetics in dogs of diethyldithiocarbamate, a metabolite of disulfiram.双硫仑的代谢产物二乙二硫代氨基甲酸盐在犬体内的处置动力学。
J Pharmacokinet Biopharm. 1978 Oct;6(5):369-87. doi: 10.1007/BF01062720.