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纳曲酮的人体药代动力学概述。

Overview of human pharmacokinetics of naltrexone.

作者信息

Licko V

出版信息

NIDA Res Monogr. 1981;28:161-71.

PMID:6791002
Abstract

Experimental data on 3H labelled naltrexone obtained from the Research Triangle Institute were analyzed. Both plasma and urine curves were resolved into their exponential components. Mean total clearance of unconjugated naltrexone was 3510 (300) ml/min, and its mean urinary clearance was 76.0 (6.8) ml/min. Fraction of dose excreted through urine was between 55 and 60%. Orally administered drug is completely absorbed into plasma. Plasma curve resulting from intravenous administration contained three exponentials: 1.9 (.5)/min, 0.18 (.07)/min and 0.00106 (.00008)/min. Distribution volumes were 7.6 (.7) liters, 60 (12) liters and 164 (16) liters. After oral administration there were two exponentials: 0.012 (.002/min and 0.00122 (.00009)/min. The faster exponential corresponds to gastrointestinal absorption with a half life of about 1 hour.

摘要

对从三角研究机构获得的3H标记纳曲酮的实验数据进行了分析。血浆和尿液曲线都被分解为各自的指数成分。未结合纳曲酮的平均总清除率为3510(300)ml/分钟,其平均尿液清除率为76.0(6.8)ml/分钟。经尿液排泄的剂量分数在55%至60%之间。口服给药的药物完全吸收进入血浆。静脉给药产生的血浆曲线包含三个指数成分:1.9(0.5)/分钟、0.18(0.07)/分钟和0.00106(0.00008)/分钟。分布容积分别为7.6(0.7)升、60(12)升和164(16)升。口服给药后有两个指数成分:0.012(0.002)/分钟和0.00122(0.00009)/分钟。较快的指数成分对应于胃肠道吸收,半衰期约为1小时。

相似文献

1
Overview of human pharmacokinetics of naltrexone.纳曲酮的人体药代动力学概述。
NIDA Res Monogr. 1981;28:161-71.
2
Naltrexone disposition in man after subcutaneous administration.皮下注射后纳曲酮在人体内的处置情况。
Drug Metab Dispos. 1984 Nov-Dec;12(6):677-82.
3
Bioequivalence, dose-proportionality, and pharmacokinetics of naltrexone after oral administration.口服纳曲酮后的生物等效性、剂量比例性及药代动力学
J Clin Psychiatry. 1984 Sep;45(9 Pt 2):15-9.
4
Metabolism and disposition of naltrexone in man after oral and intravenous administration.
Drug Metab Dispos. 1981 Jul-Aug;9(4):369-75.
5
The seminal excretion, plasma elimination, tissue distribution and metabolism of naltrexone in the rabbit.纳曲酮在兔体内的精液排泄、血浆消除、组织分布及代谢
J Pharmacol Exp Ther. 1980 May;213(2):289-99.
6
Pharmacokinetics of naloxone and naltrexone in the dog.
J Pharmacol Exp Ther. 1979 Feb;208(2):254-6.
7
A comparative study of the oral, intravenous, and subcutaneous administration of 3H-naltrexone to normal male volunteers.对正常男性志愿者口服、静脉注射和皮下注射3H-纳曲酮的比较研究。
NIDA Res Monogr. 1981;28:93-101.
8
The clinical pharmacology of naltrexone: pharmacology and pharmacodynamics.
NIDA Res Monogr. 1981;28:147-58.
9
Elimination of radioactivity following administration of [15,16-3H]naltrexone to rats and guinea pigs.给大鼠和豚鼠注射[15,16 - 3H]纳曲酮后放射性的消除情况。
Drug Metab Dispos. 1978 May-Jun;6(3):321-8.
10
Kinetics of a naltrexone sustained-release preparation.纳曲酮缓释制剂的动力学
Clin Pharmacol Ther. 1984 Nov;36(5):704-8. doi: 10.1038/clpt.1984.243.

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