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去甲氯氮卓单次口服给药在人体内的药代动力学。

Pharmacokinetics of chlordesmethyldiazepam after single-dose oral administration in humans.

作者信息

Bareggi S R, Pirola R, Leva S, Zecca L

出版信息

Eur J Drug Metab Pharmacokinet. 1986 Jul-Sep;11(3):171-4. doi: 10.1007/BF03189844.

DOI:10.1007/BF03189844
PMID:3102240
Abstract

The pharmacokinetics of chlordemethyldiazepam--a pharmacologically very active new 1,4-benzodiazepine derivative--in healthy subjects after administration of a single oral dose of 2 mg, was studied. Peak concentrations were reached in 1.2 +/- 0.2 hours. Plasma levels declined with a biphasic pattern, and the elimination phase had a half-life of 82.9 +/- 14.1 hours. The concentrations of the main metabolite of chlordemethyldiazepam, lorazepam, were about 7% of those of the parent compound. In urine only conjugated lorazepam could be found its 96 hour excretion reaching about 15% of the administered dose of parent drug.

摘要

研究了氯去甲安定(一种药理活性很强的新型1,4 -苯二氮䓬衍生物)在健康受试者单次口服2毫克后的药代动力学。1.2±0.2小时达到峰值浓度。血浆水平呈双相下降模式,消除相半衰期为82.9±14.1小时。氯去甲安定的主要代谢产物劳拉西泮的浓度约为母体化合物浓度的7%。在尿液中仅能检测到结合型劳拉西泮,其96小时排泄量约为母体药物给药剂量的15%。

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本文引用的文献

1
Plasma levels of chlorodesmethyldiazepam in humans.人体内氯去甲安定的血浆水平。
Biopharm Drug Dispos. 1980 Jan-Mar;1(3):123-6. doi: 10.1002/bdd.2510010306.
2
NL-FIT: a microcomputer program for non-linear fitting.NL - FIT:一种用于非线性拟合的微型计算机程序。
Comput Programs Biomed. 1983 Feb-Apr;16(1-2):35-42. doi: 10.1016/0010-468x(83)90006-5.
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The determination of 7-chloro-1,3-dihydro-5-(2',chlorophenyl)-2H-1,4-benzodiazepin-2-one (Ro 5-3027) and its metabolite (lorazepam) in blood and urine by electron-capture gas liquid chromatography.
Eur J Clin Pharmacol. 1988;34(1):109-12. doi: 10.1007/BF01061430.
4
Pharmacokinetics of intravenous and oral chlordesmethyldiazepam in patients on regular haemodialysis.
Eur J Clin Pharmacol. 1991;41(1):65-8. doi: 10.1007/BF00280109.
J Chromatogr Sci. 1973 Oct;11(10):547-52. doi: 10.1093/chromsci/11.10.547.
4
Structure-activity relationships within the class of 1,4-benzodiazepines: presence of chlorine and central nervous system activities.1,4-苯二氮䓬类药物的构效关系:氯的存在与中枢神经系统活性
Curr Ther Res Clin Exp. 1974 Apr;16(4):324-37.
5
Age-related multiple-dose pharmacokinetics and anxiolytic effects of delorazepam (chlordesmethyldiazepam).去甲氯氮卓(氯去甲安定)的年龄相关性多剂量药代动力学及抗焦虑作用。
Int J Clin Pharmacol Res. 1986;6(4):309-14.
6
Novel application of proton nuclear magnetic resonance spectroscopy in the identification of 2'-chloronordiazepam metabolites in the dog.质子核磁共振波谱在犬体内2'-氯去甲西泮代谢物鉴定中的新应用。
J Med Chem. 1979 Apr;22(4):436-40. doi: 10.1021/jm00190a016.
7
Gas chromatographic determination of chlorodesmethyldiazepam and lorazepam in rats and mice.
J Chromatogr. 1979 Jan 11;168(1):260-5. doi: 10.1016/s0021-9673(00)80722-0.
8
Pharmacokinetics and bioavailability of intravenous, intramuscular, and oral lorazepam in humans.劳拉西泮在人体中的静脉注射、肌肉注射及口服给药的药代动力学和生物利用度
J Pharm Sci. 1979 Jan;68(1):57-63. doi: 10.1002/jps.2600680119.
9
Analysis of lorazepam and its glucuronide metabolite by electron-capture gas--liquid chromatography. Use in pharmacokinetic studies of lorazepam.通过电子捕获气液色谱法分析劳拉西泮及其葡萄糖醛酸代谢物。用于劳拉西泮的药代动力学研究。
J Chromatogr. 1978 Sep 1;146(2):311-20.
10
On the hypnogenic and anticonvulsant activities of demethyldiazepam and chlordemethyldiazepam: time-effect relations.
J Pharm Pharmacol. 1977 Aug;29(8):504-6. doi: 10.1111/j.2042-7158.1977.tb11380.x.