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一名志愿者体内阿米替林及其N-氧化物的单剂量对比动力学

Comparative single-dose kinetics of amitriptyline and its N-oxide in a volunteer.

作者信息

Breyer-Pfaff U, Ewert M, Wiatr R

出版信息

Arzneimittelforschung. 1978;28(10b):1916-20.

PMID:582519
Abstract

Plasma drug levels and urinary metabolites were measured in a volunteer for 28 h after ingestion of amitriptyline hydrochloride or amitriptyline N-oxide (amitriptylinoxide) equivalent to 100 mg of amitriptyline base. The N-oxide initially produced high plasma levels and 15% of the dose was excreted unchanged within 14 h. From comparison of the metabolite excretions, it can be concluded that about 70% of the dose was reduced at the N-oxide group, while comparison of the areas under the plasma group, while comparison of the areas under the plasma level-time curves for amitriptyline pointed to a 55% reduction to the amine. Less drowsiness was experienced after ingesting the N-oxide, and there was no depressive mood.

摘要

在一名志愿者摄入相当于100毫克阿米替林碱的盐酸阿米替林或N-氧化阿米替林(阿米替林氧化物)后,对其血浆药物水平和尿液代谢物进行了28小时的测量。N-氧化物最初产生较高的血浆水平,14小时内15%的剂量以原形排出。通过比较代谢物排泄情况可以得出结论,N-氧化物组约70%的剂量被还原,而比较血浆水平-时间曲线下的面积,阿米替林组则显示胺类减少了55%。摄入N-氧化物后嗜睡感较轻,且没有抑郁情绪。

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1
Comparative single-dose kinetics of amitriptyline and its N-oxide in a volunteer.一名志愿者体内阿米替林及其N-氧化物的单剂量对比动力学
Arzneimittelforschung. 1978;28(10b):1916-20.
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引用本文的文献

1
Biotransformation of amitriptyline in depressive patients: urinary excretion of seven metabolites.抑郁症患者体内阿米替林的生物转化:七种代谢物的尿排泄情况
Eur J Clin Pharmacol. 1982;22(3):239-45. doi: 10.1007/BF00545222.
2
Urinary metabolites of amitriptylinoxide and amitriptyline in single-dose experiments and during continuous therapy.单剂量实验及持续治疗期间阿米替林氮氧化物和阿米替林的尿液代谢产物
Psychopharmacology (Berl). 1992;106(3):303-10. doi: 10.1007/BF02245409.