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[给予反苯环丙胺立体异构体的男性血浆和尿液浓度的测定与比较]

[Determination and comparison of the plasma and urine concentrations in men given tranylcypromine stereoisomers].

作者信息

Lang A, Geissler H E, Mutschler E

出版信息

Arzneimittelforschung. 1979;29(1):154-7.

PMID:582109
Abstract

The (+) and (-)isomers of DL-trans-2-phenylcyclopropylamine (tranylcypromine, Parnate, Jatrosom) were tested under cross-over conditions on 10 volunteers. (-)Tranylcypromine entered blood circulation more rapidly, reached significantly higher concentrations and was metabolized more slowly than (+)tranylcypromine. These results indicate a difference in the pharmacokinetics of the tranylcypromine isomers. In the urine collected over a period of 24 h the excretion of unmetabolized (4)tranylcypromine was lower probably resulting from the greater metabolization rate of this isomer. There is a conformity between the findings in plasma and urine.

摘要

在交叉试验条件下,对10名志愿者测试了DL - 反式 - 2 - 苯基环丙胺(反苯环丙胺,帕罗西汀,贾特罗索姆)的(+)和( - )异构体。( - )反苯环丙胺进入血液循环的速度更快,达到的浓度显著更高,并且比(+)反苯环丙胺代谢更慢。这些结果表明反苯环丙胺异构体在药代动力学上存在差异。在24小时收集的尿液中,未代谢的(4)反苯环丙胺排泄量较低,这可能是由于该异构体的代谢率较高所致。血浆和尿液中的研究结果是一致的。

相似文献

1
[Determination and comparison of the plasma and urine concentrations in men given tranylcypromine stereoisomers].[给予反苯环丙胺立体异构体的男性血浆和尿液浓度的测定与比较]
Arzneimittelforschung. 1979;29(1):154-7.
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引用本文的文献

1
The pharmacokinetics of tranylcypromine enantiomers in healthy subjects after oral administration of racemic drug and the single enantiomers.消旋曲唑酮及单一对映体口服给药后在健康受试者体内的药代动力学。
Br J Clin Pharmacol. 1993 Oct;36(4):363-5. doi: 10.1111/j.1365-2125.1993.tb00377.x.
2
Metabolism of monoamine oxidase inhibitors.单胺氧化酶抑制剂的代谢
Cell Mol Neurobiol. 1999 Jun;19(3):411-26. doi: 10.1023/a:1006901900106.
3
Tranylcypromine isomers and Parkinson's disease: new aspects of an old drug.反苯环丙胺异构体与帕金森病:一种老药的新情况
J R Soc Med. 1981 Sep;74(9):649-52. doi: 10.1177/014107688107400905.
4
Monoamine oxidase inhibition by tranylcypromine: assessment in human volunteers.
Eur J Clin Pharmacol. 1982;22(4):301-8. doi: 10.1007/BF00548397.
5
Tranylcypromine isomers: single-dose effects in normal human subjects.反苯环丙胺异构体:对正常人类受试者的单剂量效应。
Psychopharmacology (Berl). 1981;75(4):400-3. doi: 10.1007/BF00435862.
6
Neurochemical and neuropharmacological properties of 4-fluorotranylcypromine.4-氟反苯环丙胺的神经化学和神经药理学特性
Cell Mol Neurobiol. 1987 Sep;7(3):271-90. doi: 10.1007/BF00711304.