Literature DB >> 2903030

Metabolism of diazepam in vitro by human liver. Independent variability of N-demethylation and C3-hydroxylation.

T Inaba1, A Tait, M Nakano, W A Mahon, W Kalow.   

Abstract

The interindividual variability of diazepam metabolism was studied using human livers. The formation of N-desmethyldiazepam (NDZ) and 3-hydroxydiazepam (temazepam, TMZ), was monitored by gas chromatography. In 10 livers, Km values for NDZ and TMZ formation varied independently from each other, each by a factor of 4, from 100 to 400 microM. This variability is consistent with the presence of at least two different cytochrome P-450 species controlling formation of these metabolites. In the same livers, Vmax for NDZ and TMZ production varied 6-fold and 15-fold, respectively.

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Year:  1988        PMID: 2903030

Source DB:  PubMed          Journal:  Drug Metab Dispos        ISSN: 0090-9556            Impact factor:   3.922


  8 in total

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2.  Concentration-dependent metabolism of diazepam in mouse liver.

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Journal:  J Pharmacokinet Biopharm       Date:  1995-06

3.  Oxidation of reduced haloperidol to haloperidol: involvement of human P450IID6 (sparteine/debrisoquine monooxygenase).

Authors:  R F Tyndale; W Kalow; T Inaba
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4.  Diazepam metabolism by human liver microsomes is mediated by both S-mephenytoin hydroxylase and CYP3A isoforms.

Authors:  T Andersson; J O Miners; M E Veronese; D J Birkett
Journal:  Br J Clin Pharmacol       Date:  1994-08       Impact factor: 4.335

5.  Metabolism of diazepam and related benzodiazepines by human liver microsomes.

Authors:  W D Hooper; J A Watt; G E McKinnon; P E Reilly
Journal:  Eur J Drug Metab Pharmacokinet       Date:  1992 Jan-Mar       Impact factor: 2.441

6.  The screening of selected microorganisms for use as models of mammalian drug metabolism.

Authors:  D A Griffiths; D J Best; S G Jezequel
Journal:  Appl Microbiol Biotechnol       Date:  1991-06       Impact factor: 4.813

7.  Intracellular nucleotide pools and ratios as tools for monitoring dedifferentiation of primary porcine hepatocytes in culture.

Authors:  Dirk Rocker; Friedemann Hesse; Augustinus Bader; Roland Wagner
Journal:  Cytotechnology       Date:  2006-11-21       Impact factor: 2.058

Review 8.  Pharmacogenetics in Primary Headache Disorders.

Authors:  Irina I Belyaeva; Anna G Subbotina; Ivan I Eremenko; Vadim V Tarasov; Vladimir N Chubarev; Helgi B Schiöth; Jessica Mwinyi
Journal:  Front Pharmacol       Date:  2022-02-10       Impact factor: 5.810

  8 in total

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