New metabolites of imipramine

Crammer, J. L.; Scott, Bernard

doi:10.1007/bf00406495

Cited by 38 publications

(8 citation statements)

References 5 publications

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“…The major metabolites identified included 2hydroxyimipramine (II), 10-hydroxyimipramine (III), iminodibenzyl (IV), imipramine-N-oxide (V), and desipramine (VI). These microbial metabolites also correspond to major human and mammalian metabolites of imipramine (8)(9)(10)(11)(12)20). The results of this study clearly suggest that microorganisms can be used to study drug metabolism (biotransformation), with the'added advantage of producing large quantities of metabolites so that complete biological evaluation as well as complete and rigorous structural elucidation studies can be obtained.…”

Section: Discussionmentioning

confidence: 65%

Metabolism of Imipramine by Microorganisms

Huffordx

Capiton

Clark

et al. 1981

Journal of Pharmaceutical Sciences

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Section: Discussionmentioning

confidence: 65%

Metabolism of Imipramine by Microorganisms

Huffordx

Capiton

Clark

et al. 1981

Journal of Pharmaceutical Sciences

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“…Other metabolites, such as iminodibenzyl, 2-and 10-OHiminodibenzyl, 2-and 10-OH-DDMI (Bickel and Baggiolini 1966;Crammer and Scott 1966) were not considered, as they were formed only in small amounts and have no known pharmacological activity.…”

mentioning

confidence: 99%

Comparison of the metabolism of the three antidepressants amitriptyline, imipramine, and chlorimipramine in vitro in rat liver microsomes

Krüger¹,

Hölzl²,

Kuss³

et al. 1986

Psychopharmacology

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The metabolism of the tricyclic antidepressants amitriptyline (AMI), imipramine (IMI), chlorimipramine (CMI) and some of their metabolites was studied in vitro in isolated liver microsomes of female Spraque-Dawley rats. Nine metabolites of AMI, seven metabolites of IMI, and 11 metabolites of CMI were quantitatively determined with high-performance liquid chromatography. The main metabolic reactions, mediated by an NADPH generating system, were hydroxylation, demethylation, and N-oxidation. The ratio of these reactions was different for the three drugs. AMI was hydroxylated more than CMI and CMI more than IMI. The order for demethylation was CMI greater than AMI = IMI, the order for N-oxidation IMI greater than CMI less than or equal to AMI. The substrate dependence of metabolism was investigated. Demethylation and N-oxidation increased proportionally to increasing substrate concentrations, whereas formation of hydroxylated metabolites became saturated (in the concentration range of 10(-6)-10(-5) M). The in vitro metabolism was compared with the in vivo metabolism in humans, reflected by the plasma concentrations of these drugs and their metabolites. A good agreement in metabolic pathways was found.

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“…2 position of the ring or in the ethylene bridge. 3 NT has been reported to be extensively hydroxylated in the ethylene bridge. 15 The 2 drugs are also demethylated, but evidently this pathway is of little importance in man.…”

Section: Discussionmentioning

confidence: 99%

A comparative study of the metabolism of desmethylimipramine, nortriptyline, and oxyphenylbutazone in man

Hammer

Mårtens

Sjöqvist

1969

Clin Pharma and Therapeutics

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Large individual differences have been found in the steady-state plasma levels of desmethylimipramine ( DMI) and nortriptyline (NT) in patients treated for 2 to 3 weeks with doses of 25 mg., three times a day. 8 • 10 · 21 Moody and associates 16 found large differences for imipramine ( IP) and DMI when IP was administered. Hammer and Sji:iqvist 10 observed that patients who developed high or low plasma levels (in steady state) of DMI or NT also developed

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New metabolites of imipramine

Cited by 38 publications

References 5 publications

Metabolism of Imipramine by Microorganisms

Metabolism of Imipramine by Microorganisms

Comparison of the metabolism of the three antidepressants amitriptyline, imipramine, and chlorimipramine in vitro in rat liver microsomes

A comparative study of the metabolism of desmethylimipramine, nortriptyline, and oxyphenylbutazone in man

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