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Doxylamine metabolism in rat and monkey.

D A Ganes, K W Hindmarsh, K K Midha

    Xenobiotica; the Fate of Foreign Compounds in Biological Systems
    |September 1, 1986
    PubMed
    Summary

    Doxylamine metabolites were identified in rat and monkey urine, including N-desmethyl and N,N-didesmethyldoxylamine. N-acetyl conjugates were also detected, with variations between species, revealing key metabolic pathways.

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    Area of Science:

    • Pharmacology
    • Drug Metabolism
    • Analytical Chemistry

    Background:

    • Doxylamine is an antihistamine used for treating insomnia and nausea.
    • Understanding its metabolic fate is crucial for assessing drug efficacy and safety.
    • Previous studies on doxylamine metabolism are limited, particularly in vivo across different species.

    Purpose of the Study:

    • To comprehensively identify and characterize the metabolites of doxylamine in vitro and in vivo.
    • To compare the metabolic profiles of doxylamine in rats and squirrel monkeys.
    • To elucidate the metabolic pathways and excretion patterns of doxylamine.

    Main Methods:

    • Incubation of doxylamine with rat-liver homogenate for in vitro studies.
    • Collection and analysis of urine samples from Wistar rats and squirrel monkeys following doxylamine administration.
    • Separation of metabolites using gas-liquid chromatography (g.l.c.), high-performance liquid chromatography (h.p.l.c.), and thin-layer chromatography (t.l.c.).
    • Tentative identification of metabolites through mass spectrometry (MS).

    Main Results:

    • N-Desmethyldoxylamine was identified in vitro.
    • N-desmethyl and N,N-didesmethyldoxylamine were detected in both rat and monkey urine.
    • N-acetyl conjugates of N-desmethyl and N,N-didesmethyldoxylamine were found in rat urine and in vitro.
    • Only the N-acetyl conjugate of N,N-didesmethyldoxylamine was detected in monkey urine.
    • Nine additional metabolites were tentatively identified in rat urine, including hydroxylated and dealkylated forms, as well as doxylamine pyridine N-oxide.
    • Excretion of doxylamine aliphatic N-oxide in rat urine was confirmed.

    Conclusions:

    • Doxylamine undergoes significant metabolism in rats and squirrel monkeys, involving dealkylation and conjugation.
    • Species-specific differences exist in doxylamine metabolism, particularly regarding N-acetyl conjugation.
    • The identified metabolites provide insights into the pharmacokinetic and pharmacodynamic properties of doxylamine.
    • Further research may explore the biological activity of these metabolites.

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