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Triazolam disposition.

F S Eberts, Y Philopoulos, L M Reineke

    Clinical Pharmacology and Therapeutics
    |January 1, 1981
    PubMed
    Summary
    This summary is machine-generated.

    Triazolam (T), a potent hypnotic, is rapidly absorbed and eliminated. Its major metabolites, alpha-hydroxytriazolam and 4-hydroxytriazolam, are excreted primarily in urine, mostly as conjugates, consistent with T's short action.

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    Area of Science:

    • Pharmacology
    • Drug Metabolism
    • Clinical Pharmacokinetics

    Background:

    • Triazolam (T) is a potent hypnotic agent.
    • Its short duration of action in humans necessitates understanding its pharmacokinetic profile.

    Purpose of the Study:

    • To investigate the absorption, distribution, metabolism, and excretion (ADME) of Triazolam in humans.
    • To identify the major metabolites of Triazolam and their pharmacokinetic properties.

    Main Methods:

    • Administration of an oral dose of 14C-labeled Triazolam (0.88 mg) to six healthy male subjects.
    • Quantification of radioactivity in urine and feces.
    • Identification and quantification of Triazolam and its metabolites in plasma and urine using chromatographic and radiometric techniques.

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    Main Results:

    • Rapid absorption of Triazolam with a mean absorption half-life of 2.8 minutes.
    • Mean elimination half-life of Triazolam was 2.3 hours.
    • Major urinary metabolites were alpha-hydroxytriazolam (69%) and 4-hydroxytriazolam (11%), primarily in conjugated forms.
    • Plasma levels of alpha-HT-glucuronide and 4-HT-glucuronide were also characterized with elimination half-lives around 3.8-3.9 hours.

    Conclusions:

    • The rapid absorption and elimination of Triazolam, along with its metabolism to hydroxylated conjugates, are consistent with its short duration of hypnotic action.
    • The pharmacokinetic data provide a basis for understanding Triazolam's clinical effects and potential for drug interactions.