Journal Article

Urinary Excretion Profiles of Two Major Triazolam Metabolites α-Hydroxytriazolam and 4-Hydroxytnazolam

Kenji Tsujikawa, Kenji Kuwayama, Hajime Miyaguchi, Tatsuyuki Kanamori, Yuko Iwata, Hiroyuki Inoue and Tohru Kishi

in Journal of Analytical Toxicology

Volume 29, issue 4, pages 240-243
Published in print May 2005 | ISSN: 0146-4760
Published online May 2005 | e-ISSN: 1945-2403 | DOI: http://dx.doi.org/10.1093/jat/29.4.240
Urinary Excretion Profiles of Two Major Triazolam Metabolites α-Hydroxytriazolam and 4-Hydroxytnazolam

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The objective of this study was to examine urinary excretion profiles of two major triazolam metabolites, α-hydroxytriazolam (α-OHTRZ) and 4-hydroxytriazolam (4-OHTRZ) in humans. Urine samples were collected from three healthy male volunteers who had been previously administered single 0.25- and 0.5-mg doses of triazolam 24 h and 48 h, respectively, before sample collection. After enzymatic hydrolysis and extraction, each sample was analyzed by liquid chromatography-mass spectrometry, α-OHTRZ was rapidly excreted, with the maximum concentrations appearing in the first or second sample collected after ingestion, with the majority of the drug being excreted within 12 h. Meanwhile, 4-OHTRZ was excreted more slowly than α-OHTRZ. The α-OHTRZ/4-OHTRZ ratios were initially greater than 19.7, then decreased rapidly, reaching a nearly constant value for times in excess of 12 h.

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Subjects: Medical Toxicology ; Toxicology (Non-medical)

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