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Urinary excretion profiles of two major triazolam metabolites, alpha-hydroxytriazolam and 4-hydroxytriazolam.

Author(s): Tsujikawa K, Kuwayama K, Miyaguchi H, Kanamori T, Iwata Y, Inoue H, Kishi T

Affiliation(s): National Research Institute of Police Science 6-3-1, Kashiwanoha, Kashiwa, Chiba 277-0882, Japan. tujikawa@nrips.go.jp

Publication date & source: 2005-05, J Anal Toxicol., 29(4):240-3.

The objective of this study was to examine urinary excretion profiles of two major triazolam metabolites, alpha-hydroxytriazolam (alpha-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. alpha-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 alpha-OHTRZ. The alpha-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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