Urinary excretion profiles of two major triazolam metabolites, alpha-hydroxytriazolam and 4-hydroxytriazolam.
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.
Tsujikawa
Kenji
K
National Research Institute of Police Science 6-3-1, Kashiwanoha, Kashiwa, Chiba 277-0882, Japan. tujikawa@nrips.go.jp
Kuwayama
Kenji
K
Miyaguchi
Hajime
H
Kanamori
Tatsuyuki
T
Iwata
Yuko
Y
Inoue
Hiroyuki
H
Kishi
Tohru
T
D002853:Chromatography, Liquid; D006801:Humans; D006993:Hypnotics and Sedatives / Q000378:metabolism*; D008297:Male; D015203:Reproducibility of Results; D012680:Sensitivity and Specificity; D021241:Spectrometry, Mass, Electrospray Ionization; D014229:Triazolam / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000378:metabolism / Q000652:urine*
D006993:Hypnotics and Sedatives; D014229:Triazolam; C028638:alpha-hydroxytriazolam; C028637:4-hydroxytriazolam