Urinary excretion of selegiline N-oxide, a new indicator for selegiline administration in man.
1. The metabolism of selegiline (SG) has been studied by investigating the time-course of urinary excretion of SG and its metabolites using high-performance liquid chromatography-electrospray ionization mass spectrometry (LC-ESI MS) in combination with solid-phase extraction. 2. The excretion profiles of SG and its four major metabolites, selegiline-N-oxide (SGO), N-desmethylselegiline (DM-SG), methamphetamine (MA) and amphetamine (AP), were investigated in six healthy volunteers after oral administrations of SG hydrochloride in a single dose of 2.5 or 7.5mg, and a repeat twice-daily dose of 5.0 mg day(-1) (for 3 days). 3. The cumulative amount of SGO excreted within approximately the first 8-12h was comparable with MA, and the amount in the first 72 h was 2.0-7.8 times larger (2.8-13.2% of the dose) than that of DM-SG. 4. These results demonstrate that SGO can be used in place of DM-SG, which is known to be a main specific metabolite of SG, as a new indicator for the discrimination of SG use compared with MA abuse.
Katagi
M
M
Forensic Science Laboratory, Osaka Prefectural Police HQ, 1-3-18, Hommachi, Chuoku, Osaka 541-0053, Japan. kataginohito@mth.biglobe.ne.jp
Tatsuno
M
M
Tsutsumi
H
H
Miki
A
A
Kamata
T
T
Nishioka
H
H
Nakajima
K
K
Nishikawa
M
M
Tsuchihashi
H
H
D018759:Adrenergic Uptake Inhibitors / Q000652:urine; D000328:Adult; D000661:Amphetamine / Q000652:urine; D000662:Amphetamines / Q000652:urine; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008694:Methamphetamine / Q000652:urine; D008956:Models, Chemical; D008996:Monoamine Oxidase Inhibitors / Q000652:urine*; D012642:Selegiline / Q000008:administration & dosage* / Q000031:analogs & derivatives* / Q000652:urine*; D021241:Spectrometry, Mass, Electrospray Ionization; D013997:Time Factors
D018759:Adrenergic Uptake Inhibitors; D000662:Amphetamines; D008996:Monoamine Oxidase Inhibitors; C442552:selegiline-N-oxide; D012642:Selegiline; D008694:Methamphetamine; C017861:desmethylselegiline; D000661:Amphetamine