Journal ArticleDOI
Detection of the designer benzodiazepine metizolam in urine and preliminary data on its metabolism: Metizolam identification in urine
Pascal Kintz,Camille Richeval,Carole Jamey,Alice Ameline,Delphine Allorge,Jean-Michel Gaulier,Jean-Sébastien Raul +6 more
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TLDR
The most relevant potential CYP- and UGT-dependent metabolites of metizolam were investigated in vitro using human liver microsome incubation and, subsequently, liquid chromatography coupled with quadrupole-time of flight mass spectrometry (UHPLC-Q-TOF-MS) analysis.Abstract:
Designer benzodiazepines provide an attractive alternative to prescribed benzodiazepines for abuse purposes as they are readily available via the Internet without control. Metizolam was ordered via the Internet and a 2 mg blue tablet was orally administered to a 54-year-old man. Urine samples were collected over 6 days in polypropylene tubes. After liquid/liquid extraction at pH 9.5, metizolam was analyzed by ultra-performance liquid chromatography-electrospray ionization-tandem mass spectrometry (UPLC-ESI-MS/MS) using a standard method devoted to benzodiazepines, and ions transitions, at m/z 328.9 > 275.0 and 328.9 > 300.0. Metizolam was detectable in hydrolyzed urine during the 46-h period, with concentrations always lower than 11 ng/mL. About 0.3% of the initial dose was excreted in urines as total unchanged metizolam during the first 24 h. The most relevant potential CYP- and UGT-dependent metabolites of metizolam were investigated in vitro using human liver microsome incubation and, subsequently, liquid chromatography coupled with quadrupole-time of flight mass spectrometry (UHPLC-Q-TOF-MS) analysis. Three mono-hydroxylated metabolites were produced including a hydroxylation compound at the 2-ethyl moiety of metizolam (M1) as quantitatively main metabolite, and a N-hydroxymetiazolam (M2). The structure of the third metabolite (M3) could not be elucidated because of a too low experimental production rate. Two authentic urine samples were analyzed using the same analytical method to search for metabolites of metizolam. M1, together with its glucuronide (M1-Glu), and M2 were observed in urine at the 8 h mark, whereas only M1 and M1-Glu were still detected in urine at 30 h post administration. Copyright © 2016 John Wiley & Sons, Ltd.read more
Citations
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Journal ArticleDOI
The emergence of new psychoactive substance (NPS) benzodiazepines: A review
TL;DR: This review collates the available information on benzodiazepines and provides a starting point for the further investigation of their pharmacokinetics which is clearly required.
Book ChapterDOI
Designer Benzodiazepines: Another Class of New Psychoactive Substances
Bjoern Moosmann,Volker Auwärter +1 more
TL;DR: This chapter describes the phenomenon of designer benzodiazepines and summarizes the available data on pharmacokinetics and pharmacodynamics as well as analytical approaches for their detection.
Journal ArticleDOI
An expanding world of new psychoactive substances-designer benzodiazepines.
TL;DR: The misuse/abuse of "designer benzodiazepines" (DBZD), a common name for the Benzodiazepine class NPS, has become an increasing problem in many countries and members of the DBZD group are presented.
Journal ArticleDOI
Prevalence of new psychoactive substances and prescription drugs in the Belgian driving under the influence of drugs population.
S.M.R. Wille,Camille Richeval,M. Nachon-Phanithavong,Jean-Michel Gaulier,V. Di Fazio,Luc Humbert,Nele Samyn,Delphine Allorge +7 more
TL;DR: The effects of combined drug use on driving ability and the physical/psychological signs after NPS use should be performed to improve the on-site DUID detection of NPS by police officers, so they can engage in blood sampling for a general unknown screening.
Journal ArticleDOI
'New/Designer Benzodiazepines': An Analysis of the Literature and Psychonauts' Trip Reports.
Laura Orsolini,John Corkery,Stefania Chiappini,Amira Guirguis,Amira Guirguis,Alessandro Vento,Domenico De Berardis,Duccio Papanti,Fabrizio Schifano +8 more
TL;DR: Given the limited information on their pharmacology/toxicity, variations in dosage, onset of effects, combination of substances, potency, and general patient or individual variability, the concomitant use of these substances with other drugs entails several and unpredictable risks.
References
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Journal ArticleDOI
Flubromazolam – A new life-threatening designer benzodiazepine
Magdalena Łukasik-Głębocka,Karina Sommerfeld,Artur Teżyk,Barbara Zielińska-Psuja,Paweł Panieński,Czesław Żaba +5 more
TL;DR: Flubromazolam is a new designer drug that mostly causes sedative effects but also has moderate anti-anxiety and muscle relaxant effects and may be a cause of prolonged, severe intoxication associated with coma, hypotension, and rhabdomyolysis.
Journal ArticleDOI
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TL;DR: It is pointed out that designer benzodiazepines have become a rapidly growing class of drugs of abuse in their own right in the last two years and that mental health professionals should be aware of this new development.
Journal ArticleDOI
Detection and identification of the designer benzodiazepine flubromazepam and preliminary data on its metabolism and pharmacokinetics.
Bjoern Moosmann,Bjoern Moosmann,Laura M. Huppertz,Melanie Hutter,Melanie Hutter,Armin Buchwald,Sascha Ferlaino,Volker Auwärter +7 more
TL;DR: Flubromazepam appears to have an extremely long elimination half-life of more than 100 h, which means that it could be misused in drug-withdrawal settings or in other circumstances requiring regular drug testing, and may be used indrug-facilitated crimes without being detected.