Flubromazolam Explained

Flubromazolam (JYI-73) [1] [2] [3] is a triazolobenzodiazepine (TBZD), which are benzodiazepine (BZD) derivatives.[4] [5] [6] [7] [8] [9] [10] Flubromazolam is reputed to be highly potent, and concerns have been raised that clonazolam and flubromazolam in particular may pose comparatively higher risks than other designer benzodiazepines, due to their ability to produce strong sedation and amnesia at oral doses of as little as 0.5 mg.[11] [12] Life-threatening adverse reactions have been observed at doses of only 3 mg of flubromazolam.[13]

Legal status

Sweden

Flubromazolam has been classified as an illegal substance in Sweden after seizures by customs and police, as well as indications from the EMCDDA of wider use as a recreational drug.[14]

Switzerland

Flubromazolam is illegal in Switzerland as of December 2015.[15]

United Kingdom

In the UK, flubromazolam has been classified as a Class C drug by the May 2017 amendment to The Misuse of Drugs Act 1971 along with several other designer benzodiazepine drugs.[16]

Australia

In Australia, flubromazolam is Schedule 9 under federal law.[17]

United States

Flubromazolam is controlled in Virginia. On December 23, 2022, the DEA announced it had begun consideration on the matter of placing Flubromazolam under temporary Schedule I status. [18] Later on July 25, 2023, the DEA published a pre-print notice that Flubromazolam would become temporarily scheduled as a Schedule I controlled substance from 26 July 2023 to 26 July 2025.[19]

See also

Notes and References

  1. Cook JM, et al. Stereospecific anxiolytic and anticonvulsant agents with reduced muscle-relaxant, sedative-hypnotic and ataxic effects. US7618958
  2. Web site: Patent EP 0072029 B1 - Triazolobenzazepines, process and intermediates for their preparation and medicines containing them . 22 October 1986 . 6 August 2015 . Borer R, Gerecke M, Kyburz E .
  3. Hester JB, Rudzik AD, Kamdar BV . 6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines which have central nervous system depressant activity . Journal of Medicinal Chemistry . 14 . 11 . 1078–81 . November 1971 . 5165540 . 10.1021/jm00293a015 .
  4. Web site: Flubromazolam . Cayman Chemical . 20 November 2015.
  5. Huppertz LM, Bisel P, Westphal F, Franz F, Auwärter V, Moosmann B . Characterization of the four designer benzodiazepines clonazolam, deschloroetizolam, flubromazolam, and meclonazepam, and identification of their in vitro metabolites . July 2015 . Forensic Toxicology . 33 . 2 . 388–395 . 10.1007/s11419-015-0277-6. 33278305 .
  6. Chaslot M, El Balkhi S, Robin T, Morichon J, Picard N, Saint-Marcoux F . Exploration des métabolites de 8 benzodiazépines de synthèse . Toxicologie Analytique et Clinique . June 2016 . 28 . 2 . S32 . 10.1016/j.toxac.2016.03.053.
  7. Pettersson Bergstrand M, Helander A, Hansson T, Beck O . Detectability of designer benzodiazepines in CEDIA, EMIT II Plus, HEIA, and KIMS II immunochemical screening assays . Drug Testing and Analysis . 9 . 4 . 640–645 . April 2017 . 27366870 . 10.1002/dta.2003 .
  8. Høiseth G, Tuv SS, Karinen R . Blood concentrations of new designer benzodiazepines in forensic cases . Forensic Science International . 268 . 35–38 . November 2016 . 27685473 . 10.1016/j.forsciint.2016.09.006 .
  9. Manchester KR, Maskell PD, Waters L . Experimental versus theoretical log D7.4, pKa and plasma protein binding values for benzodiazepines appearing as new psychoactive substances . Drug Testing and Analysis . 10 . 8 . 1258–1269 . March 2018 . 29582576 . 10.1002/dta.2387 . 31098917 .
  10. Wohlfarth A, Vikingsson S, Roman M, Andersson M, Kugelberg FC, Green H, Kronstrand R . Looking at flubromazolam metabolism from four different angles: Metabolite profiling in human liver microsomes, human hepatocytes, mice and authentic human urine samples with liquid chromatography high-resolution mass spectrometry . Forensic Science International . 274 . 55–63 . May 2017 . 27863836 . 10.1016/j.forsciint.2016.10.021 . Special Issue on the 54th Annual Meeting of the International Association of Forensic Toxicologists (TIAFT) Brisbane from August 28 to September 1, 2016 .
  11. Moosmann B, King LA, Auwärter V . Designer benzodiazepines: A new challenge . World Psychiatry . 14 . 2 . 248 . June 2015 . 26043347 . 4471986 . 10.1002/wps.20236 .
  12. Huppertz LM, Moosmann B, Auwärter V . Flubromazolam - Basic pharmacokinetic evaluation of a highly potent designer benzodiazepine . Drug Testing and Analysis . 10 . 1 . 206–211 . January 2018 . 28378533 . 10.1002/dta.2203 .
  13. Łukasik-Głębocka M, Sommerfeld K, Teżyk A, Zielińska-Psuja B, Panieński P, Żaba C . Flubromazolam--A new life-threatening designer benzodiazepine . Clinical Toxicology . 54 . 1 . 66–8 . 2016 . 26585557 . 10.3109/15563650.2015.1112907 . 4114360 .
  14. Web site: Fler ämnen föreslås bli klassade som narkotika eller hälsofarlig vara . 28 March 2024 . Folkhälsomyndigheten . Swedish.
  15. Web site: Verordnung des EDI über die Verzeichnisse der Betäubungsmittel, psychotropen Stoffe, Vorläuferstoffe und Hilfschemikalien . Der Bundesrat . German.
  16. Web site: The Misuse of Drugs Act 1971 (Amendment) order 2017. 4 April 2023.
  17. https://www.tga.gov.au/book-page/26-flubromazolam Scheduling proposals referred to the November 2015 meeting of the Advisory Committee on Medicines Scheduling (ACMS#16) 2.6 Flubromazolam
  18. Web site: Schedules of Controlled Substances: Temporary Placement of Etizolam, Flualprazolam, Clonazolam, Flubromazolam, and Diclazepam in Schedule I . Federal Register . 23 December 2022 . 4 April 2023.
  19. Web site: July 25, 2023 . Schedules of Controlled Substances: Temporary Placement of Etizolam, Flualprazolam, Clonazolam, Flubromazolam, and Diclazepam in Schedule I . 2023-07-25 . . DEA.

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