Clonazolam

Summary

Clonazolam (also known as clonitrazolam) is a drug of the triazolobenzodiazepine (TBZD) class, which are benzodiazepines (BZDs) fused with a triazole ring. Little research has been done about its effects and metabolism, and is sold online as a designer drug.[2][3][4][5][6]

Clonazolam
Clinical data
Dependence
liability
Very high
Routes of
administration
Oral
Legal status
Legal status
Identifiers
  • 6-(2-Chlorophenyl)-1-methyl-8-nitro-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
CAS Number
  • 33887-02-4
PubChem CID
  • 12317881
ChemSpider
  • 15468596
UNII
  • HJH52YYC1X
KEGG
  • C22814
CompTox Dashboard (EPA)
  • DTXSID301014166 Edit this at Wikidata
Chemical and physical data
FormulaC17H12ClN5O2
Molar mass353.77 g·mol−1
3D model (JSmol)
  • Interactive image
  • CC1=NN=C2N1C3=C(C=C(C=C3)[N+](=O)[O-])C(=NC2)C4=CC=CC=C4Cl
  • InChI=1S/C17H12ClN5O2/c1-10-20-21-16-9-19-17(12-4-2-3-5-14(12)18)13-8-11(23(24)25)6-7-15(13)22(10)16/h2-8H,9H2,1H3
  • Key:XJRGLCAWBRZUFC-UHFFFAOYSA-N

The synthesis of clonazolam was first reported in 1971 and the drug was described as the most active compound in the series tested.[7]

Depending on dose consumed, clonazolam may pose comparatively higher risk than other designer benzodiazepines due to its ability to produce strong sedation and amnesia at doses as small as 0.5 mg.[2][8]

Legality edit

United Kingdom edit

In the UK, clonazolam 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.[9]

United States edit

It is a Schedule I controlled substance in the United States and is not FDA approved for human consumption. Virginia State Law has declared all of the following medications are now schedule I: clonazolam, etizolam, flualprazolam, flubromazolam, and flubromazepam.[10] Minnesota declared clonazolam a Schedule I drug in August 2020.

On December 23, 2022, the DEA announced it had begun consideration on the matter of placing Clonazolam under temporary Schedule I status.[11] Later on July 25, 2023, the DEA published a pre-print notice that Clonazolam would become temporarily scheduled as a controlled substance from 07/26/2023 to 07/26/2025.[12]

Australia edit

In Australia, clonazolam is Schedule 9 under federal law.[13]

Sweden edit

Sweden's public health agency suggested classifying clonazolam as a hazardous substance on June 1, 2015.[14]

Effects edit

Clonazolam's effects are similar to other benzodiazepines, such as anxiolysis, disinhibition, lethargy, muscle relaxation, and euphoria.[2][8] While no dose of clonazolam is considered "safe" due to its lack of research and extreme potency, doses higher than 0.5 mg can cause benzodiazepine overdose in some individuals.[2][8] The effects of a benzodiazepine overdose include sedation, confusion, amnesia, insufficient breathing, loss of consciousness, and death.[2][8] Because dependence can occur in a short period of time, or even with a large initial dose, withdrawal symptoms (including seizures and death) may occur acutely following the period of intoxication.[2][8]

See also edit

References edit

  1. ^ Anvisa (31 March 2023). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 4 April 2023). Archived from the original on 2023-08-03. Retrieved 2023-08-16.
  2. ^ a b c d e f Huppertz LM, Bisel P, Westphal F, et al. (July 2015). "Characterization of the four designer benzodiazepines clonazolam, deschloroetizolam, flubromazolam, and meclonazepam, and identification of their in vitro metabolites". Forensic Toxicology. 33 (2): 388–395. doi:10.1007/s11419-015-0277-6. S2CID 33278305.
  3. ^ Meyer MR, Bergstrand MP, Helander A, Beck O (May 2016). "Identification of main human urinary metabolites of the designer nitrobenzodiazepines clonazolam, meclonazepam, and nifoxipam by nano-liquid chromatography-high-resolution mass spectrometry for drug testing purposes". Analytical and Bioanalytical Chemistry. 408 (13): 3571–91. doi:10.1007/s00216-016-9439-6. PMID 27071765. S2CID 25831532.
  4. ^ Chaslot M, El Balkhi S, Robin T, Morichon J, Picard N, Saint-Marcoux F (June 2016). "Exploration des métabolites de 8 benzodiazépines de synthèse". Toxicologie Analytique et Clinique. 28 (2): S32. doi:10.1016/j.toxac.2016.03.053.
  5. ^ Pettersson Bergstrand M, Helander A, Hansson T, Beck O (April 2017). "Detectability of designer benzodiazepines in CEDIA, EMIT II Plus, HEIA, and KIMS II immunochemical screening assays". Drug Testing and Analysis. 9 (4): 640–645. doi:10.1002/dta.2003. PMID 27366870.
  6. ^ Høiseth G, Tuv SS, Karinen R (November 2016). "Blood concentrations of new designer benzodiazepines in forensic cases". Forensic Science International. 268: 35–38. doi:10.1016/j.forsciint.2016.09.006. PMID 27685473.
  7. ^ Hester JB, Rudzik AD, Kamdar BV (November 1971). "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. doi:10.1021/jm00293a015. PMID 5165540.
  8. ^ a b c d e Moosmann B, King LA, Auwärter V (June 2015). "Designer benzodiazepines: A new challenge". World Psychiatry. 14 (2): 248. doi:10.1002/wps.20236. PMC 4471986. PMID 26043347.
  9. ^ "The Misuse of Drugs Act 1971 (Amendment) Order 2017". Retrieved 2023-04-15.
  10. ^ "§ 54.1-3446. Schedule I".
  11. ^ "(Proposed Rule) Schedules of Controlled Substances: Temporary Placement of Etizolam, Flualprazolam, Clonazolam, Flubromazolam, and Diclazepam in Schedule I". Federal Register. DEA. 23 December 2022.
  12. ^ "Schedules of Controlled Substances: Temporary Placement of Etizolam, Flualprazolam, Clonazolam, Flubromazolam, and Diclazepam in Schedule I" (PDF). Federal Register. DEA. 25 July 2023. Retrieved 2023-07-25.
  13. ^ "Therapeutic Goods (Poisons Standard—February 2023) Instrument 2023". legislation.gov.au. Retrieved 2023-04-15.
  14. ^ "23 nya ämnen kan klassas som narkotika eller hälsofarlig vara" (in Swedish). Folkhälsomyndigheten. Retrieved 2015-08-06.