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clonazolamClonazolam – A Designer Drug in the Benzodiazepine Family of Chemicals

Clonazolam (a.k.a. clonitrazolam) is designer drug in the benzodiazepine family of chemicals, and the subfamily nitrobenzodiazepines because of its nitro (NO2) group. This chemical is intended only for laboratory research.

The core chemical structure contains both benzene and diazepine rings. The structure also contains an amine group and at least one monohydroxylated metabolite.

Its formal IUPAC name is 6-(2-chlorophenyl)-1-methyl-8-nitro-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine. Its molar mass is 353.07 g/mol and its formula is C17H12ClN5O2.

Benzodiazepines are used as sedatives, sleeping pills, anti-anxiety medications, muscle relaxants, and as an anticonvulsant. They can also be used prior to dental or medical procedures or for alcohol withdrawal. Benzodiazepines can have short, intermediate, or long-term effects. While benzodiazepines are generally safe for quick and short usage, there is a high risk of overdosing on clonazolam.

This class of chemicals is often abused, leading to cycles of ups and downs through self-medication. It is reported to have heavy hypnotic effects. Seizures may occur if taken three days sequentially.

Clonazolam causes strong amnesia and sedation. Other reported effects include delusions, dizziness, dream potentiation, motor control loss, muscle relaxation and respiratory depression. This can pose a more significant risk than other benzodiazepines, even at a 0.5 mg oral dose.

Note that clonazolam is not approved as a medicine in any country. In Sweden, clonazolam is illegal, and in Canada it is listed under Schedule IV. The UK classifies it as Class C.

Clonazolam works by enhancing GABA (gamma-aminobutyric acid) at the GABAA receptor. GABA is a neurotransmitter. When GABA binds it triggers GABAA receptors to open chloride channels, enabling chlorine ions to enter neurons which make the neurons hyperpolarized, thus firing less frequently.

Clonazolam, as well as flubromazolam, deschloroetizolam and meclonazepam became available through online purchase in 2012, complementing other benzodiazepines available only through prescriptions.

Clonazolam, similar to flubromazolam and described as highly potent, was first synthesized in 1971. Like other drugs in this class, pharmaceutical companies synthesized clonazolam as a potential drug candidate. It has undergone basic animal testing. Along with nifoxipam and meclonazepam it has become particularly popular since 2014.

Clonazolam can be detected in human urine and blood through nano-liquid chromatography-high-resolution mass spectrometry and by ultra-performance liquid chromatography-tandem mass spectrometry, respectively. It can be detected in blood at a concentration as low as 0.0019 mg/L.

Clonazolam is metabolized extensively. It is excreted as its acetamino and amino metabolites. The best urine-testing target for clonazolam is 7-aminoclonazolam. Both the KIMS II and the CEDIA immunoassays are the best kits for detection in urine.

Overall the scientific, medical, toxicological, and psychiatric literature is behind the increasing use of this drug. Further pharmacological and chemical characterization is needed.

See Also:

  • Nitrobenzodiazepines
  • 7-aminoclonazolam
  • Flubromazolam
  • Adinazolam
  • Benzene
  • Alprazolam
  • Amine group
  • Benzodiazepine
  • Deschloroetizolam
  • Pyrazolam
  • Diazepine
  • Monohydroxylated metabolite
  • Drug testing
  • Clonazepam (this does not have a triazole ring)
  • Illicit drugs
  • Meclonazepam
  • Clonitrazolam
  • CEDIA immunoassay
  • Estazolam (licenced)
  • Triazolam
  • Nitrazolam
  • Nifoxipam