Diclazepam Explained

Diclazepam (Ro5-3448), also known as chlorodiazepam and 2'-chloro-diazepam, is a benzodiazepine and functional analog of diazepam. It was first synthesized by Leo Sternbach and his team at Hoffman-La Roche in 1960.[1] It is not currently approved for use as a medication, but rather sold as an unscheduled substance.[2] [3] [4] [5] Efficacy and safety have not been tested in humans.

In animal models, its effects are similar to diazepam, possessing long-acting anxiolytic, anticonvulsant, hypnotic, sedative, skeletal muscle relaxant, and amnestic properties.

Metabolism

Metabolism of this compound has been assessed, revealing diclazepam has an approximate elimination half-life of 42 hours and undergoes N-demethylation to delorazepam, which can be detected in urine for 6 days following administration of the parent compound.[6] Other metabolites detected were lorazepam and lormetazepam which were detectable in urine for 19 and 11 days, respectively, indicating hydroxylation by cytochrome P450 enzymes occurring concurrently with N-demethylation.

Legal status

United Kingdom

In the UK, diclazepam has been classified as a Class C drug by the May 2017 amendment to The Misuse of Drugs Act 1971 along with several other benzodiazepine drugs.[7]

United States

On December 23, 2022, the DEA announced it had begun consideration on the matter of placing Diclazepam under temporary Schedule I status.[8]

Later on July 25, 2023, the DEA published a pre-print notice that Diclazepam would become temporarily scheduled as a Schedule I controlled substance from 07/26/2023 to 07/26/2025.[9]

See also

Notes and References

  1. US . 3136815 . Amino substituted benzophenone oximes and derivatives thereof.
  2. 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 .
  3. 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 .
  4. 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 .
  5. Manchester KR, Waters L, Haider S, Maskell PD . The blood-to-plasma ratio and predicted GABAA-binding affinity of designer benzodiazepines . Forensic Toxicology . 40 . 2 . 349–356 . July 2022 . 36454409 . 9715504 . 10.1007/s11419-022-00616-y . 247455284 . free .
  6. Bareggi SR, Truci G, Leva S, Zecca L, Pirola R, Smirne S . Pharmacokinetics and bioavailability of intravenous and oral chlordesmethyldiazepam in humans . European Journal of Clinical Pharmacology . 34 . 1 . 109–112 . 1988 . 2896126 . 10.1007/bf01061430 . 1574555 .
  7. Web site: The Misuse of Drugs Act 1971 (Amendment) Order 2017.
  8. Web site: December 23, 2022 . (Proposed Rule) Schedules of Controlled Substances: Temporary Placement of Etizolam, Flualprazolam, Clonazolam, Flubromazolam, and Diclazepam in Schedule I . . DEA.
  9. 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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