Chemistry:Diclazepam

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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.


Metabolism

Metabolism of this compound has been assessed,[6] 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.[7] 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.

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.[8]

United States

On December 23, 2022, the DEA announced it had begun consideration on the matter of placing Diclazepam under temporary Schedule I status.[9]

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.[10] On July 25, 2025, and effective the following day, the DEA extended the temporary scheduling until July 26, 2026.[11]

See also

References

  1. ↑ "Amino substituted benzophenone oximes and derivatives thereof" US patent 3136815
  2. ↑ "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. doi:10.1002/dta.2003. PMID 27366870. 
  3. ↑ "Blood concentrations of new designer benzodiazepines in forensic cases". Forensic Science International 268: 35–38. November 2016. doi:10.1016/j.forsciint.2016.09.006. PMID 27685473. 
  4. ↑ "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. doi:10.1002/dta.2387. PMID 29582576. https://rke.abertay.ac.uk/en/publications/527a634d-decc-4d3a-bdca-08659bb13ed6. 
  5. ↑ "The blood-to-plasma ratio and predicted GABAA-binding affinity of designer benzodiazepines". Forensic Toxicology 40 (2): 349–356. July 2022. doi:10.1007/s11419-022-00616-y. PMID 36454409. 
  6. ↑ Cite error: Invalid <ref> tag; no text was provided for refs named pmid24604775
  7. ↑ "Pharmacokinetics and bioavailability of intravenous and oral chlordesmethyldiazepam in humans". European Journal of Clinical Pharmacology 34 (1): 109–112. 1988. doi:10.1007/bf01061430. PMID 2896126. 
  8. ↑ "The Misuse of Drugs Act 1971 (Amendment) Order 2017". http://www.legislation.gov.uk/uksi/2017/634/contents/made. 
  9. ↑ "(Proposed Rule) Schedules of Controlled Substances: Temporary Placement of Etizolam, Flualprazolam, Clonazolam, Flubromazolam, and Diclazepam in Schedule I". DEA. December 23, 2022. https://www.federalregister.gov/documents/2022/12/23/2022-27278/schedules-of-controlled-substances-temporary-placement-of-etizolam-flualprazolam-clonazolam. 
  10. ↑ "Schedules of Controlled Substances: Temporary Placement of Etizolam, Flualprazolam, Clonazolam, Flubromazolam, and Diclazepam in Schedule I". DEA. July 25, 2023. https://public-inspection.federalregister.gov/2023-15748.pdf. 
  11. ↑ "Schedules of Controlled Substances: Extension of Temporary Placement of Clonazolam, Diclazepam, Etizolam, Flualprazolam, and Flubromazolam in Schedule I of the Controlled Substances Act" (in en). 2025-07-25. https://www.federalregister.gov/documents/2025/07/25/2025-14037/schedules-of-controlled-substances-extension-of-temporary-placement-of-clonazolam-diclazepam. 



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