Diclazepam

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Diclazepam
Clinical data
Routes of
administration		Oral, sublingual
Legal status
Legal status
Pharmacokinetic data
Bioavailability?
MetabolismHepatic
Elimination half-life~42 hours[2]
ExcretionRenal
Identifiers
  • 7-Chloro-5-(2-chlorophenyl)-1-methyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one
JSmol)
  • CN1C2=C(C=C(C=C2)Cl)C(C3=C(Cl)C=CC=C3)=NCC1=O
  • InChI=1S/C16H12Cl2N2O/c1-20-14-7-6-10(17)8-12(14)16(19-9-15(20)21)11-4-2-3-5-13(11)18/h2-8H,9H2,1H3
  • Key:VPAYQWRBBOGGPY-UHFFFAOYSA-N
 ☒NcheckY (what is this?)  (verify)

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.[3] It is not currently approved for use as a medication, but rather sold as an unscheduled substance.[4][5][6][7] Efficacy and safety have not been tested in humans.

In animal models, its effects are similar to diazepam, possessing long-acting

amnestic properties.[citation needed
]

Metabolism

Metabolism of this compound has been assessed,[2] 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.[8] 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.[9]

United States

On December 23, 2022, the DEA announced it had begun consideration on the matter of placing Diclazepam under temporary Schedule I status.[10]

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.[11]

See also

References

  1. ^ Anvisa (2023-03-31). "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 2023-04-04). Archived from the original on 2023-08-03. Retrieved 2023-08-16.
  2. ^
    PMID 24604775
    .
  3. ^ US 3136815, "Amino substituted benzophenone oximes and derivatives thereof" 
  4. PMID 27366870
    .
  5. PMID 27685473
    .
  6. PMID 29582576
    .
  7. S2CID 247455284
    .
  8. S2CID 1574555
    .
  9. ^ "The Misuse of Drugs Act 1971 (Amendment) Order 2017".
  10. DEA
    . December 23, 2022.
  11. DEA
    . July 25, 2023. Retrieved 2023-07-25.
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