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.
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.
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]
^
abMoosmann B, Bisel P, Auwärter V (July–August 2014). "Characterization of the designer benzodiazepine diclazepam and preliminary data on its metabolism and pharmacokinetics". Drug Testing and Analysis. 6 (7–8): 757–763.
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^US 3136815, "Amino substituted benzophenone oximes and derivatives thereof"
^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.
PMID27366870.
^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.
PMID27685473.
^Bareggi SR, Truci G, Leva S, Zecca L, Pirola R, Smirne S (1988). "Pharmacokinetics and bioavailability of intravenous and oral chlordesmethyldiazepam in humans". European Journal of Clinical Pharmacology. 34 (1): 109–112.
doi:
10.1007/bf01061430.
PMID2896126.
S2CID1574555.