Diclazepam (Ro5-3448), also known aschlorodiazepam and2'-chloro-diazepam, is abenzodiazepine andfunctional analog ofdiazepam. It was first synthesized byLeo 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 undergoesN-demethylation todelorazepam, which can be detected in urine for 6 days following administration of the parent compound.[8] Other metabolites detected werelorazepam andlormetazepam which were detectable in urine for 19 and 11 days, respectively, indicatinghydroxylation bycytochrome P450 enzymes occurring concurrently withN-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] On July 25, 2025, and effective the following day, the DEA extended the temporary scheduling until July 26, 2026.[12]
^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.doi:10.1002/dta.1628.PMID24604775.
^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.
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