Routes ofadministration Oral, sublingual Metabolism Excretion Renal | Bioavailability ? Biological half-life ~42 hours Molar mass 319.185 g/mol | |
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Legal status CA: Schedule IVDE: Anlage II (Prohibited) | ||
Diclazepam experience report
Diclazepam (Ro5-3448), also known as chlorodiazepam and 2'-chloro-diazepam, is a benzodiazepine designer drug and functional analog of diazepam. It was first synthesized by Leo Sternbach and his team at Hoffman-La Roche in 1960. It is not currently approved for use as a medication, but rather sold as a designer drug. Efficacy and safety have not been tested in humans.
Contents
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. 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. The protein-binding of this compound has not been analysed but the figures for the metabolites are, delorazepam >90%, lorazepam 91.5% (parenterally) & 85% (orally) and delorazepam >90%.