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diclazepamDiclazepam is a benzodiazepine often abused as a relaxant

Diclazepam (a.k.a. 2’chlorodiazepam or chlorodiazepam) was one of the first benzodiazepine designer drugs available online as a ‘research chemical’ and became readily available in the UK around 2014. Diclazepam is not approved as a medicine but has substantially grown in popularity for abuse since 2014. Leo Sternbach first synthesized diclazepam while at the pharmaceutical company Hoffman-La Roche in 1960. It is functionally analogous to diazepam and is considered a psychoactive depressant.

Its formal IUPAC name is 7-Chloro-5-(2-chlorophenyl)-1-methyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one. It has a molar mass of 319.185 g/mol and it has the formula C16H12Cl2N2O.

As with other benzodiazepines, the structure of diclazepam is based on rings of benzene and diazepine with nitrogen situated at R1 and R4. A methyl group is at the R1 position. A phenyl with a chlorine atom is attached to R5. The R7 is a chlorine atom instead of a carbon atom. At R2 there is a ketone (a double bonded oxygen group). Note that this ketone is also found in other benzodiazepines ending in ‘-azepam’.

Benzodiazepines are in muscle relaxants, sleeping pills, anti-anxiety medications, sedatives, and anticonvulsants. Users report lethargic states or the sense of sleep deprivation. Benzodiazepines can also be used before medicinal or dental procedures and through the duration of withdrawing from alcohol. Benzodiazepines may have long-term, intermediate, or short-term effects. Though safety tests for humans have not been conducted, generally, it is considered safe to use benzodiazepines for a short period of time.

Diclazepam, as with other benzodiazepines, bind to receptors thereby magnifying the effects of gamma aminobutyric acid (GABA), a neurotransmitter. Binding to sodium channels instead of benzodiazepine receptors may cause the anticonvulsant effects.

In animals, diclazepam is roughly ten times more potent than diazepam. Efficacy in humans is not recorded. Reports of human usage are ‘boring’ and include effects of lethargy, calmness, warmness and looseness in muscles, wobbliness, sleepiness, fogginess, dizziness, hypnosis, and temporary amnesia. Cognitively, effects may also include thought deceleration, and suppression of anxiety or emotions or information processing or analysis. Further it could induce delusions of sobriety or dream potentiation. Amnesic effects render diclazepam dangerous due to the potential for overdosing.

High dosages may result in feeling as though about to pass out, unconsciousness, injuries or fatalities. Dangerous interactions may occur in the presence of depressants, dissociatives, or stimulants.

The rough elimination half-life of diclazepam is 42 hours. During this time it is N-demethylated resulting in delorazepam, which is detectable in urine for six days after ingesting diclazepam. Lormetazepam and lorazepam (other metabolites) can be detected in urine for 11 and 19 days after ingestion, respectively. Concurrent with N-demethylation, cytochrome P450 exzymes augment hydroxylation.

See Also

  • Benzodiazepine
  • Chlorodiazepam
  • Diazepine
  • 2’chlorodiazepam
  • Lormetazepam
  • Gamma aminobutyric acid
  • GABA
  • Neurotransmitter
  • Diazepam
  • Delorazepam (also known as Nordiclazepam)
  • Lorazepam
  • Phenazepam
  • Ro5-4864 (or 4′-Chlorodiazepam)