Diclazepam

Composition

Diclazepam is a drug of the benzodiazepine class. Benzodiazepine drugs contain a benzene ring fused to a diazepine ring, which is a seven-membered ring with the two nitrogen constituents located at R₁ and R₄. At R₁, diclazepam is substituted with methyl group. Further, the benzodiazepine ring is bonded at R₅ to a 2-chlorinated phenyl ring. R₇ of the benzyl ring is also substituted with a chlorine group. Diclazepam also contains an oxygen group double bonded to R₂ of its diazepine ring to form a ketone. This oxygen substitution at R₂ is shared with other benzodiazepine drugs with the suffix -azepam.

Benzodiazepines produce a variety of effects by binding to the benzodiazepine receptor site and magnifying the efficiency and effects of the neurotransmitter gamma aminobutyric acid (GABA) by acting on its receptors.^[9] As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the sedating (or calming effects) of diclazepam on the nervous system.

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.^[10] 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 anticonvulsant properties of benzodiazepines may be, in part or entirely, due to binding to voltage-dependent sodium channels rather than benzodiazepine receptors.^[11]

Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), a research literature based on anecdotal reports and the personal experiences of PsychonautWiki contributors. As a result, they should be regarded with a healthy degree of skepticism. It is worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become much more likely with higher doses and may include addiction, serious injury, or death.

Experience reports

Anecdotal reports which describe the effects of this compound within our experience index include:

• Experience: 100ug ALD-52 - Nice weekend trip

Additional experience reports can be found here:

• Erowid Experience Vaults: Diclazepam

• Volumetric liquid dosing - If one's benzodiazepines are in powder form, they are unlikely to weigh out accurately without the most expensive of scales due to their extreme potency. To avoid this, one can dissolve the benzodiazepine volumetrically into a non-polar solution such as propylene glycol and dose it accurately based upon the methodological instructions linked within this tutorial.

Diclazepam likely has a low toxicity relative to dose.^[18] However, it is potentially lethal when mixed with depressants like alcohol or opioids.

It is strongly recommended that one use harm reduction practices, such as volumetric dosing, when using this substance to ensure the accurate administration of the intended dose.

Tolerance and addiction potential

Diclazepam is extremely physically and psychologically addictive.

Tolerance will develop to the sedative-hypnotic effects within 3-4 days of continuous use. After cessation, the tolerance returns to baseline in 7 - 14 days. However, in certain cases, this may take significantly longer in a manner which is proportional to the duration and intensity of one's long-term usage.

Withdrawal symptoms or rebound symptoms may occur after ceasing usage abruptly following a few weeks or longer of steady dosing, and may necessitate a gradual dose reduction. For more information on tapering from benzodiazepines in a controlled manner, please see this guide.

Benzodiazepine discontinuation is notoriously difficult; it is potentially life-threatening for individuals using regularly to discontinue use without tapering their dose over a period of weeks. There is an increased risk of hypertension, seizures, and death.^[19] Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal.

Diclazepam presents cross-tolerance with all GABAergics, meaning that after its consumption all benzodiazepines will have a reduced effect.

Overdose

Benzodiazepine overdose may occur when a benzodiazepine is taken in extremely heavy quantities or concurrently with other depressants. This is particularly dangerous with other GABAergic depressants such as barbiturates and alcohol since they work in a similar fashion, but bind to distinct allosteric sites on the GABA_A receptor. Thus, their effects potentiate one another. Benzodiazepines increase the frequency in which the chlorine ion pore opens on the GABA_A receptor while barbiturates increase the duration in which they are open, meaning when both are consumed, the ion pore will open more frequently and stay open longer^[20]. Benzodiazepine overdose is a medical emergency that may lead to a coma, permanent brain injury or death if not treated promptly and properly. Symptoms of a benzodiazepine overdose may include severe thought deceleration, slurred speech, confusion, delusions, respiratory depression, coma or death. Benzodiazepine overdoses may be treated effectively in a hospital environment, with generally favorable outcomes. Benzodiazepine overdoses are sometimes treated with flumazenil, a GABA_A antagonist,^[21] however care is primarily supportive in nature.

Dangerous interactions

Although many drugs are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption.

• Depressants (1,4-Butanediol, 2-methyl-2-butanol, alcohol, barbiturates, GHB/GBL, methaqualone, opioids) - This combination can result in dangerous or even fatal levels of respiratory depression. These substances potentiate the muscle relaxation, sedation and amnesia caused by one another and can lead to unexpected loss of consciousness at high doses. There is also an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
• Dissociatives - This combination can result in an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
• Stimulants - It is dangerous to combine benzodiazepines with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of benzodiazepines, which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of benzodiazepines will be significantly increased, leading to intensified disinhibition as well as other effects. If combined, one should strictly limit themselves to only dosing a certain amount of benzodiazepines per hour. This combination can also potentially result in severe dehydration if hydration is not monitored.

• Canada: All benzodiazepines are listed in Schedule IV.^[22]
• Germany: Diclazepam is controlled under Anlage II BtMG (Narcotics Act, Schedule II)^[23] as of November 21, 2015.^[24] It is illegal to manufacture, possess, import, export, buy, sell, procure or dispense it without a license.^[25]
• Russia: Diclazepam is a Schedule III controlled substance since 2017.^[26]
• Switzerland: Diclazepam is a controlled substance specifically named under Verzeichnis E.^[27]
• Turkey: Diclazepam is a classed as drug and is illegal to possess, produce, supply, or import.^[28]
• United Kingdom: Diclazepam is a Class C controlled substance as of May 31, 2017. It is illegal to possess, produce or supply it.^[29]
• United States: Diclazepam is unregulated in the United States.^{[citation needed]}

• Responsible use
  • Volumetric liquid dosing
• Depressants
• Benzodiazepines
• Diazepam
• Etizolam

• Diclazepam (Wikipedia)
• Diclazepam (Isomer Design)