Diclazepam

Fatal overdose may occur when benzodiazepines are combined with other depressants such as opiates, barbiturates, gabapentinoids, thienodiazepines, alcohol or other GABAergic substances.

It is strongly discouraged to combine these substances, particularly in common to heavy doses.

Not to be confused with Diazepam.

Summary sheet: Diclazepam

Diclazepam
Chemical Nomenclature
Common names	Diclazepam
Substitutive name	Ro5-3448, Chlorodiazepam, 2'-chloro-diazepam
Systematic name	7-chloro-5-(2-chlorophenyl)-1-methyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one
Class Membership
Psychoactive class	Depressant
Chemical class	Benzodiazepine
Routes of Administration
WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section. ⇣ Oral Dosage Threshold 0.5 mg Light 0.5 - 1 mg Common 1 - 3 mg Strong 3 - 4 mg Heavy 4 mg + Duration Total 8 - 12 hours Onset 10 - 45 minutes DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.
Interactions

Diclazepam (also known as chlorodiazepam) is a lesser-known novel depressant substance of the benzodiazepine class. It is a structural analog of diazepam (Valium) and is reported to produce similar effects.

Diclazepam was first synthesized by Leo Sternbach and his team at Hoffman-La Roche in 1960. Diclazepam is not currently marketed as a medication, but rather sold online as a research chemical.

Subjective effects are similar to diazepam and include anxiety suppression, disinhibition, anticonvulsant, hypnotic, muscle relaxing, and amnesia. In animal studies, it has a potency of approximately ten times that of diazepam. Its potency has not been systematically tested in humans, but its closest relatives and two main metabolites are lormetazepam with a potency value of x10-12 of delorazepam which is roughly x10 the potency of diazepam.

It should be noted that the sudden discontinuation of benzodiazepines can be potentially dangerous or life-threatening for individuals using regularly for extended periods of time, sometimes resulting in seizures or death. It is highly recommended to taper one's dose by gradually lowering the amount taken each day over a prolonged period of time rather than stopping use abruptly, as this can lead to severe, potentially life-threatening withdrawal symptoms.

Chemistry

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.

Pharmacology

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. 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. 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.

Subjective effects

Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWiki contributors. As a result, they should be viewed with a healthy degree of skepticism.

It is also 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 increasingly likely with higher doses and may include addiction, severe injury, or death ☠.

Physical effects

• • Muscle relaxation
  • Sedation - In terms of energy level alterations, this drug has the potential to be extremely sedating and often results in an overwhelmingly lethargic state. At higher levels, this causes users to suddenly feel as if they are extremely sleep deprived and have not slept for days, forcing them to sit down and generally feel as if they are constantly on the verge of passing out instead of engaging in physical activities. This sense of sleep deprivation increases proportional to dosage and eventually becomes powerful enough to force a person into complete unconsciousness.
  • Motor control loss
  • Respiratory depression
  • Dizziness

Paradoxical effects

• Paradoxical reactions to benzodiazepines such as increased seizures (in epileptics), aggression, increased anxiety, violent behavior, loss of impulse control, irritability and suicidal behavior sometimes occur (although they are rare in the general population, with an incidence rate below 1%).

  These paradoxical effects occur with greater frequency in recreational abusers, individuals with mental disorders, children, and patients on high-dosage regimes.

Cognitive effects

• The cognitive effects of diclazepam can be broken down into several components which progressively intensify proportional to dosage. The general head space of diclazepam is described by many as one of intense sedation and decreased inhibition. It contains a large number of typical depressants cognitive effects. The most prominent of these cognitive effects generally include:
  • Amnesia
  • Disinhibition
  • Anxiety suppression
  • Thought deceleration
  • Analysis suppression
  • Compulsive redosing
  • Emotion suppression - Although this compound primarily suppresses anxiety, it also dulls other emotions in a manner which is distinct but less intensive than that of antipsychotics.
  • Delusions of sobriety - This is the false belief that one is perfectly sober despite obvious evidence to the contrary such as severe cognitive impairment and an inability to fully communicate with others. It most commonly occurs at heavy dosages.
  • Dream potentiation

After effects

• • Rebound anxiety - Rebound anxiety is a commonly observed effect with anxiety relieving substances like benzodiazepines. It typically corresponds to the total duration spent under the substance's influence along with the total amount consumed in a given period, an effect which can easily lend itself to cycles of dependence and addiction.
  • Dream potentiation or Dream suppression
  • Residual sleepiness - While benzodiazepines can be used as an effective sleep-inducing aid, their effects may persist into the morning afterward, which may lead users to feeling "groggy" or "dull" for up to a few hours.
  • Thought deceleration
  • Thought disorganization
  • Irritability

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

Preparation methods

• 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.

Toxicity and harm potential

Radar plot showing relative physical harm, social harm, and dependence of benzodiazepines in comparison to other drugs.

Further information: Research chemicals § Toxicity and harm potential

Diclazepam likely has a low toxicity relative to dose. 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. 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. 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, 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.

Legal status

This legality section is a stub. As such, it may contain incomplete or wrong information. You can help by expanding it.

• Canada: All benzodiazepines are listed in Schedule IV.
• Germany: Diclazepam is controlled under Anlage II BtMG (Narcotics Act, Schedule II) as of November 21, 2015. It is illegal to manufacture, possess, import, export, buy, sell, procure or dispense it without a license.
• Poland: Diclazepam is under the IV-P group as of January 27, 2022. It is illegal to own, possess, and sell in Poland.
• Russia: Diclazepam is a Schedule III controlled substance since 2017.
• Switzerland: Diclazepam is a controlled substance specifically named under Verzeichnis E.
• Turkey: Diclazepam is a classed as drug and is illegal to possess, produce, supply, or import.
• United Kingdom: Diclazepam is a Class C controlled substance as of May 31, 2017. It is illegal to possess, produce or supply it.
• United States: Diclazepam is a Schedule I controlled substance as of January 23, 2023.

See also

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

External links

• Diclazepam (Wikipedia)
• Diclazepam (Isomer Design)