Diclazepam

Ro5-3448

Chlorodiazepam, 2'-chloro-diazepam

Psychoactive Class

Depressant Anxiolytic Sedative Muscle Relaxant Anticonvulsant GABAergic

Chemical Class

Diclazepam is a benzodiazepine and functional analog of diazepam (Valium).¹ Leo Sternbach and colleagues at Hoffman-La Roche first synthesized it in 1960,²¹ but it is not approved for medical use and is instead sold as a research chemical.¹ In animal models, diclazepam exhibits long-acting anxiolytic, sedative, hypnotic, anticonvulsant, muscle relaxant, and amnestic properties comparable to diazepam.¹³ Its efficacy and safety have not been evaluated in humans.¹³

Dosage & Duration

Dosage

Threshold~0.5 mg

Light0.5-1 mg

Moderate1-2 mg

Strong2-4 mg

Heavy4+ mg

Duration

Onset15-90 minutes

After Effects1-24 hours

Total8-12 hours

Half-life

~42 hours

Subjective Effects

Effects vary widely by individual, dose, and context.

Physical

The physical effects of diclazepam can be broken down into several components which progressively intensify proportional to dosage.

Motor control loss Respiratory depression Muscle relaxation Dizziness

Cognitive

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 depressant cognitive 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.

Amnesia Anxiety suppression Thought deceleration Disinhibition Information processing suppression Euphoria Compulsive redosing

Forked from Subjective Effect Documentation

by Josie KinsSeptember 2015.

Reagent Testing

Loading reagent data

Expected colorimetric results are being prepared.

Pharmacology

Pharmacodynamics

Diclazepam acts as a positive allosteric modulator of the GABA-A receptor at the benzodiazepine binding site, enhancing the inhibitory activity of gamma-aminobutyric acid (GABA). In animal models, it exhibits approximately ten times the potency of diazepam. Its anticonvulsant properties may also involve binding to voltage-dependent sodium channels, a mechanism that has been proposed for benzodiazepines more broadly.⁴ Efficacy and safety have not been systematically tested in humans.

Pharmacokinetics

Diclazepam has an approximate elimination half-life of 42 hours.⁵ It undergoes N-demethylation to produce delorazepam, with concurrent hydroxylation by cytochrome P450 enzymes yielding lorazepam and lormetazepam as additional metabolites.⁵ Delorazepam is detectable in urine for approximately 6 days following administration of the parent compound, while lorazepam and lormetazepam remain detectable for up to 19 and 11 days, respectively.⁵

Interactions

Dangerous

Highest risk

These combinations are considered extremely harmful and should always be avoided. Reactions to these drugs taken in combination are highly unpredictable and have a potential to cause death.

AlcoholGHB/GBLOpioidsTramadol

Unsafe

Avoid

There is considerable risk of physical harm when taking these combinations, they should be avoided where possible.

DiphenhydraminePCP

Caution

Use caution

These combinations are not usually physically harmful, but may produce undesirable effects, such as physical discomfort or overstimulation. Extreme use may cause physical health issues. Synergistic effects may be unpredictable. Care should be taken when choosing to use this combination.

DXMKetamineMXE

TripSit

Tolerance

Full Tolerance

Tolerance to the sedative-hypnotic effects develops rapidly, typically within 3-4 days of continuous use.

Cross Tolerance

GABAergic substances, Benzodiazepines

Baseline Reset

Tolerance returns to baseline within 7-14 days after cessation of use. However, following prolonged or intensive use, this process may take significantly longer in proportion to the duration and intensity of prior consumption.

Harm Potential

Addiction & Dependence

Psychological

Extremely High

Diclazepam is described as extremely psychologically addictive. Compulsive redosing is commonly reported, and rebound anxiety following use can drive cycles of dependence and repeated administration.⁶

Physical

Extremely High

Physical dependence develops with regular use and can become severe. Abrupt discontinuation after extended use is potentially life-threatening, with risks including hypertension, seizures, and death.⁶ Gradual tapering over weeks is essential for safely discontinuing use.⁷

Psychosis Risk

Paradoxical reactions including aggression, violent behavior, irritability, and loss of impulse control occur rarely, with an incidence rate below 1% in the general population.⁸ These effects are more common in recreational abusers, individuals with mental disorders, children, and those on high-dose regimens. Delusions of sobriety may occur at heavy doses.

Seizure Risk

Diclazepam possesses anticonvulsant properties during active use. Paradoxical increases in seizures may occur rarely in epileptics, with incidence below 1%. The primary seizure risk is during abrupt withdrawal from chronic use, where discontinuation without tapering can trigger potentially fatal seizures.⁹⁷

History & Culture

Diclazepam was first synthesized in 1960 by Leo Sternbach and his research team at Hoffman-La Roche, the same laboratory responsible for developing numerous other benzodiazepines including diazepam (Valium).¹⁰ Despite being created during the golden age of…

Legality

By Country

United StatesSchedule I

Controlled as a Schedule I substance under the Controlled Substances Act since January 23, 2023. Classified as having high abuse potential with no currently accepted medical use.

GermanyAnlage II BtMG

Controlled under Anlage II of the Betäubungsmittelgesetz (Narcotics Act) since November 21, 2015.¹³ Manufacturing, possession, import, export, purchase, sale, procurement, or dispensing without a license is prohibited.

RussiaSchedule III

Controlled as a Schedule III substance since 2017 under Russian narcotics legislation.

TurkeyIllegal

Classified as a controlled drug substance.¹⁰ Possession, production, supply, and importation are prohibited.

CanadaSchedule IV CDSA

Listed as a controlled benzodiazepine under Schedule IV of the Controlled Drugs and Substances Act. All benzodiazepines fall under this classification in Canada.

PolandIV-P (controlled)

Classified under the IV-P group since January 27, 2022.¹⁴ Ownership, possession, and sale are illegal.

SwitzerlandControlled (Verzeichnis E)

Specifically named as a controlled substance under Verzeichnis E of Swiss narcotics legislation.

United KingdomClass C

Controlled as a Class C substance under the Misuse of Drugs Act since May 31, 2017.¹¹ Possession, production, and supply are illegal.

References

Source Pages

Citations

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