Metizolam

4-(2-chlorophenyl)-2-ethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine

Desmethyletizolam

Psychoactive Class

Depressant Anxiolytic GABAergic Muscle Relaxant

Chemical Class

Metizolam is a synthetic depressant of the thienotriazolodiazepine class and the demethylated analogue of etizolam.¹ A Japanese company patented it in 1995 as a possible anxiolytic, but it saw little to no human use before appearing as a grey-area research chemical in September 2015. Compared to etizolam, it is reportedly half as potent with a 60% longer half-life, producing similar anxiolytic, sedative, and muscle relaxant effects.

Dosage & Duration

Dosage

Threshold1 mg

Light1-2 mg

Moderate2-4 mg

Strong4-6 mg

Heavy6+ mg

Duration

Onset30-90 minutes

After Effects10-30 hours

Total5-8 hours

Half-life

~3.4 hours

Subjective Effects

Effects vary widely by individual, dose, and context.

Physical

Sedation Motor control loss Respiratory depression Muscle relaxation Dizziness

Cognitive

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

Forked from Subjective Effect Documentation work

by Josie KinsAugust 2016.

Reagent Testing

Loading reagent data

Expected colorimetric results are being prepared.

Pharmacology

Pharmacodynamics

Metizolam acts as a full agonist at the benzodiazepine binding site of the GABA-A receptor, enhancing the efficiency and effects of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA).² It is the demethylated analogue of etizolam, reported to be approximately half as potent.

Pharmacokinetics

Metizolam is absorbed fairly rapidly, with peak plasma levels reached between 30 minutes and 2 hours, and has a mean elimination half-life of approximately 3.4 hours. As a thienotriazolodiazepine, it is easily oxidized and rapidly metabolized,³ which contributes to a lower risk of accumulation even after prolonged use.

Metabolitesnone documented yet

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

Repeated dosing for only a few days can reduce sensitivity to metizolam's sedative-hypnotic effects.

Baseline Reset

1-2 weeks

Half Tolerance

3-7 days

Cross Tolerance

Thienodiazepines, Benzodiazepines

Harm Potential

Addiction & Dependence

Psychological

High

Thienodiazepines are described as extremely addictive with significant abuse potential.⁴ Compulsive redosing is a commonly reported effect, and tolerance to sedative-hypnotic effects develops within a couple days of repeated administration.⁵

Physical

Extremely High

Physical dependence develops with regular use. Abrupt discontinuation can be potentially dangerous or life-threatening, sometimes resulting in seizures or death.⁶⁷ Withdrawal symptoms include rebound anxiety and insomnia.⁴ Gradual tapering over weeks is strongly recommended for regular users.⁶

Psychosis Risk

Paradoxical reactions including violent behavior, loss of impulse control, and irritability occur rarely, with an incidence rate below 1% in the general population.⁸ These occur with greater frequency in recreational abusers, individuals with mental disorders, children, and patients on high-dose regimes.⁸ Delusions may occur during overdose.

Seizure Risk

Seizure risk is primarily associated with abrupt discontinuation following regular use, which can be life-threatening.⁶⁷ Paradoxical seizures during use are rare, occurring with greater frequency in epileptics. Drugs that lower the seizure threshold should be avoided during withdrawal.

History & Culture

Metizolam was first patented in 1995 by a Japanese pharmaceutical company as a potential medication for treating anxiety disorders. Despite this early patent, the compound was never developed for clinical use and has no documented history of medical application.…

Legality

By Country

CanadaSchedule IV

Controlled under the Controlled Drugs and Substances Act.¹⁰ All benzodiazepine compounds are classified as Schedule IV controlled substances in Canada, which restricts possession, trafficking, and importation.¹⁰

SwedenIllegal

Classified as an illegal substance on January 26, 2016, following its emergence on the designer drug market.¹⁴ Possession, sale, and distribution are prohibited.

TurkeyIllegal

Classified as a controlled drug under Turkish narcotics legislation.¹⁶ Possession, production, supply, and importation are all prohibited activities.¹⁶

GermanyNpSG (Controlled)

Regulated under the Neue-psychoaktive-Stoffe-Gesetz (New Psychoactive Substances Act) since July 18, 2019.¹¹ Production, importation with intent to distribute, administration to others, and trafficking are criminally punishable offenses.¹² Possession is prohibited but does not carry criminal penalties.¹³

SwitzerlandControlled (Verzeichnis E)

Specifically named as a controlled substance under Verzeichnis E of Swiss narcotics scheduling.¹⁵ Production, distribution, and possession without authorization are prohibited.¹⁵

United KingdomPsychoactive Substances Act

Production, supply, and importation are prohibited under the Psychoactive Substances Act 2016, effective May 26, 2016.¹⁷ This blanket legislation covers psychoactive substances not specifically exempted.¹⁷ Personal possession is not criminalized under this act.¹⁷

References

Source Pages

Citations

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