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Adinazolam

Adinazolam molecule structureAdinazolam molecule structure
8-Chloro-1-((dimethylamino)methyl)-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
Deracyn, U-41,123, U-41123, AdinazolamumOpen in Piru

Adinazolam is a triazolobenzodiazepine1, a designer benzodiazepine expected to have central nervous system depressant-like effects similar to those of other known benzodiazepines2 with anxiolytic (reported in animal models)1, sedative1, anticonvulsant (reported in animal models)1, and antidepressant (reported in animal models, with mixed results in human effectiveness studies)1 properties. Its fused triazole ring distinguishes it within the benzodiazepine class. Jackson B. Hester developed adinazolam while seeking to enhance alprazolam’s antidepressant effects. It is sold as tablets or powders under its chemical name1, although it was never FDA approved1.

Dosage & Duration

Log in Piru

Dosage

Doses are population estimates that vary widely between individuals.

Threshold~5 mg
Light5-15 mg
Moderate15-30 mg
Strong30-50 mg
Heavy50+ mg

Duration

Onset10-25 minutes
After Effects1-16 hours
Total2-5 hours

Subjective Effects

Subjective Effects not written up yet

Reagent Testing

Expected colorimetric results for common reagent tests. Colors show reaction change over 1–2 minutes.

Marquis(MQ)
No reaction
No reaction
Mecke(ME)
No reaction
No reaction
Mandelin(MD)
No reaction
No reaction
Liebermann(LB)
No reaction
No reaction
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Pharmacology

Pharmacodynamics

Adinazolam positively allosterically modulates central benzodiazepine sites on GABA-A receptors, increasing the receptor's response to GABA and enhancing chloride influx and neuronal inhibition. Adinazolam and N-desmethyladinazolam bind to benzodiazepine receptors, as measured by displacement of [3H]flunitrazepam, with Ki values of 208 and 6.96 nM, respectively; modelling predicted moderate binding affinity of adinazolam at the GABA-A receptor.1 Benzodiazepine-site activity is associated with GABA-A receptor subunits implicated in sedative, anticonvulsant, anxiolytic, and muscle-relaxant actions.

Pharmacokinetics

Adinazolam is primarily metabolized by N-dealkylation through enteric and hepatic pathways. It is a CYP3A4 substrate, with intestinal metabolism contributing substantially before hepatic metabolism.1 In human liver microsomes, cytochrome P450-mediated N-demethylation converted adinazolam to N-desmethyladinazolam and then to didesmethyladinazolam.3

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
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Tolerance

Tolerance timelines are rules of thumb, not exact schedules, and vary widely between individuals and use patterns.

Full Tolerance
Prolonged use could lead to tolerance, with higher doses required to achieve the same therapeutic effects.

Harm Potential

Addiction & Dependence

Psychological

High

Extended use carries the possibility of psychological dependence, where individuals may become reliant on the medication to manage anxiety symptoms. As a benzodiazepine, it is classified as habit-forming.

Physical

High

Prolonged use can result in physical dependence. Reducing the dose too quickly may cause withdrawal, from rebound anxiety and insomnia through severe outcomes such as seizures.

Toxicity

Central Nervous System

Prolonged use may contribute to cognitive impairment affecting memory, concentration, and overall cognitive function; these effects are associated with extended therapeutic or recreational use patterns.

Seizure Risk

Moderate

Seizures can occur as a withdrawal symptom following rapid dose reduction or cessation after prolonged use. This risk is associated with benzodiazepine dependence rather than acute intoxication.

History & Culture

Adinazolam was developed by Jackson B. Hester, who sought to enhance the antidepressant properties of alprazolam, another compound he developed. It was studied as an antidepressant during the 1980s and 1990s4 but was never approved by the FDA1 or…

Legality

Legality not written up yet

References

Source Pages

  1. DrugBank: Adinazolam
  2. TripSit: Factsheet – Adinazolam
  3. Wikipedia

Citations

  1. Adinazolam: Critical Review Report. World Health Organization (2022). https://cdn.who.int/media/docs/default-source/controlled-substances/45th-ecdd/adinazolam_draft.pdf?sfvrsn=17900a82_1123456789101112
  2. Schedules of Controlled Substances: مراجعات and Recommendations to WHO. Federal Register (2022). https://www.govinfo.gov/content/pkg/FR-2022-08-03/pdf/2022-16572.pdf1
  3. Kinetic characterization and identification of the enzymes responsible for the hepatic biotransformation of adinazolam and N-desmethyladinazolam in man. Journal of Pharmacy and Pharmacology (1998). https://doi.org/10.1111/j.2042-7158.1998.tb06859.x1
  4. Anxiolytic Antidepressant Augmentation. Journal of Clinical Psychiatry (1998). https://www.psychiatrist.com/product/anxiolytic-antidepressant-augmentation-pdf1

Further Reading

  1. Amsterdam et al. 1986 - Adinazolam and imipramine in major depressive disorder
  2. Brogden RN et al. - Adinazolam review of pharmacology & therapeutic use
  3. Brunetti et al. 2021 - Designer Benzodiazepines: A Review of Toxicology and Public Health Risks
  4. Feighner JP et al. 1990 - Controlled trial of adinazolam vs desipramine in geriatric depression
  5. Feighner JP et al. Controlled trial of adinazolam vs desipramine in geriatric depression
  6. Moosmann et al. 2016 - Characterization and metabolism of designer benzodiazepines
  7. Pieters et al. 2021 - 'New/Designer Benzodiazepines': Analysis of Literature and Trip Reports
  8. Psychotropics Database – Adinazolam monograph
  9. Reddit user reports compilation (search query: "Adinazolam experience")
  10. Schütz E. Pharmacokinetics of adinazolam in humans
  11. Sethy et al. 1984 - Determination of biological activity of adinazolam and metabolites
  12. Tripsitter Adinazolam: A Powerful Benzodiazepine Known For Causing Mental Unpleasantness
  13. Nowak et al. 2021 - Fatal intoxication with U-47700 in combination with other NPS (N-ethylhexedrone, adinazolam, 4-CIC, 4-CMC) confirmed by identification and quantification in autopsy specimens and evidences

Article Status

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