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    Adinazolam molecular structure

    Adinazolam Stats & Data

    Deracyn U-41,123 Adinazolamum
    NPS DataHub
    MW351.84
    FormulaC19H18ClN5
    CAS37115-32-5
    IUPAC1-(8-chloro-6-phenyl-4H-[1,2,4]triazolo[4,5-a][1,4]benzodiazepin-1-yl)-N,N-dimethylmethanamine
    SMILESCN(C)Cc1nnc2CN=C(c3ccccc3)c3cc(Cl)ccc3n12
    InChIKeyGJSLOMWRLALDCT-UHFFFAOYSA-N
    Benzodiazepines; 2020/3. Benzodiazepine; 2021/3. Benzodiazepine; 2022/3. Benzodiazepine
    Chemical Class Benzodiazepine
    Psychoactive Class Depressant
    Half-Life Parent: ~2–3 h in healthy adults (mean ≈2.7 h); prolonged in hepatic impairment (~7.7 h). Active metabolite N-desmethyl-adinazolam: ~4–8 h depending on population and regimen.

    Pharmacology

    DrugBank
    Half-life Less than 3 hours. State Solid

    Description

    Adinazolam (Deracyn®) is a benzodiazepine derivative with anxiolytic, anticonvulsant, sedative, and antidepressant properties. Adinazolam was first developed to enhance the antidepressant effects of alprazolam. It has never been approved by the FDA for clinical use.

    Mechanism of Action

    Adinazolam binds to peripheral-type benzodiazepine receptors which interact allosterically with GABA receptors. This potentiates the effects of the inhibitory neurotransmitter GABA, increasing the inhibition of the ascending reticular activating system and blocking the cortical and limbic arousal that occurs following stimulation of the reticular pathways.

    Pharmacodynamics

    Adinazolam is a benzodiazepine derivative used to treat anxiety, status epilepticus, and for sedation induction and anterograde amnesia. Adinazolam binds with high affinity to the GABA benzodiazepine receptor complex. Considerable evidence suggest that the central pharmacologic/therapeutic actions of alprazolam are mediated via interaction with this receptor complex.

    Metabolism

    The drug primarily undergoes hepatic metabolism to form the main metabolite N-desmethyladinazolam, alpha-hydroxyalprazolam, and estazolam.

    Toxicity

    Signs of overdose may include muscle weakness, ataxia, dysarthria and particularly in children paradoxical excitement. In more severe cases diminished reflexes, confusion, and coma may ensue.

    Indication

    For the treatment of anxiety and status epilepticus.

    Receptor Profile

    Receptor Actions

    Modulators
    GABA-A receptor positive allosteric modulator (benzodiazepine site)

    Effect Profile

    Curated
    Benzodiazepine 7.3

    Strong anxiolysis, cognitive impairment, and euphoria with moderate sedation

    Anxiolysis×3
    10
    Sedation / Relaxation×2
    6
    Motor / Cognitive Impairment×1
    10
    Euphoria / Mood Lift×1
    9

    Tolerance & Pharmacokinetics

    drugs.wiki
    Half-Life
    Parent: ~2–3 h in healthy adults (mean ≈2.7 h); prolonged in hepatic impairment (~7.7 h). Active metabolite N-desmethyl-adinazolam: ~4–8 h depending on population and regimen.
    Addiction Potential
    Moderate-to-high, comparable to other short-/intermediate-acting benzodiazepines. Physical dependence and severe withdrawal (including seizures) can develop with continuous use; risk rises with higher or more frequent dosing, and polydrug use with other depressants.

    Tolerance Decay

    Full tolerance 14d Half tolerance 7d Baseline ~42d

    Benzodiazepine tolerance develops to most effects with repeated use over days–weeks; cross-tolerance exists across the class and with Z-drugs. On discontinuation, tolerance decays slowly over weeks; clinical practice favors long, individualized tapers to minimize withdrawal. Data are derived largely from class-wide evidence and user reports rather than adinazolam-specific trials.

    Cross-Tolerances

    Other benzodiazepines
    80% ●●○
    Non-benzodiazepine Z-drugs
    60% ●○○
    Barbiturates
    40% ●○○
    Other GABA-A positive modulators
    40% ●○○

    Harm Reduction

    drugs.wiki

    Reasoning for additions and key harm-reduction points (with sources): 1) Classification and active metabolites: Adinazolam is a triazolobenzodiazepine that acts as a positive allosteric modulator at GABA-A; it forms active metabolites (notably N-desmethyladinazolam), which contribute to effects. This supports conservative dosing and awareness of prolonged sedation. Source: DrugBank DB00546 overview and metabolism citations. 2) Short parent half-life with active metabolite: In healthy subjects, adinazolam t1/2 is about 2.7 h on average; the active metabolite persists longer, so redosing to chase effects can lead to delayed over-sedation. Source: Cirrhotic vs. healthy PK study summary; elderly PK summary. 3) Special populations: Exposure increases in hepatic impairment and older adults (reduced clearance; longer half-life), necessitating lower starting doses and slower titration to avoid accumulation and falls. Source: PK studies above. 4) CYP3A4 substrate: Strong CYP3A4 inhibitors (e.g., azole antifungals, certain macrolides) can raise levels; inducers can lower them. Users on such medicines should reduce dose and avoid rapid redosing. Source: DrugBank lists adinazolam as a CYP3A4 substrate and enumerates interaction propensity. 5) Polydrug risks: Combining benzodiazepines with alcohol, opioids, or GHB/GBL markedly increases risk of respiratory depression and fatal overdose; tramadol is flagged specifically as dangerous in combination with benzos. Source: TripSit combination and HR pages; Erowid benzodiazepine/alprazolam pages. 6) Gabapentinoids and other sedatives: Additive CNS/respiratory depression when combined with benzos warrants avoidance or dose minimization and sitter/monitoring if prescribed together. Source: TripSit benzodiazepine HR. 7) Overdose management caveat: Flumazenil can precipitate acute withdrawal and seizures in benzodiazepine-dependent or mixed-overdose patients; airway/ventilation support is the priority. Source: NCBI StatPearls; Erowid alprazolam FAQ. 8) Withdrawal/tapering: Abrupt cessation after sustained use can be severe or life-threatening. A cautious taper (often 5–10% dose reductions every 1–2 weeks, individualized and often slower at low doses) is commonly advised by clinicians and communities; switching to a long-acting benzodiazepine is sometimes used. Source: Clinical caution in StatPearls (qualitative), community consensus examples on Bluelight; Erowid notes on severe withdrawal. 9) Measurement accuracy: Because many RC benzos are potent at low mg-levels, volumetric dosing in propylene glycol/ethanol and using an oral syringe reduces dosing errors. Source: TripSit benzodiazepines harm-reduction page. 10) Drug checking: Adinazolam appears on analyte lists for professional drug checking; where available, consider FTIR/GC-MS services for verification of contents and dose. Source: drugchecking.community guidance/coverage list. 11) Driving/operating machinery: Expect psychomotor and cognitive impairment (ataxia, reaction-time slowing); avoid driving until fully unimpaired (often the next day after higher doses). Source: NCBI StatPearls overview of benzodiazepine toxicity/impairment.

    References

    Data Sources

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