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    Triazolam molecular structure

    Triazolam Stats & Data

    Hypam Trilam Halcion Novodorm Up johns
    Chemical Class Benzodiazepine
    Psychoactive Class Depressant

    Pharmacology

    DrugBank
    Half-life 1.5-5.5 hours State Solid

    Description

    Withdrawn in the United Kingdom due to risk of psychiatric adverse drug reactions. This drug continues to be available in the U.S. Internationally, triazolam is a Schedule IV drug under the Convention on Psychotropic Substances.

    Mechanism of Action

    Benzodiazepines bind nonspecifically to bezodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.

    Pharmacodynamics

    A short-acting benzodiazepine used as a hypnotic agent in the treatment of insomnia. Some countries temporarily withdrew triazolam from the market because of concerns about adverse reactions, mostly psychological, associated with higher dose ranges. Its use at lower doses with appropriate care and labeling has been reaffirmed by the FDA and most other countries. Triazolam has a shorter half-life than chlordiazepoxide, flurazepam, and prazepam and does not generate active metabolites.

    Metabolism

    Hepatic. Small amounts of unmetabolized triazolam appear in the urine.

    Absorption

    Bioavailability is 44% (oral) and 53% (sublingual).

    Toxicity

    Symptoms of overdose include drowsiness, slurred speech, motor inco-ordination, coma, and respiratory depression.

    Indication

    For the short-term treatment of insomnia.

    Elimination

    Triazolam and its metabolites, principally as conjugated glucuronides, which are presumably inactive, are excreted primarily in the urine. Only small amounts of unmetabolized triazolam appear in the urine. The two primary metabolites accounted for 79.9% of urinary excretion.

    Receptor Profile

    Receptor Actions

    Modulators
    GABA-A receptor positive allosteric modulator (benzodiazepine site)
    Other
    Voltage-gated sodium channel blocker (anticonvulsant properties)

    Receptor Binding

    Translocator protein modulator

    History & Culture

    Triazolam was patented in 1970 and subsequently entered the pharmaceutical market in the United States in 1982 under the brand name Halcion. The drug gained widespread clinical adoption, and by 2017 it ranked as the 289th most commonly prescribed medication in the United States with over one million prescriptions annually. Following its market introduction, triazolam became the subject of regulatory scrutiny in several countries due to concerns about adverse psychological reactions, particularly at higher dose ranges. Some nations temporarily withdrew the drug from their markets, though subsequent review by the FDA and regulatory bodies in most other countries reaffirmed its safety profile when used at lower doses with appropriate clinical guidance and labeling. Beyond its primary indication for insomnia, triazolam has found particular utility in specific clinical and practical contexts. It is frequently prescribed to airline passengers as a sleep aid for short- to medium-duration flights. Additionally, the drug's pronounced amnestic properties have made it a common choice in sedation dentistry, where its ability to induce anterograde amnesia helps patients undergo dental procedures with minimal subsequent recall of the experience.

    Effect Profile

    Curated + 48 Reports
    Benzodiazepine 8.3

    Strong anxiolysis, cognitive impairment, euphoria, and sedation

    Anxiolysis×3
    10
    Sedation / Relaxation×2
    96.9
    Motor / Cognitive Impairment×1
    106.0
    Euphoria / Mood Lift×1
    103.4
    Catalog Erowid

    Tolerance & Pharmacokinetics

    drugs.wiki

    Tolerance Decay

    Full tolerance 3d Half tolerance 37d Baseline ~60d

    Cross-Tolerances

    Alprazolam
    30% ●○○
    Diazepam
    30% ●○○
    Clonazepam
    30% ●○○
    Lorazepam
    30% ●○○
    Etizolam
    30% ●○○
    Bromazolam
    30% ●○○
    Clonazolam
    30% ●○○
    Flualprazolam
    30% ●○○

    Experience Report Analysis

    Erowid
    48 Reports
    2002–2025 Date Range
    18 With Age Data
    15 Effects Detected

    Demographics

    Gender Distribution

    Age Distribution

    Reports Over Time

    Effect Analysis

    Erowid

    Effects aggregated from 48 experience reports (48 Erowid)

    48 Reports
    15 Effects Detected
    8 Positive
    3 Adverse
    4 Neutral

    Effect Sentiment Distribution

    Confidence Distribution

    Positive Effects 8

    Sedation 45.8% 70%
    Anxiety Suppression 39.6% 70%
    Stimulation 37.5% 70%
    Euphoria 22.9% 70%
    Music Enhancement 16.7% 70%
    Color Enhancement 10.4% 70%
    Empathy 10.4% 70%
    Tactile Enhancement 6.2% 70%

    Adverse Effects 3

    Memory Suppression 22.9% 70%
    Confusion 20.8% 70%
    Motor Impairment 16.7% 70%

    Dosage Distribution

    Dose distribution from experience reports

    Median: 0.5 mg IQR: 0.2–1.0 mg n=14

    Real-World Dose Distribution

    62K Doses

    From 30 individual dose entries

    Oral (n=21)

    Median: 0.5mg 25th: 0.25mg 75th: 2.0mg 90th: 2.0mg
    mg/kg median: 0.006 mg/kg 75th: 0.015

    Form / Preparation

    Most common forms and preparations reported

    Body-Weight Dosing

    Dose relative to body weight from reports with weight data

    Median: 0.01 mg/kg IQR: 0.003–0.018 mg/kg n=14

    Redose Patterns

    Redosing behavior across 44 reports

    20.5% Redosed
    1.2 Avg Doses
    840m Median Interval

    Benzodiazepine Equivalence

    0.5 mg Triazolam = 10.0 mg Diazepam
    Potency ratio 20.0

    Triazolam - 0.5mg ~=10mg Diazepam.

    All other CNS depressants.

    Legal Status

    UN Convention on Psychotropic Substances 1971 (Schedule IV)
    Country Status Notes
    United Kingdom Withdrawn Withdrawn from the market due to concerns about psychiatric adverse drug reactions associated with its use. Unlike in other countries where it remains available, triazolam is not prescribed in the UK despite being a medically used benzodiazepine elsewhere.
    United States Schedule IV Controlled substance under the Controlled Substances Act (DEA Number 2887). Remains available for medical prescription use. Schedule IV classification indicates accepted medical use with relatively lower abuse potential compared to more restrictive schedules.
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