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    Triazolam molecular structure

    Triazolam Stats & Data

    Hypam Trilam Halcion Novodorm Up johns
    PubChem
    MW343.2
    FormulaC17H12Cl2N4
    LogP2.4
    IUPAC8-chloro-6-(2-chlorophenyl)-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
    InChIKeyJOFWLTCLBGQGBO-UHFFFAOYSA-N
    Chemical Class Triazolobenzodiazepine
    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    Withdrawn in the United Kingdom due to risk of psychiatric adverse drug reactions.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).

    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

    Measured Affinities

    Guide to PHARMACOLOGY

    Measured binding and functional data for triazolam, curated by the IUPHAR/BPS Guide to PHARMACOLOGY. Each row cites the paper it came from. Lower concentrations mean tighter binding — a value in the sub-nanomolar range indicates a very potent interaction.

    Target Action Measure Value Concentration Species Source
    GABAA receptor α2 subunit GABRA2 Positive pKi 9.23 0.589 nM Human PMID 10633039
    GABAA receptor α1 subunit GABRA1 Positive pKi 9.1 0.794 nM Human PMID 10633039
    GABAA receptor α1 subunit GABRA1 Positive pKd 9 1 nM Human PMID 18537233
    GABAA receptor α3 subunit GABRA3 Positive pKi 8.84 1.45 nM Human PMID 10633039
    GABAA receptor α5 subunit GABRA5 Positive pKi 8.81 1.55 nM Human PMID 10633039
    GABAA receptor α5 subunit GABRA5 Positive pKd 8.4 3.98 nM Human PMID 18537233

    Reading this. pKi, pEC50 and pIC50 are negative log molar values, so a higher number means a tighter interaction; the concentration column converts them for you. Values from non-human species are laboratory measurements and do not translate directly to human effect. Receptor affinity is not a dose — it describes what a molecule binds, not how much of it is safe to take.

    Receptor data from the IUPHAR/BPS Guide to PHARMACOLOGY (v2026.2), licensed CC BY-SA 4.0. Matched to this substance by InChIKey.

    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.

    Toxicity

    PubChem DrugBank

    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 (GABA<sub>A</sub>) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor.

    LD50

    • LD50: >1000 mg/kg (Oral, Mouse)
    • LD50: >5000 mg/kg (Oral, Rat)

    Carcinogenicity

    No indication of carcinogenicity to humans (not listed by IARC).

    Liver injury risk

    Ambiguous (limited data)

    FDA LiverTox / DILIrank. Reflects published case reports of liver injury, not absolute risk.

    Health effects (PubChem excerpts)

    Following acute overdose, clinical symptoms or manifestations may include sleepiness, which, following larger overdose can range from stage zero to stage one coma. Initially, excitement may be seen as a result of the disinhibition effects of these drugs, which then progresses to central nervous system depression, hypotension, respiratory depression, and coma (A629).

    Effect Profile

    Curated + 33 Reports
    Benzodiazepine 8.6

    Strong anxiolysis, sedation, and euphoria with strong cognitive impairment

    Anxiolysis×3
    10
    Sedation / Relaxation×2
    107.3
    Motor / Cognitive Impairment×1
    105.1
    Euphoria / Mood Lift×1
    102.7
    Catalog Erowid
    Based on reports from:

    Tolerance & Pharmacokinetics

    drugs.wiki

    No tolerance chart. Our decay curves for these drugs were estimates, and a curve can make tolerance look longer-lasting than it is, which is the dangerous direction.

    How fast tolerance to these drugs fades after a break has not been measured well enough to draw, so don't count on a dose you used to take still being safe: after time off, start with a much smaller amount and don't use alone. Mixing sedatives with each other, with alcohol or with opioids sharply raises the risk of a fatal overdose. If you've been using regularly, don't stop suddenly: withdrawal from benzodiazepines, alcohol or GHB/GBL can cause seizures or delirium, so get medical help to cut down gradually.

    Sources: FRANK: benzodiazepines · Alcohol and Drug Foundation: GHB · FDA 2020: benzodiazepine boxed warning · FDA 2019: gabapentinoids and breathing · NHS: alcohol use disorder

    Cross-Tolerances

    Alprazolam
    Diazepam
    Clonazepam
    Lorazepam
    Etizolam
    Bromazolam
    Clonazolam
    Flualprazolam

    Experience Report Analysis

    Erowid
    48 Reports
    33 Single-substance
    2002–2025 Date Range
    18 With Age Data
    8 Effects Detected

    Demographics

    Gender Distribution

    Age Distribution

    Reports Over Time

    Effect Analysis

    Erowid

    Effects aggregated from 33 experience reports (33 single-substance Erowid)

    33 Reports
    8 Effects Detected
    4 Positive
    3 Adverse
    1 Neutral

    Effect Sentiment Distribution

    Confidence Distribution

    Each bar is the share of reports mentioning the effect; its whisker, and the band on the rows below, is the 95% interval: where the share could plausibly be with other reports of the same kind.

    Positive Effects 4

    Sedation 48.5% (95% interval 32 to 65 percent) 70%
    Stimulation 42.4% (95% interval 27 to 59 percent) 70%
    Euphoria 18.2% (95% interval 9 to 34 percent) 70%
    Music Enhancement 9.1% (95% interval 3 to 24 percent) 70%

    Adverse Effects 3

    Memory Suppression 21.2% (95% interval 11 to 38 percent) 70%
    Confusion 15.2% (95% interval 7 to 31 percent) 70%
    Motor Impairment 12.1% (95% interval 5 to 27 percent) 70%
    Show 1 neutral or unclassified mention
    Auditory Effects 15.2% (95% interval 7 to 31 percent)

    Dosage Distribution

    Dose distribution from experience reports, one dose per report (the first listed). Doses above Q3 + 3×IQR, far above what people typically take, are left out of the median and range and listed under each route: most are real heavy doses or overdoses, not mistakes.

    Median: 0.5 mg IQR: 0.2–1.0 mg n=13

    1 report gave a dose above the typical range (3.75 mg), so it is not in the figures above. Listing a dose here does not mean it is safe.

    Show the report

    Real-World Dose Distribution

    Erowid

    From 21 of 30 recorded dose entries: those that state a weight (mg, g or µg), in routes with at least five of them. Values above Q3 + 3×IQR, far above what people typically take, are left out; they can include real heavy doses and overdoses, not only mistakes.

    Oral (n=21)

    Median: 0.5mg 25th: 0.25mg 75th: 2.0mg 90th: 2.0mg

    Common Combinations

    Most co-occurring substances, as a share of all 48 reports filed under Triazolam; whiskers are 95% intervals

    Form / Preparation

    Most common forms and preparations, as a share of the 41 reports that give one; whiskers are 95% intervals

    Body-Weight Dosing

    Dose per kg of body weight, one dose per report (the first listed), from reports giving a weight of 30–250 kg. Doses above Q3 + 3×IQR, far above what people typically take, are left out of the median and range and listed under each route.

    Median: 0.008 mg/kg IQR: 0.003–0.017 mg/kg n=14

    Redose Patterns

    Redosing behavior across 44 reports

    20.5% (95% interval 11 to 34 percent) 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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