Pharmacology
DrugBankDescription
Withdrawn in the United Kingdom due to risk of psychiatric adverse drug reactions.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
Receptor Binding
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 ReportsStrong anxiolysis, cognitive impairment, euphoria, and sedation
Tolerance & Pharmacokinetics
drugs.wikiTolerance Decay
Cross-Tolerances
Experience Report Analysis
ErowidDemographics
Gender Distribution
Age Distribution
Reports Over Time
Effect Analysis
ErowidEffects aggregated from 48 experience reports (48 Erowid)
Effect Sentiment Distribution
Confidence Distribution
Positive Effects 8
Adverse Effects 3
Dosage Distribution
Dose distribution from experience reports
Real-World Dose Distribution
62K DosesFrom 30 individual dose entries
Oral (n=21)
Form / Preparation
Most common forms and preparations reported
Body-Weight Dosing
Dose relative to body weight from reports with weight data
Redose Patterns
Redosing behavior across 44 reports
Benzodiazepine Equivalence
Triazolam - 0.5mg ~=10mg Diazepam.
Legal Status
| 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. |
References
Cited References
- Drugs.com: Triazolam Prescribing Information
- Erowid: Triazolam Vault
- FDA: Halcion (Triazolam) Label
- Mayo Clinic: Triazolam
- MedlinePlus: Triazolam
- NCBI LiverTox: Triazolam
- PMC: The effect of triazolam premedication on anxiety, sedation, and amnesia
- PsychonautWiki: Triazolam
- PubChem: Triazolam
- Roth et al. 1983: Pharmacology and hypnotic efficacy of triazolam