Triazolam
- Atc Codes:N05CD05
- CAS Codes:28911-01-5
- PHARMGKB ID:28911-01-5
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Halcion; Belgium: Halcion; Denmark: Halcion; Estonia: Halcion; Finland: Halcion; Germany: Halcion; Greece: Halcion; Italy: Halcion, Songar, Triazolam; Latvia: Halcion; Lithuania: Halcion; Luxembourg: Halcion; Portugal: Halcion; Spain: Halcion; Sweden: Halcion; UK: Halcion.
North America
Canada: Apo-Triazo, Triazolam; USA: Halcion, Triazolam.
Latin America
Mexico: Halcion.
Asia
Japan: Asasion, Ascomarna, Camriton, Halcion, Halrack, Minzain, Nesgen, Paruleon, Trialam, Triazolam.
Drug combinations
Chemistry
Triazolam: C~17~H~12~Cl~2~N~4~. Mw: 343.21. (1) 4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine, 8-chloro-6-(2-chlorophenyl)-1-methyl-; (2) 8-Chloro-6-(o-chlorophenyl)-1-methyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine. CAS-28911-01-5 (1973).
Pharmacologic Category
Anxiolytics, Sedatives, and Hypnotics; Benzodiazepines. (ATC-Code: N05CD05).
Mechanism of action
Binds to stereospecific benzodiazepine receptors on postsynaptic GABA neuron at several sites within CNS, including limbic system, reticular formation. Enhancement of inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions. This shift in chloride ions results in hyperpolarization (less excitable state) and stabilization.
Therapeutic use
Short-term treatment of insomnia.
Pregnancy and lactiation implications
Use of triazolam contraindicated in pregnancy. Excretion in breast milk unknown (not recommended in nursing women).
Unlabeled use
Contraindications
Hypersensitivity to triazolam or any component of the formulation (cross-sensitivity with other benzodiazepines may exist). Concurrent therapy with itraconazole, ketoconazole, nefazodone, and other moderate/strong CYP3A4 inhibitors. Pregnancy.
Warnings and precautions
Use caution in depression, particularly if suicidal risk may be present. Use of hypnotic/sedative agents for sleep associated with hypersensitivity reactions including anaphylaxis as well as angioedema. Use with caution in renal impairment. Paradoxical reactions, including hyperactive or aggressive behavior, reported with benzodiazepines, particularly in adolescent/pediatric or psychiatric patients. Use with caution in respiratory compromise, COPD or sleep apnea. Increased risk for hazardous sleep-related activities such as sleep-driving; cooking and eating food, and making phone calls while asleep also noted. Use with caution in history of drug abuse or acute alcoholism (potential for drug dependency exists). Tolerance, psychological and physical dependence may occur with prolonged use. Benzodiazepines associated with anterograde amnesia. Use with caution in hepatic impairment. May cause CNS depression. Use with caution in impaired gag reflux, and in patients receiving other CNS depressants or psychoactive medication (effects with other sedative drugs or ethanol may be potentiated), taking strong CYP3A4 inhibitors, moderate or strong CYP3A4 inducers and major CYP3A4 substrates. Use with caution in debilitated patients. Use with extreme caution in patients at risk of falls (benzodiazepines associated with falls and traumatic injury). Rebound or withdrawal symptoms may occur following abrupt discontinuation or large decreases in dose. Failure of sleep disturbance to resolve after 7-10 days may indicate psychiatric or medical illness.