Triazolam

Triazolam
Triazolam.svg
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number
PubChem
DrugBank
ChemSpider
KEGG

Triazolam is a benzodiazepine medication primarily used for the short-term treatment of insomnia. It is known for its fast onset of action and short duration of effect. Triazolam is marketed under various brand names, with Halcion being one of the most well-known.

Medical uses

Triazolam is prescribed for the short-term management of insomnia, particularly in patients who have difficulty falling asleep. Due to its rapid onset, it is effective in reducing the time it takes to fall asleep. However, it is generally recommended for short-term use, typically not exceeding 7 to 10 days, due to the risk of dependence and other adverse effects.

Pharmacology

Triazolam works by enhancing the effect of the neurotransmitter gamma-aminobutyric acid (GABA) at the GABA_A receptor, which results in sedative, hypnotic, anxiolytic, anticonvulsant, and muscle relaxant properties. Its short half-life makes it suitable for use as a sleep aid, as it reduces the likelihood of next-day sedation.

Side effects

Common side effects of triazolam include drowsiness, dizziness, headache, and nausea. More serious side effects can include memory impairment, confusion, and hallucinations. Due to its potential for abuse and dependence, triazolam is classified as a Schedule IV controlled substance in the United States.

Contraindications

Triazolam is contraindicated in patients with a known hypersensitivity to benzodiazepines, as well as in those with myasthenia gravis, severe respiratory insufficiency, or sleep apnea. It should be used with caution in patients with a history of substance abuse or depression.

Interactions

Triazolam can interact with other medications that depress the central nervous system, such as alcohol, opioids, and other benzodiazepines, leading to increased sedation and respiratory depression. It is also metabolized by the cytochrome P450 enzyme system, particularly CYP3A4, and its effects can be altered by inhibitors or inducers of this enzyme.

History

Triazolam was first introduced in the 1970s and quickly became a popular treatment for insomnia due to its efficacy and short duration of action. However, concerns about its safety profile, particularly regarding its potential for abuse and adverse psychiatric effects, have led to more cautious prescribing practices.

Related pages

• Benzodiazepine
• Insomnia
• GABA_A receptor

Triazolam

• 
  Chemical structure of Triazolam
• 
  Ball-and-stick model of Triazolam