Triazolam

Products

Triazolam is commercially available in tablet form (Halcion). It has been approved in many countries since 1978.

Structure and properties

Triazolam (C17H12Cl2N4, Mr = 343.2 g/mol) exists as a white crystalline powder that is poorly soluble in water. It is a triazole derivative (triazol-am).

Effects

Triazolam (ATC N05CD05) has sedative, antianxiety, anticonvulsant, amnesic, and sleep-inducing properties. It binds to the GABAA receptor, enhancing the inhibitory properties of the neurotransmitter GABA.

Indications

For the short-term treatment of sleep disorders.

Abuse

Triazolam is abused as an intoxicant and for other purposes because of its psychoactive properties.

Dosage

According to the prescribing information. Tablets are taken immediately before bedtime.

Contraindications

  • Hypersensitivity
  • Myasthenia gravis
  • Severe respiratory disorders
  • Severe psychiatric disorders
  • Triazolam should not be co-administered with strong CYP inhibitors such as azole antifungals and HIV protease inhibitors because they may inhibit the metabolism of triazolam and lead to increased concentrations and side effects.

For complete precautions, see the drug label.

Interactions

Triazolam is a substrate of CYP3A4. Corresponding drug-drug interactions with CYP inhibitors and inducers are possible and should be considered during treatment. Combination with centrally depressant drugs and alcohol should be avoided because potentiation of effects and adverse effects may occur.

Adverse effects

The most common possible adverse effects include drowsiness, dizziness, gait and coordination problems. Other possible side effects include confusion, insomnia, memory impairment, visual disturbances, respiratory depression, and fatigue. Like other benzodiazepines, triazolam can be addictive and cause withdrawal symptoms when discontinued after prolonged use.