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Triazolam !

A very short-acting benzodiazepine for brief treatment of insomnia. It can cause next-day memory gaps and interacts strongly with CYP3A inhibitors.

Updated 2026-11-01

  • Class: Benzodiazepines
  • Receptor: GABA-A receptor, benzodiazepine site
  • ATC code: N05CD05

The figure shows alprazolam, a closely related triazolobenzodiazepine that occupies the same site, bound to the human GABA-A receptor; no structure with triazolam is available.

Target in 3D: GABA-A receptor, benzodiazepine site. PDB structure 6HUO (RCSB PDB, public domain). View the structure at RCSB PDB

Mechanism of action

Triazolam binds the benzodiazepine site of the GABA-A receptor and makes GABA open the chloride channel more often, which brings on sleep. CYP3A4 breaks it down quickly, so its effect is brief, but CYP3A inhibitors can raise its levels a great deal.

  1. Binds the benzodiazepine site of the GABA-A receptor
  2. GABA opens the chloride channel more often
  3. Sleep onset; CYP3A4 clears it within hours

Pharmacokinetics

Metabolism
Hydroxylation by CYP3A4
Half-life
About 1.5 to 5.5 hours

Indications

Adverse effects

Common

  • Drowsiness and dizziness
  • Memory loss for events after the dose (anterograde amnesia)
  • Daytime anxiety

Contraindications

  • Hypersensitivity to benzodiazepines
  • Strong CYP3A inhibitors: ketoconazole, itraconazole, nefazodone, some HIV protease inhibitors

Key interactions

Opioids
Profound sedation, respiratory depression, coma and death
Alcohol and other central nervous system depressants
Additive sedation and breathing depression
Strong CYP3A inhibitors
Much higher triazolam levels: contraindicated
Grapefruit and grapefruit juice
Higher triazolam levels; avoided

What is monitored

  • Next-day memory and alertness
  • Falls and sedation in older adults
  • Insomnia lasting beyond a short course, which needs evaluation

Administration and safety

  • Given by mouth at bedtime, only when a full night of sleep is possible
  • Controlled medicine; short courses only

Nursing care

  • Before each dose, check level of alertness, breathing rate and oxygen saturation
  • Ask about opioids, alcohol and other sedatives
  • Prevent falls, especially in older adults (unsteadiness, confusion)
  • Teach not to drive or drink alcohol and not to stop the medicine suddenly
  • Teach to avoid grapefruit and to report new medicines

Pregnancy and breastfeeding

Use late in pregnancy can cause sedation and withdrawal symptoms in the newborn, who is watched after birth.

Test yourself

Think of the answer, then tap the question to see it.

Which fruit is avoided with triazolam, and why?

Grapefruit, because it raises triazolam levels (CYP3A).

Which memory effect is typical of triazolam?

Anterograde amnesia: no memory of events after the dose.

Which two antifungals are contraindicated with triazolam?

Ketoconazole and itraconazole (also nefazodone).

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← Back to the class: Benzodiazepines

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: DailyMed - TRIAZOLAM tablet (DailyMed (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.