Triazolam: a review of its pharmacological properties and therapeutic efficacy in patients with insomnia

Drugs. 1981 Aug;22(2):81-110. doi: 10.2165/00003495-198122020-00001.

Abstract

Triazolam is a triazolobenzodiazepine with hypnotic properties, advocated for use in acute or chronic insomnia, situational insomnia in hospitalised patients, and insomnia associated with other disease states. As triazolam has a relatively short half-life of about 2 to 3 hours in healthy subjects and has only 1 short acting active metabolite, alpha-hydroxytriazolam, it would seem more suitable as an hypnotic than longer acting drugs such as flurazepam, nitrazepam or flunitrazepam, particularly when residual sedative effects on the day after ingestion are undesirable. Thus, with usual hypnotic doses of triazolam (0.25 or 0.5 mg) impairment of psychomotor and cognitive function is generally not carried over into the day after ingestion, although at doses of 1 mg or greater, residual effects may appear. In short term comparative studies triazolam was clearly superior to a placebo, and was at lest as effective as flurazepam, or other benzodiazepines such as nitrazepam or diazepam, in hastening sleep onset, reducing nocturnal awakenings, and increasing sleep duration. In other studies it was often superior to chloral hydrate, methyprylone or quinalbarbitone (secobarbital). In a small number of patients with chronic insomnia receiving extended treatment with triazolam in a clinical setting or in some sleep laboratory studies, no evidence of tolerance occurred; however, some evidence of reduced effect with repeated administration has been reported in one sleep laboratory study. Thus, a definitive statement about the likelihood of tolerance occurring on repeated administration is difficult to make at this time.

Publication types

  • Clinical Trial
  • Comparative Study
  • Review

MeSH terms

  • Animals
  • Anti-Anxiety Agents / metabolism
  • Anti-Anxiety Agents / pharmacology*
  • Clinical Trials as Topic
  • Cognition / drug effects
  • Humans
  • Kinetics
  • Sleep Initiation and Maintenance Disorders / drug therapy*
  • Sleep Stages / drug effects
  • Triazolam / metabolism
  • Triazolam / pharmacology*
  • Triazolam / therapeutic use

Substances

  • Anti-Anxiety Agents
  • Triazolam