A Comprehensive Monograph on Triazolam (Halcion): Pharmacology, Clinical Use, and Safety Profile

Executive Summary

Triazolam is a potent, short-acting hypnotic agent belonging to the triazolobenzodiazepine class, a derivative of benzodiazepines.[1] Marketed principally under the brand name Halcion, its primary and sole approved indication is for the short-term management of insomnia, specifically sleep-onset difficulties, with a recommended treatment duration of generally 7 to 10 days.[2] Its mechanism of action involves the positive allosteric modulation of the gamma-aminobutyric acid-A ($GABA_A$) receptor, which enhances the inhibitory effects of GABA throughout the central nervous system (CNS), resulting in sedation, anxiolysis, and anterograde amnesia.[4]

The defining characteristic of triazolam is its unique pharmacokinetic profile, marked by rapid oral absorption and an exceptionally short elimination half-life of 1.5 to 5.5 hours.[1] This profile is directly responsible for both its therapeutic utility and its significant safety concerns. The rapid onset and short duration of action make it highly effective for inducing sleep without causing significant next-day sedation or "hangover" effects.[1] However, this same property renders it ineffective for maintaining sleep and contributes to a high incidence of rebound insomnia upon discontinuation, where sleep quality can become significantly worse than at baseline.[1]