Molecule

Drug Groups

illicit; approved; withdrawn

Description

Withdrawn in the United Kingdom due to risk of psychiatric adverse drug reactions. This drug continues to be available in the U.S. Internationally, triazolam is a Schedule IV drug under the Convention on Psychotropic Substances.

Indication

For the short-term treatment of insomnia.

Pharmacology

A short-acting benzodiazepine used as a hypnotic agent in the treatment of insomnia. Some countries temporarily withdrew triazolam from the market because of concerns about adverse reactions, mostly psychological, associated with higher dose ranges. Its use at lower doses with appropriate care and labeling has been reaffirmed by the FDA and most other countries. Triazolam has a shorter half-life than chlordiazepoxide, flurazepam, and prazepam and does not generate active metabolites.

Toxicity

Symptoms of overdose include drowsiness, slurred speech, motor inco-ordination, coma, and respiratory depression.

Affected Organisms

Biotransformation

Hepatic. Small amounts of unmetabolized triazolam appear in the urine.

Absorption

Bioavailability is 44% (oral) and 53% (sublingual).

Half Life

1.5-5.5 hours

Elimination

Triazolam and its metabolites, principally as conjugated glucuronides, which are presumably inactive, are excreted primarily in the urine. Only small amounts of unmetabolized triazolam appear in the urine. The two primary metabolites accounted for 79.9% of urinary excretion.

References

External Links