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Triazolam
- indication:For the short-term treatment of insomnia.
- pharmacologypharmacology:
- mechanism: Benzodiazepines bind nonspecifically to bezodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABA<sub>A</sub>) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.
- toxicity: Symptoms of overdose include drowsiness, slurred speech, motor inco-ordination, coma, and respiratory depression.
- absorprion: Bioavailability is 44% (oral) and 53% (sublingual).
- halflife: 1.5-5.5 hours
- roouteelimination: 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.
- volumedistribution:
- clearance: