| Item |
Information |
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Drug Groups
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illicit; approved; withdrawn |
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Description
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Withdrawn in the United Kingdom due to risk of psychiatric adverse drug reactions.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 |
| • |
Humans and other mammals |
|
| 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 |
| • |
Rickels K: The clinical use of hypnotics: indications for use and the need for a variety of hypnotics. Acta Psychiatr Scand Suppl. 1986;332:132-41.
[Pubmed]
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| • |
Oelschlager H: [Chemical and pharmacologic aspects of benzodiazepines] Schweiz Rundsch Med Prax. 1989 Jul 4;78(27-28):766-72.
[Pubmed]
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| • |
Noguchi H, Kitazumi K, Mori M, Shiba T: Electroencephalographic properties of zaleplon, a non-benzodiazepine sedative/hypnotic, in rats. J Pharmacol Sci. 2004 Mar;94(3):246-51.
[Pubmed]
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| • |
Tokunaga S, Takeda Y, Shinomiya K, Hirase M, Kamei C: Effects of some H1-antagonists on the sleep-wake cycle in sleep-disturbed rats. J Pharmacol Sci. 2007 Feb;103(2):201-6. Epub 2007 Feb 8.
[Pubmed]
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| • |
Veje JO, Andersen K, Gjesing S, Kielgast H: [Prescription of tranquilizers and hypnotics in the municipality of Holbaek] Ugeskr Laeger. 1989 Aug 21;151(34):2134-6.
[Pubmed]
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| External Links |
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