Product Name

Triazolam

CAS Number

28911-01-05

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Product Name:
Triazolam
CAS Number:
28911-01-05
Indication:
For the short-term treatment of insomnia.
Mode of Action:

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 (GABAA) 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.

Pharmacodynamics:

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.

Metabolism:

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

Toxicity:

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

IUPAC:
12-chloro-9-(2-chlorophenyl)-3-methyl-2, 4, 5, 8-tetraazatricyclo[8.4.0.0, {2, 6}]tetradeca-1(10), 3, 5, 8, 11, 13-hexaene
ATC:
N05CD05
PubChem:
5556
DrugBank:
DB00897 (APRD00313)
Formula:
C10H11F3N2O5
Molecular Mass:
343.21
Synonyms:
DEA No. 2887 Triazolamum [INN-Latin]
SMILES:
CC1=NN=C2CN=C(C3=CC=CC=C3Cl)C3=C(C=CC(Cl)=C3)N12
AHFS Code:
28:24.1
InChi:
JOFWLTCLBGQGBO-UHFFFAOYSA-N
General Reference:
General Reference:

  1. 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
  2. Oelschlager H: [Chemical and pharmacologic aspects of benzodiazepines] Schweiz Rundsch Med Prax. 1989 Jul 4;78(27-28):766-72. Pubmed
  3. 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
  4. 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
  5. 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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