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Pathway Description
Triazolam Action Pathway
Homo sapiens
Drug Action Pathway
Triazolam is a short-acting benzodiazepine used for the short-term treatment of insomnia (hypnotic agent). This drug binds to various regions of the brain and spinal cord where GABA A receptors are. It binds to an allosteric site between the alpha and gamma subunits of the receptor increasing the inhibitory effects of GABA. Benzodiazepines bind nonspecifically to BNZ1, which acts on sleep, and BNZ2, which acts on muscle relaxation, anticonvulsant activity, motor coordination, and memory. These 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. In consequence, when GABA binds the site, it opens the chloride channel, resulting in a hyperpolarized cell membrane. Since the neuron cell is hyperpolarized, it prevents further excitation of the cell. Triazolam is administered orally as a tablet. Overdosing of triazolam usually has the symptoms of more intense therapeutic effects with extreme overdosage leading to coma, cardio-respiratory depression, and apnoea. Due to its high affinity for plasma proteins, diazepam also has a high volume of distribution and can cross the blood-brain barrier. This drug has been withdrawn in the United Kingdom due to the risk of psychiatric adverse drug reactions. This drug continues to be available in the U.S..
References
Triazolam Pathway References
Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M: DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. doi: 10.1093/nar/gkx1037.
Pubmed: 29126136
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. doi: 10.1111/j.1600-0447.1986.tb08990.x.
Pubmed: 2883820
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. doi: 10.1111/j.1600-0447.1986.tb08990.x.
Pubmed: 2883820
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. doi: 10.1254/jphs.94.246.
Pubmed: 15037809
Zhu S, Noviello CM, Teng J, Walsh RM Jr, Kim JJ, Hibbs RE: Structure of a human synaptic GABA(A) receptor. Nature. 2018 Jul;559(7712):67-72. doi: 10.1038/s41586-018-0255-3. Epub 2018 Jun 27.
Pubmed: 29950725
Sigel E, Steinmann ME: Structure, function, and modulation of GABA(A) receptors. J Biol Chem. 2012 Nov 23;287(48):40224-31. doi: 10.1074/jbc.R112.386664. Epub 2012 Oct 4.
Pubmed: 23038269
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