2605 Triazolam Triazolam is only found in individuals that have used or taken this drug. It is withdrawn in the United Kingdom due to risk of psychiatric adverse drug reactions.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.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_A) 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. 28911-01-5 5556 C17H12Cl2N4 342.043900 White crystalline powder (RxList, A308). 233-235°C 4.53 mg/L Inhalation; dermal or skin contact; ingestion (MSDS, A308). Bioavailability is 44% (oral) and 53% (sublingual). 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_A) 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. Hepatic. Small amounts of unmetabolized triazolam appear in the urine. Triazolam undergoes hepatic microsomal oxidation to inactive hydroxylated metabolites that are eliminated primarily as glucuronide conjugates (A630). Route of 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. Half Life: 1.5-5.5 hours LD50: >1000 mg/kg (Oral, Mouse) LD50: >5000 mg/kg (Oral, Rat) No indication of carcinogenicity to humans (not listed by IARC). For the short-term treatment of insomnia (A308). Following acute overdose, clinical symptoms or manifestations may include sleepiness, which, following larger overdose can range from stage zero to stage one coma. Initially, excitement may be seen as a result of the disinhibition effects of these drugs, which then progresses to central nervous system depression, hypotension, respiratory depression, and coma (A629). Symptoms of overdose include drowsiness, slurred speech, motor inco-ordination, coma, and respiratory depression. Flumazenil, a specific benzodiazepine receptor antagonist, is indicated for the complete or partial reversal of the sedative effects of benzodiazepines and may be used in situations when an overdose with a benzodiazepine is known or suspected. Prior to the administration of flumazenil, necessary measures should be instituted to secure airway, ventilation and intravenous access. (L1712) 2009-07-05T03:14:44Z 2026-05-14T16:52:12Z Cytochrome P450 3A4 (CYP3A4) (P08684) (A308). Triazolam 9674 Triazolam DB00897 true Cytochrome P450 3A4 (P08684) (A308) CC1=NN=C2CN=C(C3=CC=CC=C3Cl)C3=C(C=CC(Cl)=C3)N12 C17H12Cl2N4 InChI=1S/C17H12Cl2N4/c1-10-21-22-16-9-20-17(12-4-2-3-5-14(12)19)13-8-11(18)6-7-15(13)23(10)16/h2-8H,9H2,1H3 JOFWLTCLBGQGBO-UHFFFAOYSA-N 343.21 342.043901818 Exogenous Solid 2.42 HMDB15034 CHEMBL646 5355 CHEM002090 DTXSID6046763 NS00010468 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 43.07 103.68380000000002 34.18780241753372 1 3 0 18.078355810244943 4.322260521653215 0 4 2.94 -4.27 1.83e-02 g/l