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QuickView for Triazolam (compound)


PubChem
Name: Triazolam
PubChem Compound ID: 5556
Description: A short-acting benzodiazepine used 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.
Molecular formula: C17H12Cl2N4
Molecular weight: 343.21 g/mol
Synonyms:
8-Chloro-6-(o-chlorophenyl)-1-methyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine; nchembio747-comp15; 4H-s-Triazolo(4,3-a)(1,4)benzodiazepine, 8-chloro-6-(o-chlorophenyl)-1-methyl-; DEA No. 2887; Triazolam [USAN:BAN:INN:JAN]; 4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine, 8-chloro-6-(2-chlorophenyl)-1-methyl-; 28911-01-5; 8-Chloro-6-(o-chlorophenyl)-1-methyl-4H-s-triazolo(4,3-a)(1,4)benzodiazepine; EINECS 249-307-3; Triazolam.
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DrugBank
Identification
Name: Triazolam
Name (isomeric): DB00897
Drug Type: small molecule
Description: A short-acting benzodiazepine used 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.
Synonyms:
DEA No. 2887; Triazolamum [INN-Latin]
Brand: Novidorm, Clorazolam, Songar, Halcion, Novo-Triolam, Novodorm, Gen-Triazolam, Apo-Triazo, Alti-Triazolam
Category: Adjuvants, Anesthesia, Benzodiazepines, Anti-anxiety Agents, GABA Modulators
CAS number: 28911-01-5
Pharmacology
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 ot...
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Mechanism 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 ...
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Absorption: Bioavailability is 44% (oral) and 53% (sublingual).
Biotransformation: Hepatic. Small amounts of unmetabolized triazolam appear in the urine.
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
Toxicity: Symptoms of overdose include drowsiness, slurred speech, motor inco-ordination, coma, and respiratory depression.
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
RitonavirThe protease inhibitor, ritonavir, may increase the effect of the benzodiazepine, triazolam.
AprepitantAprepitant may increase the effect and toxicity of the benzodiazepine, triazolam.
AtazanavirAtazanavir may increase the effect and toxicity of the benzodiazepine, triazolam.
JosamycinThe macrolide, josamycin, may increase the effect of the benzodiazepine, triazolam.
FosamprenavirFosamprenavir may increase the effect and toxicity of the benzodiazepine, triazolam.
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Targets


Enzymes