triazolam Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
diazepam derivatives 2729 28911-01-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • triazolam
  • U-33,030
  • U 33,030
  • U33,030
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 weight: 343.21
  • Formula: C17H12Cl2N4
  • CLOGP: 2.62
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 43.07
  • ALOGS: -4.27
  • ROTB: 1

Drug dosage:

DoseUnitRoute
0.25 mg O
0.20 mg SL

Approvals:

DateAgencyCompanyOrphan
Nov. 15, 1982 FDA PHARMACIA AND UPJOHN

FDA Adverse Event Reporting System

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Overdose 123.45 53.24 34 211 43525 4595222
Completed suicide 119.61 53.24 33 212 42412 4596335
Sopor 117.46 53.24 23 222 6503 4632244
Intentional self-injury 79.38 53.24 17 228 7366 4631381
Suicide attempt 76.10 53.24 20 225 20822 4617925
Drug abuse 74.87 53.24 21 224 27926 4610821
Purpura senile 73.96 53.24 8 237 27 4638720
Tarsal tunnel syndrome 60.60 53.24 7 238 48 4638699
Intentional overdose 56.52 53.24 16 229 21750 4616997

Pharmacologic Action:

SourceCodeDescription
ATC N05CD05 NERVOUS SYSTEM
PSYCHOLEPTICS
HYPNOTICS AND SEDATIVES
Benzodiazepine derivatives
MeSH PA D000759 Adjuvants, Anesthesia
MeSH PA D014151 Anti-Anxiety Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D018682 GABA Agents
MeSH PA D018757 GABA Modulators
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D011619 Psychotropic Drugs
FDA EPC N0000175694 Benzodiazepine
FDA Chemical/Ingredient N0000007542 Benzodiazepines
MeSH PA D014149 Tranquilizing Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Insomnia indication 193462001
Suicidal thoughts contraindication 6471006
Alcohol intoxication contraindication 25702006
Depressive disorder contraindication 35489007
Substance abuse contraindication 66214007
Psychotic disorder contraindication 69322001
Sleep apnea contraindication 73430006 DOID:0050847
Kidney disease contraindication 90708001 DOID:557
Myasthenia gravis contraindication 91637004 DOID:437
Hypoalbuminemia contraindication 119247004
Disease of liver contraindication 235856003 DOID:409
Sleep automatism contraindication 247962006
Syncope contraindication 271594007
Pregnancy, function contraindication 289908002
Breastfeeding (mother) contraindication 413712001
Chronic lung disease contraindication 413839001

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 5.22 Basic
pKa2 4.62 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
GABA A receptor alpha-5/beta-3/gamma-3 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 8.70 WOMBAT-PK CHEMBL
GABA-A receptor alpha-1/beta-2/gamma-3 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 8.64 WOMBAT-PK CHEMBL
GABA A receptor alpha-5/beta-2/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 9.22 WOMBAT-PK CHEMBL
GABA A receptor alpha-5/beta-2/gamma-3 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 8.70 WOMBAT-PK CHEMBL
GABA-A receptor Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 9.10 IUPHAR CHEMBL
GABA-A receptor alpha-5/beta-3/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 9.02 WOMBAT-PK CHEMBL
GABA-A receptor alpha-1/beta-2/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 9.15 WOMBAT-PK CHEMBL
GABA-A receptor alpha-1/beta-3/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 9.10 WOMBAT-PK CHEMBL
GABA-A receptor alpha-2/beta-3/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 9.23 WOMBAT-PK CHEMBL
GABA A receptor alpha-3/beta-2/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 8.88 WOMBAT-PK CHEMBL
GABA-A receptor alpha-3/beta-3/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 8.84 WOMBAT-PK CHEMBL
GABA A receptor alpha-3/beta-2/gamma-3 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 8.11 WOMBAT-PK CHEMBL
Cytochrome P450 3A4 Enzyme Ki 4.27 WOMBAT-PK
Platelet-activating factor receptor GPCR Ki 5.88 PDSP
GABA-A receptor; anion channel Ion channel Ki 9.10 CHEMBL
Cholecystokinin receptor type A GPCR IC50 4.41 CHEMBL

External reference:

IDSource
4018066 VUID
N0000146407 NUI
C0040879 UMLSCUI
D00387 KEGG_DRUG
1HM943223R UNII
3409 INN_ID
111128007 SNOMEDCT_US
4018066 VANDF
3103 MMSL
10767 RXNORM
386984001 SNOMEDCT_US
5618 MMSL
d00397 MMSL
001466 NDDF
CHEMBL646 ChEMBL_ID
DB00897 DRUGBANK_ID
D014229 MESH_DESCRIPTOR_UI
5556 PUBCHEM_CID
7313 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Halcion HUMAN PRESCRIPTION DRUG LABEL 1 0009-0017 TABLET 0.25 mg ORAL NDA 19 sections
Triazolam HUMAN PRESCRIPTION DRUG LABEL 1 0054-4858 TABLET 0.13 mg ORAL ANDA 18 sections
Triazolam HUMAN PRESCRIPTION DRUG LABEL 1 0054-4859 TABLET 0.25 mg ORAL ANDA 18 sections
TRIAZOLAM HUMAN PRESCRIPTION DRUG LABEL 1 16590-236 TABLET 0.25 mg ORAL NDA authorized generic 14 sections
Triazolam HUMAN PRESCRIPTION DRUG LABEL 1 21695-284 TABLET 0.25 mg ORAL ANDA 13 sections
Triazolam HUMAN PRESCRIPTION DRUG LABEL 1 21695-303 TABLET 0.13 mg ORAL ANDA 13 sections
Triazolam HUMAN PRESCRIPTION DRUG LABEL 1 43063-996 TABLET 0.25 mg ORAL ANDA 18 sections
Triazolam HUMAN PRESCRIPTION DRUG LABEL 1 43353-451 TABLET 0.25 mg ORAL NDA AUTHORIZED GENERIC 15 sections
Triazolam HUMAN PRESCRIPTION DRUG LABEL 1 50090-0522 TABLET 0.25 mg ORAL NDA AUTHORIZED GENERIC 15 sections
Triazolam HUMAN PRESCRIPTION DRUG LABEL 1 50090-4733 TABLET 0.25 mg ORAL ANDA 18 sections
Triazolam HUMAN PRESCRIPTION DRUG LABEL 1 50436-3718 TABLET 0.25 mg ORAL NDA AUTHORIZED GENERIC 15 sections
Triazolam HUMAN PRESCRIPTION DRUG LABEL 1 55289-787 TABLET 0.25 mg ORAL NDA authorized generic 18 sections
Triazolam HUMAN PRESCRIPTION DRUG LABEL 1 59762-3717 TABLET 0.13 mg ORAL NDA AUTHORIZED GENERIC 19 sections
Triazolam HUMAN PRESCRIPTION DRUG LABEL 1 59762-3718 TABLET 0.25 mg ORAL NDA AUTHORIZED GENERIC 19 sections
Triazolam HUMAN PRESCRIPTION DRUG LABEL 1 67544-725 TABLET 0.25 mg ORAL ANDA 14 sections