oxazepam indications/contra

Stem definitionDrug idCAS RN
diazepam derivatives 2015 604-75-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • oxazepam
  • droxacepam
  • durazepam
  • noctazepam
  • tazepam
  • zaxopam
A benzodiazepine used in the treatment of anxiety, alcohol withdrawal, and insomnia.
  • Molecular weight: 286.72
  • Formula: C15H11ClN2O2
  • CLOGP: 2.31
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 2
  • TPSA: 61.69
  • ALOGS: -3.51
  • ROTB: 1

Drug dosage:

DoseUnitRoute
50 mg O

Approvals:

DateAgencyCompanyOrphan
June 4, 1965 FDA

FDA Adverse Event Reporting System

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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
Toxicity to various agents 1887.43 57.76 431 756 46623 3338049
Overdose 468.25 57.76 137 1050 33841 3350831
Intentional overdose 423.21 57.76 107 1080 15118 3369554
Coma 302.84 57.76 79 1108 12473 3372199
Completed suicide 272.20 57.76 89 1098 31025 3353647
Hypotension 213.82 57.76 84 1103 49430 3335242
Loss of consciousness 203.91 57.76 70 1117 28077 3356595
Accidental overdose 196.50 57.76 50 1137 7068 3377604
Suicide attempt 190.70 57.76 58 1129 15789 3368883
Fall 147.42 57.76 68 1119 58815 3325857
Electrocardiogram QT prolonged 131.70 57.76 40 1147 10755 3373917
Respiratory depression 130.99 57.76 32 1155 3802 3380870
Pneumonia aspiration 129.69 57.76 36 1151 7052 3377620
Confusional state 120.88 57.76 52 1135 37946 3346726
Drug abuse 110.90 57.76 40 1147 18290 3366382
Somnolence 108.72 57.76 46 1141 32158 3352514
Poisoning deliberate 92.66 57.76 19 1168 1012 3383660
Pulmonary oedema 87.26 57.76 30 1157 11881 3372791
Bezoar 82.65 57.76 14 1173 257 3384415
Oesophageal obstruction 81.53 57.76 13 1174 161 3384511
Cardiac arrest 75.69 57.76 34 1153 27285 3357387
Blood creatine phosphokinase increased 73.39 57.76 27 1160 12986 3371686
Drug interaction 69.24 57.76 38 1149 46774 3337898
Tachycardia 67.63 57.76 30 1157 23341 3361331
Pulmonary congestion 67.39 57.76 18 1169 3032 3381640
Exposure during pregnancy 65.97 57.76 31 1156 27532 3357140
Delirium 65.64 57.76 23 1164 9605 3375067
Aggression 61.88 57.76 23 1164 11362 3373310
Hyponatraemia 61.03 57.76 26 1161 18333 3366339
Neuroleptic malignant syndrome 60.69 57.76 18 1169 4423 3380249

Pharmacologic Action:

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SourceCodeDescription
ATC N05BA04 NERVOUS SYSTEM
PSYCHOLEPTICS
ANXIOLYTICS
Benzodiazepine derivatives
FDA EPC N0000175694 Benzodiazepine
FDA Chemical/Ingredient N0000007542 Benzodiazepines
MeSH PA D014151 Anti-Anxiety Agents
CHEBI has role CHEBI:35474 anxiolytic drug
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 D006993 Hypnotics and Sedatives
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014149 Tranquilizing Agents

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Alcohol withdrawal delirium indication 8635005
Anxiety indication 48694002
Suicidal thoughts contraindication 6471006
Disorder of lung contraindication 19829001 DOID:850
Borderline personality disorder contraindication 20010003 DOID:10930
Alcohol intoxication contraindication 25702006
Shock contraindication 27942005
Depressive disorder contraindication 35489007 DOID:2848
Low blood pressure contraindication 45007003
Substance abuse contraindication 66214007
Psychotic disorder contraindication 69322001
Sleep apnea contraindication 73430006 DOID:0050848
Decreased respiratory function contraindication 80954004
Kidney disease contraindication 90708001 DOID:2527
Hypoalbuminemia contraindication 119247004
Disease of liver contraindication 235856003 DOID:409
Sleep automatism contraindication 247962006
Syncope contraindication 271594007
Pregnancy, function contraindication 289908002
Coma contraindication 371632003
Porphyria contraindication 418470004 DOID:13268
Behavioral Disorders contraindication

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.41 acidic
pKa2 11.87 acidic
pKa3 1.83 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
GABA-A receptor alpha-1/beta-3/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR IC50 7.75 WOMBAT-PK CHEMBL

External reference:

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IDSource
4018020 VUID
N0000146364 NUI
C0029997 UMLSCUI
7253 IUPHAR_LIGAND_ID
D00464 KEGG_DRUG
CHEMBL568 ChEMBL_ID
6GOW6DWN2A UNII
1507 INN_ID
DB00842 DRUGBANK_ID
4616 PUBCHEM_CID
4018020 VANDF
4493 MMSL
7781 RXNORM
387455006 SNOMEDCT_US
79225003 SNOMEDCT_US
5211 MMSL
d00040 MMSL
N0000007438 NDFRT
N0000146364 NDFRT
001462 NDDF
CHEBI:7823 CHEBI
D010076 MESH_DESCRIPTOR_UI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Oxazepam HUMAN PRESCRIPTION DRUG LABEL 1 0228-2067 CAPSULE, GELATIN COATED 10 mg ORAL ANDA 16 sections
Oxazepam HUMAN PRESCRIPTION DRUG LABEL 1 0228-2069 CAPSULE, GELATIN COATED 15 mg ORAL ANDA 16 sections
Oxazepam HUMAN PRESCRIPTION DRUG LABEL 1 0228-2073 CAPSULE, GELATIN COATED 30 mg ORAL ANDA 16 sections
Oxazepam HUMAN PRESCRIPTION DRUG LABEL 1 0781-2809 CAPSULE 10 mg ORAL ANDA 16 sections
Oxazepam HUMAN PRESCRIPTION DRUG LABEL 1 0781-2810 CAPSULE 15 mg ORAL ANDA 16 sections
Oxazepam HUMAN PRESCRIPTION DRUG LABEL 1 0781-2811 CAPSULE 30 mg ORAL ANDA 16 sections
OXAZEPAM HUMAN PRESCRIPTION DRUG LABEL 1 16590-304 CAPSULE 15 mg ORAL ANDA 13 sections
Oxazepam HUMAN PRESCRIPTION DRUG LABEL 1 43353-074 CAPSULE, GELATIN COATED 30 mg ORAL ANDA 15 sections
Oxazepam HUMAN PRESCRIPTION DRUG LABEL 1 43353-965 CAPSULE 10 mg ORAL ANDA 14 sections
Oxazepam HUMAN PRESCRIPTION DRUG LABEL 1 43353-980 CAPSULE 30 mg ORAL ANDA 14 sections
Oxazepam HUMAN PRESCRIPTION DRUG LABEL 1 61786-910 CAPSULE 15 mg ORAL ANDA 16 sections
Oxazepam HUMAN PRESCRIPTION DRUG LABEL 1 62584-812 CAPSULE, GELATIN COATED 10 mg ORAL ANDA 17 sections
Oxazepam HUMAN PRESCRIPTION DRUG LABEL 1 62584-813 CAPSULE, GELATIN COATED 15 mg ORAL ANDA 17 sections
Oxazepam HUMAN PRESCRIPTION DRUG LABEL 1 62584-814 CAPSULE, GELATIN COATED 30 mg ORAL ANDA 17 sections
Oxazepam HUMAN PRESCRIPTION DRUG LABEL 1 67544-117 CAPSULE, GELATIN COATED 10 mg ORAL ANDA 15 sections
Oxazepam HUMAN PRESCRIPTION DRUG LABEL 1 67544-268 CAPSULE, GELATIN COATED 15 mg ORAL ANDA 15 sections
Oxazepam HUMAN PRESCRIPTION DRUG LABEL 1 67544-294 CAPSULE 15 mg ORAL ANDA 16 sections
Oxazepam HUMAN PRESCRIPTION DRUG LABEL 1 69189-2810 CAPSULE 15 mg ORAL ANDA 14 sections