diazepam indications/contra

Stem definitionDrug idCAS RN
diazepam derivatives 852 439-14-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • RO-5-2807
  • diazepam
  • valium
A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.
  • Molecular weight: 284.74
  • Formula: C16H13ClN2O
  • CLOGP: 2.96
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 0
  • TPSA: 32.67
  • ALOGS: -4.37
  • ROTB: 1

Drug dosage:

DoseUnitRoute
10 mg O
10 mg P
10 mg R

Approvals:

DateAgencyCompanyOrphan
Nov. 15, 1963 FDA ROCHE

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 9501.15 41.51 2565 10054 44489 3328751
Drug abuse 8465.61 41.51 1950 10669 16380 3356860
Completed suicide 6312.12 41.51 1716 10903 29398 3343842
Overdose 3281.67 41.51 1062 11557 32916 3340324
Respiratory arrest 3159.57 41.51 811 11808 10557 3362683
Cardiac arrest 2796.86 41.51 894 11725 26425 3346815
Poisoning 2093.21 41.51 499 12120 4613 3368627
Cardio-respiratory arrest 1877.53 41.51 578 12041 14862 3358378
Death 1717.52 41.51 1050 11569 151274 3221966
Intentional overdose 1716.16 41.51 538 12081 14687 3358553
Suicide attempt 1413.01 41.51 469 12150 15378 3357862
Coma 1406.74 41.51 442 12177 12110 3361130
Somnolence 1377.54 41.51 554 12065 31650 3341590
Intentional product misuse 1123.55 41.51 374 12245 12327 3360913
Exposure via father 987.34 41.51 185 12434 410 3372830
Accidental overdose 954.30 41.51 288 12331 6830 3366410
Respiratory depression 931.70 41.51 247 12372 3587 3369653
Sopor 874.28 41.51 234 12385 3530 3369710
Small for dates baby 816.38 41.51 189 12430 1498 3371742
Drug interaction 738.90 41.51 405 12214 46407 3326833
Hypotension 592.70 41.51 358 12261 49156 3324084
Intentional self-injury 580.99 41.51 183 12436 5002 3368238
Drug dependence 568.51 41.51 173 12446 4203 3369037
Confusional state 528.62 41.51 303 12316 37695 3335545
Agitation 477.19 41.51 228 12391 19478 3353762
Exposure via ingestion 458.52 41.51 116 12503 1377 3371863
Sedation 453.44 41.51 158 12461 5943 3367297
Depressed level of consciousness 439.21 41.51 183 12436 11282 3361958
Loss of consciousness 430.45 41.51 239 12380 27908 3345332
Poisoning deliberate 381.32 41.51 93 12526 938 3372302

Pharmacologic Action:

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SourceCodeDescription
ATC N05BA01 NERVOUS SYSTEM
PSYCHOLEPTICS
ANXIOLYTICS
Benzodiazepine derivatives
MeSH PA D000759 Adjuvants, Anesthesia
MeSH PA D000777 Anesthetics
MeSH PA D018681 Anesthetics, General
MeSH PA D018686 Anesthetics, Intravenous
MeSH PA D014151 Anti-Anxiety Agents
CHEBI has role CHEBI:35474 anxiolytic drug
CHEBI has role CHEBI:35623 anticonvulsant
CHEBI has role CHEBI:35717 sedative
MeSH PA D000927 Anticonvulsants
MeSH PA D000932 Antiemetics
MeSH PA D001337 Autonomic 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 D005765 Gastrointestinal Agents
MeSH PA D006993 Hypnotics and Sedatives
MeSH PA D009125 Muscle Relaxants, Central
MeSH PA D009465 Neuromuscular Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014149 Tranquilizing Agents
FDA EPC N0000175694 Benzodiazepine
FDA Chemical/Ingredient N0000007542 Benzodiazepines

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Alcohol withdrawal delirium indication 8635005
Anxiety indication 48694002
Sedation indication 72641008
Tetanus indication 76902006 DOID:11338
Epilepsy indication 84757009 DOID:1826
Alcohol withdrawal syndrome indication 191480000
Spasticity indication 221360009
Status epilepticus indication 230456007 DOID:1824
Preoperative Anxiety indication
Induce Anterograde Amnesia indication
Disorder of lung contraindication 19829001 DOID:850
Alcohol intoxication contraindication 25702006
Depressive disorder contraindication 35489007 DOID:2848
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Substance abuse contraindication 66214007
Sleep apnea contraindication 73430006 DOID:0050848
Decreased respiratory function contraindication 80954004
Open-angle glaucoma contraindication 84494001 DOID:1067
Myasthenia gravis contraindication 91637004 DOID:437
Hypoalbuminemia contraindication 119247004
Disease of liver contraindication 235856003 DOID:409
Pregnancy, function contraindication 289908002
Severe chronic obstructive pulmonary disease contraindication 313299006
Angle-closure glaucoma contraindication 392291006 DOID:13550
Breastfeeding (mother) contraindication 413712001
Panic disorder off-label use 371631005 DOID:594
Cocaine-Associated Acute Ischemic Heart Disease off-label use

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.06 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-2/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR EC50 7.14 WOMBAT-PK CHEMBL
GABA-A receptor alpha-1/beta-3/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 7.85 WOMBAT-PK CHEMBL
GABA-A receptor alpha-2/beta-3/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 7.70 WOMBAT-PK CHEMBL
GABA A receptor alpha-3/beta-2/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 7.94 WOMBAT-PK CHEMBL
GABA-A receptor alpha-5/beta-3/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 7.96 WOMBAT-PK CHEMBL
GABA A receptor alpha-5/beta-2/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 8.00 WOMBAT-PK CHEMBL
GABA A receptor alpha-5/beta-2/gamma-3 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 7.20 WOMBAT-PK CHEMBL
GABA A receptor alpha-5/beta-3/gamma-3 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 7.20 WOMBAT-PK CHEMBL
GABA-A receptor alpha-1/beta-2/gamma-3 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 6.71 WOMBAT-PK CHEMBL
GABA A receptor alpha-3/beta-2/gamma-3 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 6.67 WOMBAT-PK CHEMBL
GABA-A receptor alpha-3/beta-3/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 7.65 WOMBAT-PK CHEMBL
Cytochrome P450 3A4 Enzyme Ki 4.42 WOMBAT-PK
Alpha-1A adrenergic receptor GPCR ALLOSTERIC MODULATOR Ki 4.10 IUPHAR
Gamma-aminobutyric acid receptor subunit alpha-5 Ion channel Kd 7.64 CHEMBL
Adenosine receptor A3 GPCR IC50 7.92 CHEMBL
Translocator protein Membrane receptor Kd 6.67 CHEMBL
Cholinesterase Enzyme Ki 7.37 CHEMBL
GABA-A receptor; anion channel Ion channel Ki 8.54 CHEMBL
GABA-A receptor; anion channel Ion channel Ki 4.07 CHEMBL
GABA A receptor alpha-2/beta-2/gamma-2 Ion channel Ki 7.70 CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-2 Ion channel Ki 7.82 CHEMBL
Thyrotropin-releasing hormone receptor GPCR ANTAGONIST Ki 5.15 IUPHAR
GABA-A receptor; alpha-1/beta-2/gamma-2 Ion channel Ki 7.92 CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-1 Ion channel Ki 7.96 CHEMBL
Fatty acid-binding protein, liver Unclassified Ki 6.27 CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-5 Ion channel Ki 8.01 CHEMBL
GABA-A receptor; anion channel Ion channel Ki 8 CHEMBL
GABA A receptor alpha-3/beta-2/gamma-2 Ion channel Ki 7.86 CHEMBL
Acetylcholinesterase Enzyme Ki 4.89 CHEMBL
GABA A receptor alpha-5/beta-3/gamma-2 Ion channel Ki 7.96 CHEMBL
GABA A receptor alpha-6/beta-2/gamma-2 Ion channel Ki 8.68 CHEMBL

External reference:

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IDSource
3364 IUPHAR_LIGAND_ID
4017796 VUID
N0000146157 NUI
C0012010 UMLSCUI
D00293 KEGG_DRUG
CHEMBL12 ChEMBL_ID
DB00829 DRUGBANK_ID
3016 PUBCHEM_CID
387264003 SNOMEDCT_US
48546005 SNOMEDCT_US
4573 MMSL
4017796 VANDF
3322 RXNORM
N0000006321 NDFRT
N0000146157 NDFRT
001461 NDDF
d00148 MMSL
894 MMSL
CHEBI:49575 CHEBI
D003975 MESH_DESCRIPTOR_UI
Q3JTX2Q7TU UNII
1295 INN_ID
DZP PDB_CHEM_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Diazepam Intensol HUMAN PRESCRIPTION DRUG LABEL 1 0054-3185 SOLUTION, CONCENTRATE 5 mg ORAL ANDA 13 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0054-3188 SOLUTION 5 mg ORAL ANDA 13 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0093-6137 GEL 2.50 mg RECTAL NDA authorized generic 13 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0093-6138 GEL 10 mg RECTAL NDA authorized generic 13 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0093-6139 GEL 20 mg RECTAL NDA authorized generic 13 sections
Valium HUMAN PRESCRIPTION DRUG LABEL 1 0140-0004 TABLET 2 mg ORAL NDA 15 sections
Valium HUMAN PRESCRIPTION DRUG LABEL 1 0140-0005 TABLET 5 mg ORAL NDA 15 sections
Valium HUMAN PRESCRIPTION DRUG LABEL 1 0140-0006 TABLET 10 mg ORAL NDA 15 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0172-3925 TABLET 2 mg ORAL ANDA 14 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0172-3926 TABLET 5 mg ORAL ANDA 14 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0172-3927 TABLET 10 mg ORAL ANDA 14 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0179-1429 TABLET 5 mg ORAL ANDA 12 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0179-1431 TABLET 10 mg ORAL ANDA 12 sections
Diastat HUMAN PRESCRIPTION DRUG LABEL 1 0187-0658 GEL 10 mg RECTAL NDA 14 sections
Diastat HUMAN PRESCRIPTION DRUG LABEL 1 0187-0659 GEL 20 mg RECTAL NDA 14 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0378-0271 TABLET 2 mg ORAL ANDA 14 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0378-0345 TABLET 5 mg ORAL ANDA 14 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0378-0477 TABLET 10 mg ORAL ANDA 14 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0409-1273 INJECTION, SOLUTION 5 mg INTRAMUSCULAR ANDA 15 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0409-3213 INJECTION, SOLUTION 5 mg INTRAMUSCULAR ANDA 13 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0527-1767 SOLUTION 5 mg ORAL ANDA 12 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0527-1768 SOLUTION, CONCENTRATE 5 mg ORAL ANDA 12 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0591-5619 TABLET 5 mg ORAL ANDA 12 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0591-5620 TABLET 10 mg ORAL ANDA 12 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0591-5621 TABLET 2 mg ORAL ANDA 12 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0603-3213 TABLET 2 mg ORAL ANDA 14 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0603-3214 TABLET 5 mg ORAL ANDA 14 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0603-3215 TABLET 10 mg ORAL ANDA 14 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0615-7800 TABLET 10 mg ORAL ANDA 12 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0615-8049 TABLET 5 mg ORAL ANDA 12 sections