flumazenil indications/contra

Stem definitionDrug idCAS RN
benzodiazepine receptor antagonists/agonists (benzodiazepine derivatives) 1195 78755-81-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • flumazenil
  • anexate
  • flumazepil
  • mazicon
  • Ro-15-1788
A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses.
  • Molecular weight: 303.29
  • Formula: C15H14FN3O3
  • CLOGP: 1.29
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 0
  • TPSA: 64.43
  • ALOGS: -2.46
  • ROTB: 3

Drug dosage:

None

Approvals:

DateAgencyCompanyOrphan
Dec. 20, 1991 FDA

FDA Adverse Event Reporting System

None

Pharmacologic Action:

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SourceCodeDescription
ATC V03AB25 VARIOUS
ALL OTHER THERAPEUTIC PRODUCTS
ALL OTHER THERAPEUTIC PRODUCTS
Antidotes
FDA EPC N0000175680 Benzodiazepine Antagonist
CHEBI has role CHEBI:65259 GABA antagonist
CHEBI has role CHEBI:90757 antidote to benzodiazepine poisoning
MeSH PA D000931 Antidotes
MeSH PA D018682 GABA Agents
MeSH PA D018757 GABA Modulators
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D020011 Protective Agents

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Benzodiazepine Induced Sedation indication
Benzodiazepine Toxicity indication
Benzodiazepine Maintained Anesthesia indication
Anxiety contraindication 48694002
Neuromuscular block, function contraindication 55394004
Heart disease contraindication 56265001 DOID:114
Injury of head contraindication 82271004
Epilepsy contraindication 84757009 DOID:1826
Benzodiazepine dependence contraindication 231473004
Disease of liver contraindication 235856003 DOID:409
Panic disorder contraindication 371631005 DOID:594
Tricyclic Antidepressant Toxicity contraindication

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 1.93 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-6/beta-3/gamma-2 Ion channel ALLOSTERIC ANTAGONIST Ki 6.83 WOMBAT-PK CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-4 Ion channel ALLOSTERIC ANTAGONIST Ki 8.70 CHEMBL CHEMBL
GABA-A receptor alpha-1/beta-3/gamma-2 Ion channel ALLOSTERIC ANTAGONIST Ki 9.10 WOMBAT-PK CHEMBL
GABA-A receptor alpha-2/beta-3/gamma-2 Ion channel ALLOSTERIC ANTAGONIST Ki 9.05 WOMBAT-PK CHEMBL
GABA-A receptor alpha-3/beta-3/gamma-2 Ion channel ALLOSTERIC ANTAGONIST Ki 8.98 WOMBAT-PK CHEMBL
GABA-A receptor alpha-5/beta-3/gamma-2 Ion channel ALLOSTERIC ANTAGONIST Ki 9.22 WOMBAT-PK CHEMBL
GABA-A receptor; anion channel Ion channel Ki 9.05 CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-1 Ion channel Kd 8.70 CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-2 Ion channel Ki 8.24 CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-3 Ion channel Ki 8.09 CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-5 Ion channel Kd 9.30 CHEMBL
GABA A receptor alpha-6/beta-2/gamma-2 Ion channel Ki 7.82 CHEMBL
GABA-A receptor; anion channel Ion channel Ki 9.10 CHEMBL
GABA-A receptor; anion channel Ion channel Ki 10.05 CHEMBL
GABA-A receptor; alpha-1/beta-2/gamma-2 Ion channel Ki 9.30 CHEMBL
GABA A receptor alpha-3/beta-2/gamma-2 Ion channel Ki 9.22 CHEMBL

External reference:

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IDSource
4192 IUPHAR_LIGAND_ID
4020178 VUID
N0000148120 NUI
C0016293 UMLSCUI
D00697 KEGG_DRUG
CHEMBL407 ChEMBL_ID
40P7XK9392 UNII
5311 INN_ID
4457 RXNORM
387575000 SNOMEDCT_US
96247007 SNOMEDCT_US
4736 MMSL
d01407 MMSL
4020178 VANDF
60236 MMSL
N0000007021 NDFRT
N0000148120 NDFRT
003625 NDDF
3373 PUBCHEM_CID
CHEBI:5103 CHEBI
D005442 MESH_DESCRIPTOR_UI
DB01205 DRUGBANK_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
FLUMAZENIL HUMAN PRESCRIPTION DRUG LABEL 1 0069-0093 INJECTION, SOLUTION 0.10 mg INTRAVENOUS ANDA 14 sections
FLUMAZENIL HUMAN PRESCRIPTION DRUG LABEL 1 0069-0105 INJECTION, SOLUTION 0.10 mg INTRAVENOUS ANDA 14 sections
Flumazenil HUMAN PRESCRIPTION DRUG LABEL 1 0143-9683 INJECTION, SOLUTION 0.10 mg INTRAVENOUS ANDA 15 sections
Flumazenil HUMAN PRESCRIPTION DRUG LABEL 1 0143-9684 INJECTION, SOLUTION 0.10 mg INTRAVENOUS ANDA 15 sections
Flumazenil HUMAN PRESCRIPTION DRUG LABEL 1 0143-9783 INJECTION, SOLUTION 0.10 mg INTRAVENOUS ANDA 15 sections
Flumazenil HUMAN PRESCRIPTION DRUG LABEL 1 0143-9784 INJECTION, SOLUTION 0.10 mg INTRAVENOUS ANDA 15 sections
Flumazenil HUMAN PRESCRIPTION DRUG LABEL 1 0641-6031 INJECTION 0.10 mg INTRAVENOUS ANDA 14 sections
Flumazenil HUMAN PRESCRIPTION DRUG LABEL 1 0641-6032 INJECTION 0.10 mg INTRAVENOUS ANDA 14 sections
Flumazenil HUMAN PRESCRIPTION DRUG LABEL 1 0781-3003 INJECTION 0.10 mg INTRAVENOUS ANDA 14 sections
Flumazenil HUMAN PRESCRIPTION DRUG LABEL 1 25021-600 INJECTION, SOLUTION 0.10 mg INTRAVENOUS ANDA 14 sections
Flumazenil HUMAN PRESCRIPTION DRUG LABEL 1 36000-148 INJECTION 0.10 mg INTRAVENOUS ANDA 14 sections
Flumazenil HUMAN PRESCRIPTION DRUG LABEL 1 36000-149 INJECTION 0.10 mg INTRAVENOUS ANDA 14 sections
Flumazenil HUMAN PRESCRIPTION DRUG LABEL 1 50090-1337 INJECTION, SOLUTION 0.10 mg INTRAVENOUS ANDA 15 sections
Flumazenil HUMAN PRESCRIPTION DRUG LABEL 1 52584-093 INJECTION 1 mg INTRAVENOUS ANDA 12 sections
Flumazenil HUMAN PRESCRIPTION DRUG LABEL 1 52584-783 INJECTION, SOLUTION 0.10 mg INTRAVENOUS ANDA 12 sections
Flumazenil HUMAN PRESCRIPTION DRUG LABEL 1 52584-784 INJECTION 0.10 mg INTRAVENOUS ANDA 14 sections
Flumazenil HUMAN PRESCRIPTION DRUG LABEL 1 54868-5715 INJECTION 0.10 mg INTRAVENOUS ANDA 13 sections
Flumazenil HUMAN PRESCRIPTION DRUG LABEL 1 55154-7474 INJECTION, SOLUTION 0.10 mg INTRAVENOUS ANDA 15 sections
Flumazenil HUMAN PRESCRIPTION DRUG LABEL 1 63323-424 INJECTION, SOLUTION 0.10 mg INTRAVENOUS ANDA 13 sections
Flumazenil HUMAN PRESCRIPTION DRUG LABEL 1 67457-444 INJECTION, SOLUTION 0.10 mg INTRAVENOUS ANDA 12 sections
Flumazenil HUMAN PRESCRIPTION DRUG LABEL 1 70385-2021 INJECTION, SOLUTION 0.10 mg INTRAVENOUS ANDA 15 sections
Flumazenil HUMAN PRESCRIPTION DRUG LABEL 1 71872-7008 INJECTION, SOLUTION 0.10 mg INTRAVENOUS ANDA 15 sections
Flumazenil HUMAN PRESCRIPTION DRUG LABEL 1 71872-7038 INJECTION, SOLUTION 0.10 mg INTRAVENOUS ANDA 15 sections