flumazenil Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| benzodiazepine receptor antagonists/agonists (benzodiazepine derivatives) | 1195 | 78755-81-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.13 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0.50 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.16 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 16 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.80 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 16 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.58 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 0.78 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 20, 1991 | FDA |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Drug withdrawal convulsions | 238.16 | 219.03 | 28 | 87 | 326 | 2357644 |
| Drug dependence | 223.73 | 219.03 | 34 | 81 | 3011 | 2354959 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| 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)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 1.93 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| D005442 | MESH_DESCRIPTOR_UI |
| 4020178 | VUID |
| N0000148120 | NUI |
| C0016293 | UMLSCUI |
| D00697 | KEGG_DRUG |
| 40P7XK9392 | UNII |
| 5311 | INN_ID |
| 96247007 | SNOMEDCT_US |
| 4457 | RXNORM |
| 387575000 | SNOMEDCT_US |
| 4736 | MMSL |
| d01407 | MMSL |
| 4020178 | VANDF |
| 60236 | MMSL |
| 003625 | NDDF |
| CHEBI:5103 | CHEBI |
| CHEMBL407 | ChEMBL_ID |
| DB01205 | DRUGBANK_ID |
| 3373 | PUBCHEM_CID |
| 4192 | IUPHAR_LIGAND_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 | 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 | 51662-1253 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | ANDA | 15 sections |
| FLUMAZENIL | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1254 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | ANDA | 15 sections |
| Flumazenil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52584-088 | INJECTION | 0.10 mg | INTRAVENOUS | ANDA | 13 sections |
| Flumazenil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52584-089 | INJECTION | 0.10 mg | INTRAVENOUS | ANDA | 14 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, SOLUTION | 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 | 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 | 67457-447 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | ANDA | 12 sections |
| Flumazenil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70385-2002 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | ANDA | 15 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 |
| Flumazenil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71872-7206 | INJECTION | 0.10 mg | INTRAVENOUS | ANDA | 14 sections |