Stem definition | Drug id | CAS RN |
---|---|---|
benzodiazepine receptor antagonists/agonists (benzodiazepine derivatives) | 1195 | 78755-81-4 |
None
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 |
Date | Agency | Company | Orphan |
---|---|---|---|
Dec. 20, 1991 | FDA |
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 | 187.72 | 54.07 | 30 | 722 | 1311 | 46683999 |
Intentional overdose | 153.94 | 54.07 | 52 | 700 | 64892 | 46620418 |
Drug dependence | 135.15 | 54.07 | 36 | 716 | 19865 | 46665445 |
Intentional product misuse | 100.64 | 54.07 | 35 | 717 | 47093 | 46638217 |
Product use issue | 76.96 | 54.07 | 35 | 717 | 94609 | 46590701 |
Seizure | 59.60 | 54.07 | 32 | 720 | 123022 | 46562288 |
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 |
---|---|---|---|---|---|---|
Intentional overdose | 86.50 | 38.21 | 35 | 793 | 41446 | 29910204 |
Drug withdrawal convulsions | 71.27 | 38.21 | 14 | 814 | 1145 | 29950505 |
Coma | 63.73 | 38.21 | 28 | 800 | 40421 | 29911229 |
Drug dependence | 54.91 | 38.21 | 21 | 807 | 21274 | 29930376 |
Intentional product misuse | 51.35 | 38.21 | 23 | 805 | 34644 | 29917006 |
Product use issue | 42.24 | 38.21 | 22 | 806 | 45994 | 29905656 |
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 | gamma-aminobutyric acid receptor antagonists |
CHEBI has role | CHEBI:90757 | antidote to benzodiazepine overdose |
MeSH PA | D000931 | Antidotes |
MeSH PA | D018682 | GABA Agents |
MeSH PA | D018757 | GABA Modulators |
MeSH PA | D018377 | Neurotransmitter Agents |
MeSH PA | D020011 | Protective Agents |
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 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 1.93 | Basic |
None
None
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 |
ID | Source |
---|---|
4020178 | VUID |
N0000148120 | NUI |
D00697 | KEGG_DRUG |
4020178 | VANDF |
C0591091 | UMLSCUI |
CHEBI:5103 | CHEBI |
FYP | PDB_CHEM_ID |
CHEMBL407 | ChEMBL_ID |
DB01205 | DRUGBANK_ID |
D005442 | MESH_DESCRIPTOR_UI |
3373 | PUBCHEM_CID |
4192 | IUPHAR_LIGAND_ID |
5311 | INN_ID |
40P7XK9392 | UNII |
4457 | RXNORM |
4736 | MMSL |
60236 | MMSL |
d01407 | MMSL |
003625 | NDDF |
387575000 | SNOMEDCT_US |
96247007 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Flumazenil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9683 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | ANDA | 30 sections |
Flumazenil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9684 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | ANDA | 30 sections |
Flumazenil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9783 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | ANDA | 29 sections |
Flumazenil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9784 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | ANDA | 29 sections |
Flumazenil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-6031 | INJECTION | 0.10 mg | INTRAVENOUS | ANDA | 31 sections |
Flumazenil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-6032 | INJECTION | 0.10 mg | INTRAVENOUS | ANDA | 31 sections |
Flumazenil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 36000-148 | INJECTION | 0.10 mg | INTRAVENOUS | ANDA | 30 sections |
Flumazenil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 36000-149 | INJECTION | 0.10 mg | INTRAVENOUS | ANDA | 30 sections |
Flumazenil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-1337 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | ANDA | 29 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 | 51662-1579 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | ANDA | 14 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 | 29 sections |
Flumazenil | Human Prescription Drug Label | 1 | 63323-424 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | ANDA | 12 sections |
Flumazenil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67457-444 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | ANDA | 17 sections |
Flumazenil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67457-447 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | ANDA | 17 sections |
Flumazenil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70385-2002 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | ANDA | 29 sections |
Flumazenil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70385-2021 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | ANDA | 29 sections |
Flumazenil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71872-7008 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | ANDA | 29 sections |
Flumazenil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71872-7038 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | ANDA | 29 sections |
Flumazenil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71872-7206 | INJECTION | 0.10 mg | INTRAVENOUS | ANDA | 30 sections |