All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

flumazenil 🐶 Veterinary Use | 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
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 Status: OFP 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	185.95	55.06	30	913	1332	56289792
Intentional overdose	149.14	55.06	52	891	68065	56223059
Drug dependence	124.56	55.06	35	908	22498	56268626
Intentional product misuse	92.37	55.06	34	909	51470	56239654
Seizure	77.85	55.06	39	904	125080	56166044
Coma	73.51	55.06	30	913	59625	56231499
Depressed level of consciousness	71.65	55.06	29	914	56404	56234720
Toxicity to various agents	56.64	55.06	39	904	224525	56066599

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
Intentional overdose	94.76	38.83	37	810	41352	31655145
Drug withdrawal convulsions	71.63	38.83	14	833	1154	31695343
Drug dependence	54.40	38.83	21	826	22558	31673939
Intentional product misuse	53.27	38.83	24	823	37927	31658570
Coma	39.33	38.83	20	827	41130	31655367

FDA Adverse Event Reporting System (Geriatric)

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	249.34	36.52	44	1829	2104	70924467
Intentional overdose	230.10	36.52	89	1784	98346	70828225
Drug dependence	172.04	36.52	56	1817	37265	70889306
Intentional product misuse	134.03	36.52	57	1816	79538	70847033
Seizure	100.93	36.52	61	1812	177901	70748670
Coma	98.28	36.52	48	1825	91796	70834775
Product use issue	90.11	36.52	57	1816	179880	70746691
Depressed level of consciousness	73.92	36.52	39	1834	87392	70839179
Toxicity to various agents	70.80	36.52	67	1806	382105	70544466
Psychogenic seizure	70.65	36.52	15	1858	1881	70924690
Suicide attempt	49.44	36.52	29	1844	79481	70847090
Unresponsive to stimuli	43.35	36.52	23	1850	51908	70874663
Overdose	41.66	36.52	35	1838	169710	70756861
Electrocardiogram QRS complex shortened	40.91	36.52	8	1865	665	70925906
Electrocardiogram QRS complex prolonged	38.21	36.52	13	1860	9793	70916778

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	V03AB25	VARIOUS ALL OTHER THERAPEUTIC PRODUCTS ALL OTHER THERAPEUTIC PRODUCTS Antidotes
CHEBI has role	CHEBI:65259	GABA 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
FDA EPC	N0000175680	Benzodiazepine Antagonist

Drug Use | Suggest Off label Use Form| |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

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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-2/beta-3/gamma-2	Ion channel	P18507 P28472 P47869	GBRG2_HUMAN GBRB3_HUMAN GBRA2_HUMAN	ALLOSTERIC ANTAGONIST	Ki	9.05		WOMBAT-PK	CHEMBL
GABA-A receptor alpha-3/beta-3/gamma-2	Ion channel	P18507 P28472 P34903	GBRG2_HUMAN GBRB3_HUMAN GBRA3_HUMAN	ALLOSTERIC ANTAGONIST	Ki	8.98		WOMBAT-PK	CHEMBL
GABA-A receptor alpha-5/beta-3/gamma-2	Ion channel	P18507 P28472 P31644	GBRG2_HUMAN GBRB3_HUMAN GBRA5_HUMAN	ALLOSTERIC ANTAGONIST	Ki	9.22		WOMBAT-PK	CHEMBL
GABA-A receptor alpha-1/beta-3/gamma-2	Ion channel	P14867 P18507 P28472	GBRA1_HUMAN GBRG2_HUMAN GBRB3_HUMAN	ALLOSTERIC ANTAGONIST	Ki	9.10		WOMBAT-PK	CHEMBL
GABA-A receptor alpha-6/beta-3/gamma-2	Ion channel	P18507 P28472 Q16445	GBRG2_HUMAN GBRB3_HUMAN GBRA6_HUMAN	ALLOSTERIC ANTAGONIST	Ki	6.83		WOMBAT-PK	CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-4	Ion channel	P48169	GBRA4_HUMAN	ALLOSTERIC ANTAGONIST	Ki	8.70		CHEMBL	CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-1	Ion channel	P14867	GBRA1_HUMAN		Kd	8.70		CHEMBL
GABA-A receptor; anion channel	Ion channel	O00591 O14764 P14867 P18505 P18507 P28472 P31644 P34903 P47869 P47870 P48169 P78334 Q16445 Q8N1C3 Q99928 Q9UN88	GBRP_HUMAN GBRD_HUMAN GBRA1_HUMAN GBRB1_HUMAN GBRG2_HUMAN GBRB3_HUMAN GBRA5_HUMAN GBRA3_HUMAN GBRA2_HUMAN GBRB2_HUMAN GBRA4_HUMAN GBRE_HUMAN GBRA6_HUMAN GBRG1_HUMAN GBRG3_HUMAN GBRT_HUMAN		Ki	9.05		CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-2	Ion channel	P47869	GBRA2_HUMAN		Ki	8.24		CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-3	Ion channel	P34903	GBRA3_HUMAN		Ki	8.09		CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-5	Ion channel	P31644	GBRA5_HUMAN		Kd	9.30		CHEMBL
GABA A receptor alpha-3/beta-2/gamma-2	Ion channel		GBRG2_RAT GBRA3_RAT GBRB2_RAT		Ki	9.22		CHEMBL
GABA A receptor alpha-6/beta-2/gamma-2	Ion channel		GBRG2_RAT GBRA6_RAT GBRB2_RAT		Ki	7.82		CHEMBL
GABA-A receptor; alpha-1/beta-2/gamma-2	Ion channel		GBRG2_RAT GBRA1_RAT GBRB2_RAT		Ki	9.30		CHEMBL
GABA-A receptor; anion channel	Ion channel		GBRP_RAT GBRB1_RAT GBRD_RAT GBRG2_RAT GBRA5_RAT GBRA3_RAT GBRG1_RAT GBRA2_RAT GBRA4_RAT GBRG3_RAT GBRA6_RAT GBRA1_RAT GBRB3_RAT GBRB2_RAT Q91ZM7_RAT GBRE_RAT		Ki	9.10		CHEMBL
GABA-A receptor; anion channel	Ion channel		GBRA1_BOVIN GBRB1_BOVIN GBRA2_BOVIN GBRA3_BOVIN GBRA4_BOVIN GBRG2_BOVIN		Ki	10.05		CHEMBL

External reference:

ID	Source
4020178	VUID
N0000148120	NUI
D00697	KEGG_DRUG
4020178	VANDF
C0016293	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

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	30 sections
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	0143-9684	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	0404-9859	INJECTION	0.10 mg	INTRAVENOUS	ANDA	14 sections
Flumazenil	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9859	INJECTION	0.10 mg	INTRAVENOUS	ANDA	14 sections
Flumazenil	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9860	INJECTION	0.10 mg	INTRAVENOUS	ANDA	14 sections
Flumazenil	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9860	INJECTION	0.10 mg	INTRAVENOUS	ANDA	14 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	51662-1253	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	51662-1254	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	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	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	70518-3456	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	ANDA	12 sections
Flumazenil	HUMAN PRESCRIPTION DRUG LABEL	1	71872-7008	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	ANDA	29 sections
Flumazenil	HUMAN PRESCRIPTION DRUG LABEL	1	71872-7008	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	ANDA	29 sections