flumazenil

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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

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	1.082		High	1
caco2-efflux	Caco-2 efflux ratio (BA/AB)	0.887		High	1
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	64.269	10^-6 cm/s	High	1
dh-clint	Dog hepatocyte intrinsic clearance	13.614	uL/min/10^6 cells	High	1
dppb	Dog plasma protein binding (% unbound)	69.320	%	High	1
fcs-ppb	Fetal calf serum protein binding (% unbound)	77.010	%	High	1
herg	hERG pIC50	4.166	pIC50	High	1
hh-clint	Human hepatocyte intrinsic clearance	3.597	uL/min/10^6 cells	High	1
hlm-clint	Human liver microsomal intrinsic clearance	11.588	uL/min/mg protein	High	1
hppb	Human plasma protein binding (% unbound)	62.400	%	High	1
kinase-safety-class	ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,MAPK7,PDK1,PDK2,PIK3CD,PRKDC,TEK	16
mdck-mdr1-bcrp-efflux	MDCK-MDR1-BCRP efflux ratio	1.127		High	1
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	1.180		High	1
mh-clint	Mouse hepatocyte intrinsic clearance	35.481		High	1
mppb	Mouse plasma protein binding (% unbound)	64.690		High	1
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	1.928		High	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pppb	Pig plasma protein binding (% unbound)	66.150	%	High	1
rat-kpuu-brain	Rat brain Kpuu	0.514	%	High	1
rh-clint	Rat hepatocyte intrinsic clearance	12.190	uL/min/10^6 cells	High	1
rh-fuinc	Rat hepatocyte fraction unbound in incubation	96.510	%	High	1
rppb	Rat plasma protein binding (% unbound)	54.080	%	High	1
solubility-dd	Solubility at pH 7.4 in DMSO	933.254	uM	High	1

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	188.23	48.78	30	1242	1470	90625705
Intentional overdose	187.44	48.78	64	1208	93770	90533405
Drug dependence	103.75	48.78	31	1241	29296	90597879
Coma	97.43	48.78	37	1235	72595	90554580
Seizure	94.89	48.78	45	1227	152584	90474591
Depressed level of consciousness	93.75	48.78	36	1236	72748	90554427
Intentional product misuse	86.49	48.78	36	1236	89568	90537607
Electrocardiogram QRS complex shortened	61.68	48.78	10	1262	542	90626633
Suicide attempt	55.34	48.78	25	1247	75374	90551801

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	111.64	40.24	44	1070	51412	42568809
Drug withdrawal convulsions	70.02	40.24	14	1100	1324	42618897
Coma	45.83	40.24	24	1090	53530	42566691
Intentional product misuse	45.31	40.24	25	1089	61875	42558346

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	281.74	34.83	107	2371	132394	110454427
Drug withdrawal convulsions	250.67	34.83	44	2434	2405	110584416
Drug dependence	130.15	34.83	47	2431	49973	110536848
Seizure	126.55	34.83	72	2406	221113	110365708
Coma	124.44	34.83	58	2420	117811	110469010
Intentional product misuse	120.81	34.83	59	2419	132845	110453976
Depressed level of consciousness	105.46	34.83	51	2427	112227	110474594
Product use issue	70.16	34.83	57	2421	311638	110275183
Psychogenic seizure	69.79	34.83	15	2463	2349	110584472
Toxicity to various agents	68.76	34.83	68	2410	480487	110106334
Suicide attempt	68.08	34.83	37	2441	103357	110483464
Electrocardiogram QRS complex shortened	53.03	34.83	10	2468	810	110586011
Unresponsive to stimuli	50.97	34.83	26	2452	63764	110523057
Generalised tonic-clonic seizure	45.77	34.83	23	2455	54657	110532164
Electrocardiogram QRS complex prolonged	44.43	34.83	15	2463	13006	110573815
Overdose	38.82	34.83	36	2442	233758	110353063
Agitation	37.19	34.83	26	2452	113025	110473796
Hypotension	35.97	34.83	51	2427	523798	110063023
Sinus tachycardia	35.14	34.83	18	2460	44475	110542346

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flumazenil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

Drug Use | Suggest Off label Use Form| |View source of the data|

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products:

Source	Code	Description
ATC	V03AB25	VARIOUS ALL OTHER THERAPEUTIC PRODUCTS ALL OTHER THERAPEUTIC PRODUCTS Antidotes
MeSH PA	D000931	Antidotes
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018682	GABA Agents
MeSH PA	D018757	GABA Modulators
MeSH PA	D020011	Protective Agents
CHEBI has role	CHEBI:35474	anxiolytic drug
CHEBI has role	CHEBI:48407	antiparkinson drug
CHEBI has role	CHEBI:65259	GABA antagonist
CHEBI has role	CHEBI:90757	antidote to benzodiazepine poisoning
FDA EPC	N0000175680	Benzodiazepine Antagonist

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

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	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

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
40P7XK9392	INXIGHT DRUGS

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	0404-9793	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	ANDA	14 sections
FLUMAZENIL	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9794	INJECTION, SOLUTION	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	36000-148	INJECTION	0.10 mg	INTRAVENOUS	ANDA	30 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	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	51662-1699	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	ANDA	12 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	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
Flumazenil	HUMAN PRESCRIPTION DRUG LABEL	1	71872-7321	INJECTION	0.10 mg	INTRAVENOUS	ANDA	30 sections
Flumazenil	HUMAN PRESCRIPTION DRUG LABEL	1	71872-7375	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	ANDA	12 sections
Flumazenil	HUMAN PRESCRIPTION DRUG LABEL	1	84549-783	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	ANDA	29 sections
Flumazenil	HUMAN PRESCRIPTION DRUG LABEL	1	84549-784	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	ANDA	29 sections