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warfarin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	2847	81-81-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: warfarin warfarin sodium warfarin potassium	An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide. Molecular weight: 308.33 Formula: C19H16O4 CLOGP: 2.90 LIPINSKI: 0 HAC: 4 HDO: 1 TPSA: 63.60 ALOGS: -3.82 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

warfarin
warfarin sodium
warfarin potassium

An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.

Molecular weight: 308.33
Formula: C19H16O4
CLOGP: 2.90
LIPINSKI: 0
HAC: 4
HDO: 1
TPSA: 63.60
ALOGS: -3.82
ROTB: 4

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
7.50	mg	O
7.50	mg	P

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	93 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	29 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	1 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.54 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution)	0.13 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	0.06 mL/min/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.02 mg/mL	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.02 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
June 8, 1954	FDA	BRISTOL MYERS SQUIBB

FDA Adverse Event Reporting System (Female)

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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
International normalised ratio increased	8844.96	10.40	3811	193470	42614	63249127
Drug interaction	1322.35	10.40	2470	194811	226661	63065080
Calciphylaxis	1044.61	10.40	384	196897	2688	63289053
International normalised ratio decreased	899.05	10.40	383	196898	4118	63287623
International normalised ratio abnormal	892.19	10.40	349	196932	2955	63288786
Pulmonary arterial hypertension	888.21	10.40	659	196622	21918	63269823
Drug ineffective	870.97	10.40	1192	196089	1043573	62248168
Dyspnoea	654.77	10.40	3888	193393	657425	62634316
Gastrointestinal haemorrhage	615.90	10.40	989	196292	80187	63211554
Fluid retention	600.33	10.40	830	196451	58856	63232885

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FDA Adverse Event Reporting System (Male)

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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
International normalised ratio increased	11187.21	10.73	5190	168106	42137	34741498
Gastric haemorrhage	2029.01	10.73	999	172297	9262	34774373
Haemorrhage	1965.97	10.73	1792	171504	49578	34734057
International normalised ratio abnormal	1809.54	10.73	665	172631	2670	34780965
International normalised ratio decreased	1205.73	10.73	543	172753	4024	34779611
Gastrointestinal haemorrhage	1070.93	10.73	1718	171578	86759	34696876
Anticoagulation drug level above therapeutic	1027.43	10.73	389	172907	1727	34781908
Drug interaction	849.65	10.73	2752	170544	223194	34560441
Haematuria	736.31	10.73	1065	172231	49001	34734634
Subdural haematoma	734.59	10.73	689	172607	19732	34763903

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FDA Adverse Event Reporting System (Geriatric)

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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
International normalised ratio increased	18570.57	9.93	8295	314616	76426	79345051
Haemorrhage	2389.02	9.93	2357	320554	88761	79332716
International normalised ratio abnormal	2211.65	9.93	845	322066	4923	79416554
Gastric haemorrhage	2075.82	9.93	1076	321835	13974	79407503
Drug interaction	2015.32	9.93	4878	318033	410305	79011172
International normalised ratio decreased	1795.12	9.93	801	322110	7269	79414208
Gastrointestinal haemorrhage	1653.46	9.93	2482	320429	145237	79276240
Anticoagulation drug level above therapeutic	1608.98	9.93	591	322320	3029	79418448
Calciphylaxis	1239.22	9.93	494	322417	3276	79418201
Subdural haematoma	1220.86	9.93	1015	321896	30419	79391058

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	B01AA03	BLOOD AND BLOOD FORMING ORGANS ANTITHROMBOTIC AGENTS ANTITHROMBOTIC AGENTS Vitamin K antagonists
CHEBI has role	CHEBI:33288	rodenticides
CHEBI has role	CHEBI:50249	anticoagulants
CHEBI has role	CHEBI:50390	NAD(P)H dehydrogenase (quinone) inhibitors
CHEBI has role	CHEBI:55347	vitamin K antagonists
FDA EPC	N0000175476	Vitamin K Antagonist
FDA MoA	N0000175964	Vitamin K Inhibitors
MeSH PA	D000925	Anticoagulants
MeSH PA	D006401	Hematologic Agents
MeSH PA	D010575	Pesticides

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

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Disease	Relation	SNOMED_ID	DOID
Cerebral embolism	indication	75543006	DOID:4372
Deep venous thrombosis	indication	128053003
Pulmonary thromboembolism	indication	233935004
Thromboembolic disorder	indication	371039008
Thrombosis	indication	439127006
Prevention of deep vein thrombosis	indication	439993001
Thromboembolism due to Prosthetic Heart Valves	indication
Myocardial Reinfarction Prevention	indication
Prevention of Thromboembolism with Chronic Atrial Fibrillation	indication
Deep Vein Thrombosis with Pulmonary Embolism	indication

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	4.96	acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Vitamin K epoxide reductase complex subunit 1	Enzyme	Q9BQB6	VKOR1_HUMAN	INHIBITOR	IC50	7	WOMBAT-PK	CHEMBL
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN		Ki	3.98	WOMBAT-PK
Cytochrome P450 2C9	Enzyme	P11712	CP2C9_HUMAN		Ki	4.87	WOMBAT-PK
Proprotein convertase subtilisin/kexin type 7	Enzyme	Q16549	PCSK7_HUMAN		IC50	4.61	CHEMBL
Vitamin K epoxide reductase complex subunit 1-like protein 1	Enzyme	Q8N0U8	VKORL_HUMAN		Ki	4.28	SCIENTIFIC LITERATURE

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External reference:

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ID	Source
002084	NDDF
002085	NDDF
004065	NDDF
11289	RXNORM
1258	MMSL
129-06-6	SECONDARY_CAS_RN
2610-86-8	SECONDARY_CAS_RN
341	INN_ID
372756006	SNOMEDCT_US
4018548	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Jantoven	HUMAN PRESCRIPTION DRUG LABEL	1	0832-1211	TABLET	1 mg	ORAL	ANDA	30 sections
Jantoven	HUMAN PRESCRIPTION DRUG LABEL	1	0832-1211	TABLET	1 mg	ORAL	ANDA	30 sections
Jantoven	HUMAN PRESCRIPTION DRUG LABEL	1	0832-1212	TABLET	2 mg	ORAL	ANDA	30 sections
Jantoven	HUMAN PRESCRIPTION DRUG LABEL	1	0832-1212	TABLET	2 mg	ORAL	ANDA	30 sections
Jantoven	HUMAN PRESCRIPTION DRUG LABEL	1	0832-1213	TABLET	2.50 mg	ORAL	ANDA	30 sections
Jantoven	HUMAN PRESCRIPTION DRUG LABEL	1	0832-1213	TABLET	2.50 mg	ORAL	ANDA	30 sections
Jantoven	HUMAN PRESCRIPTION DRUG LABEL	1	0832-1214	TABLET	3 mg	ORAL	ANDA	30 sections
Jantoven	HUMAN PRESCRIPTION DRUG LABEL	1	0832-1214	TABLET	3 mg	ORAL	ANDA	30 sections
Jantoven	HUMAN PRESCRIPTION DRUG LABEL	1	0832-1215	TABLET	4 mg	ORAL	ANDA	30 sections
Jantoven	HUMAN PRESCRIPTION DRUG LABEL	1	0832-1215	TABLET	4 mg	ORAL	ANDA	30 sections

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