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

Stem definition	Drug id	CAS RN
analgesic anti-inflammatory	880	22494-42-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: diflunisal difludol diflusinal fluniget fluodonil difluorophenylsalicylic acid MK-647	A salicylate derivative and anti-inflammatory analgesic with actions and side effects similar to those of ASPIRIN. Molecular weight: 250.20 Formula: C13H8F2O3 CLOGP: 4.40 LIPINSKI: 0 HAC: 3 HDO: 2 TPSA: 57.53 ALOGS: -3.55 ROTB: 2 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

diflunisal
difludol
diflusinal
fluniget
fluodonil
difluorophenylsalicylic acid
MK-647

A salicylate derivative and anti-inflammatory analgesic with actions and side effects similar to those of ASPIRIN.

Molecular weight: 250.20
Formula: C13H8F2O3
CLOGP: 4.40
LIPINSKI: 0
HAC: 3
HDO: 2
TPSA: 57.53
ALOGS: -3.55
ROTB: 2

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.75	g	O

ADMET properties:

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Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	99.92 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	85 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	6 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	10 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	0.10 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.10 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.00 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
April 19, 1982	FDA

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
Drug hypersensitivity	41.70	31.19	26	412	310661	63177923

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FDA Adverse Event Reporting System (Male)

None

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
Urine protein/creatinine ratio increased	58.16	33.07	10	704	1224	79742450
Urinary occult blood positive	34.33	33.07	5	709	210	79743464

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N02BA11	NERVOUS SYSTEM ANALGESICS OTHER ANALGESICS AND ANTIPYRETICS Salicylic acid and derivatives
CHEBI has role	CHEBI:35475	non-steroidal anti-inflammatory agent
FDA CS	M0001335	Anti-Inflammatory Agents, Non-Steroidal
FDA EPC	N0000175722	Nonsteroidal Anti-inflammatory Drug
FDA MoA	N0000000160	Cyclooxygenase Inhibitors
MeSH PA	D000700	Analgesics
MeSH PA	D018712	Analgesics, Non-Narcotic
MeSH PA	D000893	Anti-Inflammatory Agents
MeSH PA	D000894	Anti-Inflammatory Agents, Non-Steroidal
MeSH PA	D018501	Antirheumatic Agents

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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
Pain	indication	22253000
Rheumatoid arthritis	indication	69896004	DOID:7148
Chronic pain	indication	82423001
Osteoarthritis	indication	396275006
Arthritis	off-label use	3723001	DOID:848
Vascular headache	off-label use	128187005
Peptic ulcer	contraindication	13200003	DOID:750
Myocardial infarction	contraindication	22298006	DOID:5844
Hypertensive disorder	contraindication	38341003	DOID:10763
Gastrointestinal ulcer	contraindication	40845000

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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	2.81	acidic
pKa2	12.64	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
Prostaglandin G/H synthase 2	Enzyme	P35354	PGH2_HUMAN	INHIBITOR	IC50	5.09	WOMBAT-PK	CHEMBL
Prostaglandin G/H synthase 1	Enzyme	P23219	PGH1_HUMAN	INHIBITOR	IC50	4.40	WOMBAT-PK	CHEMBL
Carbonic anhydrase 2	Enzyme	P00918	CAH2_HUMAN		Ki	5.03	CHEMBL
Transthyretin	Secreted	P02766	TTHY_HUMAN		Kd1	7.13	WOMBAT-PK
Carbonic anhydrase 1	Enzyme	P00915	CAH1_HUMAN		Ki	5.07	CHEMBL
Dihydrofolate reductase	Enzyme	P00374	DYR_HUMAN	INHIBITOR	Ki	4.47	IUPHAR
2-amino-3-carboxymuconate-6-semialdehyde decarboxylase	Unclassified	Q8TDX5	ACMSD_HUMAN		Ki	5.59	CHEMBL

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External reference:

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ID	Source
1FL	PDB_CHEM_ID
001599	NDDF
1247	MMSL
20865003	SNOMEDCT_US
3059	PUBCHEM_CID
3393	RXNORM
3774	INN_ID
387116004	SNOMEDCT_US
4017950	VUID
4017950	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Diflunisal	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0755	TABLET, FILM COATED	500 mg	ORAL	ANDA	25 sections
Diflunisal	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0755	TABLET, FILM COATED	500 mg	ORAL	ANDA	25 sections
Diflunisal	HUMAN PRESCRIPTION DRUG LABEL	1	0093-9222	TABLET, FILM COATED	500 mg	ORAL	ANDA	25 sections
Diflunisal	HUMAN PRESCRIPTION DRUG LABEL	1	0093-9222	TABLET, FILM COATED	500 mg	ORAL	ANDA	25 sections
diflunisal	HUMAN PRESCRIPTION DRUG LABEL	1	14539-673	TABLET, FILM COATED	500 mg	ORAL	ANDA	21 sections
DIFLUNISAL	HUMAN PRESCRIPTION DRUG LABEL	1	52959-379	TABLET, FILM COATED	500 mg	ORAL	ANDA	13 sections
Diflunisal	HUMAN PRESCRIPTION DRUG LABEL	1	54868-3049	TABLET, FILM COATED	500 mg	ORAL	ANDA	14 sections
Diflunisal	HUMAN PRESCRIPTION DRUG LABEL	1	62135-456	TABLET, FILM COATED	500 mg	ORAL	ANDA	21 sections
DIFLUNISAL	HUMAN PRESCRIPTION DRUG LABEL	1	64980-181	TABLET, FILM COATED	500 mg	ORAL	ANDA	25 sections
Diflunisal	HUMAN PRESCRIPTION DRUG LABEL	1	68151-0848	TABLET, FILM COATED	500 mg	ORAL	ANDA	27 sections

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