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 |
|---|---|
|
Synonyms:
|
A salicylate derivative and anti-inflammatory analgesic with actions and side effects similar to those of ASPIRIN.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.75 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 6 % | Benet LZ, Broccatelli F, Oprea TI |
| 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 |
| Vd (Volume of distribution) | 0.10 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 0.10 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.00 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 10 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 19, 1982 | 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 hypersensitivity | 41.70 | 31.19 | 26 | 412 | 310661 | 63177923 |
FDA Adverse Event Reporting System (Male)
None
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 |
|---|---|---|---|---|---|---|
| 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 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N02BA11 | NERVOUS SYSTEM ANALGESICS OTHER ANALGESICS AND ANTIPYRETICS Salicylic acid and derivatives |
| FDA CS | M0001335 | Anti-Inflammatory Agents, Non-Steroidal |
| 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 |
| MeSH PA | D016861 | Cyclooxygenase Inhibitors |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D018689 | Sensory System Agents |
| FDA EPC | N0000175722 | Nonsteroidal Anti-inflammatory Drug |
| CHEBI has role | CHEBI:35475 | non-steroidal anti-inflammatory agent |
Drug Use | Suggest Off label Use Form| |View source of the data|
| 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 | |
| Chronic heart failure | contraindication | 48447003 | |
| Disorder of cardiovascular system | contraindication | 49601007 | DOID:1287 |
| Blood coagulation disorder | contraindication | 64779008 | DOID:1247 |
| Gastrointestinal hemorrhage | contraindication | 74474003 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Coronary artery bypass graft | contraindication | 232717009 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Pregnancy, function | contraindication | 289908002 | |
| Cardiovascular event risk | contraindication | 395112001 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Smokes tobacco daily | contraindication | 449868002 |
🐶 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Prostaglandin G/H synthase 2 | Enzyme | INHIBITOR | IC50 | 5.09 | WOMBAT-PK | CHEMBL | |||
| Prostaglandin G/H synthase 1 | Enzyme | INHIBITOR | IC50 | 4.40 | WOMBAT-PK | CHEMBL | |||
| Carbonic anhydrase 2 | Enzyme | Ki | 5.03 | CHEMBL | |||||
| Transthyretin | Secreted | Kd1 | 7.13 | WOMBAT-PK | |||||
| Carbonic anhydrase 1 | Enzyme | Ki | 5.07 | CHEMBL | |||||
| Dihydrofolate reductase | Enzyme | INHIBITOR | Ki | 4.47 | IUPHAR | ||||
| 2-amino-3-carboxymuconate-6-semialdehyde decarboxylase | Unclassified | Ki | 5.59 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4017950 | VUID |
| N0000146300 | NUI |
| D00130 | KEGG_DRUG |
| 3393 | RXNORM |
| 4017950 | VANDF |
| C0012228 | UMLSCUI |
| CHEBI:39669 | CHEBI |
| 1FL | PDB_CHEM_ID |
| CHEMBL898 | ChEMBL_ID |
| DB00861 | DRUGBANK_ID |
| D004061 | MESH_DESCRIPTOR_UI |
| 3059 | PUBCHEM_CID |
| 7162 | IUPHAR_LIGAND_ID |
| 3774 | INN_ID |
| 7C546U4DEN | UNII |
| 1247 | MMSL |
| 4595 | MMSL |
| d00208 | MMSL |
| 001599 | NDDF |
| 20865003 | SNOMEDCT_US |
| 387116004 | SNOMEDCT_US |
Pharmaceutical products:
| 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 |
| Diflunisal | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68382-530 | TABLET | 500 mg | ORAL | ANDA | 15 sections |
| Diflunisal | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70771-1083 | TABLET | 500 mg | ORAL | ANDA | 17 sections |
| Diflunisal | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70771-1083 | TABLET | 500 mg | ORAL | ANDA | 17 sections |