azapropazone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| anti-inflammatory analgesics, phenylbutazone derivatives | 266 | 13539-59-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An anti-inflammatory agent used in the treatment of rheumatoid arthritis. It also has uricosuric properties and has been used to treat gout.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.75 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 4 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.15 mg/mL | Bocci G, Oprea TI, Benet LZ |
| EoM (Fraction excreted unchanged in urine) | 60 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 89.18 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 0.12 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 0.14 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) | 17 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1972 | YEAR INTRODUCED |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | M01AX04 | MUSCULO-SKELETAL SYSTEM ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS Other antiinflammatory and antirheumatic agents, non-steroids |
| 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 | D006074 | Gout Suppressants |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D018689 | Sensory System Agents |
| MeSH PA | D014528 | Uricosuric Agents |
| CHEBI has role | CHEBI:35475 | non-steroidal anti-inflammatory agent |
| CHEBI has role | CHEBI:35841 | uricosuric drugs |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Ankylosing spondylitis | indication | 9631008 | DOID:7147 |
| Rheumatoid arthritis | indication | 69896004 | DOID:7148 |
| Gout | indication | 90560007 | DOID:13189 |
| Osteoarthritis | indication | 396275006 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 6.24 | acidic |
| pKa2 | 0.41 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Prostaglandin G/H synthase 1 | Enzyme | WOMBAT-PK | |||||||
| Xanthine dehydrogenase/oxidase | Enzyme | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| N0000167162 | NUI |
| D02966 | KEGG_DRUG |
| 22304-30-9 | SECONDARY_CAS_RN |
| 1029 | RXNORM |
| C0003524 | UMLSCUI |
| CHEBI:38010 | CHEBI |
| AZQ | PDB_CHEM_ID |
| CHEMBL1565476 | ChEMBL_ID |
| DB07402 | DRUGBANK_ID |
| 26098 | PUBCHEM_CID |
| 329543000 | SNOMEDCT_US |
| 391798003 | SNOMEDCT_US |
| D001032 | MESH_DESCRIPTOR_UI |
| 2276 | INN_ID |
| BF18764H96 | UNII |
| 003712 | NDDF |
Pharmaceutical products:
None