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phenazone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| anti-inflammatory analgesics, phenylbutazone derivatives | 861 | 60-80-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An analgesic and antipyretic that has been given by mouth and as ear drops. Antipyrine is often used in testing the effects of other drugs or diseases on drug-metabolizing enzymes in the liver. (From Martindale, The Extra Pharmacopoeia, 30th ed, p29)
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 3 | g | O |
| 3 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 1700 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0.50 % | Benet LZ, Broccatelli F, Oprea TI |
| BA (Bioavailability) | 97 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.77 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 0.64 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.93 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 12 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,ERBB2,FLT3,GRK2,ITK,MAP3K21,MAP3K7,MAPK7,MAPK9,MARK4,NTRK2,PDK4,PIK3CB,PIK3CD,PRKDC,SIK2,SIK3,STK33,TEK,TTK | 31 | |||
| kinase-selectivity-class | ACVR2B,AXL,GRK2 | 3 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| rat-kpuu-brain | Rat brain Kpuu | 0.381 | % | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1964 | 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 | N02BB01 | NERVOUS SYSTEM ANALGESICS OTHER ANALGESICS AND ANTIPYRETICS Pyrazolones |
| ATC | N02BB51 | NERVOUS SYSTEM ANALGESICS OTHER ANALGESICS AND ANTIPYRETICS Pyrazolones |
| ATC | N02BB71 | NERVOUS SYSTEM ANALGESICS OTHER ANALGESICS AND ANTIPYRETICS Pyrazolones |
| ATC | S02DA03 | SENSORY ORGANS OTOLOGICALS OTHER OTOLOGICALS Analgesics and anesthetics |
| MeSH PA | D000700 | Analgesics |
| MeSH PA | D000893 | Anti-Inflammatory Agents |
| MeSH PA | D000894 | Anti-Inflammatory Agents, Non-Steroidal |
| MeSH PA | D018501 | Antirheumatic Agents |
| MeSH PA | D018689 | Sensory System Agents |
| MeSH PA | D018712 | Analgesics, Non-Narcotic |
| CHEBI has role | CHEBI:35475 | non-steroidal anti-inflammatory drug |
| CHEBI has role | CHEBI:35480 | analgesic |
| CHEBI has role | CHEBI:35481 | non-narcotic analgesic |
| CHEBI has role | CHEBI:35493 | antipyretic |
| CHEBI has role | CHEBI:35703 | xenobiotic |
| CHEBI has role | CHEBI:65023 | anti-asthmatic agent |
| CHEBI has role | CHEBI:73263 | cyclooxygenase 3 inhibitor |
| CHEBI has role | CHEBI:78298 | environmental contaminant |
Related Drugs by ATC class:
N02BB Pyrazolones 4 drugs
S02DA Analgesics and anesthetics 3 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Infective otitis media | indication | 312218008 | |
| Otalgia | off-label use | 16001004 | |
| Impacted cerumen | off-label use | 18070006 | |
| Migraine | off-label use | 37796009 | DOID:6364 |
| Vascular headache | off-label use | 128187005 | |
| Tension-type headache | off-label use | 398057008 | |
| Alcoholism | contraindication | 7200002 | |
| Glaucoma | contraindication | 23986001 | DOID:1686 |
| Acute cerebrovascular insufficiency | contraindication | 29322000 | |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Heart disease | contraindication | 56265001 | DOID:114 |
| Acute nephropathy | contraindication | 58574008 | |
| Hepatic failure | contraindication | 59927004 | |
| Perforation of tympanic membrane | contraindication | 60442001 | |
| Poisoning by acetaminophen | contraindication | 70273001 | |
| Arteriosclerotic vascular disease | contraindication | 72092001 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Arterial aneurysm | contraindication | 233981004 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
| Peripheral vascular disease | contraindication | 400047006 | |
| Disorder of coronary artery | contraindication | 414024009 | |
| Porphyria | contraindication | 418470004 | |
| Organic Cardiac Disease | contraindication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
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 |
|---|---|---|---|---|---|---|---|---|---|
| Transient receptor potential cation channel subfamily A member 1 | Ion channel | BLOCKER | IC50 | 3.08 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Nicotinate phosphoribosyltransferase | Enzyme | Ki | 9 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4018116 | VUID |
| N0000146454 | NUI |
| D01776 | KEGG_DRUG |
| 1001 | RXNORM |
| 4018116 | VANDF |
| C0003420 | UMLSCUI |
| CHEBI:31225 | CHEBI |
| CHEMBL277474 | ChEMBL_ID |
| DB01435 | DRUGBANK_ID |
| C027436 | MESH_SUPPLEMENTAL_RECORD_UI |
| 2206 | PUBCHEM_CID |
| 4210 | MMSL |
| 72847 | MMSL |
| 001607 | NDDF |
| 412090007 | SNOMEDCT_US |
| 55486005 | SNOMEDCT_US |
| D000983 | MESH_DESCRIPTOR_UI |
| 413 | INN_ID |
| T3CHA1B51H | UNII |
| T3CHA1B51H | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Antipyrine and Benzocaine | HUMAN PRESCRIPTION DRUG LABEL | 2 | 21695-216 | SOLUTION | 54 mg | AURICULAR (OTIC) | Unapproved drug other | 13 sections |
| OrtizolOtic Solution | HUMAN OTC DRUG LABEL | 3 | 61841-180 | LIQUID | 50 mg | AURICULAR (OTIC) | Export only | 7 sections |