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

Stem definitionDrug idCAS RN
anti-inflammatory analgesics, phenylbutazone derivatives 2528 57-96-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • sulfinpyrazone
  • diphenylpyrazone
  • sulfinpyrazon
  • sulfoxyphenylpyrazolidine
  • sulphinpyrazone
  • sulfoxyphenylpyrazolidin
A uricosuric drug that is used to reduce the serum urate levels in gout therapy. It lacks anti-inflammatory, analgesic, and diuretic properties.
  • Molecular weight: 404.48
  • Formula: C23H20N2O3S
  • CLOGP: 2.43
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 0
  • TPSA: 57.69
  • ALOGS: -3.10
  • ROTB: 6
  • Status: OFM
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.30 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.32 mg/mL Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine) 39 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 28.25 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 99 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.12 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.34 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.02 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 6.20 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
May 13, 1959 FDA

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:

SourceCodeDescription
ATC M04AB02 MUSCULO-SKELETAL SYSTEM
ANTIGOUT PREPARATIONS
ANTIGOUT PREPARATIONS
Preparations increasing uric acid excretion
MeSH PA D018501 Antirheumatic Agents
MeSH PA D006074 Gout Suppressants
MeSH PA D014528 Uricosuric Agents
CHEBI has role CHEBI:35841 uricosuric drugs

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

DiseaseRelationSNOMED_IDDOID
Hyperuricemia indication 35885006 DOID:1920
Chronic gouty arthritis indication 68451005
Renal colic contraindication 7093002
Inflammatory bowel disease contraindication 24526004 DOID:0050589
Dehydration contraindication 34095006
Gastrointestinal ulcer contraindication 40845000
Kidney disease contraindication 90708001 DOID:557
Urolithiasis contraindication 95566004
Chronic peptic ulcer contraindication 128287004
Disease of blood AND/OR blood-forming organ contraindication 191124002 DOID:74
Acute peptic ulcer contraindication 196682000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 2.92 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Solute carrier family 22 member 12 Transporter INHIBITOR IC50 4 CHEMBL CHEMBL
Multidrug resistance-associated protein 1 Transporter WOMBAT-PK
fMet-Leu-Phe receptor GPCR Ki 4.70 WOMBAT-PK
Nicotinate phosphoribosyltransferase Enzyme Ki 9.30 CHEMBL

External reference:

IDSource
4018786 VUID
N0000147089 NUI
D00449 KEGG_DRUG
4018786 VANDF
C0038742 UMLSCUI
CHEBI:9342 CHEBI
CHEMBL832 ChEMBL_ID
D013442 MESH_DESCRIPTOR_UI
DB01138 DRUGBANK_ID
5342 PUBCHEM_CID
777 INN_ID
V6OFU47K3W UNII
10205 RXNORM
2070 MMSL
5530 MMSL
d00380 MMSL
002322 NDDF
19261005 SNOMEDCT_US
387108008 SNOMEDCT_US

Pharmaceutical products:

None