Sulindac

CAS No:
38194-50-2 Category:
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  • #LGM Pharma offers this active ingredient but not the finished dosage forms.

Product Details:

  • CAS No: 38194-50-2
  • AHFC code: 28:08.04.92
  • Synonyms:
  • ATC Code: M01AB02
  • Chemical Formula: C13H14N2
  • Molecular Weight: 356.411
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB00605 (APRD01243)
  • SMILES: CC1=C(CC(O)=O)C2=CC(F)=CC=C2C1=C/C1=CC=C(C=C1)S(C)=O
  • InChl: MLKXDPUZXIRXEP-MFOYZWKCSA-N
  • PubChem: 5352
  • IUPAC: 2-[(1Z)-5-fluoro-1-[(4-methanesulfinylphenyl)methylidene]-2-methyl-1H-inden-3-yl]acetic acid

Additional Details

Indication:
For acute or long-term use in the relief of signs and symptoms of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute painful shoulder (acute subacromial bursitis/supraspinatus tendinitis), and acute gouty arthritis.
Pharmacodynamics:
Sulindac is a non-steroidal anti-inflammatory indene derivative, also possessing analgesic and antipyretic activities.
Mode of Action:
Sulindac's exact mechanism of action is unknown. Its antiinflammatory effects are believed to be due to inhibition of both COX-1 and COX-2 which leads to the inhibition of prostaglandin synthesis. Antipyretic effects may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation.
Metabolism:
Undergoes two major biotransformations: reversible reduction to the sulfide metabolite, and irreversible oxidation to the sulfone metabolite. Sulindac and its sulfide and sulfone metabolites undergo extensive enterohepatic circulation. Available evidence indicates that the biological activity resides with the sulfide metabolite. Side chain hydroxylation and hydration of the double bond also occur.
Toxicity:
Acute oral toxicity (LD50) in rats is 264 mg/kg. Cases of overdose have been reported and rarely, deaths have occurred. The following signs and symptoms may be observed following overdose: stupor, coma, diminished urine output and hypotension.
General Reference:
Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

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