Product Name

Sulindac

CAS Number

38194-50-2

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Product Name:
Sulindac
CAS Number:
38194-50-2
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.
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.

Pharmacodynamics:

Sulindac is a non-steroidal anti-inflammatory indene derivative, also possessing analgesic and antipyretic activities.

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.

IUPAC:
2-[(1Z)-5-fluoro-1-[(4-methanesulfinylphenyl)methylidene]-2-methyl-1H-inden-3-yl]acetic acid
ATC:
M01AB02
PubChem:
5352
DrugBank:
DB00605 (APRD01243)
Formula:
C13H14N2
Molecular Mass:
356.411
SMILES:
CC1=C(CC(O)=O)C2=CC(F)=CC=C2C1=C/C1=CC=C(C=C1)S(C)=O
AHFS Code:
28:08.04.92
InChi:
MLKXDPUZXIRXEP-MFOYZWKCSA-N

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