Sulindac

Sulindac is an arylalkanoic acid nonsteroidal anti-inflammatory drug (NSAID) used to treat acute and chronic inflammatory conditions. It is a prodrug that is converted in the liver to an active sulfide metabolite, which inhibits cyclooxygenase (COX-1 and COX-2) enzymes, reducing prostaglandin synthesis and thereby relieving pain and inflammation. Due to enterohepatic circulation of its active metabolite, sulindac may be associated with fewer gastrointestinal side effects than some other traditional NSAIDs, although its exact mechanism of action is not fully understood.

Sulindac is an NSAID used to treat osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute subacromial bursitis or supraspinatus tendinitis, and acute gouty arthritis.

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.

• Ankylosing Spondylitis (AS)
• Colorectal Polyps
• Gouty Arthritis
• Osteoarthritis (OA)
• Rheumatoid Arthritis
• Tendonitis exacerbated
• Acute Subacromial bursitis
• Acute supraspinatus tendinitis

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

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.

Approximately 90% absorbed in humans following oral administration.

At 1 mcg/ml concentrations, approximately 93% sulindac and 98% of its sulfide metabolite are bound to human serum albumin.

Sulindac is excreted in rat milk; concentrations in milk were 10 to 20% of those levels in plasma. It is not known if sulindac is excreted in human milk. Approximately 50% of the administered dose of sulindac is excreted in the urine with the conjugated sulfone metabolite accounting for the major portion. Hepatic metabolism is an important elimination pathway.

The mean half-life of sulindac is 7.8 hours while the mean half-life of the sulfide metabolite is 16.4 hours.

• Renal cl=68.12 +/- 27.56 mL/min [NORMAL (19-41 yrs)]

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.

• Avoid alcohol. Ingesting alcohol may increase the risk of gastrointestinal bleeding.
• Take with food.