Sulindac

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

France: Arthrocine; Malta: Sulindac; Netherlands: Sulindac; Poland: Sudaclin.

North America

Canada: Apo-Sulin, Novo-Sundac, Sulindac; USA: Clinoril, Sulindac.

Latin America

Mexico: Atriser, Bio-Dac, Clinoril, Renidac, Sulifur, Sulindaco, Vindacín, Zulsol.

Asia

Japan: Clinoril, Kulilolel, Skanoorin, Sukurinoru, Sulindac, Sulinpen.

Drug combinations

Chemistry

Sulindac: C~20~H~17~FO~3~S. Mw: 356.41. (1) 1H-Indene-3-acetic acid, 5-fluoro-2-methyl-1-[[4-(methylsulfinyl)phenyl]methylene]-, (Z)-; (2) cis-5-Fluoro-2-methyl-1-[(p-methylsulfinyl)benzylidene]indene-3-acetic acid. CAS-38194-50-2 (1975).

Pharmacologic Category

Other Nonsteroidal Anti-inflammatory Agents. (ATC-Code: M01AB02).

Mechanism of action

Reversibly inhibits cyclooxygenase-1 and 2 (COX-1/PTGS1 and COX-2/PTGS2) enzymes, which results in decreased formation of prostaglandin precursors. Has antipyretic, analgesic, and anti-inflammatory properties.

Therapeutic use

Inflammatory diseases including osteoarthritis, rheumatoid arthritis, acute gouty arthritis, ankylosing spondylitis, acute painful shoulder (bursitis/tendonitis).

Pregnancy and lactiation implications

Potential for premature ductus arteriosus closure, particularly in late pregnancy. Avoid use in 3^rd^ trimester. Excretion in breast milk unknown (not recommended in nursing women).

Unlabeled use

Contraindications

Hypersensitivity to sulindac, any component, aspirin, or other NSAIDs. Acute asthmatic attacks, urticaria, or rhinitis precipitated by aspirin or other NSAIDs. «Aspirin triad» (asthma, rhinitis (with or without nasal polyps), and aspirin intolerance)(fatal asthmatic and anaphylactoid reactions may occur in these patients), perioperative pain in setting of coronary artery bypass graft.

Warnings and precautions

Anaphylactoid reactions may occur; patients with «aspirin triad» (bronchial asthma, aspirin intolerance, rhinitis) may be at increased risk. Do not use in patients who experience bronchospasm, asthma, rhinitis, or urticaria with NSAID or aspirin therapy. May increase risk of aseptic meningitis, especially in systemic lupus erythematosus and mixed connective tissue disorders. Platelet adhesion and aggregation may be decreased (may prolong bleeding time). Anemia may occur. NSAIDs are associated with increased risk of adverse cardiovascular thrombotic events (myocardial infarction, stroke, and new onset or worsening of pre-existing hypertension). Use caution with fluid retention, heart failure, or hypertension. NSAIDs may increase risk of GI irritation, inflammation, ulceration, bleeding, and perforation. Use caution with history of GI disease, concurrent therapy with aspirin, anticoagulants and/or corticosteroids, smoking, use of alcohol, elderly or debilitated patients. When used concomitantly with ≤325 mg of aspirin, a substantial increase in risk of GI complications occurs. Pancreatitis reported. NSAIDs may cause serious skin adverse events including exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis. Use contraindicated for treatment of perioperative pain in setting of coronary artery bypass graft surgery (risk of MI and stroke). Use with caution in decreased hepatic function (severe hepatic reactions occurred). NSAID use may compromise existing renal function; dose-dependent decreases in prostaglandin synthesis may result from NSAID use, reducing renal blood flow which may cause renal decompensation. Patients with impaired renal function, dehydration, heart failure, liver dysfunction, those taking diuretics, ACEIs, and the elderly are at greater risk of renal toxicity. Not recommended for use in advanced renal disease. Long-term NSAID use may result in renal papillary necrosis. Use caution in renal lithiasis (sulindac metabolites reported as components of renal stones). Withhold prior to surgical or dental procedures. May cause increased chloride, increased sodium, increased bleeding time.

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