Table of contents

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

Brand Names

North America

USA: Tolectin, Tolmetin.

Latin America

Mexico: Tolectin.

Drug combinations


Tolmetin Sodium: C~15~H~14~NNaO~3~ 2H~2~O. Mw: 315.30. (1) 1H-Pyrrole-2-acetic acid, 1-methyl-5-(4-methylbenzoyl)-, sodium salt, dihydrate; (2) Sodium 1-methyl-5-p-toluoylpyrrole-2-acetate dihydrate. CAS-64490-92-2; CAS-35711-34-3 (anhydrous)(1976).

Pharmacologic Category

Analgesics and Antipyretics; Other Nonsteroidal Anti-inflammatory Agents. (ATC-Code: M01AB03; M02AA21).

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

Treatment of rheumatoid arthritis and osteoarthritis, juvenile rheumatoid arthritis.

Pregnancy and lactiation implications

Teratogenic effects not observed in animal studies. Use of NSAIDs late in pregnancy may cause premature closure of ductus arteriosus and may inhibit uterine contractions. This drug should not be used in 3^rd^ trimester of pregnancy. Enters breast milk (not recommended in nursing women).

Unlabeled use


Hypersensitivity to tolmetin, aspirin, other NSAIDs, or any component of the formulation. Perioperative pain in setting of coronary artery bypass graft surgery.

Warnings and precautions

NSAIDs associated with increased risk of adverse cardiovascular thrombotic events, including MI, stroke, and new onset or worsening of pre-existing hypertension (risk may be increased with duration of use or pre-existing cardiovascular risk factors or disease; use caution with fluid retention, heart failure, or hypertension). Concurrent administration of ibuprofen, and potentially other nonselective NSAIDs, may interfere with cardioprotective effect of aspirin. Even in patients without prior exposure 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). NSAIDs may increase risk of gastrointestinal irritation, inflammation, ulceration, bleeding, and perforation (use caution with history of GI disease (bleeding or ulcers), concurrent therapy with aspirin, anticoagulants and/or corticosteroids, smoking, use of alcohol, elderly or debilitated patients). When used concomitantly with ≤325 mg of aspirin, substantial increase in risk of GI complications (e.g. ulcer) occurs. Platelet adhesion and aggregation may be decreased (may prolong bleeding time). Anemia may occur. Use contraindicated for treatment of perioperative pain in setting of coronary artery bypass graft surgery (risk of MI and stroke may be increased with use following coronary artery bypass graft surgery). NSAIDs may cause serious skin adverse events including exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis. Do not administer to patients with aspirin-sensitive asthma (severe bronchospasm may occur); use caution in other forms of asthma. NSAID use may compromise existing renal function (patients with impaired renal function, dehydration, heart failure, liver dysfunction, those taking diuretics and 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 with caution in decreased hepatic function. Severe hepatic reactions occurred with NSAID use, rarely. Withhold for at least 4-6 half-lives prior to surgical or dental procedures.



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