Introduction
Nimesulide is a relatively COX-2 selective, non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. Its approved indications are the treatment of acute pain, the symptomatic treatment of osteoarthritis and primary dysmenorrhoea in adolescents and adults above 12 years old. Due to concerns about the risk of hepatotoxicity, nimesulide has been withdrawn from market in many countries.
Uses
Nimesulide is a cyclooxygenase 2 inhibitor used to treat acute pain and primary dysmenorrhea.
For the treatment of acute pain, the symptomatic treatment of osteoarthritis and primary dysmenorrhoea in adolescents and adults above 12 years old.
Associated Conditions
Pharmacodynamics
Food, gender and advanced age have negligible effects on nimesulide pharmacokinetics.
Mechanism of Action
The therapeutic effects of Nimesulide are the result of its complete mode of action which targets a number of key mediators of the inflammatory process such as: COX-2 mediated prostaglandins, free radicals, proteolytic enzymes and histamine.
Absorption
Rapidly absorbed following oral administration.
Protein Binding
>97.5%
Route of Elimination
Renal (50%), fecal (29%)
Half Life
1.8–4.7 hours
Toxicity
Oral TDLO (human): 1.429 mg/kg; Oral TDLO (woman): 2 mg/kg; Oral LD50 (rat): 200 mg/kg; Oral LD50 (mouse): 392 mg/kg