indication

For the treatment of acute pain, the symptomatic treatment of osteoarthritis and primary dysmenorrhoea in adolescents and adults above 12 years old.

pharmacology

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.

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

biotransformation

Hepatic. Extensive biotransformation, mainly to 4-hydroxynimesulide (which also appears to be biologically active).

absorption

Rapidly absorbed following oral administration.

half life

1.8–4.7 hours

route of elimination

Renal (50%), fecal (29%)