DESCRIPTION
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 Due to concerns about the risk of hepatotoxicity, nimesulide has been withdrawn from market in many countries.
CATEGORIES
Anti-Inflammatory Agents, Non-Steroidal
CHEMICAL FORMULA
C13H12N2O5S
COMPOSITION
Nimesulide 100 MG
INDICATION
For the treatment of acute pain, the symptomatic treatment of osteoarthritis and primary dysmenorrhoea in adolescents and adults above 12 years old.
PHARMACODYNAMICS
Food, gender and advanced age have negligible effects on nimesulide pharmacokinetics.
MECHANISM
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.
METABOLISM
Hepatic. Extensive biotransformation, mainly to 4-hydroxynimesulide (which also appears to be biologically active).
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
FOOD INTERACTIONS
avoid alcohol
SIDE EFFECTS
Nimesulide may cause dizziness. If you feel dizzy, do not drive or take part in any activity in which you need to be alert. Nimesulide is likely to cause stomach discomfort such as nausea, diarrhoea and stomach pain. Be sure to take it with food. This will help minimise the stomach discomfort.