| Item |
Information |
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Drug Groups
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experimental |
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Description
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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 Due to concerns about the risk of hepatotoxicity, nimesulide has been withdrawn from market in many countries. |
| 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. |
| 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 |
| Affected Organisms |
| • |
Humans and other mammals |
|
| 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 |
| Protein Binding |
>97.5% |
| Elimination |
Renal (50%), fecal (29%) |
| External Links |
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