Nimesulide is a non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. Its approved indications are the treatment of acute pain, symptomatic treatment of osteoarthritis and primary dysmenorrhea in adolescents and adults over 12 years of age. It is usually taken by mouth.
The anti-inflammatory effect of nimesulide is due to the inhibition of cyclooxygenase-2 (COX-2), an enzyme involved in prostaglandin synthesis via the arachidonic acid pathway. This results in decreased levels of prostaglandins that mediate pain, fever, and inflammation.
Nimesulide is rapidly absorbed after oral administration. Nimesulide has a relatively rapid onset of action, with significant reductions in pain and inflammation observed within 15 minutes of drug ingestion. Plasma protein binding is greater than 97%. Nimesulide undergoes extensive biotransformation, primarily to 4-hydroxynimesulide. 4-Hydroxynimesulide is also biologically active. Elimination is largely renal and to a lesser extent fecal. The half-life of nimesulide is 2-4 hours.
Due to concerns about the risk of liver toxicity, nimesulide has been withdrawn from the market in several countries (Spain, Finland, Belgium, Ireland and the USA). Liver problems have led to both deaths and the need for transplantation. This can occur as early as three days after starting the drug.
Folgende Nebenwirkungen sind ebenfalls aufgetreten:
LD50 (rat, oral): 200 mg-kg-1
| ATC Code | M01AX17, M02AA26 |
| Formula | C13H12N2O5S |
| Molar Mass (g·mol−1) | 308,31 |
| Physical State | solid |
| Melting Point (°C) | 143–144,5 |
| CAS Number | 51803-78-2 |
| PUB Number | 4495 |
| Drugbank ID | DB04743 |
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