Nimesulide
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| AHFS/Drugs.com | International Drug Names |
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By mouth, rectal, topical |
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| Pharmacokinetic data | |
| Protein binding | >97.5% |
| Metabolism | Hepatic |
| Biological half-life | 1.8–4.7h |
| Excretion | Renal (50%), fecal (29%) |
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| ECHA InfoCard | 100.052.194 |
| Chemical and physical data | |
| Formula | C13H12N2O5S |
| Molar mass | 308.311 g/mol |
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Nimesulide is a relatively COX-2 selective, non-steroidal anti-inflammatory drug (NSAID) with pain medication and fever reducing 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. It has a multifactorial mode of action and is characterized by a fast onset of action.
It works by blocking the production of prostaglandins (a chemical associated with pain) thereby relieving pain and inflammation.
Continuous use of nimesulide (more than 15 days) can cause the following side effects:
Women should use the drug with caution during lactation; Nimesulide is contraindicated during pregnancy.
Due to concerns about the risk of hepatotoxicity, nimesulide has been withdrawn from market in several countries (Spain, Finland, Belgium and Ireland).
Nimesulide is rapidly absorbed following oral administration.
Nimesulide undergoes extensive biotransformation, mainly to 4-hydroxynimesulide (which also appears to be biologically active).
Food, gender and advanced age have negligible effects on nimesulide pharmacokinetics.
Moderate renal impairment does not necessitate dosage adjustment, while in patients with severe renal impairment or hepatic impairment Nimesulide is contraindicated.
Nimesulide has a relatively rapid onset of action, with meaningful reductions in pain and inflammation observed within 15 minutes from drug intake.
The therapeutic effects of Nimesulide are the result of its complex 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. Clinical evidence is available to support a particularly good profile in terms of gastrointestinal tolerability.
It was launched in Italy for the first time as Aulin and Mesulid in 1985 and is available in more than 50 countries worldwide, including among others France, Portugal, Greece, Switzerland, Belgium, Russia, Thailand and Brazil. Nimesulide has never been filed for Food and Drug Administration (FDA) evaluation in the United States, where it is not marketed.
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Wikipedia