Nimesulide

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Information about Nimesulide

Nimesulide is a nonsteroidal antiinflammatory drug (NSAID) with relative specificity for COX-2 that is not available in the United States, but is used widely in other countries in the treatment of acute pain.

Liver safety of Nimesulide

Nimesulide has been linked to a low rate of transient serum enzyme elevations during therapy, but also to many instances of clinically apparent acute liver injury that can be severe and can result in acute liver failure, need for emergency liver transplantation and death.

Mechanism of action of Nimesulide

Nimesulide (ni mes' sul ide) is a unique NSAID that has a basic sulfonanilide structure. Like other NSAIDs, nimesulide inhibits the enzyme cyclo-oxygenase (COX), thereby blocking the formation of prostaglandins that are important in pain and inflammatory pathways. Unlike most conventional NSAIDs, however, nimesulide has a relative specificity for COX-2 activity, the form that is most closely related to pain pathways as opposed to COX-1, which has major effects of gastric mucosa cell protection and platelet function. Nimesulide has analgesic as well as antipyretic and antiinflammatory activities mediated by COX-2 actions, but has relatively scant effect on platelet function or loss of gastric cytoprotection which is associated with COX-1 activity. Nimesulide has a rapid onset of action and has other activities besides its effects of cyclo-oxygenases that may be important in its antiinflammatory and analgesic actions.

FDA approval information for Nimesulide

Nimesulide was never marketed in the United States, but has been widely used in many countries of the world since its introduction in the 1990s.

Clinical use of Nimesulide

Current indications vary by country, but are generally limited to mild-to-moderate acute pain for which the recommended dose in adults is 100 mg twice daily for no more than 15 days. Chronic therapy is not generally recommended, and nimesulide is considered contraindicated in children.

Dosage and administration for Nimesulide

Nimesulide is available by prescription in the form of capsules or granules for oral suspension of 100 mg and as suppositories of 200 mg in both generic and trade formulations (Sulide, Nimside and others).

Side effects of Nimesulide

Nimesulide is generally well tolerated, but side effects can include headache, dizziness, somnolence, gastrointestinal upset, nausea, abdominal discomfort, diarrhea, peripheral edema and hypersensitivity reactions.

Nonsteroidal Antiinflammatory Drugs (NSAIDs)

Acetaminophen, Celecoxib, Diclofenac, Diflunisal, Etodolac, Fenoprofen, Flurbiprofen, Ibuprofen, Indomethacin, Ketoprofen, Ketorolac, Mefenamic Acid, Meloxicam, Nabumetone, Naproxen, Nimesulide, Oxaprozin, Phenylbutazone, Piroxicam, Rofecoxib, Sulindac, Tolmetin

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