Nimesulide

Nimesulide is a prescription non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties and its approved indications are the treatment of acute pain, the symptomatic treatment of osteoarthrosis and primary dysmenorrhoea in adolescents and adults above 12 years old. Nimesulide is among the top 5 non-steroidal anti-inflammatory drugs worldwide.

History

It was launched in Italy for the first time as Aulin and Mesulid in 1985 and is presently available in more than 50 countries worldwide, among others France, Portugal, Greece, Switzerland, Belgium, Mexico, Brazil. Nimesulide has never been filed for FDA evaluation in the United States, where it is not marketed.

In 2002 nimesulide benefit/risk profile was reviewed by the EMEA following decision to temporarily suspend the drug from the market in March 2002, in relation to the reporting of hepatic adverse effects in patients apparently treated with nimesulide. It was later demonstrated that the occurrence of hepatic reactions with nimesulide is similar to that of any other NSAIDs  as confirmed by a study published by the British Medical Journal in 2003.

Availability

It is available in a variety of forms: tablets, powder for dissolution in water, suppositories and topical gel. A recent evaluation from EMEA (the European Medicines Agency) concluded that the overall benefit/risk profile of nimesulide is favourable and in line with that of the other NSAIDs (such as for example, diclofenac,ibuprofen, naproxen).

Trade names

Nimesulide is available through the world as original product with the following trademarks: Aulin, Ainex, Drexel, Donulide, Edrigyl, Eskaflam, Heugan, Mesulid, Minapon, Nexen, Nimed, Nimedex,Nimutab, Nisulid, Scaflam, Scaflan. Sulidene and Zolan for veterinary use. Many generic and copy-products also exist (Coxtral, Lusemin, Medicox, Nidol, Nimalox, Nimesil, Nimotas, Nimulid, Nise, Ventor, Willgo among others).

Pharmacokinetics

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 patients with severe renal impairment or hepatic impairment are contraindicated

Nimesulide has a relatively rapid onset of action, with meaningful reductions in pain and inflammation observed within 15 minutes from drug intake. As many as almost 498 million patients have been treated with nimesulide from its launch until today. 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^. Clinical evidence is available to support a particularly good profile in terms of gastrointestinal tolerability.

As all anti-inflammatory drugs, it should be taken in compliance with the recommendations included in the patient leaflet.

Side effects

Like most drugs in NSAID category, nimesulide is known to be hepatotoxic (damaging to the liver) in rare but unpredictable cases and should be taken with care. The patient information leaflet informs that the use of nimesulide in children under the age of 12 is contraindicated.