Nimesulide is a nonsteroidal 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. Side effects may include liver problems. 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.
Medical uses It may be used for pain, including period pains. Nimesulide is not recommended long-term, as for chronic conditions such as arthritis. This is due to its association with an increased risk of liver toxicity, including liver failure. Despite its risk of hepatotoxicity, a 2012 evaluation by the European Medicines Agency (EMA) concluded that the overall benefit/risk profile of nimesulide is favourable and in line with that of the other NSAIDs such as diclofenac, ibuprofen, and naproxen provided that the duration of use is limited to 15 days and the dose does not exceed 200 mg/day.
Children Less than 10 days of nimesulide does not appear to increase the risk of hypothermia, gastrointestinal bleeding, epigastric pain, vomiting, diarrhea, or transient, asymptomatic elevation of liver enzymes compared to ketoprofen, paracetamol, mefenamic acid, aspirin, or ibuprofen in children. However, data does not speak to populations less than 6 months old.
Pregnancy and lactation Women should use the drug with caution during lactation and nimesulide is contraindicated during pregnancy, and research suggest that it is also contraindicated in lactating women.
Available forms
Nimesulide is available in a variety of forms: tablets, powder for dissolution in water, suppositories, mouth dissolving tablets, and topical gel.
Contraindications It should be avoided by children under 12 and people with liver problems.
Side effects Due to concerns about the risk of liver toxicity, nimesulide has been withdrawn from market in several countries (Mexico, Spain, Finland, Belgium, and Ireland). Liver problems have resulted in both deaths and the need for transplantation. The frequency of nimesulide-induced liver injury is estimated at around 1 in 50,000 patients, severe injury has occurred in as little as three days after starting the medication. Shorter (≤ 15 days) duration of therapy does not prevent serious nimesulide hepatotoxicity. Continuous use of nimesulide (more than 15 days) may cause the following side effects:
Diarrhea Vomiting Skin rash Itchiness Dizziness Bitterness in mouth
Pharmacology
Pharmacodynamics Nimesulide is a nonsteroidal anti-inflammatory drug (NSAID), acting specifically as a relatively selective cyclooxygenase-2 inhibitor. However, the pharmacological profile of nimesulide is peculiar, and additional, unknown/yet-to-be-identified mechanisms appear to also be involved. One pathway that has been implicated in its actions is the ecto-5'-nucleotidase (e-5′NT/CD73)/adenosine A2A receptor pathway.
Pharmacokinetics Nimesulide is absorbed rapidly following oral administration. Nimesulide undergoes extensive biotransformation, mainly to 4-hydroxynimesulide (which also appears to be biologically active). Food, sex, and advanced age have negligible effects on nimesulide pharmacokinetics. Moderate chronic kidney disease does not necessitate dosage adjustment, while in patients with severe chronic kidney disease or liver disease, 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.
History Nimesulide 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 Portugal, Greece, 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.
Society and culture
Brand names Nimesulide is available throughout the world as original product with the following trademarks: Sulide, Nimalox, Mesulid (Novartis, Brazil, Boehringer Ingelheim, Greece, Italy, Hungary), Coxtal (Sanofi, China, Bulgaria), Sintalgin (Abbott, Brazil), Eskaflam (GSK, Brazil, Mexico), Octaprin, Nimside (Teva, Pakistan), Nise (Russia, Venezuela, Vietnam, Ukraine), Nilsid (Egypt); Aulin (Bulgaria, Czech Republic, Italy, Romania, Poland), Ainex, Drexel, Donulide, Edrigyl, Enetra, Heugan, Mesulid, Minapon, NeRelid, Nexen, Nidolon, Nilden (Mexico); Emsulide, Nimed, Nimedex, Nimesil (Czech Republic, Moldova, Latvia, Lithuania, Kazakhstan, Georgia, Poland, Russia, Ukraine), Nimulid (Trinidad & Tobago, Serbia), Nimutab, Nimdase, Nimopen-MP Nise, Nimuwin, Nisulid, Nodard Plus, Nicip, Nimcap, Nic-P, Nic-Spas, Nimupain (India); Mesulid, Novolid, Relmex (Ecuador); Remisid (Ukraine); Coxulid, Emulid, Frenag, Fuzo, Motival, Nimeksil, Nimelid, Nîmes, Nimesdin, Romasulid, Sulidin, Suljel, Thermo Sulidin (Turkey), Xilox (Hungary); Modact-IR (Pakistan); and ad Sulidene and Zolan for veterinary use. Many generic and copy-products also exist (Lusemin, Medicox, Nidol, Nimalox, Nimesil, Nimotas, Nimulid, Nizer, Sorini, Ventor, Vionim, Neolide, Willgo among others), new-aid, Nexulide (Syria), Nims, Nice, Nimulide (Nepal)
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