About Nimesulide

Nimesulide is a nonsteroidal anti-inflammatory drug (NSAID) that has pain reliever and fever reducer properties.It is approved for the symptomatic treatment of acute pain, osteoarthritis and primary dysmenorrhea in adolescents and adults over 12 years of age.Side effects may include liver problems.It has a multifactorial mode of action and is characterized by a rapid onset of action.It works by blocking the production of prostaglandins (a pain-related chemical), which reduces pain and inflammation.

Medical use 

It can be used for pain, including period pain.Long-term use of nimesulide is not recommended for chronic conditions such as arthritis. This is because it is associated with an increased risk of liver toxicity including liver failure.Despite the risk of hepatotoxicity, a 2012 review by the European Medicines Agency (EMA) concluded that the overall benefit/risk profile of nimesulide was favorable and

comparable to that of other NSAIDs. as long as the duration of use is limited to 15 days and the dose does not exceed 200 mg/day.

Children

Compared with ketoprofen, paracetamol, mefenamic acid, aspirin, or ibuprofen, nimesulide for less than 10 days does not appear to increase hypothermia, gastrointestinal bleeding, upper abdominal pain, vomiting, diarrhea, or transient Risk of asymptomatic liver enzyme elevations.However, the data are not available for those under 6 months of age.

Pregnancy and breastfeeding

Women should use the drug with caution during breastfeeding. Nimesulide is contraindicated during pregnancy, and studies have shown that it is also prohibited for breastfeeding women.

Available form

Nimesulide is available in various forms: tablets, powders to dissolve in water, suppositories, orally dissolving tablets, and topical gels.

Contraindications

Children under 12 and people with liver problems or flu-like symptoms should avoid use.

Side effects

Nimesulide has been withdrawn from the market in several countries (Spain, Finland, Belgium and Ireland) due to concerns about the risk of hepatotoxicity.Liver problems lead to death and the need for a transplant.This can occur in as little as three days after starting the medication.Continuous use of nimesulide (more than 15 days) may cause the following side effects:

• Diarrhea

• Vomit

• Rash

• Itching

• Dizziness

• Bitter

Pharmacology

Pharmacodynamics

Nimesulide is a nonsteroidal anti-inflammatory drug (NSAID), specifically a relatively selective cyclooxygenase 2 inhibitor.However, the pharmacology of nimesulide is peculiar and other unknown/not yet determined mechanisms appear to be involved.One pathway implicated in its action is the ecto-5′-nucleotidase (e-5’NT/CD73)/adenosine A2A receptor pathway.

Pharmacokinetics

Nimesulide is rapidly absorbed after oral administration.Nimesulide undergoes extensive biotransformation, mainly to 4-hydroxynimesulide (which also appears to be biologically active).Food, sex and advanced age had negligible effects on the pharmacokinetics of nimesulide.Moderate chronic kidney disease does not require dose adjustment, and for patients with severe chronic kidney disease or liver disease, nimesulide is contraindicated.Nimesulide has a relatively fast onset of action, with significant reductions in pain and inflammation observed within 15 minutes of dosing.The therapeutic effect of nimesulide is the result of its complex mode of action, targeting many key mediators of the inflammatory process such as: COX-2 mediated prostaglandins, free radicals, proteolytic enzymes and histamine.Clinical evidence may support a particularly good case of gastrointestinal tolerability.