Nimesulide

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DRUGS
Nimesulide

Nimesulide is a relatively COX-2 selective, Non-Steroidal Anti-Inflammatory Drug (NSAID) with analgesic and antipyretic properties.

Introduction

Nimesulide is a relatively COX-2 selective, Non-Steroidal Anti-Inflammatory Drug (NSAID) with analgesic and antipyretic properties.

Indications

  • Acute pain
  • Dysmenorrhoea
  • Osteoarthritis
  • Headache
  • Post-operative pain
  • Sprains
  • Acute traumatic tendinitis

Pharamcological Action

Nimesulide inhibits prostaglandin synthetase/cyclooxygenase, which limits prostaglandin production. Its cyclooxygenase inhibiting potency is intermediate, but is relatively selective for the cyclo-oxygenase-2 (COX-2) thus the potential for gastric injury and intolerance is less. It is also a free radical scavenger, and helps to protect against the tissue damage that occurs during inflammation.

Dosage

Tablet:  100 mg twice daily

Suspension: 50mg/5ml

Pharmacokinetics

Nimesulide is rapidly absorbed from the gastrointestinal tract. Plasma protein binding is 97.5% and peak plasma concentrations occurring at 1-3 hours. It is metabolized in liver and extensive biotransformation, mainly to 4-hydroxynimesulide (which also appears to be biologically active) and also excreted in renal 50% and in fecal 29%. The elimination half life is approximately 2- 5 hours.

Contraindications

Use in the following conditions is contraindicated:

  • Hypersensitivity
  • Gastro-intestinal bleeding
  • Active peptic ulcer disease
  • Severe renal and heart failure
  • Hepatic impairment or known liver disease
  • Coagulation disorders
  • Pregnancy
  • Children <12 years

Drug Interactions

  • Increased risks of Gastrointestinal and hepatic adverse effects with other NSAIDs, including aspirin
  • It may increase anti-coagulant effect of warfarin.
  • Alcohol increases the risk of hepatic reactions

Side effects

Common (affect between 1 in 10 and 1 to 100 people)

  • Nausea, vomiting and diarrhea
  • Heartburn or abdominal cramps

Uncommon (affect between 1 in 100 and 1 to 1000 people)

  • Skin rash
  • Oedema
  • Dizziness & drowsiness
  • GI hemorrhage/perforation
  • Bullous/Erosive stomatitis

Very rare (affect less than 1 in 10,000 people)

  • Thrombocytopenia
  • Haematuria, oliguria, and renal failure
  • Hypersensitivity reactions (e.g. bronchospasm, rhinitis, angioedema urticaria)

Precautions

Precaution should be taken in:

  • Patients with history of Gastrointestinal tract disease, infections, edema, hypertension and liver problems
  • Elderly population
  • Pregnant and lactating females

Clinic Evidence

  • Nimesulide is an effective, fast-acting and well-tolerated oral anti-inflammatory drug with a distinct analgesic activity. Nimesulide was significantly more effective for the treatment of postoperative pain, as measured by the primary efficacy variable of summed pain intensity difference within 6 hours after first treatment (10.91 vs. 6.29). Furthermore, nimesulide also provided significantly better pain relief than naproxen on this parameter. Overall, nimesulide demonstrated superior analgesic activity as compared with naproxen for the majority of secondary efficacy and has no gastrointestinal side effects1.
  • Nimesulide is known to have better therapeutic index than diclofenac in the control of cancer-related pain. Nimesulide has fewer side effects as compare to diclofenac making it more effective in controlling cancer pain2.

References

  1. Binning A Clin J Pain. 2007 Sep; 23(7):565-70
  2.  
  3. Corli O, Cozzolino A, Scaricabarozzi I. Drugs. 1993;46 Suppl 1:152-5 http://www.ncbi.nlm.nih.gov/pubmed/7506158
  4. Suleyman H, Cadirci E, Albayrak A, Halici Z. Curr Med Chem. 2008; 15(3):278-83
  5.  
  6. Singla AK, Chawla M, Singh A. J Pharm Pharmacol. 2000 May;52(5):467-86
  7.  
  8. Weiss P, Mouallem M, Bruck R, Hassin D, Tanay A, Brickman CM, Farfel Z, Bar-Meir S. Isr Med Assoc J. 1999 Oct;1(2):89-91
  9.  
  10. Drug bank : http://www.drugbank.ca/drugs/DB04743
  11. Medindia.Net : http://www.medindia.net/doctors/drug_information/nimesulide.htm
  12. Drugs Update.com : http://www.drugsupdate.com/generic/view/348/Nimesulide
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