Nimesulide information from DrugsUpdate  

Pharmacodynamics

Pharmacokinetics

Nimesulide is a nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, anti-pyretic, and analgesic properties. It 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 protect against the tissue damage that occurs during inflammation.

Absorption
Well absorbed from GI tract following oral admin. Peak plasma levels:1-3 hours. With bid admin of 100 mg, steady-state is achieved within 24-36 hours.

Distribution
99% bound to plasma protein.

Metabolism
Hepatic biotransformation; principal metabolite is 4-hydroxy-nimesulide.

Excretion
Elimination half-life: 2-5 hours. Metabolites in urine: 80%, feces: 20% of the administered dose.9% bound to plasma protein.

Nimesulide Indications / Nimesulide Uses

Information Not Available

Nimesulide Adverse Reactions / Nimesulide Side Effects

Epigastric discomfort, heartburn or abdominal cramps, nausea, vomiting and diarrhoea; skin rash, pruritus, oedema, headache, dizziness, drowsiness; hypersensitivity reactions (e.g. bronchospasm, rhinitis, angioedema urticaria); GI haemorrhage/perforation; bullous/erosive stomatitis, purpura, thrombocytopenia, toxic epidermal necrolysis, haematuria, oliguria, and renal failure; increases in liver enzymes.

Potentially Fatal: Fatal hepatitis, Stevens Johnson syndrome.

Precautions

Information Not Available

Special Precautions

History of GI tract disease, infections, oedema, hypertension, elderly, lactation.

Other Drug Interactions

Additive hepatotoxic effects with known hepatotoxins: anti-convulsants (e.g. valproic acid), anti-fungals (e.g. ketoconazole), anti-tuberculous drugs (e.g. isoniazid), tacrine, pemoline, amiodarone, methotrexate, methyldopa, amoxicillin/clavulanic acid. May decrease the oral bioavailability of furosemide and the natriuretic and diuretic response to furosemide. Increased risks of GI and hepatic adverse effects with other NSAIDs, including aspirin. May increase anti-coagulant effect of warfarin. Potentiates the action of phenytoin. May be displaced from binding sites with fenofibrate, salicylic acid, and tolbutamide. Interactions between NSAIDs and lithium, probenecid and ciclosporin, have been documented.

Other Interactions

Food Interaction
Alcohol increases the risk of hepatic reactions.

Dosage

Oral
Dysmenorrhoea
Adult: 100 mg bid. Use in the European Union (EU) is limited to a max of 15 days.

Oral
Osteoarthritis
Adult: 100 mg bid. Use in the European Union (EU) is limited to a max of 15 days.

Oral
Postoperative pain
Adult: 100 mg bid. Use in the European Union (EU) is limited to a max of 15 days.

Oral
Acute pain
Adult: 100 mg bid. Use in the European Union (EU) is limited to a max of 15 days.

Rectal
Acute pain
Adult: 200 mg bid

Rectal
Osteoarthritis
Adult: 200 mg bid

Rectal
Primary dysmenorrhoea
Adult: 200 mg bid

Topical/Cutaneous
Acute traumatic tendinitis
Adult: 3% gel/cream: Apply thin layer to affected area bid-tid. Duration: 7-15 days.

Topical/Cutaneous
Sprains
Adult: 3% gel/cream: Apply thin layer to affected area bid-tid. Duration: 7-15 days.

Food(before/after)

Should be taken with food. (Take after meals.)

Nimesulide and Pregnancy

Contraindicated in pregnancy

Nimesulide and Lactation

Caution when used during lactation

Nimesulide and Children

Information Not Available

Nimesulide and Geriatic

Information Not Available

Nimesulide and Other Contraindications

Hypersensitivity; GI bleeding, active peptic ulcer disease; severe renal and heart failure; hepatic impairment or known liver disease; coagulation disorders; pregnancy; children <12 years.

Storage

Oral
Protect from heat and humidity; store at <25°C.

Lab interference

Oral
Protect from heat and humidity; store at <25°C.