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DESCRIPTION:
It is new non-steroid anti-inflammatory drug and after administration leads to adequate analgesia and antipyretic effect. The advantage of Nimesulide over other NSAIDs is that it causes minimal gastric irritation.
MECHANISM OF ACTION:
It is weak inhibitor of prostaglandin synthesis. It appears to act at different stages of the inflammatory reaction and mechanisms by which it exerts it action are complex. It leads to inhibition of superoxide anion generation in vitro activated neutrophilis, inhibition of histamine release from tissue mast cells and basophils, it causes inhibition of platelet activating factor synthesis in stimulated human neutrophilis inhibition of synthesis of metaloproteinase thus preventing break down of osteoarthritic human cartilage.
PHARMACOKINETICS:
After oral administration, it is rapidly and almost completely absorbed. It is highly bound to plasma proteins and is extensively metabolized in liver. The major metabolite is pharmacologically active.
Onset of Action: 30-60 minutes.
Duration of Action: 8-10 hours
ADVERSE EFFECTS:
Nausea, vomiting, diarrhea, heartburn, epigastric pain, pruritus, skin rash, headache, sometimes dizziness.
CONTRAINDICATION: Active peptic ulcer, moderate to severe hepatic impairment.
SPECIAL PRECAUTIONS:Renal impairment, hear failure.
PREGNANCY :CONTRAINDICATED
LACTATION:CONTRAINDICATED
ELDERLY: Use with caution
INTERACTION:Fenofibrate, Salicycline acid, Valproic acid and Tolbutamide: These drugs displace mimesulide from the plasma binding sites.
Methotrexate and Frusemide: These drugs may be displaced from plasma proteins by nimesulide.
Theophylline: Efficacy of slow release theophylline preparations reduced.
Warfarin: Excercise caution since efficacy may be increased.
INDICATIONS:
Osteoarthritis Rheumatoid arthritis, low back pain, dysmenorrhoea, and other gynaecological disorders, dental and postoperative pain, in reducing pain of ear, nose and throat inflammation. Pain of malignancy, sports injury.
DOSAGE AND ADMINISTRATION:
Adults: 100 mg BD.
Children: 1.5 mg/kg/day three times a day age between 3-12 years
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