|
COMPOSITION :
Each film coated tablet contains: Nimesulide BP 100 mg. PharmEvo specs.
PHARMACOLOGY :
Nimesulide is nonsteroidal anti-inflammatory drug of the sulphonanilide class. The anti-inflammatory, analgesic and antipyretic activities of Nimesulide have been demonstrated in a number of experimental models and in numerous clinical trials. The anti-inflammatory potency of Nimesulide is similar or greater than that of Indomethacin, Diclofenac, Piroxicam and Ibuprofen. Nimesulide has an analgesic potency similar to that of Ibuprofen. The antipyretic potency of Nimesulide is superior to that of Indomethacin, Ibuprofen, Aspirin and Paracetamol.
MECHANISM OF ACTION:
Nimesulide is a selective inhibitor of prostaglandin synthesis but appears to exert its therapeutic effect by a variety of other mechanisms like inhibition of platelet-activating factor (PAF), tumor necrosis factor - alpha (TNF alpha), Protease & histamine etc.
PHARMACOKINETICS:
On oral administration of Nimesulide 50-200 mg tablets to healthy volunteers, peak serum concentrations of 1.98 to 9.85 mg/L are achieved within 1.22 to 3.17 hours. Oral absorption of Nimesulide is nearly complete. Concomitant administration of food may decrease the rate but not the extent of absorption of Nimesulide. Plasma binding was high (99%) and the apparent volume of distribution ranged from 0.19 to 0.35 L/kg. Nimesulide is extensively metabolized to several metabolites which are excreted mainly in the urine (70%) and in feces (20%). In Patients with moderately impaired renal function (creatinine clearance 1 .8 to 4.8 L/h or 30 to 80 ml/min), also in children and elderly volunteers the pharmacokinetic profile of Nimesulide is not significantly altered. In patients wit moderate renal impairment, slight accumulation of 4- hydroxy Nimesulide was noted, however the clinical significance of this finding is unknown.
INDICATIONS:
Adults- Nimesulide (NISE) is indicated in the treatment of variety of painful inflammatory conditions including those associated with osteoarthritis, postoperative trauma, sports injuries, ear nose throat disorders, dental surgery, bursitis / tendinitis, thrombophlebitis, pharyngitis and gynaecological disorders. |