NIMULID (Nimesulide) is described chemically as N-(4-Nitro-2-phenoxyphenyl) methanesulphonamide. It has the following structure: Nimesulide is a yellowish crystalline powder. It is practically insoluble in water, freely soluble in acetone and slightly soluble in ethanol. The empirical formula for Nimesulide is C13 H12N2O5S, and the molecular weight is 308.311. Each tablet of Nimulid for oral administration contains 100mg of Nimesulide BP and the following inactive ingredients: Lactose, Croscarmellose Sodium, Colloidal Silicon Dioxide, Maize Starch, Povidone, Polysorbate-80 and Magnesium Stearate. Nimulid tablet is pale yellow, coloured, round, biconvex, uncoated tablet with imprints of “”NIMULID”” on one side and “”picture of Logo”” on the other.
Nimesulide is a sulfonanilide non-steroidal anti-inflammatory drug whose anti-inflammatory analgesic and antipyretic activities have been demonstrated in several widely used animal experimental models2. At the recommended dose of 100 mg b.i.d., it is as effective an analgesic and anti-inflammatory agent as classical NSAIDs, and a well-tolerated drug with fewer side effects as evidenced by a number of controlled and non-controlled comparative trials3. Nimesulide is a unique NSAID, not only due to its chemical structure but also because of its specific affinity to inhibit Cyclooxygenase-2 thus exerting milder effects on the gastrointestinal mucosa.
Nimesulide appears to exert its therapeutics effects through a variety of mechanisms viz4: Selective Cyclooxygenase-2 inhibitor Reduced generation of superoxide anions by stimulated polymorphonuclear leucocytes Inhibition of platelet aggregation factor synthesis by activated cells Scavenger of inactivation of alpha1-protease inhibitor Inhibition of histamine release Inhibition of protein kinase C through inhibition of phosphodiesterase type IV Reduced degradation of cartilage matrix through inhibition of metalloprotease synthesis Potent inhibition of induced platelet aggregation Prevention of bradykinin/cytokine induced hyperalgesia of nerves (inhibiting release of TNF- alpha) Pharmacokinetics Absorption Nimesulide is fairly rapidly absorbed from the gastrointestinal tract. After oral administration of a 100mg dose to healthy fasting volunteers, mean maximum plasma concentration (Cmax) values of 2.86 to 4.58 mg/L were achieved within 1.22 to 3.83 hours (Tmax).