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PANACEA BIOTEC LTD. [View Profile]
Ernakulam(Kochi) - India
Nimesulide is described chemically as N-(-4-nitro-2-phenoxyphenyl) methane sulfonamide.
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 C13H12N2O5 S, and the molecular weight is 308.311.
Willgo is light yellow/ yellow coloured, bilayered, round, biconvex, uncoated tablet.
Each uncoated long acting tablet contains:
Nimesulide BP ............................ 200mg
Colour: Quinoline Yellow
Clinical Pharmacology :
Mechanism of Action
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 200 mg per day, it is as effective as 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 un-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 is the only NSAID able to affect all the mediators of pain and inflammation. Nimesulide inhibits COX-1 to some extent, leading to better treatment of inflammatory pain. Nimesulide also reduces pain at central level through a spinalsupraspinal mechanism. Moreover, Nimesulide also has a potent and long lasting anti-pyretic affect.
Nimesulide appears to exert its therapeutic effects through a variety of mechanisms viz4:
Preferential Cyclooxygenase_2 inhibition at its origin (gene Expression)
Reduced generation of superoxide anions by stimulated polymorphonuclear leucocytes
Inhibition of platelet aggregation factor synthesis by activated cells
Nimesulide induces production of nitric oxide.
Scavenger of inactivation of a1-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- a).
The drug reduces superoxide anion generation by activated neutrophils without influencing their phagocytic or chemotactic responsiveness and inhibits the leucocyte respiratory burst through inhibition of phosphodiesterase (PDE) type IV, the principal enzyme responsible for the degradation of leucocyte cAMP.
Also, Nimesulide protects chondrocytes, the cells that in normal conditions produces cartilage.
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Description: Nimesulide is described chemically as N-(-4-nitro-2-phenoxyphenyl) methane sulfonamide. Nimesulide is a yellowish crystalline powder. It is practical ....
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