Nimesulide, a selective cyclooxygenase 2 (COX-2) inhibitor, has antiinflamm
atory and analgesic properties. It has a twin aromatic ring structure and a
relatively high pKa of approximately 6.5. This along with the moderate lip
ophilicity of nimesulide may confer it low irritant potential, thus allowin
g for good uptake into the upper gastrointestinal circulation. Like other n
onsteroidal antiinflammatory drugs (NSAIDs), nimesulide undergoes phase I m
etabolism via the cytochrome P-450 system. The phenolic metbolites undergo
phase ii metabolism to produce phenolic-glucuronides. Nimesulide has been f
ound to have a good safety record especially in the gastrointestinal tract
and is indicated for relief of a Variety of conditions involving inflammati
on and pain, such as osteoarthritis, musculoskeletal conditions and dysmeno
rrhea. (C) 2001 Prous Science. All rights reserved.