Nimesulide: Overview of properties and applications

Authors
Citation
Kd. Rainsford, Nimesulide: Overview of properties and applications, DRUGS TODAY, 37, 2001, pp. 3-7
Citations number
11
Categorie Soggetti
Pharmacology
Journal title
DRUGS OF TODAY
ISSN journal
00257656 → ACNP
Volume
37
Year of publication
2001
Supplement
B
Pages
3 - 7
Database
ISI
SICI code
0025-7656(2001)37:<3:NOOPAA>2.0.ZU;2-Y
Abstract
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.