Comparative study of anti-inflammatory and ulcerogenic activities of different cyclo-oxygenase inhibitors
- 73 Downloads
The aim of the present work was to study the in vivo anti-inflammatory activity of six NSAIDs, ibuprofen, diclofenac, nimesulide, meloxicam, celecoxib and rofecoxib, using the rat air-pouch model of inflammation to characterize the ability of these drugs to induce gastric damage and PGE2 inhibition. Selective compounds were observed to have no ulcerogenic properties at anti-inflammatory doses; however, these drugs were weaker inhibitors of several inflammatory aspects such as cell influx and exudate formation. In contrast, the non-selective and preferential compounds present anti-inflammatory properties at lower doses than presented by selective drugs. At anti-inflammatory doses, only meloxicam and ibuprofen produced gastric damage and inhibition of PGE2 synthesis, suggesting that ulcerogenic properties of NSAIDs cannot be predicted by their selectivity index, since meloxicam demonstrates ulcerogenic properties despite its preferential profile.
Key wordsNon-steroidal anti-inflammatory drugs cyclo-oxygenases air pouch prostaglandin E2 leukocyte
Unable to display preview. Download preview PDF.
- Adams, I., Neuman, R. G., Sachs, J., et al. (1990). Efficacy and gastric safety of etodolac as determined in cultured human gastric and synovial cells, Gastroenterology 24, 40–47.Google Scholar
- Dvornik, D. M. (1997). Tissue selective inhibition of prostaglandin biosynthesis by etodolac, J. Rheumatol. 14, 40–47.Google Scholar
- Gamberini, M. T., Skorupa, L. A., Souccar, C., et al. (1991). Inhibition of gastric secretion by a water extract from Baccharis triptera, Mart, Mem. Inst. Oswaldo Cruz 2, 137–139.Google Scholar
- Malmsten, C. (1984). Arachidonic acid metabolism and inflammation. A brief introduction, Scand. J. Rheumatol. 53, 31–45.Google Scholar
- Maslinska, D. and Gajewski, M. (1999). Some aspects of the inflammatory process, Folia Neuropathol. 36, 199–204.Google Scholar
- Penning, T. D., Talley, J. J., Bertenshaw, S. R., et al. (1997). Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-y1] benzenesulfonamide (SC-58635, celecoxib), J. Med. Chem. 40, 1347–1365.PubMedCrossRefGoogle Scholar
- Reicin, A. S., Shapiro, D., Sperling, R. S., et al. (2002). Comparison of cardiovascular thrombotic events in patients with osteoarthritis treated with rofecoxib versus nonselective nonsteroidal anti-inflammatory drugs (ibuprofen, diclofenac, and nabumetone), Am. J. Cardiol. 89, 204–209.PubMedCrossRefGoogle Scholar