Summary
Nimesulide (4-nitro-2-phenoxy-methansulfonanilide) is a weak acidic (pKa = 6.50) nonsteroidal anti-inflammatory drug (NSAID) belonging to a new chemical class, the sulfonanilide derivatives, and does not contain the carboxylic group. It exhibits potent anti-inflammatory, analgesic and antipyretic activities. Although nimesulide is not a cyclo-oxygenase inhibitor in gastric tissues or bovine seminal vesicle microsomes, it inhibits prostaglandin synthesis in zymosan-stimulated murine macrophages in inflammatory exudate. Nimesulide significantly antagonises the immune formation of thromboxane B2 in lung tissue. It neither induces gastrointestinal lesions nor affects renal function in animal models.
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Berti F, Rossoni G, Buschi A, Robuschi M, Villa LM. Anti-an-aphylactic and antihistaminic activity of the non-steroid anti-inflammatory compound nimesulide in guinea-pig. Arzneimittel-Forschung/Drug Research 40: 1011–1016, 1990
Berti F, Rossoni G, Buschi A, Villa LM, Robuschi M, et al. Nimesulide, a non-steroidal anti-inflammatory drug, displays anti-antaphylactic and antihistaminic activity in guinea pigs. Drug Investigation 3 (Suppl. 2): 39–47, 1991
Bevilacqua M, Vago T, Beretta A. Nimesulide as an inhibitor of Superoxide anion (O2−) production by human polymorphonuclear leukocytes. Pain and Reproduction 31: 265–272, 1988
Böttcher I, Schweizer A, Glatt M, Werner H. A sulphonamidoindanone CGP 28237 (ZK 34228), a novel non-steroidal anti-inflammatory agent without gastrointestinal ulcerogenicity in rats. Drugs Under Experimental and Clinical Research 13: 237–245, 1987
Capsoni F, Venegoni E, Minonzio F, Ongari AM, Maresca V, et al. Inhibition of neutrophil oxidative metabolism by nimesulide. Agents and Actions 21: 121–129, 1987
Carr DP, Henn R, Green JR, Böttcher I. Comparison of the systemic inhibition of thromboxane synthesis, anti-inflammatory activity and gastro-intestinal toxicity of non-steroidal anti-inflammatory drugs in the rat. Agents and Actions 19: 374–375, 1986
Ceserani R, Casciarri I, Cavalletti E, Cazzulani P. Action of nimesulide on rat gastric prostaglandins and renal function. Drug Investigation 3 (Suppl. 2): 14–21, 1991
Dallegri F, Ottonello L, Dapino P, Bevilacqua M. The anti-inflammatory drug nimesulide rescues alpha-1-proteinase inhibitor from oxidative inactivation by phagocytosing neutrophils. Respiration 59: 1–4, 1992
Dallegri F, Patrone F, Ballestrero A, Ottonello L, Ferrando F, et al. Inactivation of neutrophil-derived hypochlorous acid by nimesulide: a potential mechanism for the tissue protection during inflammation. International Journal of Tissue Reaction 12: 107–111, 1990
Marino O, Casolaro S, Meliota S, Stellato C, Guidi G, et al. Inhibition of histamine release from human FceRI+ cells by nimesulide. 20th Annual Meeting of the European Histamine Research Society, Marburg, Germany, May 1991. Agents and Actions, Special Conference Issue 32: C311–C314, 1992
Rainsford KD. The comparative gastric ulcerogenic activities of non-steroid anti-inflammatory drugs. Agents and Actions 7: 573–577, 1977
Rufer C, Schillinger E, Böttcher I, Repenthin W, Herman C. Non-steroidal anti-inflammatories — XII: mode of action of anti-inflammatory methane sulfonanilides. Biochemical Pharmacology 31: 3591–3596, 1982
Swingle KF, Grant TJ, Kvam DC. Quantal responses in the Randall-Selitto assay. Proceedings of the Society for Experimental Biology and Medicine 137: 536, 1971
Swingle KF, Moore GGI, Grant TJ. 4-Nitro-2-phenoxymetha-nesulfonanilide (R-805): a chemically novel anti-inflammatory agent. Archives Internationales de Pharmacodynamie et de Therapie 221: 132–139, 1976
Swingle KF, Moore GGI. Pre-clinical pharmacological studies with nimesulide. Drugs Under Experimental and Clinical Research 10: 587–597, 1984
Tofanetti O, Casciarri I, Cipolla PV, Cazzulani P, Omini C. Effect of nimesulide on cyclo-oxygenase activity in rats’ gastric mucosa and inflammatory exudate. Medical Science Research 17: 745, 1989
Vigdahl RL, Tukey RH. Mechanism of action of novel anti-inflammatory drugs diflumidone and R-805. Biochemical Pharmacology 26: 307–311, 1977
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Magni, E. The Effect of Nimesulide on Prostanoid Formation. Drugs 46 (Suppl 1), 10–14 (1993). https://doi.org/10.2165/00003495-199300461-00004
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DOI: https://doi.org/10.2165/00003495-199300461-00004