Physical And Pharmaceutical Properties

Synonyms: R-805.

Chemical Name: 4'-Nitro-2'-phenoxymethanesulphonanilide.

Molecular Formula: (13)H(12)N(2)O(5)S Molecular Weight: 308.3 CAS Registry: 51803-78-2.

Nimesulide is an NSAID reported to be a selective inhibitor of cyclo-oxygenase-2 (COX-2). It has been given in doses of up to 200 mg twice daily by mouth or rectally for inflammatory conditions, fever, and pain. Nimesulide betadex (nimesulide betacyclodextrin complex) has been used similarly.

References.
1. Bennett A, et al. Nimesulide: a multifactorial therapeutic approach to the inflammatory process? a 7-year clinical experiences. Drugs 1993; 46: (suppl 1): 1-283. 
2. Davis R, Brogden RN. Nimesulide: an update of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy. Drugs 1994; 48:431-54. 
3. Senna GE, et al. Nimesulide in the treatment of patients intolerant of aspirin and other NSAIDs. Drugs 1996; 14: 94-103. 
4. Vizzardi M, et al. Nimesulide beta cyclodextrin (nimesulide-betadex) versus nimesulide in the treatment of pain after arthroscopic surgery. Curr Ther Res 1998; 59: 162-71.

Adverse Effects

Although thrombocytopenia is a common feature in patients infected with HIV one group of workers considered that thrombocytopenia in one of their patients was related to the use of nimesulide. (1) There has been a report (2) of a patient who developed fulminant hepatic failure after treatment with nimesulide.

1. Pasticci MB, et al. Nimesulide, thrombocytopenic purpura, and human immunodeficiency virus (HIV) infection. Ann Intern Med 1990; 112: 233-4. 
2. McCormick PA, et al. COX 2 inhibitor and fulminant hepatic failure. Lancet 1999; 353: 40-1.

Premature Labor

Nimesulide has been tried as an alternative to indomethacin to delay labour in a patient with a history of preterm delivery. (1) Nimesulide was given from 16 to 34 weeks of gestation and a successful delivery started 6 days after withdrawal. There appeared to be no adverse effect on fetal renal function or the ductus arteriosus. The authors suggested that fetal prostaglandin synthesis might be mainly mediated through cyclo-oxygenase-1 and that a relatively selective cyclo-oxygenase-2 inhibitor such as nimesulide might produce fewer adverse effects on the fetus than other non-selective NSAIDs.

1. Sawdy R, et al. Use of a cyclo-oxygenase type-2-selective non-steroidal anti-inflammatory agent to prevent preterm delivery. Lancet 1997; 350: 265-6.

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