Affiliation:
1. Pharmaceutics Division, University Institute of Pharmaceutical Sciences, Punjab University, Chandigarh 160 014, India
2. Panacea Biotec Ltd, P.O. Lalru, Lalru, Punjab 140 501, India
Abstract
Abstract
Nimesulide, a non-steroidal anti-inflammatory drug (NSAID), is administered orally or rectally twice daily for a variety of inflammation and pain states. This is a unique NSAID, not only because of its chemical structure but also because of its specific affinity to inhibit cyclooxygenase-2 (COX-2), thus exerting milder effects on the gastrointestinal mucosa. Current data on selective COX-2 inhibitors suggest that they may have an efficacy similar to that of standard NSAIDs. Initial general clinical experience with selective COX-2 inhibitors appears to show that they are particularly promising in individuals at risk because of renal diseases, hypertension or congestive heart failure.
Various experimental models and clinical studies have demonstrated the anti-inflammatory efficacy of nimesulide. Nimesulide is superior, or at least comparable in efficacy, to other NSAIDs, but is better tolerated and has less potential for adverse reactions. Thus, selective COX-2 inhibitors should have anti-inflammatory effects devoid of side effects on the kidney and stomach. They may also demonstrate new important therapeutic benefits as anticancer agents as well as help prevention of premature labour and even retard the progression of Alzheimer's disease. No clinically significant drug interactions have been reported for nimesulide.
Not much has been reported about the pharmaceutical aspects of nimesulide. Its poor aqueous solubility poses bioavailability problems in-vivo. This could be overcome by the formation of inclusion complexes with β-cyclodextrin, as has been reported by various researchers. However, absence of any in-vivo data regarding the relative absorption of nimesulide from β-cyclodextrin complex compared with that from conventional formulations of the drug makes the use of such fast-releasing complexes rather questionable. Only a limited number of assay procedures (HPLC, spectrophotometric, spectrofluorimetric) for the determination of nimesulide and its metabolite in plasma/urine samples or in dosage forms have been reported in the literature.
The purpose of this review is to provide a concise overview of the pharmacological and pharmaceutical profile of nimesulide. Various investigations carried out recently are reported, although older references to research performed on nimesulide have also been included, where appropriate.
Publisher
Oxford University Press (OUP)
Subject
Pharmaceutical Science,Pharmacology
Reference150 articles.
1. Combined treatment of allergic rhinitis with terfenadine and nimesulide, a nonsteroidal anti-inflammatory drug;Andri;Allerg. Immunol.,1992
2. Tolerability of nimesulide in aspirin-sensitive patients;Andri;Ann. Allergy,1994
3. The treatment of ENT phlogosis: seaprose-S versus nimesulide;Antonelli;Acta Otorhinolaryngol. Ital.,1993
4. Aspirin and paracetamol tolerance in patients with nimesulide induced urticaria;Asero;Ann. Allergy Asthma Immunol.,1998
5. Action of a new non-steroidal anti-inflammatory drug, nimesulide, on activation of the complement system: an in-vitro study;Auteri;Int. J. Tissue React.,1988
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