Pharmacological properties of nimesulide

Abstract

The pharmacological and toxicological properties of nimesulide have been previously reviewed (see [1-8]). The major part of these reviews has been concerned with the preclinical actions of the drug. A key issue concerning the interpretation of the in vitro effects of nimesulide has been the relationship of these to the plasma or synovial fluid concentrations of the drug, which are found during therapy. The review by Bennett and Villa [4] is noteworthy for having discriminated the in vitro effects, which are known to occur at therapeutic drug concentrations with those which are above this range. Thus, generally speaking although nimesulide has preferential COX-2 selectivity it is also an inhibitor of histamine release and actions, leukotriene B4 and C4, and platelet activating factor (PAF) production, the adherence and activation of neutrophils, collagenase and other metalloproteinases, glucocorticoid receptor phosphorylation, interleukin-6 production, calcium channel activation and is an antioxidant within the range of drug concentrations encountered therapeutically [4]. Thus, nimesulide can be regarded as having multifactorial actions in relation to its anti-inflammatory activity.