Suppression of prostacyclin (PGI2) biosynthesis may explain the increased incidence of myocardial infarction and stroke which has been observed in placebo controlled trials of cyclooxygenase (COX)-2 inhibitors. Herein, we examine if COX-2-derived PGI2 might condition the response of the vasculature to sustained physiologic stress in experimental models that retain endothelial integrity. Deletio...

The present study was undertaken to investigate the effect of dietary supplementation with nimesulide or eugenol on N-nitrosodiethylamine (DEN)-initiated early hepatocarcinogenesis in F344 male rats. Both compounds did not alter the expression of cytochrome P450 (CYP) 2E1, the enzyme that plays a major role in the activation of DEN to genotoxic products; however, nimesulide induced the expressi...

Ligand activation of peroxisome proliferator–activated receptor-b/d (PPARb/d) and inhibition of cyclooxygenase-2 (COX2) activity by nonsteroidal anti-inflammatory drugs (NSAID) can both attenuate skin tumorigenesis. The present study examined the hypothesis that combining ligand activation of PPARb/d with inhibition of COX2 activity will increase the efficacy of chemoprevention of chemically in...

Ligand activation of peroxisome proliferator-activated receptor-β/δ (PPARβ/δ) and inhibition of cyclooxygenase-2 (COX2) activity by nonsteroidal anti-inflammatory drugs (NSAID) can both attenuate skin tumorigenesis. The present study examined the hypothesis that combining ligand activation of PPARβ/δ with inhibition of COX2 activity will increase the efficacy of chemoprevention of chemically in...

In 2002 and 2007 the European Medicines Agency (EMA) examined the signals of a greater risk of hepatopathies related to nimesulide use. In 2007 restrictive actions were adopted in Europe. Moreover, EMA initiated a new referral in February 2010. The objective of this paper is to evaluate the effects of the 2007 regulatory measures concerning nimesulide and to estimate the potential effect of fur...

Several studies point to an important function of cyclooxygenase (COX) and prostaglandin signaling in models of synaptic plasticity which is associated with N-methyl-D-aspartate receptors (NMDARs). Cyclooxygenase gene is suggested to be an immediate early gene that is tightly regulated in neurons by NMDA dependent synaptic activity. Nonsteroid Antiinflammatory Drugs (NSAIDs) exert their antiinf...

In vitro dissolution profiles are investigated to predict the behavior of drug in body and establish its effectiveness. The choice medium conditions depends on class BSC active substance or substances that part drug. this work, nimesulide was chosen as a model substance, which is sparingly soluble II BSC, when bioavailability limited only by dissolution.
 aim work optimal for determining N...

Abstract Adsorptive Stripping Voltammetric method for Nimesulide (NIM) determination was developed. As a working electrode, glassy carbon electrode (GCE) modified with black and Nafion (CB-Nafion GCE) used. All measurements were carried out in 0.1 M acetate buffer (pH 4.6). Conducted experiments allowed to optimize differential pulse voltammetry (DPV) instrumental parameters: sampling waiting t...