AULIN Gel Ref.[7325] Active ingredients: Nimesulide

When Nimesulide 3% w/w gel is applied topically, plasma concentrations of nimesulide are very low in comparison with those achieved following oral intake. After a single application of 200mg of nimesulide, in the gel form, the highest plasma level of 9.77 ng/ml was noted after 24 hours. No trace of the main metabolite 4-hydroxy-nimesulide, was detected. At steady-state (day 8) peak plasma concentrations were higher (37.25 ± 13.25 ng/ml) but almost 100 times lower than those measured following repeated oral administration.

The local tolerance and the irritation and sensitisation potential of Nimesulide 3% w/w gel have been tested in several recognised animal models. The results of these studies indicate that Nimesulide 3% w/w gel is well tolerated.

Preclinical data for systemically administered nimesulide reveal no special hazards for humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity and carcinogenic potential. In repeated dose toxicity studies, nimesulide showed gastrointestinal, renal and hepatic toxicity. In reproductive toxicity studies, embryotoxic and teratogenic effects (skeletal malformations, dilatation of cerebral ventricles) were observed in rabbits, but not in rats, at maternally non-toxic dose levels. In rats, increased mortality of offspring was observed in the early postnatal period and nimesulide showed adverse effects on fertility.