NERIDERM Cream / Ointment Ref.[8329] Active ingredients: Diflucortolone

In order to exert its antiproliferative and anti-inflammatory effects, diflucortolone valerate has to diffuse from the preparation into the living epidermis and into the upper dermis. In vitro penetration studies showed that diflucortolone valerate penetrates human skin rapidly. After application to damaged skin – as a model for diseased skin – the local corticosteroid levels were distinctly higher than in the intact skin.

Once in the skin diflucortolone valerate is partly hydrolysed into the similarly effective diflucortolone. Part of the corticosteroid applied to the skin is percutaneously absorbed, distributed into organs and tissues, metabolised and finally excreted. The extent of percutaneous absorption and the resulting systemic load depend on a series of factors: the vehicle, the exposure conditions (skin area dose, treatment area, duration of treatment), condition of treatment (open/occlusive), the status of the penetration barrier and the localisation of the treated area on the body.

After application of the radiolabelled ointment onto an intact and a “stripped” area of skin on the back of 3 volunteers, 0.7% of the dose was percutaneously absorbed during a 7 hour exposure period.

Following percutaneous absorption diflucortolone valerate is hydrolysed very rapidly into diflucortolone and the respective fatty acid. 11-keto- diflucortolone and two further metabolites have been found in the plasma in addition to diflucortolone. Diflucortolone is eliminated from the plasma with a half-life of approximately 4-5 hours, all metabolites together with a half-life of approximately 9 hours (results after i.v. administration). The metabolites are excreted with urine and faeces in a ratio of 75:25.

There are no preclinical safety data which could be of relevance to the prescriber and which are not already included in other relevant sections of the SPC.