Fluocortolone

Fluocortolone pivalate

Fluocortolone pivalate inhibits inflammatory and allergic skin reactions, and alleviates subjective complaints such as pruritus, smarting, and pain. The substance reduces dilatation of the capillaries, oedema of the interstitial cells and infiltration of the tissues. Capillary multiplication is inhibited.

After rectal application of fluocortolone in healthy male volunteers, a maximum of 15% of the dose of fluocortolone pivalate was systemically absorbed (radiolabelled active substances).

Acute toxicity

Based on the results of conventional studies into the acute toxicity, no specific risk to humans is to be expected after the therapeutic use.

Reproductive toxicity

Based on embryotoxicity studies with fluocortolone/fluocortolone hexanoate, embryotoxic/teratogenic effects in humans are not expected to occur with the use of fluocortolone.

There are hints from animal experiments that administration of systemic glucocorticoids during pregnancy might contribute to postnatal effects such as cardiovascular and/or metabolic diseases, and to permanent changes in density of glucocorticoid receptors, in neurotransmitter turnover and in behaviour in the offspring.

In general, glucocorticosteroids lead to embryotoxic and teratogenic effects (e.g. oral clefts, skeletal malformations, intrauterine growth retardations, embryolethality) in the appropriate test systems. In view of these findings, particular care should be taken when prescribing fluocortolone during pregnancy.

Fertility

The potential impact of fluocortolone on fertility has not been investigated.

No investigation on the potential effects of fluocortolone or its esters on fertility has been performed in animals.

Genotoxicity and carcinogenicity

In-vitro and in-vivo studies gave no relevant indication on a genotoxic potential of fluocortolone.

Specific tumorigenicity studies with fluocortolone/fluocortolone pivalate have not been carried out. On the basis of the pharmacodynamic mode of action, the lack of evidence of a genotoxic potential, the chemical structure and the results of chronic toxicity studies, there is no suspicion of a tumorigenic potential for fluocortolone pivalate.

Local tolerance

Investigations into the local tolerance on the skin and the mucosa did not reveal any changes beyond those topical side-effects known for glucocorticoids.

Experimental investigations for detection of possible sensitizing effects have not been carried out with the active substances of fluocortolone. Data in the literature suggest that the active substances as well as the components of the formulation base could be responsible for the allergic skin reactions observed only sporadically following use of fluocortolone. However, fluocortolone is only expected to provoke contact allergies in rare cases.