Diflucortolone

Diflucortolone is a steroid hormone from the group of glucocorticoids, which is used for external application in the symptomatic treatment of inflammatory skin diseases (e.g. neurodermatitis, eczema of the face, psoriasis) or as an additional therapy for dermatomycoses. However, the corticosteroid must not be used for the treatment of viral, bacterial or parasitic diseases of the skin.
Im Handel wird der Wirkstoff als Creme oder Salbe vertrieben.

Pharmacodynamics

The anti-inflammatory, antipruritic and vasoconstrictor effects are due to the constriction of blood vessels, which reduces the release of inflammatory substances. This effect causes soothing of the skin and reduces mucosal swelling and mucus secretion.
Diflucortolon bindet in der Zelle an Glukokortikoid-Rezeptoren, gelangt als Komplex in den Zellkern und hemmt dort die Bildung verschiedener Zytokine (Proteine). Dadurch wird die Synthese der Arachidonsäure (Fettsäure) blockiert, wodurch wiederum die Bildung, Freisetzung und Aktivität von Entzündungsmediatoren verhindert wird.

Pharmacokinetics

Absorption is percutaneous, i.e. through the skin, and bioavailability depends on the formulation of the drug, as well as the dose, treatment duration, condition and range. Less than 1% of the administered dose enters the bloodstream, which is subsequently distributed to various organs and tissues. Degradation occurs in the liver and is relatively rapid, as is elimination. The half-life of diflucortolone is approximately 4 to 5 hours.

Contraindications

In addition to viral and bacterial infections, diflucortolone should not be used in vaccination reactions, perioral dermatitis (erysipelas), rosacea, shingles, and chronic psoriasis, as well as during pregnancy and lactation.

Side effects

Adverse side effects include:

• Allergic skin reactions (itching, dry/red/burning skin, rashes).
• Thinning (atrophy) of the skin
• decreased pigmentation of the skin
• Steroid acne
• Ecchymosis (patchy bleeding under the skin)
• Excessive hair growth
• Inflammation of hair follicles

Toxicological data

LD50 (mouse, oral): >4000 mg/kg
LD50 (Maus, subkutan): 180 mg/kg
LD50 (Maus, intraperitoneal): 450 mg/kg