Diflucortolone

Diflucortolone
ATC Code D07AC06, D07XC04
Formula C22H28F2O4
Molar Mass (g·mol−1) 394,459
Physical State solid
Melting Point (°C) 220
Boiling Point (°C) 534
CAS Number 2607-06-9
PUB Number 11954369
Drugbank ID DB09095
Solubility practically insoluble in water

Basics

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.

Pharmacology

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.

Toxicity

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

Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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The contents shown do not replace the original package insert of the medicinal product, especially with regard to dosage and effect of the individual products. We cannot assume any liability for the correctness of the data, as the data was partly converted automatically. A doctor should always be consulted for diagnoses and other health questions. Further information on this topic can be found here.