Diflucortolone
Diflucortolone Uses, Dosage, Side Effects, Food Interaction and all others data.
Diflucortolone is a potent topical corticosteroid. It is commonly used in dermatology for the reduction of inflammation and itching. It was submitted to the FDA in July 1984 by the pharmaceutical company Schering AG.
Diflucortolone is a steroid with the properties of being an anti-inflammatory, antipruritic and vasoconstrictive. Its activity causes the vasoconstriction of the blood vessels and thus a decrease in the release of inflammatory substances. These actions produce the effect of skin soothed and elimination of the symptoms.
| Trade Name | Diflucortolone |
| Generic | Difluocortolone |
| Difluocortolone Other Names | Diflucortolona, Diflucortolone, Diflucortolonum |
| Type | |
| Formula | C22H28F2O4 |
| Weight | Average: 394.459 Monoisotopic: 394.195565708 |
| Protein binding | Diflucortolone gets rapidly metabolized and eliminated, thus there is a very limited circulation of the unchanged drug in blood plasma. Actually, the percutaneous absorption is so low that less than 1% of the admministered dose reaches systemyc circulation. |
| Groups | Approved, Investigational, Withdrawn |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Diflucortolone is a topical corticosteroid used for the symptomatic treatment of inflammatory skin disorders like eczema, seborrheic eczema, lichen planus and psoriasis.
Diflucortolone is used as a topical treatment of the symptoms of inflammatory skin disorders like eczema, seborrheic eczema, lichen planus and psoriasis. All these disorders present as a common characteristic the occurrence of symptoms as itching, swelling, redness and scaling.
Diflucortolone is also used to associated treatment for these conditions: Dermatitis, Gingivitis, Infectious Periodontal Diseases, Periodontitis, Stomatitis, Stomatitis, Aphthous, Corticosteroid-responsive dermatoses, Eczematous rash, Oral lesions
How Diflucortolone works
Diflucortolone performs its action by the induction of lipocortins which are phospholipase A2 inhibitory proteins and sequentially inhibiting the release of arachidonic acid. The absence of arachidonic acid translates to the inhibition of the formation, release and activity of endogenous chemical inflammatory mediators. Another mechanism of action is the transrepression in which diflucortolone binds to the glucocorticoid receptor which induces its migration to the nucleus where it stimulates the transcription of anti-inflammatory genes like tyrosine aminotransferase, phophoenolpyruvate carboxykinase, IL-10, etc. and suppress the expression of proinflammatory genes like cytokines, growth factors, adhesion molecules, etc.
Toxicity
Diflucortolone can cause skin irritation, vesicles or red patches on the skin.
Food Interaction
No interactions found.Volume of Distribution
Less of 1% of the administered dose reaches systemic circulation. In order to exert its functions, diflucortolone has to distribute into the living epidermis and upper dermis. Reports have shown that the skin absorption of diflucortolone is rapid where the absorption gets significantly increased in damaged skin. Diflucortolone gets percutaneously absorbed and distributed into organs and tissues where it will be metabolized. When diflucortolone in an ointment form is applied in healthy skin 0.7% of the administered dose is percutaneously absorbed after a 7-hour exposure.
Elimination Route
The absorption of diflucortolone is made mainly percutaneously but it may be absorbed systemically. The absorption and bioavailability of diflucortolone will be related to the type of formulation found in the medication. The percutaneous absorption depends on the vehicle, dose, treatment area, duration of treatment, the condition of treatment, the status of penetration barrier and localization of treated area in the body. Thus, rectal administration of diflucortolone produces a slow and low absorption with an AUC, Cmax and Tmax of 10.8 ng h/ml, 0.75 ng/ml and 4.7 h, respectively.
Half Life
The half-life of diflucortolone is approximately in the range of 4 to 5 h while the half-life of 3H-diflucortolone valerate is approximately 9 h.
Clearance
Diflucortolone gets rapidly eliminated and the metabolites produced are the latest in getting eliminated from the body.
Elimination Route
The elimination of diflucortolone is rapid and complete. After 24 hours of dose administration 56% of the dose was eliminated by the urine and after 7 days 98% of the administered dose was recovered. The excretion of diflucortolone is subdivided in urine which accounts for 75% of the administered dose and in feces that accounts for the other 25% of the administered dose. From the eliminated dose, 30% was formed by unconjugated steroids, 20% as steroid-glucuronides and 10% as steroid-sulfates.
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