Prednicarbate

Absorption

Absorbed systemically across the stratum corneum.

Description

Prednicarbate is a potent topical antiinflammatory agent with minimal systemic effects. It is useful in the treatment of cutaneous inflammatory disorders such as eczema and psoriasis.

Description

Prednicarbate is a synthetic corticosteroid and a derivative of prednisolone . It has anti-inflammatory activity comparable to that of desoximetasone in various murine models when administered topically but lacks activity when administered subcutaneously. Topical administration of prednicarbate (2 drops of a 0.1% solution per day) induces wound healing in hairless mice. Formulations containing prednicarbate have been used to treat chronic hand eczema.

Chemical properties

White or almost white, crystalline powder.

Originator

Hoechst AG (W. Germany)

The Uses of Prednicarbate

Topical anti-inflammatory agent. Glucocorticoid.
Prednicarbate (Dermatop E) is a synthetic nonfluorinated topical corticosteroid.

Indications

For the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.

Background

Prednicarbate is a relatively new topical corticosteroid drug that displays a similar potency as hydrocortisone. It is used in the treatment of inflammatory skin diseases, such as atopic dermatitis. It has a favorable benefit-risk ratio, with an inflammatory action similar to that of a medium potency corticosteroid, but with a low potential to cause skin atrophy. The anti-inflammation action of corticosteroids is associated with the inhibition of the interleukin 1-alpha cytokine within keratinocytes. IL-1a is also found in fibroblasts, where it is responsible for proliferation, collagenase induction and IL-6 synthesis, which are related to skin thickness.

Indications

Prednicarbate (Dermatop E) is a synthetic nonfluorinated topical corticosteroid.

Definition

ChEBI: Prednicarbate is a corticosteroid hormone.

brand name

Dermatop (Sanofi Aventis).

General Description

Prednicarbate, 17-[(ethoxycarbonyl)oxy]-11β-hydroxy-21-(1-oxopropoxy)pregna-1,4-diene-3,20-dione, is a prednisolone derivative with a C21 propionateester and a C17 ethyl carbonate group. It is availablefor use only in a 0.1% topical cream. Prednicarbate is amedium-potency GC.

Pharmacokinetics

Corticosteroids diffuse across cell membranes and complex with specific cytoplasmic receptors. These complexes then enter the cell nucleus, bind to DNA (chromatin), and stimulate transcription of messenger RNA (mRNA) and subsequent protein synthesis of various inhibitory enzymes responsible for the anti-inflammatory effects of topical corticosteroids. These anti-inflammatory effects include inhibition of early processes such as edema, fibrin deposition, capillary dilatation, movement of phagocytes into the area, and phagocytic activities. Later processes, such as capillary production, collagen deposition, and keloid formation also are inhibited by corticosteroids.

Metabolism

Primarily in skin