Methylprednisolone aceponate

ATC CodeD07AC14
CAS number86401-95-8
PUB number63019
Drugbank IDDB14643
Empirical formulaC27H36O7
Molar mass (g·mol−1)472,578
Physical statesolid

Basics

Methylprednisolone aceponate is a topical glucocorticoid and has anti-inflammatory, anti-allergic and suppressive effects on the body's immune system. It is used for the topical local treatment of skin diseases such as chronic inflammatory dermatitis, allergic contact dermatitis and other inflammations of the upper skin layer.

The active ingredient is marketed under the name Advantan® as a cream or ointment.

Pharmacology

Pharmacodynamics

After penetration into the skin, the active ingredient is metabolized by esterases (enzymes) to active intermediates. Like other topical glucocorticoids, methylpredisolone aceponate binds to intracellular glucocorticoid receptors inside the cell. The receptor-drug complex exerts an influence on DNA, causing the synthesis of anti-inflammatory proteins. This allows the antipruritic, immunosuppressive, and anti-inflammatory/allergic effects to develop.

Pharmacokinetics

The decisive factor for the absorption of topical glucocorticoids is skin age. In children under 12 months of age, it must be noted that the barrier function of the skin has not yet fully developed. In the elderly, glucocorticoid absorption may increase due to thinning of the skin as well as increased skin surface area due to wrinkling.

Contraindications

Methylprednisolone aceponate is contraindicated in:

  • Hypersensitivity
  • Bacterial skin diseases
  • viral diseases of the skin
  • Rosacea
  • Perioral dermatitis
  • Skin ulcers
  • Acne
  • Athrophic skin diseases
  • Postvaccinal skin reactions in the treatment area

Toxicity

Side effects

A burning or itching sensation at the application site is the most common adverse side effect. In addition, athrophies (thinning of the skin) may occur, as well as skin striae and visible dilatation of small blood vessels of the skin.

Toxicological data

LD50 (rat, oral): > 2 g/kg
LD50 (Ratte, subkutan): > 3 g/kg

Markus Falkenstätter, BSc

Markus Falkenstätter, BSc

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer



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