Comfoderm ointment 0.1% 15 g

The active ingredient of Comfoderm® – methylprednisolone aceponate – is a nonhalogenated steroid.

Pharmacodynamics

In external use methylprednisolone aceponate suppresses inflammatory and allergic skin reactions as well as reactions associated with increased proliferation, resulting in reduction of objective symptoms of inflammation (erythema, edema, mottling, etc.etc.) and subjective sensations (itching, irritation, pain, etc.).

When methylprednisolone aceponate is applied topically at the recommended dose, systemic effects are minimal in both humans and animals. After repeated application of the drug to large surfaces (40-60% of the skin surface), as well as after application under the occlusive dressing no adrenal disturbances are observed: the plasma cortisol level and its circadian rhythm remain within normal limits, there is no reduction of cortisol level in daily urine.

Methylprednisolone aceponate (especially its main metabolite, 6α-methylprednisolone-17-propionate) binds to intracellular glucocorticosteroid receptors. The steroid-receptor complex binds to specific DNA sites of immune response cells, thus causing a series of biological effects. In particular, binding of the steroid-receptor complex to the DNA of the immune response cells leads to induction of macrocortin synthesis.

Macrocortin inhibits the release of arachidonic acid and thus the formation of inflammatory mediators such as prostaglandins and leukotrienes. Inhibition by glucocorticosteroids of the synthesis of vasodilatory prostaglandites and potentiation of the vasoconstrictor effect of adrenaline, lead to a vasoconstrictor effect

Pharmacokinetics

Methylprednisolone aceponate is hydrolyzed in the epidermis and dermis. The main and most active metabolite is 6α-methylprednisolone-17-propionate, which has a significantly higher affinity for glucocorticosteroid receptors in the skin, indicating the presence of its “bioactivation” in the skin.

The extent of percutaneous absorption depends on the condition of the skin, the dosage form and the method of administration (with or without an occlusive dressing).

After entering the systemic bloodstream, 6α-methylprednisolone-17-propionate rapidly conjugates with glucuronic acid and is thus inactivated in the form of 6α-methylprednisolone-17-propionate glucuronide. Metabolites of methylprednisolone aceponate are eliminated mainly by the kidneys with a half-life of about 16 hours. Methylprednisolone aceponate and its metabolites do not cumulate in the body.

Indications

Inflammatory skin diseases sensitive to therapy with topical glucocorticosteroids:

Active ingredient

Composition

How to take, the dosage

Special Instructions

Contraindications

Side effects

Overdose

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