Comfoderm ointment 0,1%, 15g

Composition

>of 100 g of ointment contains: Active ingredient:  methylprednisolone aceponate in terms of 100% substance-0.1 g; Excipients:  vaseline-44.7 g; liquid paraffin-34.1 g; castor oil – 3.2 g;white beeswax-17.9 g

Pharmacological action

The active component of Comfoderm® – methylprednisolone aceponate-is a non-halogenated steroid.

Pharmacodynamics

When applied externally, methylprednisolone aceponate suppresses inflammatory and allergic skin reactions, as well as reactions associated with increased proliferation, which leads to a decrease in objective symptoms of inflammation (erythema, edema, wetness, etc. ) and subjective sensations (itching, irritation, pain, etc. ).

When using methylprednisolone aceponate externally at the recommended dose, the systemic effect is minimal in both humans and animals. After repeated application of the drug on large surfaces (40-60% of the skin surface), as well as application under an occlusive dressing, there are no violations of adrenal functions: the level of cortisol in plasma and its circadian rhythm remain within normal limits, and there is no decrease in the level of cortisol in the daily urine.

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

Macrocortin inhibits the release of arachidonic acid and thus the formation of inflammatory mediators such as prostaglandins and leukotrienes. Inhibition of the synthesis of vasodilating prostaglandites by glucocorticosteroids and potentiation of the vasoconstrictor effect of epinephrine 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 glucocorticoid receptors in the skin, which indicates the presence of its” bioactivation ” in the skin.

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

After entering the systemic circulation,6α-methylprednisolone-17-propionate rapidly conjugates with glucuronic acid and, thus, in the form of 6α-methylprednisolone-17-propionate glucuronide is inactivated. 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 accumulate in the body

Indications

Inflammatory skin diseases that are sensitive to topical corticosteroid therapy:

• atopic dermatitis, neurodermatitis, children’s eczema;
• true eczema;
• microbial eczema;
• occupational eczema;
• simple contact dermatitis;
• allergic (contact) dermatitis;
• dyshidrotic eczema.

Contraindications

• Tuberculosis or syphilitic processes in the area of application of the drug;
• viral diseases (for example, chickenpox, shingles), in the area of application of the drug;
• rosacea, perioral dermatitis in the area of application of the drug;
• children under 4 months of age;
• skin areas with reactions to vaccination;
• hypersensitivity to the components of the drug.

Side effects

the incidence of side effects is classified in accordance with the recommendations of the world health organization (who): very often (≥ 10%), often (≥ 1%, < 10%), infrequently (≥0.1%, the < 1%), rarely (≥0.01%, for <0,1%), very rare (<0,01%), frequency unknown (to estimate the frequency of occurrence is not possible). Skin and subcutaneous tissue disorders: rarely-perioral dermatitis, skin depigmentation, allergic reactions to the components of the drug; frequency unknown-skin atrophy, telangiectasia, striae, acne-like skin changes ( when using the drug for more than 4 weeks and/or on an area of 10% or more of the body surface). General disorders and disorders at the injection site: rarely-folliculitis, hypertrichosis; very rarely-itching, burning, erythema, vesicular rash; frequency unknown-systemic effects due to absorption of glucocorticosteroid ( when using the drug for more than 4 weeks and/or on an area of 10% or more of the body surface). If any of the side effects listed in the instructions get worse, or any other side effects that are not listed in the instructions are noted, you should immediately inform your doctor.

Interaction

Not studied.

How to take, course of use and dosage

Externally. Adults and children from 4 months of age. The drug is applied 1 time a day in a thin layer on the affected areas of the skin. As a general rule, the duration of continuous daily treatment with Comfoderm® should not exceed 12 weeks for adults and 4 weeks for children. For the treatment of long-term chronic inflammatory skin processes with very dry skin, an anhydrous dosage form is necessary. The occlusal effect of Comfoderm ® provides a pronounced therapeutic effect even with significant lichenification and infiltration.

Overdose

When studying the acute toxicity of methylprednisolone aceponate, there was no risk of acute intoxication with excessive single skin application (applying the drug over a large area under conditions favorable for absorption) or unintentional oral use. Skin atrophy (thinning of the skin, telangiectasia, striae) may develop if glucocorticosteroids are used for external use for too long and/or intensively. If atrophy occurs, the drug should be discontinued.

Special instructions

In the presence of bacterial complications and/ or dermatomycosis, specific antibacterial and / or antimycotic treatment should be performed in addition to therapy with Comfoderm®. Avoid contact with the eyes. As with the use of systemic glucocorticosteroids, glaucoma may develop after external use of glucocorticosteroids (for example, with high doses or very prolonged use of occlusive dressings or application to the skin around the eyes).

Storage conditions

At a temperature not exceeding 25°C. Keep out of reach of children.

Shelf life

2 years

Active ingredient

Methylprednisolone aceponate

Dosage form

ointment