Advantan^® (Ointment, Cream) Instructions for Use

ATC Code

D07AC14 (Methylprednisolone aceponate)

Active Substance

Methylprednisolone aceponate (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Topical corticosteroids for external use

Pharmacotherapeutic Group

Topical glucocorticosteroid

Pharmacological Action

When applied topically, it suppresses inflammatory and allergic skin reactions, as well as reactions associated with enhanced proliferation, leading to a reduction in objective symptoms of inflammation (including erythema, edema, weeping, etc.) and subjective sensations (including itching, irritation, pain, etc.).

When methylprednisolone aceponate is applied topically at the recommended dose, the systemic effect is minimal in both humans and animals. After multiple applications to large surfaces (40-60% of the skin surface), as well as when used under an occlusive dressing, no impairment of adrenal function was noted: plasma cortisol levels and its circadian rhythm remain within the normal range, and there is no decrease in urinary cortisol levels.

During clinical studies with the use of this agent for up to 12 weeks in adults and up to 4 weeks in children (including young children), no development of skin atrophy, telangiectasias, striae, or acneiform eruptions was detected.

Methylprednisolone aceponate (especially its main metabolite – 6α-methylprednisolone-17-propionate) binds to intracellular glucocorticoid receptors. The steroid-receptor complex binds to specific regions of DNA in immune response cells, thus causing a series of biological effects.

In particular, the 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, thereby, the formation of inflammatory mediators such as prostaglandins and leukotrienes.

Inhibition of the synthesis of vasodilating prostaglandins by glucocorticosteroids and potentiation of the vasoconstrictive action of adrenaline leads to a vasoconstrictor effect.

Pharmacokinetics

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

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

Metabolites of methylprednisolone aceponate are eliminated mainly by the kidneys, T_1/2 is about 16 hours.

Methylprednisolone aceponate and its metabolites do not accumulate in the body.

Indications

Inflammatory skin diseases responsive to therapy with topical glucocorticosteroids

• Atopic dermatitis, neurodermatitis, infantile eczema;
• True eczema;
• Microbial eczema;
• Occupational eczema;
• Dyshidrotic eczema;
• Simple contact dermatitis;
• Allergic (contact) dermatitis;
• Photodermatitis, sunburn;
• Seborrheic dermatitis/eczema.

ICD codes

Dosage Regimen

Ointment, Cream

Externally.

Adults and children from 4 months of age apply the preparation once daily in a thin layer to the affected areas of the skin.

For subacute and acute inflammation without pronounced weeping, a dosage form with a low fat content and high water content is recommended.

For subacute or chronic course of inflammatory skin diseases not accompanied by weeping, a dosage form with a balanced ratio of fat and water is recommended.

For the treatment of long-term chronic inflammatory skin processes with very dry skin, an anhydrous dosage form with a high fat content is recommended.

Methylprednisolone aceponate should be used in the dosage form appropriate for the indication.

Adverse Reactions

Very rarely (less than 0.01% of cases): local reactions such as itching, burning, erythema, formation of a vesicular rash. In case of application for more than 4 weeks and/or on an area of 10% or more of the body surface, the following reactions may occur: skin atrophy, telangiectasias, striae, acneiform skin changes, systemic effects due to corticosteroid absorption.

In rare cases (0.01-0.1%): folliculitis, hypertrichosis, perioral dermatitis, skin depigmentation, allergic reactions to one of the components of the used preparation.

Contraindications

• Tuberculous or syphilitic processes in the area of application of the used preparation;
• Viral diseases in the area of application of the used preparation (for example, chickenpox, herpes zoster);
• Rosacea, perioral dermatitis in the area of application of the used preparation;
• Areas of the skin with manifestations of a reaction to vaccination;
• Children under 4 months of age;
• Hypersensitivity to the components of the used preparation.

Use in Pregnancy and Lactation

If use during pregnancy and breastfeeding is necessary, the potential risk to the fetus and the expected therapeutic benefit for the mother should be carefully weighed. Prolonged use on large skin areas is not recommended during these periods.

Nursing mothers should not apply this agent to the mammary glands.

Pediatric Use

Contraindicated in children under 4 months of age.

When used in children, the recommended duration of treatment should not be exceeded.

Special Precautions

In the presence of bacterial complications and/or dermatomycoses, specific antibacterial or antifungal treatment should be carried out in addition to therapy with methylprednisolone aceponate.

Avoid getting the used preparation into the eyes.

As with the use of systemic corticosteroids, glaucoma may develop after topical application of glucocorticosteroids (for example, when used in high doses or for a very long time with occlusive dressings or application to the skin around the eyes).

Effect on the ability to drive vehicles and operate machinery

Not identified.

Drug Interactions

No drug interactions have been identified.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Over-the-Counter

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.