Methylprednisolone aceponate (Ointment) Instructions for Use

Marketing Authorization Holder

Velpharm, LLC (Russia)

Manufactured By

Sintez PJSC (Russia)

ATC Code

D07AC14 (Methylprednisolone aceponate)

Active Substance

Methylprednisolone aceponate (Rec.INN registered by WHO)

Dosage Form

Methylprednisolone aceponate

Ointment for external use 0.1%: tubes 5 g, 10 g, 15 g, 20 g, 30 g, or 50 g

Dosage Form, Packaging, and Composition

Ointment for external use 0.1% white or almost white.

Excipients: medical petrolatum – 18 g, white beeswax – 3 g, liquid paraffin (vaseline oil) – 10 g, cetomacrogol 1000 – 3g, emulsifier “Lannete SX” No.1 – 7 g, purified water – up to 100 g.

5 g – tubes (1) – cardboard packs.
10 g – tubes (1) – cardboard packs.
15 g – tubes (1) – cardboard packs.
20 g – tubes (1) – cardboard packs.
30 g – tubes (1) – cardboard packs.
50 g – tubes (1) – cardboard packs.

Clinical-Pharmacological Group

Topical corticosteroids for external use

Pharmacotherapeutic Group

Topical glucocorticosteroid

Pharmacological Action

Glucocorticosteroid for external use. Suppresses the functions of leukocytes and tissue macrophages. Limits the migration of leukocytes to the area of inflammation. Impairs the ability of macrophages to phagocytose, as well as to form interleukin-1. Promotes stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the area of inflammation. Reduces capillary permeability caused by the release of histamine. Suppresses fibroblast activity and collagen formation.

Inhibits the activity of phospholipase A₂, which leads to suppression of the synthesis of prostaglandins and leukotrienes. Suppresses the release of COX (mainly COX-2), which also contributes to a decrease in prostaglandin production.

Reduces the number of circulating lymphocytes (T- and B-cells), monocytes, eosinophils and basophils due to their movement from the vascular bed into the lymphoid tissue; suppresses antibody formation.

Methylprednisolone aceponate suppresses the release of ACTH and β-lipotropin by the pituitary gland, but does not reduce the level of circulating β-endorphin. Inhibits the secretion of TSH and FSH.

When applied directly to blood vessels, it causes a vasoconstrictor effect.

When used externally and locally, the therapeutic activity of methylprednisolone is due to its anti-inflammatory, anti-allergic and anti-exudative (due to the vasoconstrictor effect) action.

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, indicating its “bioactivation” in the skin.

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).

Percutaneous absorption in children and adults with atopic dermatitis (neurodermatitis) and psoriasis is no more than 2.5%.

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

The 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

Exogenous eczema (atopic dermatitis, neurodermatitis), contact eczema, degenerative, dyshidrotic eczema, as well as eczema in children.

ICD codes

Dosage Regimen

Apply a thin layer of ointment to the affected skin areasonce daily.

Use in adults and children aged 4 months and older.

Limit the duration of treatment to a maximum of 6 weeks in adults.

Limit the duration of treatment to a maximum of 3 weeks in children.

Do not apply to large surface areas of the body for prolonged periods.

Avoid the use of occlusive dressings, as this increases systemic absorption.

Discontinue treatment once clinical control is achieved.

For pediatric patients, use the minimum effective dose and shortest duration necessary.

Do not use in children under 4 months of age.

Consult a physician if no improvement is observed within one week.

Adverse Reactions

Immune system disorders frequency unknown – hypersensitivity reactions.

Skin and subcutaneous tissue disorders uncommon – skin atrophy, ecchymosis, impetigo, oily skin; frequency unknown – acne, telangiectasia, striae, perioral dermatitis, skin discoloration, allergic skin reactions.

Local reactions at the application site common – itching, burning; uncommon – erythema, dry skin, vesicular rash formation, irritation, dermatitis; frequency unknown – folliculitis.

Other frequency unknown – hypertrichosis, peripheral edema. Systemic effects due to the absorption of methylprednisolone aceponate (resorptive effects) are possible.

Contraindications

Hypersensitivity to methylprednisolone aceponate; post-vaccination period, bacterial, viral (chickenpox, shingles) and fungal skin diseases (pyoderma, mycosis), skin tuberculosis, eyelid dermatitis, impaired skin integrity (ulcers, wounds), syphilitic skin lesions, skin tumors, rosacea, acne vulgaris, perioral dermatitis, children under 4 months of age.

Use in Pregnancy and Lactation

During pregnancy and lactation (breastfeeding), use only after consultation with a doctor, in cases where the intended benefit to the mother outweighs the potential risk to the fetus or child. Should not be used in the first trimester of pregnancy.

Long-term treatment, use of high doses, application to large areas of skin, and the use of occlusive dressings should be avoided.

Pediatric Use

Contraindicated for use in children under 4 months of age.

When used in children aged from 4 months to 18 years, it is necessary to limit the total duration of treatment and exclude measures leading to increased resorption and absorption (warming, fixing and occlusive dressings).

Special Precautions

For bacterial dermatoses or dermatomycosis, simultaneous therapy with antibacterial or antifungal agents is necessary. Physiotherapy should not be performed simultaneously.

Avoid getting the product into the eyes, open wounds and mucous membranes. If the product gets into the eyes or on the mucous membranes, it is recommended to rinse them with plenty of water.

As with the use of systemic glucocorticosteroids, glaucoma may develop after external use of the product (for example, when using high doses, or very long-term use of occlusive dressings, or application to the skin around the eyes).

The use of the product on large areas of the skin and/or its long-term use, application in large quantities or under occlusive dressings should be avoided, as this significantly increases the risk of side effects. When using the product on large areas of the skin, the period of application should be as short as possible due to the possibility of systemic side effects.

Use in pediatrics

Methylprednisolone aceponate can be used in children from the age of 4 months. It must be taken into account that in young children, skin folds, diapers and nappies can have an effect similar to that of an occlusive dressing and increase the systemic resorption of methylprednisolone aceponate. In addition, children may have a greater degree of systemic resorption due to the ratio between skin surface area and body weight, as well as due to insufficient skin maturity. Children are at greater risk of suppression of the hypothalamic-pituitary-adrenal system function and the development of Cushing’s syndrome when using any topical glucocorticosteroids; long-term treatment of children with glucocorticosteroids can lead to disturbances in their growth and development. Children should receive the minimum dose of methylprednisolone aceponate sufficient to achieve a therapeutic effect. Treatment should be carried out under medical supervision.

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.