Advantan ointment for external use 0.1%, 15g

Inflammatory skin diseases sensitive to topical GCS therapy:

• atopic dermatitis, neurodermatitis, childhood eczema;

• true eczema;

• microbial eczema;

• professional eczema;

• dyshidrotic eczema;

• simple contact dermatitis;

• allergic (contact) dermatitis.

Outwardly.

For adults and children from 4 months, the drug is applied 1 time / day with a thin layer to the affected skin.

Continuous daily use of Advantan in the form of a cream, ointment or oily ointment should not exceed 12 weeks for adults, 4 weeks for children. The course of treatment with Advantan in the form of an emulsion should usually not exceed 2 weeks.

The ointment is a dosage form with a balanced ratio of fat and water, therefore it is recommended for subacute or chronic inflammatory skin diseases that are not accompanied by oozing. The ointment has a therapeutic effect, also helping to eliminate dry skin and restore its normal oily content.

Active ingredients:

methylprednisolone aceponate - 1 mg

Excipients:

white soft paraffin - 350 mg, liquid paraffin - 239 mg, white beeswax - 40 mg, emulsifier Dehimuls E - 70 mg, purified water - 300 mg.

• Tuberculous or syphilitic processes in the area of ??application of the drug;

• viral diseases in the area of ??application of the drug (for example, with chickenpox, shingles);

• rosacea, perioral dermatitis in the area of ??application of the drug;

• areas of the skin with manifestations of a reaction to vaccination;

• children's age up to 4 months;

• hypersensitivity to the components of the drug.

Ointment for external use is white or slightly yellowish, homogeneous, opaque.

Ingredient: 1 g

Active ingredients:

methylprednisolone aceponate - 1 mg

Excipients:

white soft paraffin - 350 mg, liquid paraffin - 239 mg, white beeswax - 40 mg, emulsifier Dehimuls E - 70 mg, purified water - 300 mg.

Clinical and pharmacological group: GCS for external use

Pharmaco-therapeutic group: Topical glucocorticosteroid

pharmachologic effect

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

When methylprednisolone aceponate is used externally at the recommended dose, the systemic effect is minimally expressed in both humans and animals. After repeated application of Advantan to large surfaces (40-60% of the skin surface), as well as when applied under an occlusive dressing, there are no adrenal dysfunctions: the level of cortisol in the blood plasma and its circadian rhythm remain within normal limits, the level of cortisol in daily urine does not decrease. happens.

In the course of clinical studies with the use of Advantan for up to 12 weeks in adults and up to 4 weeks in children (including young children), there was no development of skin atrophy, telangiectasias, stretch marks and acne-like rashes.

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

In particular, the binding of the steroid-receptor complex to the DNA of cells of the immune response leads to the induction of the synthesis of macrocortin. Macrocortin inhibits the release of arachidonic acid and thus the formation of inflammatory mediators such as prostaglandins and leukotrienes.

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

Pharmacokinetics

Suction

The degree of percutaneous absorption depends on the condition of the skin, the dosage form and the route of administration (with or without an occlusive dressing). When using ointment, cream or fatty ointment, percutaneous absorption in children and adults with atopic dermatitis (neurodermatitis) and psoriasis was no more than 2.5%, which is only slightly higher compared to healthy volunteers (0.5-1.5%).

When using the drug in the form of an emulsion, the intensity of absorption through the skin with artificial inflammation was very low (0.27%), which is only slightly higher than through healthy skin (0.17%). In the case of whole body treatment (eg, sunburn), the systemic dose is about 4 ?g / kg bw / day, which excludes systemic effects.

Metabolism and excretion

Methylprednisolone aceponate is hydrolyzed in the epidermis and dermis. The main and most active metabolite is 6?-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.

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

Metabolites of methylprednisolone aceponate are eliminated mainly by the kidneys, T1 / 2 - about 16 hours.

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

Indications

Ointment, cream, oily ointment

Inflammatory skin diseases sensitive to topical GCS therapy:

• atopic dermatitis, neurodermatitis, childhood eczema;

• true eczema;

• microbial eczema;

• professional eczema;

• dyshidrotic eczema;

• simple contact dermatitis;

• allergic (contact) dermatitis.

Emulsion

Inflammatory skin diseases sensitive to topical GCS therapy:

• atopic dermatitis, neurodermatitis, childhood eczema;

• simple contact dermatitis;

• allergic (contact) dermatitis;

• true eczema;

• seborrheic dermatitis / eczema;

• microbial eczema;

• photodermatitis, sunburn.

Dosage regimen

Outwardly.

For adults and children from 4 months, the drug is applied 1 time / day with a thin layer to the affected skin.

Continuous daily use of Advantan in the form of a cream, ointment or oily ointment should not exceed 12 weeks for adults, 4 weeks for children. The course of treatment with Advantan in the form of an emulsion should usually not exceed 2 weeks.

The cream is a dosage form with a low fat content and a high water content, therefore it is recommended for subacute and acute inflammation without pronounced wetness. The cream provides the elimination of the inflammatory process both on smooth skin and on the scalp, incl. on oily skin.

The ointment is a dosage form with a balanced ratio of fat and water, therefore it is recommended for subacute or chronic inflammatory skin diseases that are not accompanied by oozing. The ointment has a therapeutic effect, also helping to eliminate dry skin and restore its normal oily content.

Fatty ointment is an anhydrous dosage form, therefore it is recommended for the treatment of long-term chronic inflammatory skin processes with very dry skin. The occlusive effect of the oily ointment provides a pronounced therapeutic effect even with significant lichenification and infiltration.

The emulsion is applied in a thin layer to the affected skin, rubbing lightly. For sunburn, the emulsion is used 1-2 times / day. If the skin dries excessively when using the emulsion, it is necessary to switch to the dosage form of the drug AdvantanЃ with a higher fat content (ointment or fatty ointment).

Side effect

The drug is usually well tolerated.

Very rarely (less than 0.01% of cases), local reactions can occur, such as itching, burning, erythema, and the formation of a vesicular rash. If the drug is used 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, telangiectasia, striae, acneform skin changes, systemic effects due to absorption of a corticosteroid. In clinical trials, none of the above side effects were observed when using the drug AdvantanЃ up to 12 weeks in adults and up to 4 weeks in children.

In rare cases (0.01-0.1%), folliculitis, hypertrichosis, perioral dermatitis, skin depigmentation, allergic reactions to one of the components of the drug can be observed.

Contraindications for use

• tuberculous or syphilitic processes in the area of ??application of the drug;

• viral diseases in the area of ??application of the drug (for example, with chickenpox, shingles);

• rosacea, perioral dermatitis in the area of ??application of the drug;

• areas of the skin with manifestations of a reaction to vaccination;

• children's age up to 4 months;

• hypersensitivity to the components of the drug.

Application during pregnancy and lactation

If it is necessary to use the drug AdvantanЃ during pregnancy and lactation, the potential risk to the fetus and the expected benefit of therapy for the mother should be carefully weighed. During these periods, long-term use of the drug on extensive skin surfaces is not recommended.

Breastfeeding mothers should not apply the drug to their breasts.

Application in children

Continuous daily use of Advantan in the form of a cream, ointment or oily ointment for adults is no more than 12 weeks, for children - no more than 4 weeks.

Contraindicated in children under 4 months of age.

special instructions

In the presence of bacterial complications and / or dermatomycosis, in addition to therapy with AdvantanЃ, it is necessary to carry out specific antibacterial or antifungal treatment.

Avoid getting the drug in the eyes.

As in the case of the use of systemic corticosteroids, after external use of GCS, glaucoma may develop (for example, with the use of large doses or very long-term use of occlusive dressings or application to the skin around the eyes).

Influence on the ability to drive vehicles and use mechanisms

Not found.

Overdose

When studying the acute toxicity of methylprednisolone aceponate, there was no risk of acute intoxication with excessive single external use (application of the drug over a large area under conditions favorable for absorption) or unintentional ingestion.

Symptoms: with excessively long and / or intensive local application of GCS, skin atrophy (thinning of the skin, telangiectasia, striae) may develop.

If atrophy develops, the drug must be canceled.

Drug interactions

Drug interaction of the drug AdvantanЃ has not been identified.