Methylprednisolone

Pharmacological properties

Methylprednisolone aceponate (6α-methylprednisolone aceponate) is a non-halogen-substituted corticosteroid synthetic molecule, which is characterized by an increased degree of dissociation during the implementation of its local and systemic effects.

The 6α-methyl group has a potentiating effect, and the lipophilic ester groups provide better penetration through the skin.

The local anti-inflammatory effect, confirmed by pharmacological and clinical-pharmacological studies, is similar to the effect of more powerful corticosteroids. The systemic effect of methylprednisolone aceponate with its local use, according to studies, is negligible.

The active substance of the drug Advantan quickly penetrates the skin, but the absorption is weak (1% of the dose for 24 hours on intact skin, without occlusion, 3% with occlusion).

Percutaneous absorption as a result of treatment with increased doses in patients with atopic dermatitis and psoriasis is 2.5% in adults and 0.5–2% in children.

On human skin, the active substance of the drug Advantan promotes the creation (by hydrolysis) of a highly active metabolite with increased affinity for intercellular receptors, is immediately inactivated by glucuronic conjugation immediately after absorption. In humans, after administration, excretion of inactive metabolites occurs in a ratio of 1: 5 between excretion in urine and feces. T_½ is about 16 hours, and binding to plasma proteins is 90%.

Any possibility of accumulation is excluded.

Indications

Advantan cream, ointment, oily ointment: atopic dermatitis (neurodermatitis, endogenous eczema), real (true) eczema; simple contact dermatitis and allergic contact dermatitis; dyshidrotic eczema, childhood eczema, seborrheic dermatitis (and eczema), including on the scalp; numular eczema, dermatoses of the scalp of an inflammatory nature, accompanied by itching.

Advantan emulsion: allergic contact dermatitis, simple contact dermatitis, real (true) eczema, including dyshidrotic form; numular (discoid) eczema, atopic dermatitis (neurodermatitis) of mild or moderate severity, seborrheic eczema with severe inflammation.

Application

Advantan cream, ointment, oily ointment. usually, the drug should be applied to the affected areas of the skin 1 time per day with a thin layer, unless the doctor has prescribed otherwise.

The formula of Advantan cream (1 g of Advantan cream contains 1 mg of methylprednisolone aceponate), due to the high water content, ensures the flow of exudate and, thus, is especially indicated for the treatment of wet eczematous elements in the acute phase; as well as patches of skin with maceration covered or uncovered by hair.

The formula of Advantan ointment (1 g of Advantan ointment contains 1 mg of methylprednisolone aceponate), which contains an anhydrous base and provides an occlusive effect, allows you to maintain skin moisture, softening the tightened skin layer and facilitating the penetration of the active substance. Therefore, Advantan ointment is especially indicated for dry forms and for the chronic stages of the disease.

The duration of use should usually not exceed 12 weeks for adults, 4 weeks for children. There is no data on the safety of Advantan in children under the age of 4 months.

When using Advantan for the treatment of children from 4 months of age, there is no need for dose adjustment.

Advantan Emulsion. The drug is applied topically 1 time per day with a thin layer on the affected areas of the skin, gently rubbing.

Usually, the duration of use in adults should not exceed 2 weeks.

In the treatment of seborrheic eczema with severe inflammation, the corresponding areas of the skin of the face should be treated for no more than 1 week.

The duration of treatment for children should be reduced to the necessary minimum.

In case of increased dryness of the skin due to the use of Advantan emulsion (which depends on the individual characteristics of the skin), it is recommended to prescribe additional neutral therapy using emollients for the skin (for example, an emulsion "water in oil" or ointment).

When using Advantan emulsion for the treatment of children aged 4 months or older, as well as children and adolescents, there is no need for dose adjustment.

Advantan emulsion is not used in children under the age of 4 months, since the safety of use is not confirmed. No relevant data.

In case of skipping the application of Advantan emulsion, do not use an increased dose of the drug at the next application. If the initial symptoms of skin disease appear again after completing the course of treatment, you should definitely consult a doctor.

Contraindications

Hypersensitivity to methylprednisolone aceponate or any other component of the drug; tuberculosis and syphilitic processes in the field of application of the drug; viral diseases (e.g. chickenpox, shingles), rosacea, perioral dermatitis, skin ulcers, acne vulgaris, atrophic dermatitis, skin reactions after inoculation at the site of application of the drug.

Side effects

During clinical trials, the most common side effects associated with the use of Advantan Cream were burning and itching at the site of application; ointments - folliculitis and itching at the site of application; emulsions - burning at the place of application.

The frequency of adverse reactions observed during clinical trials and shown in the table below is determined in accordance with the convention of the frequency of adverse effects of MedDRA: very often (1/10); often (1/100, 1/10); infrequently (1/1000, 1/100); rarely (1/10 000, 1/1000); very rarely (1/10 000); unknown (frequency cannot be determined based on available data). For coding, version 12.0 of MedDRA was used.

Advantan Cream

Advantan Ointment

Advantan Emulsion

Also, when applying Advantan cream, in rare cases, adverse reactions such as bacterial cellulite and skin infections can be detected.

As with the external use of other corticosteroids, the following side effects can be noted (frequency not determined): thinning of the skin (skin atrophy), the appearance of striae, inflammation of the hair follicles (folliculitis) at the site of application, excessive hair growth (hypertrichosis), telangiectasia, perioral dermatitis, discoloration of the skin, bacterial cellulitis, contact dermatitis and allergic skin reactions to any of the components of the drug.

In some cases, a systemic effect of corticosteroids in connection with their absorption is possible.

The composition of the drug includes cetostearyl alcohol, butylhydroxytoluene, which can lead to the development of local reactions such as contact dermatitis; butylhydroxytoluene may cause irritation to the eyes, mucous membranes.

If any adverse reactions occur, discontinue use of the drug and be sure to consult a doctor.

special instructions

In the treatment of the pathological process on a large area of ​​the skin, the duration of therapy should be clearly determined by the doctor.

When bacter