More info
Active ingredients
Methylprednisolone aceponate
Release form
Ointment
Composition
Methylprednisolone aceponate 1 mg. Auxiliary substances: soft white paraffin - 350 mg, liquid paraffin - 239 mg, white beeswax - 40 mg, Dehimuls E emulsifier - 70 mg, purified water - 300 mg.
Pharmacological effect
In external use Advantan; 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, weeping, etc.) and subjective sensations (including itching, irritation, pain, etc.). When methylprednisolone aceponate is used externally at the recommended dose, the systemic effect is minimal in both humans and animals. After repeated application of Advantan on large surfaces (40-60% of the skin surface), as well as when applied under the occlusive dressing, there are no violations of the adrenal glands: the plasma cortisol level and its circadian rhythm remain within the normal range, cortisol in the daily urine does not decrease occurs in clinical studies with Advantan up to 12 weeks in adults and up to 4 weeks in children (including young children) did not reveal development of skin atrophy, telangiectasia, striae and acne-like eruptions. Methylpred Nisolone aceponate (especially its main metabolite - 6α-methylprednisolone-17-propionate) binds to intracellular glucocorticoid receptors. The steroid-receptor complex binds to certain parts of the DNA of the cells of the immune response, thus causing a series of biological effects. In particular, the binding of the steroid-receptor complex to the DNA of the cells of the immune response 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 GCS synthesis of vasodilating prostaglandins and potentiation of the vasoconstrictive action of adrenaline leads to a vasoconstrictor effect.
Pharmacokinetics
Absorption Percutaneous absorption depends on the condition of the skin, the dosage form and the method of application (with or without an occlusive dressing).When using ointments, creams or oily ointments, percutaneous absorption in children and adults with atopic dermatitis (neurodermatitis) and psoriasis was no more than 2.5%, which is only slightly higher compared with 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 treatment of the whole body (for example, with sunburn), the systemic dose is about 4 mcg / kg body weight / day, which eliminates systemic effects. Metabolism and elimination 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 the glucocorticoid receptors of the skin, which indicates the presence of its bioactivation in the skin. and, thus, in the form of 6α-methylprednisolone-17-propionate glucuronide is inactivated. The metabolites of methylprednisolone aceponate are eliminated mainly by the kidneys, T1 / 2 - about 16 hours. Methylprednisolone aceponate and its o 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; - dyshydrotic eczema; - simple contact dermatitis; - allergic (contact) dermatitis. Emulsion: Inflammatory skin diseases sensitive to topical GCS therapy: - atopic dermatitis, neurodermatitis, children's eczema; - simple contact dermatitis; - allergic (contact) dermatitis; - true eczema; - se Rhine dermatitis / eczema - microbial eczema - fotodermatit, sunburn.
Contraindications
- tuberculosis or syphilitic processes in the area of application of the drug; - viral diseases in the area of application of the drug (for example, in varicella, herpes zoster); - rosacea, perioral dermatitis in the area of application of the drug; - skin areas with signs of a reaction to vaccination; - children up to 4 months; - hypersensitivity to the drug.
Precautionary measures
Use in children Continuous daily use of Advantan in the form of a cream, ointment or oily ointment is for adults no more than 12 weeks, for children - no more than 4 weeks. It is contraindicated in children under 4 months.
Use during pregnancy and lactation
If necessary, use of the drug Advantan; 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, prolonged use of the drug on the extensive surfaces of the skin is not recommended. Nursing mothers should not apply the drug to the mammary glands.
Dosage and administration
Outdoor and for adults and children from 4 months the drug is applied 1 time / day in a thin layer on the affected skin. Continuous daily use of Advantan in the form of cream, ointment or oily ointment should not exceed 12 weeks for adults and 4 weeks for children. The course of treatment with Advantan in the form of an emulsion usually should not exceed 2 weeks. The cream is a dosage form with a low fat content and high water content, therefore it is recommended for subacute and acute inflammation without pronounced soak. The cream provides the elimination of the inflammatory process on both smooth skin and scalp, including on the skin prone to fat. 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 weeping. The ointment has a therapeutic effect, also helping to eliminate dry skin and restore its normal oily skin. Fat ointment is an anhydrous drug form, therefore it is recommended for the treatment of long-term chronic inflammatory skin processes in very dry skin. The occlusal effect of oily ointment provides a pronounced therapeutic effect even with significant lichenification and infiltration. Apply a thin layer of emulsion to the affected skin, rubbing it slightly. For sunburns, the emulsion is applied 1-2 times / day. If the skin dries excessively when applying the emulsion, you must go to the dosage form of the drug Advantan; with a higher fat content (ointment or fatty ointment).
Side effects
Usually, the drug is well tolerated. Very rarely (less than in 0.01% of cases) local reactions can occur, such as itching, burning, erythema, and 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 studies, none of the above side effects were noted when using the drug Advantan; 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.
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: excessively long and / or intensive topical administration of GCS atrophy of the skin may develop (thinning of the skin, telangiectasia, striae). In case of atrophy, the drug must be canceled.
Interaction with other drugs
Drug interaction drug Advantan; not found.
special instructions
If there are bacterial complications and / or ringworms in addition to Advantan therapy; specific antibacterial or antifungal treatment should be carried out. Avoid contact with the eyes. As with systemic corticosteroids, glaucoma may develop after external use of GCS (for example, with large doses or very long use of occlusive dressings or on the skin around the eyes) .The impact on the ability to drive motor vehicles and control mechanismsNot identified.