Expiration date: 02/2027
The composition and form of issue:
Ointment for external use 0.1%. 1 g contains:
methylprednisolone aceponate 1 mg
excipients: white wax, liquid paraffin, emulsifier E white petrolatum purified water
tube 5, 10, 15, 20, 30, 50 or 100 g in a box 1 tuba.
Ointment for external use fat 0.1 %. 1 g contains:
methylprednisolone aceponate 1 mg
excipients: white soft paraffin liquid paraffin microcrystalline wax hydrogenated castor oil
in tube 5, 10, 15, 30, 50 or 60 g in a box 1 tuba.
Cream for external application 0,1%. 1 g contains:
methylprednisolone aceponate 1 mg
excipients: decillia glycerol monostearate cetostearyl alcohol * hard fat softisan 378 polyoxyl-40-stearate glycerol 85%, disodium edetate benzyl alcohol butylhydroxytoluene purified water
in tube 15, 20, 25, 30, 50 or 100 g in a box 1 tuba.
Emulsion for external application 0,1%. 1 g contains:
methylprednisolone aceponate 1 mg
excipients: medium chain triglycerides of softisan 378 polyoxyethylene-2-sterilely alcohol glycerol 85% benzyl alcohol disodium edetate purified water
in tube 20 or 50 g in a box 1 tuba.
Description pharmaceutical form:
Ointment: white to yellowish opaque homogeneous ointment.
Fatty ointment: white to yellowish translucent fatty ointment.
Cream: white or almost white, opaque cream.
Emulsion: white opaque emulsion.
Feature:
The active ingredient of the drug Advantan — methylprednisolone aceponate is negalogenizirovanny a synthetic steroid.
Pharmacokinetics:
Methylprednisolone aceponate is hydrolysed in the epidermis and the dermis. The main and most active metabolite is 6&alpha-methylprednisolone-17-propionate having a much higher affinity for the corticoid receptors from the skin that indicates the presence of its bioactivation in the skin.
The intensity of the percutaneous absorption of ointment and cream depend on the skin condition, dosage form and method of application (on open area of skin or occluzionnuyu cast). Percutaneous absorption in adolescents and adults suffering from atopic dermatitis and psoriasis, is less than 2.5%, which is only slightly different from absorption through the intact skin in adult healthy volunteers (0,5–1,5%).
For emulsions, the intensity of absorption through the skin with artificial inflammation very low (0.27% of dose) and is slightly higher than through healthy skin (0,17%). Absorption through the skin with a remote stratum corneum is much higher (15% dose). In the case of whole body treatment (such as with sunburn) systemic dose is about 4 mg/kg of body weight per day, eliminating systemic effects.
After entering into the systemic circulation 6&alpha-methylprednisolone-17-propionate is quickly anywhereelse with glucuronic acid and thus inactivated. The metabolites of methylprednisolone aceponate (main of which is 6&alpha-methylprednisolone-17-propionate-21-glucuronide) are eliminated primarily by the kidneys with a T1/2 approximately 16 h of Methylprednisolone aceponate and its metabolites do not koumouliruet in the body.
Description pharmacological action:
Topical application of Advantan suppresses inflammatory and allergic skin reactions as well as reactions associated with increased proliferation, which leads to a decrease of the objective symptoms (erythema, edema, lichenification) and the subjective sensations (itching, irritation, pain).
In the application of methylprednisolone aceponate topically in an effective dosage of systemic effects is minimal as a man and in animals. After repeated application of Advantan on large surfaces (40-60% of the surface of the skin) and the application under occlusive dressing is not marked disorders of the adrenal glands: cortisol levels in plasma and its circadian rhythm remain within normal limits, lower levels of cortisol in daily urine does not occur.
During clinical studies of use of Advantan up to 12 weeks in adults and 4 weeks in children (including early age) have been identified for the development of skin atrophy, telangiectasia, striae and prepodobnykh rashes.
Methylprednisolone aceponate (especially its main metabolite, 6&alpha-methylprednisolone-17-propionate) is associated with intracellular glucocorticoid receptors. The steroid-receptor complex interacts with specific DNA sites, thus causing a series of biological effects. In particular, this leads to the induction of the synthesis of macrocortin. Macrocortin inhibits the release of arachidonic acid and thereby the formation of inflammatory mediators type of PG and LT.
Inhibition by glucocorticoids of the synthesis of vasodilating PG and potentiation of the vasoconstrictor actions of adrenaline cause vasoconstrictor effect.
Indications:
Ointment, fatty ointment, cream
Diseases of the skin, including chronic in adults and children from 4 months of age, which makes efficient local application of corticosteroids, including:
- atopic dermatitis
- atopic dermatitis
- true eczema
- contact dermatitis
- allergic dermatitis
- disgidroticheskaya eczema
- microbial eczema
- degenerative eczema.
Emulsion
Acute inflammatory diseases of the skin in adults and children 4 months of age:
- atopic dermatitis
- atopic dermatitis
- contact dermatitis
- true eczema
- seborrheic eczema
- microbial eczema
- disgidroticheskaya eczema
- degenerative eczema
- solar dermatitis (severe sunburn).
Contraindications:
- tuberculous or syphilitic processes in the area of application of the drug
- viral diseases (e.g. varicella, herpes zoster) in the area of application of the drug
- rosacea, perioral dermatitis in the area of application of the drug
- skin reactions to the vaccine in the field of application of the drug
- hypersensitivity to the drug.
Application of pregnancy and breast-feeding:
If necessary, use of the drug Advantan during pregnancy and lactation should carefully weigh the potential risks and expected benefits of the treatment. During these periods we do not recommend prolonged use of the drug in large surfaces of the skin.
In nursing mothers, the drug should not be applied to the breast.
Side effects:
Usually the drug is well tolerated. In rare cases, there may be local reactions such as itching, burning, erythema, blistering.
As for external use of other corticosteroids, in rare cases, there may be folliculitis, hypertrichosis, perioral dermatitis, allergic reactions.
Drug interactions:
Not described.
Method of application and dose:
Externally.
The drug is applied 1 time per day thinly to the affected areas of the skin. As a rule the duration of continuous daily treatment with the drug Advantan should not exceed 12 weeks for adults and 4 weeks for children.
Ointment
For the treatment of diseases of the skin, not accompanied by oozing and the presence of infiltration, the required dosage form with a balanced ratio of fat and water. Advantan ointment makes the skin slightly greasy without delay of heat and moisture.
Fatty ointment
For treatment processes for very dry skin and chronic stages of skin diseases required anhydrous dosage form. The effect of occlusive fatty ointment provides a pronounced therapeutic effect.
Cream
Since the cream is a formulation with low fat and high water content, it is recommended for the treatment of acute inflammation and weeping stages of eczema, for very greasy skin, but also in the localization process as smooth skin and a hairy part.
Emulsion
The drug is applied 1 time per day (to treat a sunburn a maximum of 2 times a day) in a thin layer on the affected area, gently rubbing. Treatment usually should not exceed 2 weeks. If the skin is excessively dry when using emulsion Advantan, you must go to the use of formulations with a higher fat content (ointment or fatty ointment).
Overdose:
In the study of acute toxicity of methylprednisolone aceponate have not identified any risk of acute intoxication by excessive of a single cutaneous application (applying the product to a large area under conditions favourable to absorption) or inadvertent ingestion.
In the over-long and/or intensive local use of corticosteroids may develop skin atrophy (thinning of the skin, telangiectasia, striae). In such cases, the drug should be stopped.
Special instructions:
In the presence of bacterial dermatitis and/or ringworm in addition to drug therapy Advantan necessary to carry out a specific antibacterial or antimycotic treatment.
If the skin is excessively dry during prolonged use of the cream, you must go to the dosage form with a higher fat content (ointment or fatty ointment).
Avoid falling drug in the eye. As in the case of systemic corticosteroids, may develop glaucoma after administration of local forms (for example after large doses or very prolonged use, use of occlusive dressings or application to the skin around the eyes).
Effects on ability to drive and use mechanisms
Not affected.
