2010/06/24

Advantan

Composition, structure and packing

Cream 0.1% white or almost white, opaque.

1 g of methylprednisolone atseponat 1 mg.

Excipient: detsiloleat, glycerol monostearate, tsetosterilovy alcohol, hard fat, softizan 378, polioksil-40-stearate, glycerol 85%, disodium edetate, benzyl alcohol, butilgidroksitoluol, purified water.

Ointment for external use only 0.1% of white up to yellow, opaque, homogeneous.

1 g of methylprednisolone atseponat 1 mg.

Excipients: white wax, paraffin liquid, emulsifier E, white petrolatum, purified water.

Ointment for external use fat 0.1% of white to yellowish, translucent. 1 g of methylprednisolone atseponat 1 mg Excipients: white soft paraffin, liquid paraffin, microcrystalline wax, hydrogenated castor oil.

Emulsion for external use only 0.1% of white, opaque.

1 g of methylprednisolone atseponat 1 mg.

Excipients: triglycerides with chains of medium size, softizan 378, polyoxyethylene-2-sterilovy alcohol, polyoxyethylene-21-sterilovy alcohol, glycerol 85%, benzyl alcohol, sodium edetate, purified water.

Clinical and pharmacological group: SCS for outdoor use.

Pharmacological action

SCS for external use, is a non-halogenated alternatives synthetic steroid. For exterior use Advantan suppress inflammatory and allergic skin reactions, as well as the reactions associated with enhanced proliferation, which leads to a decrease in objective symptoms (erythema, edema, lihenifikatsiya) and subjective symptoms (itching, irritation, and pain).

In the application of methylprednisolone atseponata outwardly expressed minimal systemic effects as in humans, and animals. After repeated application Advantan over a large surface (40-60% of the surface of the skin), as well as the application under occlusive dressing is not observed violations of the adrenal function either in children or adults: the level of cortisol in the blood plasma and its circadian rhythm remained within normal limits, reduce the level of cortisol in the daily urine does not occur.

In clinical studies in the application Advantan in the form of ointments, creams or oily ointments to 12 weeks in adults and up to 4 weeks in children (including toddlers) found no development of skin atrophy, telangiectasia, striae and ugrepodobnyh rash. Metilprednizolna atseponat (especially its major metabolite - 6α-methylprednisolone-17-propionate) binds to intracellular glucocorticoid receptors. Steroid-receptor complex binds to specific DNA sites, thus causing a series of biological effects.

In particular, the binding of steroid-receptor complex with DNA leads to induction of synthesis makrokortina. Makrokortin inhibits the release of arachidonic acid and, thus, the formation of inflammatory mediators such as prostaglandin and leukotrienes. Inhibition of GCS synthesis of vasodilating prostaglandins and potentiation of the vasoconstrictive action of adrenaline leads to a vasoconstrictor effect.

Pharmacokinetics

Absorption

The intensity of the absorption through the skin depends on the condition of the skin, dosage form and method of application (in an open area of the skin or under occlusive dressing).

In the application of ointments, creams or oily ointments percutaneous absorption in adolescents and adults suffering from neurodermatitis and psoriasis, was less than 2.5%, which is only slightly different from absorption through the intact skin of healthy adult volunteers (0.5-1.5%). In applying the drug in the form of an emulsion absorption through the skin with an artificial inflammation were very low (0.27%) and slightly higher than the absorption through the healthy skin (0.17%). Absorption through the skin with a remote horny layer was significantly higher (15% dose). In the case of processing the whole body (such as sunburn), systemic dose is about 4 mg / kg of body weight per day (which excludes systemic effects).

Metabolism and excretion

Methylprednisolone atseponat hydrolyzed in the epidermis and dermis. The main and most active metabolite is 6α-methylprednisolone-17-propionate, which has a much higher affinity for corticoid receptors of the skin, which indicates the presence of its bioactivation in the skin. After entering the systemic circulation 6α-methylprednisolone-17-propionate rapidly conjugates with glucuronic acid and, thus, inactivated. Metabolites of Methylprednisolone atseponata (chief among which is 6α-methylprednisolone-17-propionate-21-glucuronide) are derived primarily by the kidneys, half-life approximately 16 hours atseponat methylprednisolone and its metabolites are not cumulative in the body.

Statement

Ointment, cream, fatty ointment

Skin diseases (including chronic course), amenable to SCS therapy for external use, in adults and children aged 4 months and older:
atopic dermatitis, atopic dermatitis,
true eczema;
contact dermatitis;
dermatitis;
disgidroticheskaya eczema;
Microbial eczema
degenerative eczema.

Emulsion for external use

Acute inflammatory diseases of the skin in adults and children ages 4 months and older:
Atopic dermatitis, neurodermatitis;
Contact dermatitis;
true eczema;
seborrheic eczema;
Microbial eczema
disgidroticheskaya eczema;
degenerative eczema;
Solar dermatitis (pronounced sunburn).

Dosage regimen

The drug is applied 1 time per day with a thin layer on the affected skin. Continuous daily use Advantan in the form of a cream, ointment or fatty ointment is for adults not more than 12 weeks, for children - no more than 4 weeks. The course of treatment Advantanom in the form of an emulsion is not more than 2 weeks.

Cream Advantan a dosage form of low-fat and high water content, so it is recommended for the treatment of acute inflammation and weeping stages of eczema with very oily skin, as well as the localization process as smooth skin, and on the scalp.

Ointment for the treatment of skin diseases are not accompanied by wet and in the presence of infiltration in which the necessary dosage form with a balanced ratio of fat and water. Advantan in the form of ointment makes the skin slightly greasy without delay of heat and moisture.

Fatty ointment indicated for the treatment processes with very dry skin and chronic skin diseases at stages when required anhydrous dosage form of the drug. Occlusive effect of fatty ointment provides a pronounced therapeutic effect.

Emulsion applied on the skin, gently rubbing. If sun burns the emulsion can be applied up to 2 times per day. If the skin overly dry when applying the emulsion or prolonged use of creams, you must go to the dosage form Advantan with a higher fat content (ointment or fatty ointment).

Side effect

In rare cases: itching, burning, erythema, vesiculation at the site of application of the drug. Rare: as the use of other SCS - folliculitis, gipetrihoz, perioral dermatitis, allergic responses.

Contraindications
tuberculosis of the skin and cutaneous manifestations of syphilis in the field of application of the drug;
viral skin lesions in the application of the drug (eg, chicken pox, shingles);
rosacea, perioral dermatitis in the application of the drug;
skin manifestation of the reaction to the vaccine;
Hypersensitivity to the drug's components.

Pregnancy and lactation

If necessary, use of the drug Advantan during pregnancy and lactation should carefully weigh the potential benefits of therapy for the mother and the potential risk to the fetus or infant. This category of patients is not recommended to use the drug for a long time over a large surface of the skin. Nursing mothers should not cause the drug to breast.

Cautions

In the presence of bacterial dermatitis and / or dermatomycoses in addition to therapy Advantanom necessary to carry out specific antibacterial or antifungal medication. The emulsion should not be applied under the occlusive bandage. It must be borne in mind that the nappies (diapers) can create occlusive effect.

Avoid getting product in eyes.

As in the case of systemic corticosteroids, when applied externally SCS can develop glaucoma (eg, after high-dose or very long-term use, the use of occlusive dressings, or application to the skin around the eyes).

Effects on ability to drive vehicles and management mechanisms

Does not affect ability to drive trucks and operate machinery.

Overdose

In the study of acute toxicity of methylprednisolone atseponata not been identified any risk of acute intoxication with excessive single applied externally (putting the drug on a large area under conditions conducive to the absorption) or unintentional ingestion.

Symptoms: When too much debt and / or intense local application of GCS may develop skin atrophy (skin thinning, telangiectasia, striae).

Treatment: removal of the drug.

Drug Interactions

Drug Interactions drug Advantan not described.

Terms and Conditions of storage

Ointments, creams and emulsions should be stored at temperatures not above 25 ° C. Shelf life - 3 years.

Fat ointment should be stored at temperatures not above 30 ° C. Shelf life - 5 years. The drug should be stored out of reach of children.