Advantan 0.1%

Active substance: 

methylprednisolone aceponate 1 mg;

Excipients: 

decyl oleate - 100 mg, 

glyceryl monostearate 40-55% - 85 mg, 

cetostearyl alcohol (cetyl alcohol 60%, stearyl alcohol 40%) - 25 mg, 

solid fat - 25 mg, 

softizan 378 - 75 mg, 

macrogol stearate - 30 mg, 

glycerol 85% - 50 mg, 

disodium edetate - 1 mg, 

benzyl alcohol - 10 mg, 

butylhydroxytoluene - 60 mcg, 

purified water - 597.94 mg.

Advantan  - glucocorticoid, anti-allergic, anti-inflammatory.

Pharmacodynamics

The active component of Advantan ® - methylprednisolone aceponate - is a non-halogenated steroid. When applied externally, 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, oozing) and subjective sensations (incl. itching, irritation, pain).

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®  to large surfaces (40-60% of the skin surface), as well as application under an occlusive dressing, adrenal dysfunction is not observed: the level of cortisol in plasma and its circadian rhythm remain within normal limits, a decrease in the level of cortisol in daily urine is not going on.

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), the development of skin atrophy, telangiectasias, stretch marks and acne-like rashes was not revealed.

Methylprednisolone aceponate (especially its main metabolite - 6α-methylprednisolone-17-propionate) binds to intracellular GCS receptors. The steroid-receptor complex interacts with specific regions of the immune response cell's DNA, thus producing a series of biological effects. In particular, the binding of the steroid-receptor complex to the DNA 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 PG and LT.

Inhibition of corticosteroids synthesis of vasodilating PGs and potentiation of the vasoconstrictor action of adrenaline lead to a vasoconstrictor effect.

Pharmacokinetics

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 skin GCS receptors, which indicates the presence of its bioactivation in the skin.

The intensity of percutaneous absorption for ointment and cream depends on the condition of the skin, dosage form and method of application (on an open skin area or under an occlusive dressing). 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 this indicator in healthy volunteers (0.5–1.5%).

After entering the systemic circulation, 6α-methylprednisolone-17-propionate is rapidly conjugated with glucuronic acid and thus inactivated in the form of 6α-methylprednisolone-17-propionate-21-glucuronide. Metabolites of methylprednisolone aceponate are eliminated mainly by the kidneys with T1 / 2 about 16 hours. Methylprednisolone aceponate and its metabolites do not accumulate in the body.

Skin diseases (including chronic course), amenable to GCS therapy for external use, in adults and children aged 4 months and older:

If it is necessary to use the drug Advantan during pregnancy and lactation, you should carefully weigh the expected benefits of therapy for the mother and the potential risk to the fetus or infant.

In this category of patients, it is not recommended to use the drug for a long time on extensive skin surfaces.

Breastfeeding mothers should not apply the drug to their breasts.

The drug is usually well tolerated.

Very rarely (less than 0.01% of cases), local reactions may 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 the absorption of corticosteroid. 

In clinical studies, none of the above side effects were observed when using 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 drug components can be observed.

The drug interaction of the drug Advantan is not described.

Outwardly.

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

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

Advantan cream is a dosage form with a low fat content and a high water content, therefore it is recommended for the treatment of acute inflammatory processes and the weeping stage of eczema with very oily skin, as well as for localization of the process both on smooth skin and on the scalp.

If the skin dries excessively with prolonged use of the cream, it is necessary to switch to the dosage form of Advantan.

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.

Treatment: drug withdrawal.

In the presence of bacterial dermatoses and / or dermatomycosis, in addition to Advantan therapy, specific antibacterial or antifungal treatment should be carried out.

Avoid getting the drug in the eyes.

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

Does not affect the ability to drive vehicles and work with mechanisms.

Cream 0.1%.