Advantan®, 0.1% 15 g ointment

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

Pharmacodynamics

The active ingredient of the drug Advantan – methylprednisolone aceponate – is a nonhalogenated steroid. When applied topically, Advantan® suppresses inflammatory and allergic skin reactions, as well as reactions associated with increased proliferation, which leads to a reduction of objective symptoms of inflammation (including erythema, edema, mucous) and subjective sensations (including itching, irritation, pain).

When methylprednisolone aceponate is applied topically at the recommended dose, systemic effects are minimal in both humans and animals. No adrenal dysfunction is noted after multiple application of Advantan® over large surfaces (40-60% of skin surface) and also after application under an occlusive dressing: plasma cortisol levels and its circadian rhythm remain within normal limits, there is no reduction of cortisol levels in daily urine.

In clinical studies, use of Advantan® up to 12 weeks in adults and up to 4 weeks in children (including infants) showed no evidence of skin atrophy, telangiectasia, stricture or acne-like eruptions.

Methylprednisolone aceponate (especially its main metabolite, 6α-methylprednisolone-17-propionate) binds to intracellular GCS receptors. The steroidreceptor complex interacts with certain DNA sites of the immune response cells, thus causing a series of biological effects. In particular, binding of the steroidreceptor complex to the DNA of the immune response cells leads to induction of macrocortin synthesis. Macrocortin inhibits the release of arachidonic acid and thus the formation of inflammatory mediators like PG and LT.

The inhibition of GCS synthesis of vasodilatory PGs and potentiation of the vasoconstrictor effect 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 significantly higher affinity for skin GCS receptors, indicating its bioactivation in the skin.

The intensity of percutaneous absorption for ointment and cream depends on the skin condition, dosage form and method of application (on the exposed skin or under the occlusive dressing). Percutaneous absorption in children and adults with atopic dermatitis (neurodermatitis) and psoriasis was not more than 2.5%, which was only slightly higher than in healthy volunteers (0.5-1.5%).

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

Indications

Dermatological conditions (including chronic course) amenable to external GCS therapy in adults and children 4 months and older:

Active ingredient

Composition

1 g of the ointment contains:

Active substance:

methylprednisolone aceponate 1 mg.

Auxiliary substances:

soft white paraffin – 350 mg,

liquid paraffin – 239 mg,

beeswax white – 40 mg,

Emulsifier Dehimuls E – 70 mg,

purified water – 300 mg.

How to take, the dosage

The drug is applied once a day in a thin layer on the affected areas of the skin.

Continuous daily use of Advantan in the form of ointment is not more than 12 weeks for adults, and not more than 4 weeks for children.

The ointment is prescribed for the treatment of skin conditions not accompanied by mottling and in the presence of infiltration, which require a dosage form with a balanced fat to water ratio. Advantan in the form of an ointment makes the skin slightly oily without retaining heat and moisture.

Interaction

Drug interactions of the drug Advantan have not been described.

Special Instructions

In the presence of bacterial dermatoses and/or dermatomycoses, specific antibacterial or antifungal treatment should be given in addition to therapy with Advantan.

Contact with the drug in the eyes should be avoided.

As with systemic corticosteroids, glaucoma may develop with external use of GCS (e.g., after high doses or very prolonged use, use of occlusive dressings, or application to the skin around the eyes).

Impact on driving and operating machinery

It does not affect the ability to drive vehicles and operate machinery.

Contraindications

Side effects

The drug is usually well tolerated.

Very rare (less than 0.01% of cases) local reactions such as itching, burning, erythema, formation of vesicular rash may be observed.

If the drug is used for more than 4 weeks and/or over 10% or more of the body surface the following reactions may occur: skin atrophy, telangiectasia, stretch marks, acneiform skin changes, and systemic effects caused by absorption of the corticosteroid.

In clinical studies, none of the above side effects were noted when Advantan was used up to 12 weeks in adults and up to 4 weeks in children.

In rare cases (0.01-0.1%), folliculitis, hypertrichosis, perioral dermatitis, depigmentation of the skin and allergic reactions to one of the ingredients of the drug may occur.

Overdose

In a study of acute toxicity of methylprednisolone aceponate no risk of acute intoxication was found with excessive single external use (application of the drug to a large area under conditions favorable for absorption) or unintentional oral administration.

Symptoms: skin atrophy (thinning of the skin, telangiectasia, stretch marks) may develop with excessive long-term and/or intensive topical use of GCS.

Treatment: discontinuation of the drug.

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