Instructions for Advantan (Methylprednisolone aceponate)
Pharmacological properties:
Advantan - methylprednisolone aceponate, when applied topically, reduces inflammatory and allergic skin reactions, as well as reactions associated with cell hyperproliferation, which leads to the elimination of both objective symptoms (erythema, edema, infiltration, lichenification) and subjective complaints (itching, burning, pain).
When applying methylprednisolone aceponate at a dose effective for topical application, the systemic effect is minimal. When applied to large areas of skin in patients with skin diseases, the level of cortisol in the blood plasma remains within normal limits, and its circadian rhythm does not change. Also, there was no decrease in the concentration of cortisol in daily urine.
As with other GCS, the mechanism of action of the methylprednisolone aceponate has not been finally clarified. It is known to bind directly to intracellular glucocorticoid receptors. This is particularly true of the main metabolite of methyl rednisolone aceponate - 6α-methylprednisolone-17-propionate formed in the skin as a result of metabolism.
Binding of the receptor-steroid complex to a specific region of the DNA molecule initiates a number of biological effects.
The mechanism of anti-inflammatory action is elucidated more precisely. Binding of the receptor-steroid complex leads to the induction of the synthesis of macrocortin. Macrocortin inhibits the release of arachidonic acid and reduces the formation of inflammatory mediators such as prostaglandins and leukotrienes.
The immunosuppressive effect of GCS can be explained by inhibition of cytokinin synthesis and an anti-mitotic effect studied so far is not enough.
Inhibition of the synthesis of vasodilation prostaglandins or potentiation of the vasoconstrictor effect of adrenaline ultimately causes vasoconstrictor activity of GCS.
Methylprednisolonum (MPA) gets into thickness of skin from any form of medicine (cream, ointment, fat ointment). Its concentration in the stratum corneum and skin decreases from the surface to the middle.
MPA is hydrolyzed in epidermis and dermis. The main metabolite - 6α-methylprednisolone-17-propionate binds more strongly to corticoid receptors, which indicates the process of bioactivation in the skin.
The degree of subcutaneous absorption depends on the condition of the skin, the therapeutic form and the type of application (open or occlusive bandage). The results of the study of MPA absorption with open application on affected skin areas in adolescents and adults with neurodermitis or psoriasis showed that absorption of the drug was only slightly more (not more than 2.5%) absorption through intact skin in healthy volunteers (0.05-1.5%).
If the stratum corneum is removed before application to the skin surface, the level of corticosteroid in the skin is approximately three times higher than after application without removal of the stratum corneum.
Entering the systemic bloodstream, the main product of the hydrolysis of MPA - 6α-methylprednisolone-17-propionate - quickly conjugates with glucuronic acid and as a result of this process is inactivated.
Metabolites of MPA (main metabolite: 6α-methylprednisolone-17-propionate-21-glucoronide) are excreted mainly by kidneys with a half-life of about 16 hours. The compound and its metabolites in the body do not cumulate.
- Indications:
- fat ointment:
- atopic dermatitis,
- neurodermitis,
- eczema,
- contact dermatitis,
- allergic dermatitis,
- degenerative eczema,
- dyshydrotic eczema,
- eczema in children
- emulsion:
- acute inflammatory skin diseases: contact dermatitis,
- true eczema, seborrheic eczema, microbial eczema,
- dishydrotic eczema,
- degenerative eczema,
- atopic dermatitis,
- neurodermitis,
- acute eczema in children (starting from 4 months of age),
- solar dermatitis (severe sunburn).
Application:
In case the affected skin is very dry, it requires an anhydrous drug base with a large fat content (Adwantan ointment). If the damaged skin is not wet and not very dry, it requires a dosage form with a balanced fat and water content - Advantan ointment. Advantan cream with low fat and high water content is suitable for treating acute inflammatory processes and wet eczema. The Advantan emulsion is used for sunburn 1-2 times a day (no more than).
The preparation Advantan is applied to affected areas of skin 1 once a day in a thin layer. The duration of use usually does not exceed 12 weeks for adults, 4 weeks for children.
Contraindications:
Advantan is contraindicated in skin tuberculosis or manifestations of syphilis at the sites of application of the drug, as well as in viral infections (chickenpox, shingles, reactions to vaccination, etc.); with increased sensitivity to the active substance or any other component of the preparation.
Side effects:
In some cases, the use of Advantan may be accompanied by topical reactions such as itching, burning, erythema or vesicles.
With prolonged GCS therapy, local manifestations such as skin atrophy, telangioectasia, the appearance of striae or acne-like rashes on the skin cannot be excluded. As a result of clinical studies of the drug Advantan, which was used in adults for 12 weeks, and in children - up to 4 weeks, such side effects were not established.
In isolated cases, during treatment with Advantan, side effects characteristic of topical corticosteroid use may occur: folliculitis, hypertrichosis, perioral dermatitis, allergic skin reactions to any of the components of the drug
Special instructions:
In the case of bacterial infectious processes of the skin and/or in the case of a fungal lesion, additional special treatment is necessary. When using Advantan on the face, you should avoid getting the drug into the eyes. In rosacea or perioral dermatitis, applying Advantan to the face is not recommended.
When applying Advantan to large areas of the skin (40-60% of the skin surface) or using occlusive bandages, neither adults nor children showed impaired adrenal cortex function.
Period of pregnancy and breastfeeding. Clinical indications for Advantan treatment during pregnancy and breastfeeding need to be carefully examined, and the expected benefit of use should be carefully weighed against the risk to the fetus and baby. It is necessary to avoid the use of the drug on large areas of the skin or for a long time.
Interactions
Not described.
Overdose:
The results of studies of the acute toxicity of the drug do not indicate the existence of any risk of acute intoxication during a one-time overdose (application of overparting to large areas of the skin under favorable conditions for adsorption or with accidental oral use).
Storage conditions:
Cream, ointment and emulsion - at temperature not higher than 25 ° C, ointment - not higher than 30 ° C. Shelf life: ointment - 5 years, cream, ointment, emulsion - 3 years.
