• Document: cream. 1 g cream or ointment contains 1 mg (0.1%) methylprednisolone aceponate.
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ADVANTAN® Methylprednisolone aceponate 0.1% ointment/cream Presentation 1 g cream or ointment contains 1 mg (0.1%) methylprednisolone aceponate. Uses Actions After topical application, ADVANTAN® suppresses inflammatory and allergic skin reactions as well as reactions associated with hyperproliferation, leading to regression of the objective symptoms (erythema, edema, infiltration, lichenification) and the subjective complaints (itching, burning, pain). On application of methylprednisolone aceponate in topically effective dosage, the systemic effect is minimal in both man and animals. After large-area treatment of patients with skin disorders, the plasma cortisol values remain within the normal range, circadian cortisol rhythm is maintained and no reduction of cortisol has been ascertained in 24-hour urine. As for all other glucocorticoids, so far the mechanism of action of methylprednisolone aceponate is not completely understood. It is known that methylprednisolone aceponate itself binds to the intracellular glucocorticoid receptor and this is especially true of the principal metabolite 6-methyl - prednisolone -17-propionate, which is formed after cleavage in the skin. The steroid receptor complex binds to certain regions of DNA, thereby triggering a series of biological effects. The understanding of the mechanism of the anti-inflammatory action is more precise. Binding of the steroid receptor complex results in induction of macrocortin synthesis. Macrocortin inhibits the release of arachidonic acid and thus the formation of inflammation mediators such as prostaglandins and leukotrienes. The immunosuppressive action of glucocorticoids can be explained by inhibition of cytokine synthesis and an antimitotic effect, which so far is not well understood. Inhibition of the synthesis of vasodilating prostaglandins or potentiation of the vasoconstrictive effect of epinephrine finally results in the vasoconstrictive activity of glucocorticoids. The respective bases are of major importance to the therapeutic effect of the ADVANTAN® formulations. 1  ADVANTAN® cream As a low-fat formulation with a high water content, ADVANTAN cream is particularly suitable for acute and subacute weeping stages of eczema, for very greasy skin and for use on exposed or hairy parts of the body.  ADVANTAN® ointment Skin conditions which are neither weeping nor very dry require a base with balanced proportions of fat and water. ADVANTAN® ointment is suitable for dry, fissured, scaly or hyperkeratinised skin areas. It should not be used in areas such as axilla, groin or skin folds. ADVANTAN® ointment makes the skin slightly greasy without retaining warmth and fluid. Of the three formulations, ADVANTAN® ointment has the widest field of use. Pharmacokinetics Methylprednisolone aceponate (MPA) becomes available in the skin from all formulations (cream, ointment). The concentration in the stratum corneum and living skin decreases from outside to inside. Methylprednisolone aceponate is hydrolyzed in the epidermis and dermis to the main metabolite 6-methylprednisolone-17-propionate which binds more firmly to the corticoid receptor – an indication of "bioactivation" in the skin. The degree of percutaneous absorption depends on the state of the skin, the formulation and the conditions of application (open/occlusion). Studies in juvenile and adult patients with neurodermatitis and psoriasis have shown that the percutaneous absorption on open application was only slightly ( 2.5%) greater than the percutaneous absorption in volunteers with normal skin (0.5 - 1.5 %). When the horny layer is removed before the application, the corticoid levels in the skin are about three times higher than after application to intact skin. After reaching the systemic circulation, the primary hydrolysis product of MPA, 6methylprednisolone-17-propionate, is quickly conjugated with glucuronic acid and inactivated as a result. The metabolites of MPA (main metabolite: 6-methylprednisolone-17- propionate-21- glucuronide) are eliminated primarily via the kidneys with a half-life of about 16 hours. Following i.v. administration, excretion of the 14C- labeled substances with the urine and feces was complete within 7 days. No accumulation of substance or metabolites takes place in the body. Indications Atopic dermatitis (endogenous eczema, neurodermatitis), contact eczema, degenerative, dyshidrotic, vulgar eczema, eczema in children. 2 Dosage and Administration ADVANTAN® is for EXTERNAL TOPICAL USE ONLY and NOT FOR OPTHALMIC USE. In general, the ADVANTAN® formulation appropriate to the skin condition is applied thinly once per day to the diseased areas of skin. In general, the duration of use should not exceed 12 weeks in adults and 4 weeks in children. Contraindications ADVANTAN® is contraindicated in most viral diseases (eg vaccinia, varicel

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