Methylprednisolone aceponate - instructions for use, dose, side effects, contraindications

Excipients: Vaseline (Vaseline Medical) - 18.0 g, beeswax white - 3.0 g, paraffin liquid (Vaseline oil) - 10.0 g, cetomacrogol 1000 - 3.0 g, emulsifier No. 1 (Lanette SX) - 7.0 g, purified water - up to 100 g.

Description:Homogeneous ointment is white or almost white.

Pharmacotherapeutic group:Glucocorticosteroid for topical application

ATX: & nbsp

D.07.A.A.01 Methylprednisolone

Pharmacodynamics:

Methylprednisolone aceponate is a non-halogenated steroid.

With external application methylprednisolone aceponate suppresses inflammatory and allergic skin reactions, as well as reactions associated with increased proliferation, which leads to a reduction in the objective symptoms of inflammation (erythema, edema, mocclusion) and subjective sensations (itching, irritation, pain).

When applying methylprednisolone aceponate externally at the recommended dose, the systemic effect is minimal both in humans, as well as in animals.

Methylprednisolone aceponate (especially its main metabolite - 6α-methylprednisolone-17-propionate) binds to intracellular glucocorticosteroid receptors. The steroid-receptor complex binds to certain parts of the DNA of the cells of the immune response, thus causing a series of biological effects.

In particular, binding of the steroid-receptor complex to the DNA 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 prostaglandins and leukotrienes.

Inhibition of glucocorticosteroid synthesis of vasodilating prostaglandins and enhancement of vasoconstrictive action of epinephrine lead to a vasoconstrictive 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 much higher affinity for glucocorticosteroid skin receptors, indicating its "bioactivation" in the skin.

The degree of percutaneous absorption depends on the condition of the skin, the dosage form and the method of administration (with or without occlusive dressing).

Percutaneous absorption in children and adults with atopic dermatitis (neurodermatitis) and psoriasis was not more than 2.5%, which is only slightly higher than in healthy volunteers (0.5-1.5%).

After entering the systemic circulation 6αmethylprednisolone-17-propionate is rapidly conjugated to glucuronic acid and, thus, in the form of 6α-methylprednisolone-17-propionate, glucuronide is inactivated.

Metabolites of methylprednisolone aceponate are eliminated mainly by the kidneys with a half-life of about 16 hours. Methylprednisolone aceponate and its metabolites are not cumulated in the body.

Indications:

Neurodermatitis (atopic dermatitis), contact dermatitis, degenerative eczema, nummular (coin-like) eczema.

Contraindications:

Hypersensitivity to methylprednisolone aceponate, to auxiliary components of the drug, postvaccinal period, bacterial, viral (varicella zoster, shingles) and fungal skin diseases (pyoderma, mycosis), skin tuberculosis, dermatitis,violation of the integrity of the skin (ulcers, wounds), syphilitic skin lesions, skin tumors, rosacea, acne vulgaris, perioral dermatitis, childhood (up to 4 months).

Pregnancy and lactation:

The safety of the use of methylprednisolone aceponate during pregnancy and lactation has not been studied.

Long-term treatment, the use of high doses of glucocorticosteroid, the use of the drug on large areas of the skin, the use of occlusive dressings should be avoided.

Pregnancy

Adequate and strictly controlled studies in pregnant women were not conducted. Studies in animals have shown adverse effects on the fetus (teratogenic, embryotoxic). When pregnancy is used only after consulting a doctor, if the intended use for the mother exceeds the potential risk to the fetus. Do not use in the first trimester of pregnancy.

Breastfeeding period

It is not known whether the methylprednisolone aceponate in breast milk. During the period of breastfeeding, they should be used only after consulting a doctor if the intended benefit to the mother exceeds the potential risk for the child.Women with breastfeeding should not apply the drug to the mammary glands.

Dosing and Administration:

Outwardly. For adults and children from the age of four months, the drug is applied once a day with a thin layer on the affected areas of the skin.

The duration of the drug in adults should not exceed 6 weeks, in children - 3 weeks.

Correction of the dosing regimen in children is not required. When using ointment in children from 4 months to 18 years, it is necessary to limit the total duration of treatment and exclude activities leading to increased resorption and absorption (warming, fixation and occlusive dressings).

Side effects:

Usually the drug is well tolerated. In clinical studies, the most frequently observed reactions at the site of application in the form of burning, itching of the skin.

The incidence of adverse events is classified according to WHO recommendations: very often (> 1/10); often (≥ 1/100, <1/10); infrequently (≥ 1/1000, <1/100); rarely (≥ 1/10000, <1/1000); very rarely (<1/10000) or the frequency is unknown (can not be estimated from available data).

Immune system disorders

Frequency is unknown: hypersensitivity reactions.

Disturbances from the skin and subcutaneous tissues

Infrequent: skin atrophy, ecchymosis (bruise), impetigo, oily skin; frequency unknown: acne, telangiectasia, striae, perioral dermatitis (inflammation of the skin around the mouth), skin discoloration, allergic skin reactions.

General disorders and disorders at the injection site

Often: in the place of application: itching, burning; infrequently: at the site of application: erythema, dry skin, the formation of a vesicle rash, irritation, dermatitis, peripheral edema;

frequency unknown: hypertrichosis (increased hair growth), at the site of application: folliculitis.

Systemic effects due to glucocorticosteroid absorption (resorptive effects) are possible.

If any of the side effects indicated in the manual are aggravated, or any other side effects not indicated in the instructions are noted, you should inform the doctor immediately.

Overdose:

When studying acute toxicity of methylprednisolone aceponate, there was no risk of acute intoxication with excessive single skin application (application of the drug over a large area under conditions favorable for absorption) or unintentional ingestion.

With excessively long and / or intensive use of glucocorticosteroids, skin atrophy can develop (thinning of the skin, telangiectasia, striae).

When the appearance of atrophy drug should be canceled.

Interaction:

Not studied.

Special instructions:

In the presence of bacterial complications and / or dermatomycosis in addition to therapy with the drug, it is necessary to carry out specific antibacterial and / or antimycoticstreatment.

Avoid contact with the eyes, open wounds and mucous membranes. If the product gets into the eyes or mucous membranes, it is recommended to wash them with a sufficient amount of water.

As in the case of systemic glucocorticosteroids, glaucoma may develop after external use of the drug (for example, when using large doses or for a very long time using occlusive dressings or applying to the skin around the eyes).

Avoid application of the drug on large areas of the skin and / or prolonged use, use in large quantities or under occlusive dressings, as this greatly increases the risk of side effects.When applying the drug on large areas of the skin, the period of application should be as short as possible because of the possibility of developing systemic side effects.

Pediatric Use

A drug Methylprednisolone aceponate can be used in children from 4 months. It should be borne in mind that in young children, skin folds, diapers and diapers can have an effect similar to that of an occlusive dressing, and increase the systemic resorption of the active substance of the drug. In addition, children can have a greater degree of systemic resorption due to the relationship between skin surface and body weight, and also due to insufficient maturation of the skin. Children are at greater risk of suppressing the function of the hypothalamic-pituitary-adrenal system and the development of the Itenko-Cushing syndrome with any external glucocorticosteroids; long-term treatment of children with glucocorticosteroids can lead to disruption of their growth and development. Children should receive a minimum dose of the drug, sufficient to achieve a therapeutic effect. The drug should be administered under the supervision of a doctor.

Effect on the ability to drive transp. cf. and fur:The drug does not affect the ability to drive vehicles or engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:Ointment for external use, 0.1%.

Packaging:

By 5, 10, 15, 20, 30 and 50 g in aluminum tubes or in tubes laminated.

1 The tube with instruction for use is placed in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 of the year.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LP-003776

Date of registration:10.08.2016

Expiration Date:10.08.2021

The owner of the registration certificate:VELFARM, LLC VELFARM, LLC Republic of San Marino

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Information update date: & nbsp07.05.2018

Illustrated instructions

Instructions

Methylprednisolone aceponate (Methylprednisolone aceponate)