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Active ingredients
Pimecrolimus
Release form
Cream
Composition
Active ingredient: pimecrolimus (pimecrolimus) 150 mg
Pharmacological effect
Means for external use. Pimecrolimus is a derivative of macrolactam ascomycin. Selectively inhibits the production and release of cytokines and mediators from T-lymphocytes and mast cells. It has anti-inflammatory properties. Pimecrolimus specifically binds to macrophilin-12 and inhibits calcium-dependent phosphatase calcineurin. As a result, blocking the transcription of early cytokines, pimecrolimus suppresses the activation of T-lymphocytes. In particular, at nanomolar concentrations, pimecrolimus inhibits the synthesis of interleukin-2, interferon gamma (Th1 type), interleukin-4 and interleukin-10 (Th2 type) in human T-lymphocytes. In addition, in vitro, after interaction with the antigen / IgE complex, pimecrolimus prevents antigen / IgE-mediated release of cytokines and inflammatory mediators from mast cells. Pimecrolimus does not affect the growth of keratinocytes, fibroblasts and endothelial cells. Pimecrolimus is effective in skin inflammation, while its effect on the systemic immune response is very small. In general, the uniqueness of the mechanism of action of pimecrolimus consists in the combination of anti-inflammatory activity, selective to the skin, with a low ability to induce systemic immune responses.
Pharmacokinetics
Adults. The concentration of pimecrolimus in the blood was determined in 12 adult patients with atopic dermatitis (eczema) with a lesion of 15–59% of the body surface area treated with Elidel cream 2 times a day for 3 weeks. In 77.5% of observations, the concentration of pimecrolimus in the blood was below 0.5 ng / ml (the minimum detectable concentration), and in 99.8% - below 1 ng / ml. Cmax of pimecrolimus in the blood, registered in 1 patient, was 1.4 ng / ml. In 98% of 40 adult patients with an initial lesion of 14–62% of the body surface area after 1 year of treatment with Elidel cream, the concentration of pimecrolimus in the blood remained low and in most cases, they were below the minimum detectable concentration. A Cmax value of 0.8 ng / ml was registered after 6 weeks of treatment in only 2 patients. None of the patients showed an increase in concentration over the course of 12 months of treatment.During the 3-week period of treatment with Elidel cream, 2 times a day in 13 adult patients with hand dermatitis (using the cream on the palm and back of the hand and bandaging at night), the maximum recorded concentration of pimecrolimus in the blood was 0.91 ng / ml. In 8 patients with a pimecrolimus content in the blood above the minimum detectable concentration, the AUC value was 2.5–11.4 ng / ml. Children. Pharmacokinetic studies of pimecrolimus were conducted in 58 children aged 3 months to 14 years with atopic dermatitis (eczema) with a lesion of 10–92% of the body surface area treated with Elidel cream 2 times a day for 3 weeks. Five children received treatment for 1 year as needed. Pimecrolimus concentrations in the blood were at a consistently low level, regardless of the skin lesion area and duration of therapy, and were in the same range of values as in adult patients treated with Elidel Cream. the same doses. In 97% of cases, the concentration of pimecrolimus in the blood was below 2 ng / ml, and in 60% - below 0.5 ng / ml (the minimum detectable concentration). Cmax of pimecrolimus, registered in 2 patients aged 8 months and 14 years, was 2 ng / ml. Among the youngest children (from 3 to 23 months), Cmax of pimecrolimus was 2.6 ng / ml and was registered in 1 patient. 5 children treated with Elidel cream for 1 year, pimecrolimus concentrations were at a consistently low level. The maximum value recorded in 1 child was 1.94 ng / ml. During the entire period of treatment, no increase in drug concentrations was observed in any of the patients. In 8 children aged 2 to 14 years with pimecrolimus in the blood above the minimum detectable concentration with a threefold measurement, the AUC value ranged from 5.4 to 18.8 ng / ml. The AUC values in patients with skin lesions of less than or more than 40% were comparable. In in vitro studies, the binding of pimecrolimus to plasma proteins (mainly with various lipoproteins) was 99.6%. Since topical administration of pimecrolimus in the blood is very low, determination of metabolic parameters is not possible. Pharmacokinetics in special clinical situations. Atopic dermatitis (eczema) is rarely observed in patients aged 65 years and older.The number of patients of this age in clinical studies of 15% Elidel cream was insufficient to reveal any differences in treatment efficacy compared with young patients. Dosing recommendations for infants (3-23 months), children (2-11 years) and adolescents (12-17 years) do not differ from the recommendations for adult patients.
Indications
Atopic dermatitis (eczema) - for short-term and long-term use in adults, adolescents and children (aged from 3 months).
Contraindications
sensitivity to timecrolimus or any component of the drug; children up to 3 months (the safety and efficacy of using Elidel cream in children younger than 3 months have not been studied); the presence of acute viral, bacterial or fungal skin infections. With caution: patients with Netherton syndrome (data on there is no safety of use) - the risk of increasing the systemic absorption of the drug is possible, severe forms of inflammation or skin lesions, including generalized erythroderma (no safety data is available) - there is a risk of increased systemic absorption of the drug; weakened immunity - because efficacy and safety of use have not been studied. There are no data on the safety of long-term use of Elidel cream. Since the effects of long-term use of the drug on the skin’s immune defense and the incidence of malignant neoplasms have not been studied, Elidel cream should not be applied to damaged skin with possible malignancy or dysplastic changes. In the case of bacterial or fungal skin lesions, use of Elidel cream on the affected areas is possible only after cure. infection.
Precautionary measures
Do not apply on affected skin with acute viral infection.
Use during pregnancy and lactation
Data on the use of the drug in pregnant women do not. In experimental studies with the local application of the drug directly or indirectly, the damaging effect of Elidel cream on the course of pregnancy, the development of the embryo / fetus, the course of childbirth and the postnatal development of the offspring has not been identified. Care should be taken when appointing pregnant women.However, given the minimum degree of absorption of pimecrolimus when applied topically, the potential risk in humans is considered negligible. The release of the drug in breast milk after topical administration in experimental models has not been studied. There is no data on the content of pimecrolimus in breast milk of lactating women. Since many drugs are excreted in breast milk, care should be taken when prescribing 1% Elidel cream to nursing women. However, given the minimal degree of systemic absorption of pimecrolimus when applied topically, the potential risk to a person is considered negligible. Nursing women should not apply 1% Elidel cream on the breast area. The effect of Elidel cream on fertility in men and women has not been established.
Dosage and administration
Treatment should be started at the first manifestations of the disease to prevent the sharp development of its aggravation. Cream is applied in a thin layer on the affected surface 2 times a day and gently rubbed until completely absorbed. The cream can be applied to the skin of any parts of the body, including the head, face, neck, and also on the diaper rash area. Cream Elidel should be applied 2 times a day, until the complete disappearance of symptoms of the disease. If symptoms persist after 6 weeks of use of the drug, it is necessary to re-examine the patient to confirm the diagnosis of atopic dermatitis. After cessation of treatment, in order to avoid subsequent exacerbations, at the first signs of atopic dermatitis recurrence, therapy should be resumed. Emollients can be applied immediately after applying 1% Elidel cream. However, after water procedures, emollients should be applied before applying Elidel cream. Considering the very slight systemic absorption of pimecrolimus, the limitations of the total daily dose of the applied preparation, the area of the skin surface being treated or the duration of treatment does not exist. If Elidel cream gets into eyes, mucous membranes (oral or nasal cavity) should be removed immediately and rinsed eyes and mucous membranes with running water.
Side effects
The use of Elidel Cream may cause minor transient reactions at the site of application, such as a feeling of warmth and / or burning.With significant severity of these reactions, patients should consult a doctor. Most often, reactions in the place of use of the drug were observed in 19% of patients receiving treatment with Elidel cream, and in 16% of patients in the control group. These reactions mainly occurred at an early stage of treatment, were minor / moderate and short-lived. Very often - a burning sensation at the site of application of the cream. Frequently - local reactions (irritation, itching and redness of the skin), skin infections (folliculitis). diseases, herpes simplex, dermatitis caused by the herpes simplex virus (herpes eczema), molluscum contagiosum; local reactions, such as rash, pain, paresthesia, peeling, dryness, swelling, skin papillomas, boils. The adverse reactions presented below were observed during post-marketing use of the drug (estimated frequency by the number of cases of adverse events in an unknown population). very rarely - anaphylactic reactions. From the side of metabolism (metabolic disorders): rarely - alcohol intolerance. From the side of skin and its appendages: rarely - allergic reactions (rash, urticaria, angioedema); changes in skin color (hypopigmentation, hyperpigmentation). In most cases, immediately after ingestion of alcohol, facial flushing, rash, burning, itching or swelling developed. . The causal relationship between these adverse events and the use of the drug has not been established.
Overdose
Cases of overdose or accidental use in the application of cream Elidel were not observed.
Interaction with other drugs
The potential interaction of Elidel Cream with other drugs has not been studied. Considering that systemic absorption of pimecrolimus is very insignificant, any interaction of Elidel cream with systemic drugs is unlikely. When using Elidel cream in children 2 years of age and older, the drug did not affect the effectiveness of the vaccination. until complete disappearance of local manifestations of the post-vaccination reaction. Incompatibility. Since compatibility studies have not been conducted, it is not recommended to use the drug in conjunction with other topical agents.
special instructions
In the case of bacterial or fungal skin lesions, use is possible after the infection has cured. Since compatibility studies have not been conducted, it is not recommended to be used in conjunction with other local means.