Elidel (Elidel)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substancePimecrolimusPimecrolimus
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  • Elidel
    cream externally locally cutaneous 
    Meda Pharma GmbH & Co. KG     Germany
    • Dosage form: & nbspCream for external use

    Composition:

    1 g of cream contains 10 mg of pimecrolimus, as well as auxiliary substances: sodium hydroxide 0.20 mg, citric acid anhydrous 0.50 mg, benzyl alcohol 10.00 mg, sodium cetostearyl sulfate 10.00 mg, mono and diglycerides 20.00 mg, cetyl alcohol 40.00 mg, stearic alcohol 40.00 mg, propylene glycol 50.00 mg, oleyl alcohol 100.00 mg, medium chain triglycerides 150.00 mg, water purified 569.30 mg.



    Description:Homogenous cream from white to almost white.

    Pharmacotherapeutic group:anti-inflammatory agent for topical application
    ATX: & nbsp

    D.11.A.H.02   Pimecrolimus

    Pharmacodynamics:Pimecrolimus is a derivative of macromolactam ascomycin and has an anti-inflammatory effect. Pimecrolimus selectively inhibits the production and release of cytokines and inflammatory mediators from T-lymphocytes and mast cells.
    Pimecrolimus specifically binds to the cytosolic receptor macrophilin-12 and inhibits calcium-dependent phosphatase-calcineurin. Inhibition of calcineurin leads to inhibition of T-lymphocyte proliferation and prevents transcription and production in T-helper 1 and type 2 early cytokines such as interleukin-2,interferon-Υ, interleukin-4, interleukin-5, interleukin-10, tumor necrosis factor-α and granulocyte-macrophage colony-stimulating factor. Pimecrolimus and tacrolimus equally suppress the secondary immune response in isolated cell colonies of skin T-helper cells obtained from patients with atopic dermatitis. In vitro pimecrolimus also 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 and, unlike corticosteroids, has a selective effect on the cells of the immune system and does not cause disturbances in function, viability, differentiation processes, maturation of Langerhans cells in mice and dendritic cells of mono-human origin in humans. The drug does not affect the differentiation of "naive" T-lymphocytes in T-effector cells under the action of Langerhans cells and dendritic cells, which is one of the main mechanisms of a specific immune response.
    On experimental models of cutaneous inflammation, the high anti-inflammatory activity of pimecrolimus was demonstrated after its local and systemic use.When topically applied on experimental models of allergic contact dermatitis (AKD) pimecrolimus comparable to
    efficacy with highly active corticosteroids: clobetasol-17-propionate and fluticasone, inhibits the inflammatory response in response to skin irritants without causing a change in the consistency, compaction and atrophy of the skin.
    In addition, with topical and oral administration to
    experimental models of AKD acute flow pimecrolimus effectively reduces skin inflammation, itching and severity of histopathological changes. With topical application, the degree of penetration into the skin of tacrolimus and pimecrolimus equally good. However, the ability of pimecrolimus to penetrate the skin is less than that of tacrolimus and glucocorticosteroids. In this way, pimecrolimus has a selective effect on the skin.
    The uniqueness of the mechanism of action of pimecrolimus is the combination of a selective anti-inflammatory effect on the skin with a slight effect on the systemic immune response.
    When used for 6 weeks in children from 3 months to 17 years pimecrolimus effectively reduces itching and skin inflammation (erythema, infiltration, excoriation and lichenization). With prolonged use within 12 months pimecrolimus effectively reduces the incidence of sudden exacerbations of AKD without causing atrophy, irritation and hypersensitivity to the skin and without phototoxic or photosensitizing effects.




    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 1% Elidel cream twice a day for 3 weeks. In 77.5% of the observations, the pimecrolimus concentration in the blood was below 0.5 ng / ml (the minimum detectable concentration), and in 99.8% - below 1 ng / ml. The maximum value of pimecrolimus concentration in the blood, recorded in one 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, pimecrolimus concentrations in the blood remained low and in most cases were below the minimum detectable concentration.The maximum concentration of 0.8 ng / ml was recorded after 6 weeks of treatment in only two patients. None of the patients showed a rise in concentration during the 12 months of treatment. During the 3-week treatment period, Elidel twice a day in 13 adult patients with dermatitis of the hands (with the application of the cream on the area of ​​the palms and the back of the hands and bandaging overnight), the maximum recorded value of pimecrolimus concentration 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 performed in 58 children aged 3 to 14 years with atopic dermatitis (eczema) with 10-92% of the body surface area treated with 1% Elidel cream twice a day for 3 weeks. Five children were treated for 1 year as needed.
    Pimecrolimus concentrations in the blood were at a consistently low level, regardless of the area of ​​skin lesions and duration of therapy, and were in the same range of values ​​as in adult patients treated with Elidel at the same doses.In 97% of cases, pimecrolimus concentrations in the blood were below 2 ng / ml, and in 60% - below 0.5 ng / ml (the minimum detectable concentration). The maximum value of pimecrolimus concentration, recorded in two patients aged 8 months and 14 years, was 2.0 ng / ml.
    Among the youngest children (from 3 to 23 months), the maximum value of pimecrolimus concentration recorded in one patient was 2.6 ng / ml.
    In five children treated with Elidel for 1 year, the concentrations of pimecrolimus were at a consistently low level. The maximum value registered in one child was 1.94 ng / ml. Throughout the treatment period, the increase in drug concentrations was not observed in any of the patients.
    In 8 children aged 2 to 14 years with a pimecrolimus content in the blood above the minimum detectable concentration, the value of AUC was 5.4-18.8 ng / ml for triplicate measurement. The values ​​of AUC in patients with an area of ​​skin lesions of less than 40% and more than 40% were comparable.
    In in vitro studies, binding of pimecrolimus to plasma proteins (mainly with different lipoproteins) was 99.6%.
    Since the local application of pimecrolimus in the blood is very low, the determination of metabolic parameters is not possible.
    Application in elderly patients
    Atopic dermatitis (eczema) is rarely observed in patients aged 65 years and older. The number of patients of this age in clinical studies of Elidel cream was insufficient to detect any difference in treatment effectiveness compared to young patients.
    Use in children
    Recommendations for dosing 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).
    The drug is indicated for short-term and long-term treatment of atopic dermatitis in adults, adolescents and children (from 3 months).

    Contraindications:Hypersensitivity to pimecrolimus or any components of the drug.
    Children up to 3 months of age (because the safety and effectiveness of using Elidel cream in children younger than 3 months have not been studied).
    Elidel cream should not be applied to skin areas affected by acute viral, bacterial or fungal infections and infections.

    Carefully:Data on the safety of the use of Elidel cream in patients with the syndrome of Netherton and generalized erythroderma are not present. Given the potential for increased systemic absorption of the drug, Elidel cream is not recommended for patients with Netherton syndrome or for severe forms of inflammation or skin lesions (eg, in erythroderma).
    Since the efficacy and safety of using Elidel cream in immunocompromised patients have not been studied, the drug is not recommended for use in this category of patients.
    Data on the safety of prolonged use of Elidel cream are not available.
    Since the effect of prolonged use of the drug on the immune defense of the skin and the frequency of development of malignant neoplasms has not been studied, Elidel cream should not be applied to damaged areas of the skin with possible malignancy or dysplastic changes.
    In the case of bacterial or fungal skin lesions, the use of Elidel cream on affected areas is possible only after curing the infection.

    Pregnancy and lactation:Pregnancy. Data on the application of 1% cream Elidel in pregnant women do not.In experimental studies with local application of the drug direct or mediated damaging effects of Elidel on the course of pregnancy, the development of the embryo / fetus, the course of labor and postnatal development of the offspring was not revealed.
    Care should be taken when prescribing 1% of Elidel cream to pregnant women. However, given the minimum degree of absorption of pimecrolimus in topical application, the potential risk in humans is considered negligible.
    Lactation. Isolation of the drug with breast milk after topical application on experimental models has not been studied. There are no data on the content of pimecrolimus in breast milk in lactating women. Because many drugs are excreted in breast milk, caution should be exercised in appointing 1% of Elidel cream to lactating women. However, given the minimal degree of systemic absorption of pimecrolimus in topical application, the potential risk to humans is considered negligible.
    Nursing women should not apply 1% Elidel cream to the area of ​​the mammary glands.

    Dosing and Administration:Treatment should be started at the first manifestations of the disease in order to prevent a sharp development of its exacerbation.
    1% cream Elidel 2 times a day, apply a thin layer on the affected surface and gently rub until completely absorbed.
    1% Elidel cream can be applied to the skin of any parts of the body, including the head, face, neck, and also on the area of ​​diaper rash.
    Cream Elidel should be applied 2 times a day, until the symptoms disappear completely. If symptoms persist after 6 weeks of use, the patient should be re-examined to confirm the diagnosis of atopic dermatitis. After cessation of treatment, in order to avoid subsequent exacerbations, at the first signs of recurrence of atopic dermatitis therapy should be resumed.
    Emollients can be applied immediately after applying 1% Elidel cream. However, after water treatments, emollients should be used before applying Elidel cream.
    Considering the very insignificant systemic absorption of pimecrolimus, the limitations of the total daily dose of the applied preparation, the area of ​​the skin surface to be treated, or the duration of treatment does not exist.

    Side effects:Applying 1% of Elidel cream can cause minor transient reactions at the site of application, such as a feeling of heat and / or burning.If these reactions are significant, patients should consult a doctor.
    The most common adverse events - reactions at the site of application of the drug were noted in 19% of patients treated with 1% cream Elidel, and 16% of patients in the control group. These reactions mainly occurred at an early stage of treatment, were mild / moderate and short-lived.
    The undesirable phenomena listed below are listed by frequency, starting with the most frequent. The frequency of occurrence of undesirable reactions was evaluated as follows: "very often" >1/10, "often" - >1/100 <1/10, "sometimes" - >1/1000 <1/100, "rarely" -> 1/10 000 <1/1000, "very rarely" - <1/10 000, including individual messages.
    Often: burning in the place of application of cream. Often: local reactions (irritation, itching and redness of the skin), skin infections (folliculitis). Sometimes: suppuration; worsening of the disease; herpes simplex; Dermatitis due to herpes simplex virus (herpetic eczema); molluscum contagiosum, local reactions such as rash, pain, paresthesia, peeling, dryness, swelling, cutaneous papillomas, boils.
    The undesirable reactions presented below were notedat postmarketing use of the drug (frequency estimate by the number of cases of development of AE in an unknown population).
    From the immune system: rarely anaphylactic reactions.
    From the side of metabolism (metabolic disorders): rarely - alcohol intolerance.
    From the skin and its appendages: Rarely allergic reactions (rash, hives, angioedema); changes in skin color (hypopigmentation, hyperpigmentation).
    In most cases, immediately after drinking alcohol, reddening of the face, rash, burning, itching or swelling developed.
    In the case of Elidel cream, malignant tumors, including cutaneous and other types of lymphomas, skin cancer were rarely noted. Causal relationship between these adverse events and the use of the drug is not established.

    Overdose:
    Cases of overdose or accidental use of 1% of Elidel cream inside were not observed.

    Interaction:
    Potential interactions of 1% of Elidel cream with other drugs have not been studied. Given that the systemic absorption of pimecrolimus is very low, any interaction of Elidel cream with drugs for systemic use is unlikely.
    When using Elidel cream in children aged 2 years and older, the drug did not affect the effectiveness of vaccination.
    It is not recommended to apply cream on the area of ​​administration of the vaccine until the local manifestations of postvaccinal reaction disappear completely.
    Incompatibility
    Since compatibility studies have not been conducted, it is not recommended to use the drug in conjunction with other local remedies.


    Special instructions:
    In the treatment of local calcineurin inhibitors, including Elidel, malignant neoplasms (for example, skin tumors and lymphomas) have been observed rarely. Causal relationship between these adverse events and the use of the drug is not established.
    In clinical studies with the use of Elidel cream, 0.9% of patients (14 of 1544) had development of lymphadenopathy. Usually, lymphadenopathy was caused by infectious diseases and disappeared after the course of appropriate antibiotic therapy. All patients either managed to identify the cause of lymphadenopathy or noted the disappearance of this undesirable phenomenon.In patients receiving treatment with Elidel, with the development of lymphadenopathy, it is necessary to establish the etiology of the process and to ensure that patients are monitored until this undesirable phenomenon disappears completely. With an unidentified etiology of lymphadenopathy or the presence of acute mononucleosis in the patient, the drug should be discontinued.
    When treating with Elidel cream, patients are advised to minimize artificial or natural skin insolation to a minimum or completely avoid ultraviolet irradiation. The possible effect of the drug on skin lesions caused by ultraviolet radiation is unknown.


    Effect on the ability to drive transp. cf. and fur:
    The effect of using Elidel cream on the ability to drive vehicles or work with mechanisms is not established.

    Form release / dosage:Cream for external use 1% 15 g, 30 g and 100 g in an aluminum tube.
    Packaging:
    1 tube with instructions for use in a cardboard pack.

    Storage conditions:
    Store at a temperature of no higher than 25 ° C, do not freeze. The drug should be stored out of the reach of children.

    Shelf life:
    2 years.
    The drug should not be used after the expiration date.
    After the first autopsy, use within 1 year.

    Terms of leave from pharmacies:On prescription
    Registration number:П N014689 / 01
    Date of registration:01.10.2007
    The owner of the registration certificate:Meda Pharma GmbH & Co. KGMeda Pharma GmbH & Co. KG Germany
    Manufacturer: & nbsp
    Information update date: & nbsp12.04.2012
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