Elidel, cream 1% 30 g

Pimecrolimus is a derivative of the macrolactam ascomycin and has anti-inflammatory effects. Pimecrolimus selectively inhibits the production and release of cytokines and inflammatory mediators from T-lymphocytes and mast cells. Pimecrolimus specifically binds to cytosolic receptor macrophilin-12 and inhibits calcium-dependent phosphatase – calcineurin.

Inhibition of calcineurin leads to suppression of T-lymphocyte proliferation and prevents transcription and production of early cytokines such as interleukin-2, interferon-γ, interleukin-4, interleukin-5, interleukin-10, tumor necrosis factor-α and granulocyte-macrophage colony-stimulating factor in T helper types 1 and 2.

Pimecrolimus and tacrolimus equally suppress the secondary immune response in isolated skin T-helper cell colonies 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 cells of the immune system and does not cause disturbances in function, viability, differentiation processes, maturation of mouse Langerhans cells and human monocytic dendritic cells. The drug does not affect the differentiation of “naive” T-lymphocytes into T-effector cells under the action of Langerhans cells and dendritic cells, which is one of the main mechanisms of the specific immune response.

High anti-inflammatory activity of pimecrolimus after its local and systemic application was demonstrated on experimental models of skin inflammation. When applied topically on experimental models of allergic contact dermatitis (ACD) pimecrolimus is comparable in effectiveness with highly active corticosteroids: clobetasol – 17-propionate and fluticasone, inhibits the inflammatory response in response to skin irritants without causing changes in skin consistency, thickening and atrophy.

In addition, pimecrolimus effectively reduces skin inflammation, itching and the severity of histopathological changes when used topically and orally in experimental models of acute AKD. When applied topically, the degree of skin penetration of tacrolimus and pimecrolimus is equally good. However, the ability of pimecrolimus to penetrate the skin is less than that of tacrolimus and glucocorticosteroids. Thus, pimecrolimus has a selective action on the skin.

The uniqueness of the mechanism of action of pimecrolimus is the combination of selective anti-inflammatory action on the skin with a minor effect on the systemic immune response.

Pimecrolimus effectively decreases itching and skin inflammation (erythema, infiltration, exoriations and lichenization) when used for 6 weeks in children from 3 months to 17 years old.

With long-term use for 12 months pimecrolimus effectively reduces the frequency of sudden ACD exacerbations without causing atrophy, irritation and increased skin hypersensitivity and without having phototoxic or photosensitizing effect.

Indications

Active ingredient

Composition

How to take, the dosage

Treatment should be started at the first signs of the disease to prevent acute exacerbation.

1% Elidel cream is applied 2 times a day in a thin layer to the affected area and gently rubbed in until completely absorbed.

Eidel 1% cream can be applied to all parts of the body including the head, face and neck as well as areas of diaper rash.

Elidel cream must be used twice a day until the symptoms have completely disappeared. If symptoms persist after 6 weeks of use the patient should be examined again to confirm the diagnosis of atopic dermatitis. After cessation of treatment, in order to avoid further exacerbations, at the first signs of relapse of atopic dermatitis the therapy should be resumed.

Softeners can be used immediately after application of Elidel 1% cream. However, after water procedures, emollients should be used before the application of Elidel cream.

With very little systemic absorption of pimecrolimus, there are no restrictions on the total daily dose to be applied, the area of skin treated, or the duration of treatment.

Interaction

Potential interactions of 1% Elidel cream with other drugs have not been studied. Given that systemic absorption of pimecrolimus is very low, any interaction of Elidel cream with drugs for systemic use is unlikely.

In the use of Elidel cream in children aged 2 years and older, the drug had no effect on the effectiveness of vaccination.

Application of the cream to the vaccine administration areas is not recommended until the local manifestations of postvaccine reaction have completely disappeared.

Incompatibilities

If compatibility studies have not been done, it is not recommended to use the product with other topical agents.

Special Instructions

The treatment with topical calcineurin inhibitors, including Elidel, has rarely resulted in malignancies (e.g., skin tumors and lymphoma). A causal relationship between these adverse events and use of the drug has not been established.

In clinical studies 0.9% of patients (14 out of 1544) developed lymphoadenopathy with Elidel cream. Usually the lymphadenopathy was due to an infectious disease and disappeared after a course of appropriate antibiotic therapy. All patients either managed to identify the cause of lymphadenopathy or this undesirable phenomenon disappeared. In patients treated with Elidel, if lymphadenopathy develops, the etiology of the process should be established and patients should be monitored until this adverse event disappears completely. If the etiology of lymphadenopathy is not established or if the patient has acute mononucleosis inflammation, the drug should be discontinued.

When treating with Elidel cream, patients are recommended to minimize artificial or natural insolation of the skin or to avoid ultraviolet irradiation completely. The possible effects of using the product in UV-induced skin lesions are unknown.

The effect of using Elidel cream on the ability to drive and operate machinery

The effect of using Elidel cream on the ability to drive vehicles or operate machinery has not been established.

Contraindications

Hypersensitivity to pimecrolimus or any of the ingredients of the drug.

Children under 3 months of age (because the safety and effectiveness of Elidel cream in children younger than 3 months has not been studied).

Elidel cream should not be applied to areas of the skin affected by acute viral, bacterial or fungal infections.

With caution:

There are no data on the safety of Elidel cream in patients with Netherton’s syndrome and generalized erythroderma. Because of the possible risk of increased systemic absorption of the drug, Elidel cream is not recommended for use in patients with Netherton’s syndrome or severe inflammation or skin lesions (such as erythroderma).

Because the efficacy and safety of Elidel cream in immunocompromised patients has not been studied, it is not recommended for use in this category of patients.

There is no data on the safety of long-term use of Elidel cream.

As the effects of long-term use on the immune defense of the skin and the incidence of malignancy have not been studied, Elidel cream should not be used on areas of skin lesions with possible carcinogenesis or dysplastic changes.

In case of bacterial or fungal skin lesions, use Elidel cream on affected areas of the skin only after the infection has healed.

Side effects

The use of Elidel 1% cream may cause minor transient reactions at the application site, such as a feeling of warmth and/or burning. If these reactions are significant, patients should consult a physician.

The most common adverse events were injection site reactions in 19% of patients treated with 1% Elidel cream and in 16% of patients in the control group. These reactions occurred mostly in the early phase of treatment, were mild/moderate and of short duration.

The adverse events listed below are listed by frequency, starting with the most frequent. The frequency of adverse reactions was rated as follows: occurring “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 reports.

Very common: burning at the site of application of the cream. Often: local reactions (irritation, itching and redness of the skin), skin infections (folliculitis). Occasionally: suppuration; worsening of disease; herpes simplex; dermatitis due to herpes simplex virus (herpetic eczema); molluscum contagiosum, local reactions such as rash, pain, paresthesias, scaling, dryness, swelling, skin papillomas, furuncles.

The adverse reactions presented below have been reported in post-marketing use of the drug (frequency estimate based on the number of cases of NS in an unspecified population).

Immune system disorders: very rare – anaphylactic reactions.

Metabolic disorders (metabolic disorders): rarely – alcohol intolerance.

Skin and its appendages: rare – allergic reactions (rash, urticaria, angioedema); changes in skin color (hypopigmentation, hyperpigmentation).

In most cases, redness of the face, rash, burning, itching, or swelling developed immediately after alcohol intake.

The development of malignancies, including cutaneous and other types of lymphoma and skin cancer, has been noted in rare cases with Elidel cream. A causal relationship between these adverse events and use of the drug has not been established.

Overdose

Pregnancy use

Pregnancy. There are no data on the use of Elidel 1% cream in pregnant women. In experimental studies no direct or indirect damaging effects of Elidel on pregnancy, embryo/fetal development, the course of delivery and postnatal development of the offspring have been found in local use of the drug.

Caution should be exercised when prescribing Elidel 1% cream to pregnant women. However, given the minimal degree of absorption of pimecrolimus when applied topically, the potential risk in humans is considered negligible.

Lactation. Excretion of the drug in the breast milk after topical administration in experimental models has not been studied. There are no data on the content of pimecrolimus in breast milk in breastfeeding women. Because many drugs are excreted with breast milk, caution should be exercised when prescribing Elidel 1% cream to breastfeeding women. However, given the minimal degree of systemic absorption of pimecrolimus when administered topically, the potential risk to humans is considered negligible.

Lactating women should not apply Elidel 1% cream to the mammary gland area.