Pimecrolimus - instructions for use, doses, side effects, contraindications

Clinical and pharmacological group: & nbsp

Dermatotropona funds

Included in the formulation

Elidel

cream externally locally cutaneous

Meda Pharma GmbH & Co. KG Germany

Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

VED

ONLS

АТХ:

D.11.A.H.02 Pimecrolimus

Pharmacodynamics:Shown, that pimecrolimus has a high affinity for macrophilin-12 (FKBP-12), inhibiting Ca2 + -dependent phosphatase, calcineurin, followed by inhibition of T-cell activation by blocking the transcription of early cytokines. Besides, pimecrolimus Suppresses the synthesis of interleukin-2, interferon-γ (type Th1), interleukins-4 and -10 (type Th2), synthesized by human T-lymphocytes. It also prevents the release of inflammatory cytokines and mediators from mast cells after stimulation with an IgE antigen.

Pharmacokinetics:The connection with plasma proteins is 74-87%. Biotransformation in the liver. When pimecrolimus labeled with a radioactive isotope was ingested, various circulating O-dimethyl metabolites were detected. With local application of signs of the presence of metabolites in the blood is not recorded. Elimination after ingestion with faeces (78,4% in the form of metabolites, less than 1% - in the form of unchanged substance).

Indications:Short-term and intermittent long-term treatment of mild to moderate atopic dermatitis in patients with normal immune status at the age of 2 years and older,in whom the use of alternative conventional therapy is considered undesirable because of the potential risk, or in the treatment of patients resistant to conventional therapy.

ICD-10

XII.L20-L30.L20.8 Other atopic dermatitis

Contraindications:Individual intolerance.

Acute viral (or fungal) skin infections (before the start of therapy it is necessary to clean the affected area).

Atopic dermatitis with secondary infection (before the start of therapy it is necessary to clean the affected area).

Weakened immunity (safety and efficacy unknown).

Neterton syndrome (hereditary combination of congenital ichthyosiform erythroderma, areas of thickening of hair due to invagination of their distal parts into proximal, atopic dermatitis and cataract in women: increased systemic absorption).

Carefully:Kaposi's varioliform pustulosis, herpes simplex, herpes zoster, chicken pox, lymphadenopathy with acute infectious mononucleosis, skin papilloma, pregnancy, breast-feeding.

Pregnancy and lactation:The category of action on the fetus by FDA is C. In pregnancy, the drug can be used only if necessary.Breastfeeding women should stop breastfeeding, or use a cream.

Dosing and Administration:Locally (in the form of 1% cream), apply a thin layer on the affected skin 2 times a day, gently and completely rubbing, until the symptoms of the disease come to rest. The maximum duration of therapy is 6 weeks. If the symptoms persist during this time, a revision of the diagnosis is necessary.

Side effects:Infections: bacterial infections; viral infections: chicken pox, herpes zoster, herpes simplex; infections of the upper respiratory tract: influenza, tonsillitis, rhinopharyngitis, streptococcal pharyngitis, sinusitis; pneumonia, skin infection: folliculitis, molluscum contagiosum, impetigo; infection of the eye; ear infections, including otitis media.

Digestive system: gastroenteritis, diarrhea, abdominal pain, constipation, nausea, vomiting.

Respiratory system and ENT organs: bronchitis, asthma, dyspnoea, perspiration in the throat, nosebleeds, nasal congestion, rhinorrhea, hyperemia of the mucous membrane of the paranasal sinuses.

Hypersensitivity reactions, hives.

Reactions in the place of application of the cream, skin rupture, burning, irritation, itching at the site of application of cream, acne, erythema skin at the site of application of cream, papilloma of the skin, local reactions.

Headache.

Reproductive system: dysmenorrhea.

Carcinogenicity / mutagenicity.

Hyperthermia, back pain, arthralgia, toothache, suppuration of the skin, worsening of the existing disease. Clinical studies have described rare cases (0.9%) of lymphadenopathy due to concomitant infection, with a rapid normalization of the condition with adequate antibiotic therapy.

Changes in laboratory tests: it is possible to increase the concentration of glucose in the blood plasma.

Overdose:Clinical experience of treatment and cases of unintentional overdose inside is not described, symptomatic therapy is recommended. When deliberate admission is necessary to consult a psychiatrist. Treatment is symptomatic.

Interaction:Inhibitors of CYP3A (erythromycin, itraconazole, ketoconazole, fluconazole, calcium channel blockers, cimetidine) - should be used with caution pimecrolimus in patients with advanced skin lesions and / or erythroderma.

Potential interactions of pimecrolimus with other drugs, including vaccination, have not been studied.

With topical application of pimecrolimus, a small amount of active substance is absorbed into the systemic circulation.

It is not recommended to use simultaneously with other drugs for external use.

Special instructions:Monitoring of the dynamics of atopic dermatitis symptoms and signs of relapse (with the normalization of the treatment with pimecrolimus should be discontinued); when severe skin reactions or lack of dynamics for more than 1 week of therapy, it is necessary to consider the question of its cessation; if the condition worsens at any time of therapy or there is no improvement in atopic dermatitis within 6 weeks of therapy, consideration should also be given to discontinuing therapy.

Instructions

Pimecrolimus (Pimecrolimusum)