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

Excipients: paraffin white soft 77.47 / 77.40 t, paraffin liquid 11.00 / 11.00 g, propylene carbonate 5,00 / 5,00, beeswax white 3.50 / 3.50 g, paraffin wax 3.00 / 3.00 g

Description:Ointment of a homogeneous consistency from white to slightly yellowish color.

Pharmacotherapeutic group:anti-inflammatory for topical use.

Pharmacodynamics:

Tacrolimus belongs to the group of calcineurin inhibitors. It binds to a specific cytoplasmic protein called immunophilin (FKBP12), which is a cytosolic receptor for calcineurin (FK506). As a result, a complex is tacrolimus, FKBP12, calcium, calmodulin and calcineurin, which leads to inhibition of the phosphatase activity of calcineurin. This makes it impossible to dephosphorylate and translocate the nuclear factor of activated T cells (NFAT), necessary for the initiation of transcription of genes encoding the production of key cytokines for the T-cell immune response (IL-2 and interferon-gamma). Besides, tacrolimus inhibits the transcription of genes encoding the production of such cytokines as IL-3, IL-4, IL-5, granulocyte-macrophage colony-stimulating factor (GMPCS) and tumor necrosis factor (TNF-a) that participate in the initial stages of T-lymphocyte activation .In addition, under the influence of tacrolimus, inhibition of the release of inflammatory mediators from mast cells, basophils and eosinophils, as well as a decrease in expression FceRI (high affinity surface receptor for immunoglobulin E) on Langerhans cells, which leads to a decrease in their activity and presentation of the antigen to T lymphocytes.

Ointment tacrolimus does not affect the synthesis of collagen and, thus, does not cause skin atrophy.

Pharmacokinetics:

Tacrolimus belongs to the group of calcineurin inhibitors. It binds to a specific cytoplasmic protein called immunophilin (FKBP12), which is a cytosolic receptor for calcineurin (FK506). As a result, a complex is tacrolimus, FKBP12, calcium, calmodulin and calcineurin, which leads to inhibition of the phosphatase activity of calcineurin. This makes it impossible to dephosphorylate and translocate the nuclear factor of activated T cells (NFAT), necessary for the initiation of transcription of genes encoding the production of key cytokines for the T-cell immune response (IL-2 and interferon-gamma). Besides, tacrolimus inhibits the transcription of genes encoding the production of such cytokines as IL-3, IL-4, IL-5, granulocyte-macrophage colony-stimulating factor (GMPCS) and tumor necrosis factor (TNF-a) that participate in the initial stages of T-lymphocyte activation . In addition, under the influence of tacrolimus, inhibition of the release of inflammatory mediators from mast cells, basophils and eosinophils, as well as a decrease in expression FceRI (high affinity surface receptor for immunoglobulin E) on Langerhans cells, which leads to a decrease in their activity and presentation of the antigen to T lymphocytes.

Ointment tacrolimus does not affect the synthesis of collagen and, thus, does not cause skin atrophy.

Indications:

Ointment Protopik ® is used in a dosage of 0.03% and 0.1% in adults and only 0.03% in children from 2 to 16 years for the treatment of atopic dermatitis (moderate severity and severe forms) in case of its resistance to other agents of the external therapy or the presence of contraindications to such.

Contraindications:

Hypersensitivity to tacrolimus, to auxiliary substances, to macrolides.

Pregnancy and breastfeeding.

Do not use Protopik® patients with severe impairment epidermal barrier, in particular, syndrome, lamellar ichthyosis, cutaneous manifestations of the reaction "graft versus host," and with generalized erythroderma due to the risk of increasing systemic absorption of tacrolimus.

The use of ointment Protopik® in dosage 0.1% contraindicated in children and adolescents younger than 16 years, at a dosage of 0.03% - in children younger than 2 years.

Carefully:

Protopik ® is largely metabolized in the liver, and although its concentration in the blood for external use is very low, in patients with decompensated hepatic Insufficiency of the ointment is used with caution.

Care must be taken when using Protopik ® ointment in patients with extensive skin lesions, long courses, especially in children.

Pregnancy and lactation:contraindicated

Dosing and Administration:

Adults and children over 2 years ointment Protopik® is applied with a thin layer of affected areas of the skin. A drug can be used in any area body, including face and neck, in area of skin folds. Do not do it apply a drug on mucous membranes "Shells and under occlusive bandages.

Application v children (2 year and older) and adolescents under 16 years of age

Treatment should begin with Applying 0.03% ointment Protopik® two times a day. Duration treatment under this scheme should not exceed three weeks. AT further frequency of use is reduced to once a day, the treatment is continued until the foci of lesion are completely cleared.

Application v adults and teenagers 16 years and over

Treatment should begin with the application of 0.1% ointment Protopik ® twice a day and continue until complete clearance of lesions. As you improve, you can reduce the frequency of applying 0.1% of the ointment or switch to the use of 0.03% ointment Protopik ®. In case of recurrence of symptoms, resumption of treatment with 0.1% ointment Protopik® twice a day should be resumed. If the clinical picture allows, attempt to reduce the frequency of use of the drug, or use a lower dosage - 0.03% ointment Protopik ®.

Application v people elderly age (65 years and over)

There are no special applications for elderly people.

Usually improvement is observed in within one week from the moment initiation of therapy. If the signs improvement on the background of therapy are absent for two weeks, should consider changing therapeutic tactics.

Treatment of exacerbations

Ointment Protopik® can used for a short time or durably in the form of periodically repeated courses of therapy.

Treatment of affected skin is carried out until complete disappearance clinical manifestations atopic dermatitis. how rule, improvement is observed in during the first week of treatment. If Signs of improvement are not observed within two weeks of the beginning of the use of ointment, need to consider other options for further treatment.

Treatment should be resumed when appearance of the first signs exacerbation of atopic dermatitis.

To prevent exacerbations and increase the duration of remission in patients with frequent (more than 4 times a year) exacerbation of the disease in history, maintenance therapy with ointment Protopik® is recommended. The expediency of prescribing maintenance therapy is determined by the effectiveness of the previous treatment according to the standard schedule (2 times a day) for no more than 6 weeks.

With maintenance therapy Protipik ® ointment should be applied 2 times a week (for example, on Monday and Thursday) on skin areas, usually amazed at exacerbations.

The time between application of the drug should be at least 2-3 days. Adults and adolescents are 16 years old and over 0.1% ointment is used Protopik®, v children (2 year and older) - 0.03% ointment Protopik®. When manifestation of signs of exacerbation go to the normal mode with ointment Protopik® (see section "Treatment of exacerbations").

After 12 months of maintenance therapy, it is necessary to evaluate the clinical dynamics and decide whether to continue the prophylactic use of Protopik ® ointment. Children should be temporarily discontinued to assess clinical dynamics and then consider whether to continue supporting therapy.

Side effects:The most frequent adverse reactions are symptoms of skin irritation (burning sensation and itching, redness, pain, paresthesia and rash) at the site of application. how they are usually expressed moderately or slightly and pass during the first week after the start of treatment.

Often there is intolerance alcohol (redness of the face or symptoms of skin irritation after consumption of alcoholic beverages).

Patients who use ointment Protopik®, there is an increased risk development of folliculitis, acne and herpetic infection.

Frequency of occurrence undesirable reactions are divided into very frequent (> 1/10), frequent (> 1/100, <1/10) and rare (>1 / 1,000, <1/100). Within each group unwanted reactions are presented in order of decreasing importance.

Common Disorders and Local Reactions

Very frequent: burning and itching in place application.

Frequent: sensation of heat, redness, pain, irritation, rash in place of application

With unknown frequency: edema at the site of application

Infekia

Frequent: Local skin infections regardless of etiology. AT particular (but not limited to listed), it is herpetic eczema Kalosha, folliculitis, infection, virus-induced Herpes simplex, others infections caused by viruses of the family Herpesviridae).

Skin and subcutaneous tissue

Frequent: folliculitis, itching.

Infrequent: acne.

Nervous system

Frequent: paresthesia, hyperesthesia.

Metabolism

Frequent: alcohol intolerance (congestion of the face or symptoms irritation of the skin after use alcoholic beverages).

For the entire period of drug observation single cases of rosacea, malignancy (skin and other types of lymphomas, skin cancer).

Overdose:

When topical application of cases of overdose was not noted.

When ingested, it is necessary to take common measures, which include monitoring of vital body functions and monitoring the general condition.

Stimulation of vomiting or gastric lavage is not recommended.

Interaction:

Tacrolimus is not metabolized in the skin, which excludes the risk of drug interactions in the skin that can affect its metabolism.

Since the systemic absorption of tacrolimus when used in the form of an ointment is minimal, the interaction with inhibitors of isoenzyme CYP3A4 (at including erythromycin, itraconazole, ketoconazole, diltiazem) with simultaneous application with ointment Protopik "is unlikely, but not can be completely ruled out patients with extensive areas lesions and / or erythroderma.

Effect of the ointment Protopik on the effectiveness vaccination has not been studied. However, due to potential risk of decline effectiveness, vaccination is necessary carry out before the application of the ointment or 14 days after the last use ointment Protopik ®. When use of live attenuated vaccine, this period should be increased to 28 days, otherwise should consider use of alternative vaccines.

Use in children A study on the interaction with conjugated vaccine against Neisseria menigitidis serotype C, in which children aged 2 to 11 years. The results of this study evidence that simultaneous application of tacrolimus did not The impact on the primary response to vaccination, the formation of immune memory, as well as humoral and cellular immune response.

Ability to share applications ointments Protopik® with other external drugs, systemic glucocorticosteroids and immunosuppressants has not been studied.

Special instructions:

Ointment Protopik® can not be used for patients with congenital or acquired immunodeficiencies or in patients who take immunosuppressive drugs.

During the application of the ointment Protopik® it is necessary to minimize the impact on the skin of the sun, visit solarium, ultraviolet therapy rays B or A in combination with psoralenom (PUVA-therapy).

Protopik® ointment should not be used for the treatment of lesions that are are considered as potentially malignant or pre-cancerous.

Within 2 hours on the skin areas, on the which were applied ointment Protopik ®, It is not possible to use emollients facilities.

Efficiency and safety ointment application Protopik® in treatment infected atopic dermatitis was not evaluated. If signs of infection are present prior to the appointment of Protopik® ointment, appropriate therapy is necessary. The use of Protopik® ointment may be associated with an increased risk of developing a herpetic infection. In the presence of signs of herpetic infection, one should individually evaluate the relationship between the benefit and the risk of using Protopika.

In the presence of lymphadenopathy, the patient should be examined before starting therapy and observed during the period of application of the ointment. In the absence of an obvious cause of lymphadenopathy or in the presence of symptoms of acute infectious mononucleosis, it is necessary to stop using the Protopik® ointment.Avoid contact with ointment in the eyes and mucous membranes (in case of accidental ingestion, the ointment should be carefully removed and / or rinsed with water). It is not recommended to apply Protopik® ointment for occlusive dressings and wear tight, airtight clothing.

As with any other topical medication, patients should wash their hands after applying the ointment, except when the ointment is applied to the area of the hands with therapeutic purpose.

Use in children

As part of a clinical study, conducted on children aged 2 to 11 years to study the impact on their at the stage of development immune system, it was demonstrated that the treatment with ointment tacrolimus 0.03% against vaccination conjugated vaccine against Neisseria menigitidis serotype C is not influenced the primary response to vaccination, induction of T-cell immune response and the formation of immune memory.

Effect on the ability to drive transp. cf. and fur:

Studies on the influence of ointment on ability to drive and speed of reaction when working with complex technique, requiring increased attention, were not conducted. Ointment Protopik ® is applied externally and not reason to believe that it can influence the ability of drive and work with mechanisms.

Form release / dosage:

Ointment for external use 0.03% and 0.1%.

For 10, 30 or 60 grams of ointment for external use in plastic tubes.

1 tube with instructions for use in cardboard pack.

Packaging:plastic tubes (1) - packs, cardboard

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years. Do not use the product after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-001885/10

Date of registration:12.03.2010

The owner of the registration certificate:Astellas Farma Europe BVAstellas Farma Europe BV Netherlands

Manufacturer: & nbsp

ASTELLAS PHARMA TECH, Co Ltd. Japan

Representation: & nbspASTELLAS PHARMA YUROP BV ASTELLAS PHARMA YUROP BV Netherlands

Information update date: & nbsp02.09.2015

Illustrated instructions

Instructions

Protopik® (Protopic®)