Tacropic - instructions for use, dose, side effects, contraindications

active substance: tacrolimus in terms of 100% substance - 0.03 g; Excipients: Macrogol-400 - 10.0 g; paraffin liquid - 20.0 g; Vaseline white soft - 5.0 g; wax emulsion - 10,0 g; disodium edetate - 0.05 g; preservative Euxyl PE 9010 (phenoxyethanol 90%, ethylhexylglycerol 10%) in terms of phenoxyethanol - 0.45 g; purified water - up to 100 g.

100 g ointments (0.1%) contain:

active substance: tacrolimus in terms of 100% substance - 0.10 g; Excipients: Macrogol-400 - 15.0 g; paraffin liquid - 20.0 g; Vaseline white soft - 5.0 g; wax emulsion - 10.0 g; disodium edetate - 0.05 g; preservative Euxyl PE 9010 (phenoxyethanol 90%, ethylhexylglycerol 10%) in terms of phenoxyethanol - 0.45 g; purified water - up to 100 g.

Description:

Homogeneous ointment is white or almost white. A weak specific odor is allowed.

Pharmacotherapeutic group:Anti-inflammatory agent for topical application

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, FKBPI2, 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-α). which take part in the initial stages of activation of T-lymphocytes. In addition, under the influence of tacrolimus, the release of inflammatory mediators from mast cells, basophils and eosinophils is inhibited, as well as a decrease in expression FcɛRI (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:

Absorption. Absorption of tacrolimus in the systemic blood stream with topical application is minimal. In most patients with atopic dermatitis (in adults and children), both in single application and repeated use of 0.03% and 0.1% of tacrolimus ointment, its plasma concentration was <1.0 ng / ml.Systemic absorption depends on the area of the lesion and decreases with the disappearance of clinical manifestations of atopic dermatitis. Cumulation of the drug with prolonged use (up to 1 year) in children and adults was not noted.

Distribution. Due to the fact that systemic absorption of the tacrolimus ointment is low, a high ability to bind to plasma proteins (more than 98.8%) is regarded as clinically insignificant.

Metabolism. Tacrolimus not metabolized in the skin. When entering the systemic circulation tacrolimus is largely metabolized in the liver by isoenzyme CYP3A4.

Excretion. With repeated local application of the tacrolimus ointment, the elimination half-life is 75 hours in adults and 65 hours in children.

Indications:

Takropik® drug used in a dosage of 0.03% and 0.1% for adults and adolescents over 16 years, and only 0.03% for children 2 to 16 years for the treatment of atopic dermatitis (moderate and severe) in the event its resistance to other means of external therapy or the presence of contraindications to such.

Contraindications:

Hypersensitivity to tacrolimus, auxiliary components of the drug, macrolides.

Pregnancy and the period of breastfeeding.

Tacropic® should not be used in patients with severe disorders of the epidermal barrier, in particular, the Netherton syndrome, lamellar ichthyosis, cutaneous manifestations of the "graft versus host" reaction, and generalized erythroderma due to the risk of increased systemic absorption of tacrolimus. The use of Tacropic® in a dosage of 0.1% is contraindicated in children and adolescents under 16 years of age, at a dosage of 0.03% in children under 2 years of age.

Carefully:

Tacrolimus is largely metabolized in the liver, and although its concentration in the blood with external application is very low, in patients with uncompensated hepatic insufficiency, ointment is used with caution.

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

Dosing and Administration:

Adults and children over 2 years of preparation Tacropic® are applied a thin layer on the affected skin areas. The drug can be used on any part of the body, including the face and neck, in the area of skin folds.Do not apply the drug to the mucous membranes and under occlusive dressings.

Use in children (2 years and older) and adolescents under 16 years

Treatment should begin with the application of 0.03% Tacropic® ointment twice a day. The duration of treatment under this scheme should not exceed three weeks. In the future, the frequency of application is reduced to once a day, the treatment is continued until the foci of lesion are completely cleared.

Application in adults and adolescents 16 years and older

Treatment should begin with the application of 0.1% Tacropic® ointment twice a day and continue until the foci of lesion are completely cleared. As you improve, you can reduce the frequency of applying 0.1% of the ointment, or switch to using 0.03% of Tacropic® ointment. In case of recurrence of symptoms, resumption of treatment with 0.1% Tacropic® ointment should be resumed twice a day. If the clinical picture allows, an attempt should be made to reduce the frequency of application of the drug, or use a lower dosage of 0.03% Tacropic® ointment.

Use in elderly people (65 years and older)

There are no special applications for elderly people.Usually, improvement is observed within one week from the start of therapy. If signs of improvement in the background of therapy are absent for two pedlels, consideration should be given to changing the therapeutic tactics.

Treatment of exacerbations

The drug Tacropic® can be used for a short time or for a long time in the form of periodically repeated courses of therapy. Treatment of affected areas of the skin is carried out until the disappearance of clinical manifestations of atopic dermatitis. As a rule, improvement is observed during the first week of treatment. If signs of improvement are not observed within two weeks of starting the use of the ointment, other options for further treatment should be considered. Treatment should be resumed with the appearance of the first signs of exacerbation of atopic dermatitis.

Prevention of exacerbations

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, supportive therapy with Tacropic® 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, Tacropic® ointment should be applied 2 times a week (for example, on Monday and Thursday) on skin areas usually affected by exacerbations.

The time between application of the drug should be at least 2-3 days.

Adults and adolescents 16 years of age and older use 0.1% Tacropic® ointment, in children (2 years and older) - 0.03% Tacropic® ointment. If signs of exacerbation appear, you should switch to the usual regimen of Tacropic® ointment (see "Treatment of exacerbations").

After 12 months of maintenance therapy, it is necessary to assess the clinical dynamics and decide whether to continue the prophylactic use of Tacropic®. 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 application site.

As a rule, they are moderately expressed and pass within the first week after the start of treatment.

Often there is intolerance to alcohol (redness of the face or symptoms of skin irritation after drinking alcohol).

Patients using the drug Tacropic®, there is an increased risk of developing folliculitis, acne and herpetic infection.

But the frequency of occurrence of unwanted reactions are distributed as follows: very often (≥ 1/10); often (≥ 1/100, <1/10); infrequently (≥ 1/1 000, <1/100); rarely (≥ 1/10 000, <1/1 000), very rarely (<1/10 000), the frequency is unknown (insufficient data to estimate the frequency of development). Within each group, undesirable reactions are presented in descending order of significance.

Infectious diseases: often - local skin infections, regardless of etiology (in particular, but not limited to, herpes zoster Kaposi, folliculitis, infection caused by the virus Herpes simplex, Other infections caused by viruses in the family Herpesviridae).

Disorders from the metabolism and nutrition: often - alcohol intolerance (face hyperemia or symptoms of skin irritation after drinking).

Impaired nervous system: often - paresthesia, hyperesthesia.

Disturbances from the skin and subcutaneous tissues: often - folliculitis, itching; infrequently - acne.

General disorders and disorders at the site of administration: very often - burning and itching in the area of application; often - a feeling of warmth, redness, pain, irritation, rash in the area of application; frequency unknown - edema in the field of application.

During the entire period of observation of the drug, single cases of rosacea, malignization (cutaneous and other types of lymphomas, skin cancer) were recorded.

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 ns is metabolized in the skin, which eliminates 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 isoenzyme inhibitors CYP3A4 (including erythromycin, itraconazole, ketoconazole, diltiazem) with simultaneous use with the drug Tacropic® is unlikely, but can not be completely ruled out in patients with extensive lesionsand / or erythroderma.

The effect of Tacropic® on the effectiveness of vaccination has not been studied. However, due to the potential risk of decreased efficacy, vaccination should be given prior to the application of the ointment or 14 days after the last use of Tacropic®. If a live attenuated vaccine is used, this period should be increased to 28 days, otherwise alternative vaccines should be considered.

The simultaneous use of tacrolimus with a conjugate vaccine against Neisseria meningitidis Serotype C in children from 2 to 11 years of age has no effect on the primary response to vaccination, the formation of immune memory, as well as the humoral and cellular immune response.

The possibility of using Tacropic® together with other external drugs, systemic glucocorticosteroids and immunosuppressants has not been studied.

Special instructions:

Tacropic® can not be used with nazis with congenital or acquired immunodeficiencies or in patients who take immunosuppressive drugs.

During application of Tacropic® ointment, skin contact with sunlight should be avoided. rays, a visit to the solarium, therapy with ultraviolet rays B or A in combination with psoralenom (PUVA-therapy).

Tacropic® should not be used to treat lesions that are considered to be potentially malignant or pre-malignant.

For 2 hours on the skin areas on which the drug Tacropic® was applied, you can not use emollients.

The efficacy and safety of Tacropic® in the treatment of infected atopic dermatitis was not assessed. If signs of infection exist prior to the administration of Tacropic®, appropriate therapy is necessary. The use of Tacropic® may be associated with an increased risk of developing herpetic infection. In the presence of signs of herpetic infection, the relationship between the benefits and risks of using Tacropic® should be evaluated individually.

In the presence of lymphadenopathy, the patient should be examined before starting therapy and observed during the period of application of the drug. In the absence of an obvious cause of lymphadenopathy or in the presence of symptoms of acute infectious mononucleosis, the use of Tacropic® should be discontinued.

Avoid contact with eyes and mucous membranes (if accidentally ingested, the ointment must be carefully removed and / or rinsed with water).

It is not recommended to apply Tacropic® Ointment under occlusive dressings and wear tight, airtight clothing.

Just like using 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 for therapeutic purposes.

It was shown that in children aged 2 to 11 years, treatment with tacrolimus ointment 0.03% against vaccination with conjugated vaccine against Neisseria meningitidis Serotype C does not affect the primary response to vaccination, the induction of the T-cell immune response, and the formation of immune memory.

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

Studies on the effect of the drug on the ability to drive a car and on the speed of reaction when working with complex techniques that require increased attention were not conducted. Tacropic® is used externally and there is no reason to believe that it can affect the ability to drive and work with machinery.

Form release / dosage:

Ointment for external use 0.03% and 0.1%.

Packaging:

For 15 g in an aluminum tube. Each tube together with the instruction for use is placed in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LP-003169

Date of registration:31.08.2015

The owner of the registration certificate:AKRIKHIN HFK, JSC AKRIKHIN HFK, JSC Russia

Manufacturer: & nbsp

AKRIKHIN HFK, JSC Russia

Information update date: & nbsp02.03.2016

Illustrated instructions

Instructions

Tacropic® (Tacropic)