Tacropic ointment 0.1%, 15 g

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

For adults and children over 2 years of age, TacropicЃ is applied in a thin layer to the affected skin. The drug can be used on any part of the body, including the face and neck, in the area of ??skin folds. The drug should not be applied to mucous membranes and under occlusive dressings.
Use in children (2 years of age and older) and adolescents under 16 years of age

Treatment should begin with the application of 0.03% TacropicЃ ointment twice a day. The duration of treatment according to this scheme should not exceed three weeks. In the future, the frequency of use is reduced to once a day, the treatment continues until the lesions are completely cleared.
Application in adults and adolescents 16 years of age and older
Treatment should begin with the use of 0.1% TacropicЃ ointment twice a day and continue until the lesions are completely cleared. As you improve, you can reduce the frequency of applying 0.1% ointment and switch to using 0.03% TacropicЃ ointment. In case of recurrence of symptoms of the disease, treatment with 0.1% TacropicЃ ointment should be resumed twice a day.
If the clinical picture allows, an attempt should be made to reduce the frequency of drug use, or use a lower dosage - 0.03% TacropicЃ ointment.
Application in elderly people (65 years and older) There are no
specific features of application in elderly people. Usually, improvement is observed within one week from the start of therapy. If there are no signs of improvement with therapy within two weeks, a change in therapeutic tactics should be considered.
Treatment of exacerbations
The drug TakropicЃ can be used short-term or long-term in the form of periodically repeated courses of therapy. Treatment of the affected skin areas is carried out until the clinical manifestations of atopic dermatitis disappear completely. Typically, improvement is seen within the first week of treatment. If signs of improvement are not observed within two weeks of starting using the ointment, other options for further treatment should be considered. Treatment should be resumed at the first signs of exacerbation of atopic dermatitis.
Prevention of exacerbations
To prevent exacerbations and increase the duration of remission in patients with a history of frequent (more than 4 times a year) exacerbations of the disease, maintenance therapy with TacropicЃ is recommended.
The feasibility of prescribing maintenance therapy is determined by the effectiveness of previous treatment according to the standard scheme (2 times a day) for no more than 6 weeks.
With maintenance therapy, TacropicЃ ointment should be applied 2 times a week (for example, on Monday and Thursday) to the areas of the skin usually affected by exacerbations.
The time interval between application of the drug should be at least 2 - 3 days.
In adults and adolescents 16 years of age and older, 0.1% TacropicЃ ointment is used, in children (2 years and older) - 0.03% TacropicЃ ointment. If signs of exacerbation appear, you should switch to the usual regimen of therapy with TacropicЃ ointment (see the section 'Treatment of exacerbations'). After 12 months of maintenance therapy, it is necessary to assess the clinical dynamics and decide on the advisability of continuing the prophylactic use of TacropicЃ. In children, to assess clinical dynamics, the drug should be temporarily discontinued and then the need to continue supportive therapy should be considered.

.100 g of ointment (0.1%) contain:
active substance: tacrolimus in terms of 100% substance - 0.10 g;
excipients : macrogol - 400 - 15.0 g; liquid paraffin - 20.0 g; white soft petroleum jelly - 5.0 g; emulsion wax - 10.0 g; disodium edet - 0.05 g; preservative Euxyl PE 9010 (phenoxyethanol 90%, ethylhexylglycerol 10%) in terms of phenoxyethanol - 0.45 g; purified water - up to 100 g.

Hypersensitivity to tacrolimus, auxiliary components of the drug, macrolides.
Pregnancy and the period of breastfeeding.
TacropicЃ should not be used in patients with serious disorders of the epidermal barrier, in particular, Netherton's syndrome, lamellar ichthyosis, skin manifestations of the graft-versus-host reaction, as well as in generalized erythroderma due to the risk of increased systemic absorption of tacrolimus.
The use of TacropicЃ in a dosage of 0.1% is contraindicated in children and adolescents under 16 years of age, in a dosage of 0.03% in children under 2 years of age.
Carefully

Tacroldimus is largely metabolized in the liver, and although its concentration in the blood when applied topically is very low, the ointment is used with caution in patients with decompensated liver failure.
Care must be taken when using TacropicЃ ointment in patients with extensive skin lesions, long courses, especially in children.

Trade name of the drug:

TacropicЃ

International non-proprietary name:

tacrolimus

Dosage form:

topical ointment

Composition:

100 g of ointment (0.03%) contain:
active substance: tacrolimus in terms of 100% substance - 0.03 g;
excipients : macrogol - 400 - 10.0 g; liquid paraffin - 20.0 g; white soft petrolatum -5.0 g; emulsion wax - 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 of ointment (0.1%) contain:
active substance: tacrolimus in terms of 100% substance - 0.10 g;
excipients : macrogol - 400 - 15.0 g; liquid paraffin - 20.0 g; white soft petroleum jelly - 5.0 g; emulsion wax - 10.0 g; disodium edet - 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 white or almost white ointment. The presence of a weak specific odor is allowed

Pharmacotherapeutic group:

anti-inflammatory agent for topical use.

ATX code:

D11AH01

Pharmacological properties

Pharmacodynamics
Tacrolimus belongs to the group of calcineurin inhibitors. It binds to a specific cytoplasmic protein immunophilin (FKBP12), which is the cytosolic receptor for calcineurin (FK506). As a result, a complex is formed that includes tacrolimus, FKBP12, calcium, calmodulin and calcineurin, which leads to inhibition of the phosphatous activity of calcineurin. This makes it impossible for dephosphorylation and translocation of the nuclear factor of activated T cells (NFAT), which is necessary for the initiation of transcription of genes encoding the production of cytokines, key for the T-cell immune response (IL-2 and interferon-gamma). In addition, tacrolimus inhibits the transcription of genes encoding the production of cytokines such as IL-3, IL-4, IL-5, granulocyte macrophage colony-stimulating factor (GM-CSF) and tumor necrosis factor (TNF-?),which take part in the initial stages of T-lymphocyte activation. 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 the expression of FcsRI (high-affinity surface receptor for immunoglobulin E) on Langerhans cells, which leads to a decrease in their activity and antigen presentation to T-lymphocytes. Tacrolimus ointment does not interfere with collagen synthesis and thus does not cause skin atrophy.which leads to a decrease in their activity and antigen presentation to T-lymphocytes. Tacrolimus ointment does not interfere with collagen synthesis and thus does not cause skin atrophy.which leads to a decrease in their activity and antigen presentation to T-lymphocytes. Tacrolimus ointment does not interfere with collagen synthesis and thus does not cause skin atrophy.

Pharmacokinetics
Absorption . The absorption of tacrolimus into the systemic circulation when applied topically is minimal. In most patients with atopic dermatitis (in adults and children), both with a single application and with repeated use of 0.03% and 0.1% tacrolimus ointment, its concentration in blood plasma was <1.0 ng / ml. Systemic absorption depends on the area of ??the lesion and decreases as the clinical manifestations of atopic dermatitis disappear. Cumulation of the drug with prolonged use (up to 1 year) in children and adults was not observed.
Distribution. Due to the fact that the systemic absorption of tacrolimus ointment is low, the high ability to bind to plasma proteins (more than 98.8%) is considered clinically insignificant.
Metabolism... Tacrolimus is not metabolized in the skin. When it enters the systemic circulation, tacrolimus is largely metabolized in the liver by the CYP3A4 isoenzyme.
Excretion . With repeated topical application of tacrolimus ointment, the half-life is 75 hours in adults and 65 hours in children.

Indications for use

The drug TacropicЃ is used at a dosage of 0.03% and 0.1% in adults and adolescents over 16 years old, and only 0.03% in children from 2 to 16 years old for the treatment of atopic dermatitis (moderate and severe) in the case of 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.
TacropicЃ should not be used in patients with serious disorders of the epidermal barrier, in particular, Netherton's syndrome, lamellar ichthyosis, skin manifestations of the graft-versus-host reaction, as well as in generalized erythroderma due to the risk of increased systemic absorption of tacrolimus.
The use of TacropicЃ in a dosage of 0.1% is contraindicated in children and adolescents under 16 years of age, in a dosage of 0.03% in children under 2 years of age.
Carefully

Tacroldimus is largely metabolized in the liver, and although its concentration in the blood when applied topically is very low, the ointment is used with caution in patients with decompensated liver failure.
Care must be taken when using TacropicЃ ointment in patients with extensive skin lesions, long courses, especially in children.

Method of administration and dosage

For adults and children over 2 years of age, TacropicЃ is applied in a thin layer to the affected skin. The drug can be used on any part of the body, including the face and neck, in the area of ??skin folds. The drug should not be applied to mucous membranes and under occlusive dressings.
Use in children (2 years of age and older) and adolescents under 16 years of age

Treatment should begin with the application of 0.03% TacropicЃ ointment twice a day. The duration of treatment according to this scheme should not exceed three weeks. In the future, the frequency of use is reduced to once a day, the treatment continues until the lesions are completely cleared.
Application in adults and adolescents 16 years of age and older
Treatment should begin with the use of 0.1% TacropicЃ ointment twice a day and continue until the lesions are completely cleared. As you improve, you can reduce the frequency of applying 0.1% ointment and switch to using 0.03% TacropicЃ ointment. In case of recurrence of symptoms of the disease, treatment with 0.1% TacropicЃ ointment should be resumed twice a day.
If the clinical picture allows, an attempt should be made to reduce the frequency of drug use, or use a lower dosage - 0.03% TacropicЃ ointment.
Application in elderly people (65 years and older) There are no
specific features of application in elderly people. Usually, improvement is observed within one week from the start of therapy. If there are no signs of improvement with therapy within two weeks, a change in therapeutic tactics should be considered.
Treatment of exacerbations
The drug TakropicЃ can be used short-term or long-term in the form of periodically repeated courses of therapy. Treatment of the affected skin areas is carried out until the clinical manifestations of atopic dermatitis disappear completely. Typically, improvement is seen within the first week of treatment. If signs of improvement are not observed within two weeks of starting using the ointment, other options for further treatment should be considered. Treatment should be resumed at the first signs of exacerbation of atopic dermatitis.
Prevention of exacerbations
To prevent exacerbations and increase the duration of remission in patients with a history of frequent (more than 4 times a year) exacerbations of the disease, maintenance therapy with TacropicЃ is recommended.
?елесообразность назначени¤ поддерживающей терапии определ¤етс¤ эффективностью предшествующего лечени¤ по стандартной схеме (2 раза в день) на прот¤жении не более 6 недель.
ѕри поддерживающей терапии мазь “акропикЃ следует наносить 2 раза в неделю (например, в понедельник и четверг) на участки кожи, обычно поражаемые при обострени¤х.
ѕромежуток времени между нанесением препарата должен составл¤ть не менее 2 - 3 дней.
In adults and adolescents 16 years of age and older, 0.1% TacropicЃ ointment is used, in children (2 years and older) - 0.03% TacropicЃ ointment. If signs of exacerbation appear, you should switch to the usual regimen of therapy with TacropicЃ ointment (see the section 'Treatment of exacerbations'). After 12 months of maintenance therapy, it is necessary to assess the clinical dynamics and decide on the advisability of continuing the prophylactic use of TacropicЃ. In children, to assess clinical dynamics, the drug should be temporarily discontinued and then the need to continue supportive therapy should be considered.

Side effect

The most common adverse reactions are symptoms of skin irritation (burning and itching sensations, redness, pain, paresthesias and rashes) at the site of application. As a rule, they are moderately expressed and disappear within the first week after the start of treatment.
Alcohol intolerance (flushing of the face or symptoms of skin irritation after drinking alcohol) is common.
Patients using TacropicЃ have an increased risk of developing folliculitis, acne, and herpes infection.
By the frequency of occurrence, undesirable reactions are distributed as follows: very often ( > 1/10); often ( > 1/100, <1/10); infrequently ( > 1/1000, <1/100), rarely ( >1/10 000, <1/1000), very rarely (1/10 000), the frequency is unknown (there is not enough data to estimate the frequency of development). Within each group, adverse reactions are presented in decreasing order of importance.
Infectious diseases : often - local skin infections, regardless of etiology (in particular, but not limited to those listed, Kaposi's herpetic eczema, folliculitis, infection caused by the Herpes simplex virus, other infections caused by viruses of the Herpesviridae family).
Metabolic and nutritional disorders : often - alcohol intolerance (flushing of the face or symptoms of skin irritation after drinking alcohol).
Disturbance from the nervous system : often - paresthesia, hyperesthesia.
Violation of the skin and subcutaneous tissues : often - folliculitis, itching; infrequently - acne.
General disorders and disorders at the injection site : 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 area of ??application.
Over the entire period of observation of the drug, isolated cases of rosacea, malignancy (cutaneous and other types of lymphomas, skin cancer) were recorded.

Overdose

When applied topically, there were no cases of overdose.
If ingested, it is necessary to take generally accepted measures, which include monitoring the vital functions of the body and monitoring the general condition. Induction of vomiting or gastric lavage is not recommended.

Interaction with other medicinal products

Tacrolimus is not metabolized in the skin, which eliminates the risk of drug interactions in the skin that could affect its metabolism. Since the systemic absorption of tacrolimus when used in the form of an ointment is minimal, interaction with inhibitors of the CYP3A4 isoenzyme (including erythromycin, itraconazole, ketoconazole, diltiazem) when used simultaneously with TacropicЃ is unlikely, but cannot be completely excluded in patients with extensive lesions and / or erythroderma.
The effect of TacropicЃ on the effectiveness of vaccination has not been studied. However, due to the potential risk of reduced efficacy, vaccination should be carried out before starting to use the ointment or 14 days after the last use of TacropicЃ.
If a live attenuated vaccine is used, this period should be extended to 28 days, otherwise alternative vaccines should be considered.
The simultaneous use of tacrolimus with the conjugated vaccine against Neisseria meningitidis serotype C in children from 2 to 11 years old does not affect the primary response to vaccination, the formation of immune memory, as well as the humoral and cellular immune response. The possibility of joint use of TacropicЃ with other external drugs, systemic glucocorticosteroids and immunosuppressants has not been studied.

special instructions

TacropicЃ should not be used in patients with congenital or acquired immunodeficiencies or in patients taking immunosuppressive drugs. When using TacropicЃ ointment, avoid exposure to the sun's rays, visiting a solarium, therapy with ultraviolet B or A rays in combination with psoralen (PUVA therapy).
TacropicЃ should not be used to treat lesions that are considered potentially malignant or precancerous. Do not use emollients on the skin areas where TacropicЃ has been applied for 2 hours.
The efficacy and safety of TacropicЃ in the treatment of infected atopic dermatitis has not been evaluated. If there are signs of infection, appropriate therapy is required prior to prescribing TacropicЃ. The use of TacropicЃ may be associated with an increased risk of developing herpes infection. If there are signs of herpes infection, the benefit / risk ratio of using TacropicЃ should be individually assessed.
In the presence of lymphadenopathy, it is necessary to examine the patient before starting therapy and monitor him during the period of drug use. In the absence of an obvious cause of lymphadenopathy or in the presence of symptoms of acute infectious mononucleosis, the use of TacropicЃ should be discontinued.
It is necessary to avoid getting the drug in the eyes and on the mucous membranes (in case of accidental contact with the ointment, carefully remove and / or rinse with water).
It is not recommended to apply TacropicЃ ointment under occlusive dressings and wear tight, airtight clothing.
As with any topical medication, patients should wash their hands after applying the ointment, unless the ointment is applied to the hand area for therapeutic purposes.
It has been shown that in children aged 2 to 11 years, treatment with 0.03% tacrolimus ointment against the background of vaccination with a conjugated vaccine against Neisseria meningitidis seropitis C does not affect the primary response to vaccination, induction of the T-cell immune response and the formation of immune memory.

Influence on the ability to drive vehicles and mechanisms
Studies on the effect of the drug on the ability to drive and on the speed of reaction when working with complex equipment requiring increased attention have not been conducted. The drug TacropicЃ is used externally and there is no reason to believe that it can affect the ability to drive and operate machinery.

Release form

Ointment for external use 0.03% and 0.1%. 15 g in an aluminum tube. Each tube, together with instructions for use, is placed in a cardboard box.

Storage conditions

At a temperature not higher than 25 ? C.
Keep out of the reach of children. SHELF LIFE

Shelf life

2 years. Do not use the drug after the expiration date indicated on the package.

Vacation conditions

On prescription.