Tacropic ointment 0.03% 15g
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Active ingredients
Tacrolimus
Release form
Ointment
Composition
100 g Tacrolimus 30 mg. Excipients: macrogol 400 - 10 g, liquid paraffin - 20 g, white soft petroleum jelly - 5 g, emulsion wax - 10 g, disodium edetate - 0.
Pharmacological effect
Tacrolimus belongs to the calcineurin inhibitor group. It binds to a specific cytoplasmic protein immunophilin (FKBP12), which is a cytosolic receptor for calcineurin (FK506). As a result, a complex is formed, including 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 initiating transcription of genes encoding the production of cytokines that are key to 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 (GMXF) and tumor necrosis factor (TNFα), which participate in the initial stages of activation of T lymphocytes. In addition, under the influence of tacrolimus, inhibition of the release of inflammatory mediators from mast cells, basophils and eosinophils occurs, as well as a decrease in FcRI expression (high affinity surface receptor for immunoglobulin E) on Langerhans cells, which leads to a decrease in their activity and presentation of the T-lymphocyte antigen. Tacrolimus ointment does not affect the synthesis of collagen and, thus, does not cause skin atrophy.
Pharmacokinetics
Suction: 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 single application and with repeated use of 0.03% and 0.1% tacrolimus ointment, its plasma concentration was less than 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 systemic absorption of tacrolimus ointment is low, a high ability to bind to plasma proteins (more than 98.8%) is considered to be clinically insignificant. Metabolism: Tacrolimus is not metabolized in the skin. When released into the systemic circulation, tacrolimus is extensively metabolized in the liver by the CYP3A4 isoenzyme.Withdrawal: With repeated topical application of tacrolimus T1 / 2 ointment is 75 hours in adults and 65 hours in children.
Indications
- treatment of atopic dermatitis (moderate severity and severe forms) in the case of its resistance to other means of external therapy or the presence of contraindications to such. In adults and adolescents over the age of 16, the drug Tacropic is used in the form of 0.03% ointment and 0.1% ointment in children from 2 to 16 years old only in the form of 0.03% ointment.
Contraindications
- serious violations of the epidermal barrier, in particular, Netherton syndrome, lamellar ichthyosis, skin manifestations of graft versus host reaction, as well as generalized erythroderma (due to the risk of increasing systemic absorption of tacrolimus) - children under 2 years old (for 0.03% ointment) - childhood and adolescence to 16 years (for 0.1% ointment) - pregnancy - breastfeeding period - hypersensitivity to tacrolimus, auxiliary components of the drug, macrolides. With caution, Tacrolimus is extensively metabolized in the liver, and although its concentration in the blood when used topically is very low, in patients with decompensated liver failure, the ointment should be used with caution. Care must be taken when using Tacropic ointment in patients with extensive skin lesions, long courses, especially in children.
Use during pregnancy and lactation
Use of the drug is contraindicated during pregnancy and lactation.
Dosage and administration
For adults and children over 2 years old, Tacropic is applied with a thin layer to the affected skin. The drug can be used on any parts 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 of age. Treatment should be started with applying 0.03% Tacropic ointment 2 times / day. The duration of treatment according to this scheme should not exceed 3 weeks. In the future, the frequency of use is reduced to 1 time / day, the treatment continues until the lesions are completely cleared. Use in adults and adolescents 16 years and older. Treatment should begin with the use of 0.1% Tacropic ointment 2 times / day and continue until complete cleansing of the lesions.As you improve, you can reduce the frequency of applying 0.1% ointment or switch to using 0.03% Tacropic ointment. In the case of recurrence of the symptoms of the disease, treatment with 0.1% Takropik ointment should be resumed 2 times / day. If the clinical picture allows, an attempt should be made to reduce the frequency of use of the drug, or use a lower dosage - 0.03% Tacropic ointment. Use in the elderly (65 years and older) Features of use in the elderly are absent. Usually, an improvement is observed within 1 week after the start of therapy. If there are no signs of improvement on the background of therapy for 2 weeks, consideration should be given to changing the therapeutic tactics. Treatment of exacerbations The drug Tacropic can be used briefly or for a long time in the form of periodically repeated courses of therapy. Treatment of the affected skin is carried out until the complete 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 the start of the use of 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 frequent (more than 4 times a year) exacerbations of the disease in history, supportive therapy with Tacropic is recommended. The feasibility of prescribing maintenance therapy is determined by the effectiveness of previous treatment according to the standard regimen (2 times / 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 the skin that is usually affected by exacerbations. The time interval between the application of the drug should be at least 2-3 days. In adults and adolescents 16 years and older, 0.1% Tacropic ointment is used, in children (2 years and older) - 0.03% Tacropic ointment. When signs of exacerbation appear, proceed with the usual regimen of Tacropic ointment therapy. After 12 months of maintenance therapy, it is necessary to evaluate the clinical dynamics and decide whether to continue the prophylactic use of Tacropic. In children, to evaluate the clinical dynamics, the drug should be temporarily discontinued and then the need to continue maintenance therapy should be considered.
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. As a rule, they are moderately expressed and disappear within the first week after the start of treatment. Alcohol intolerance often occurs (facial flushing or skin irritation symptoms after drinking alcohol). In patients using the drug Tacropic, there is an increased risk of developing folliculitis, acne and herpes infection. According to the frequency of occurrence, undesirable reactions are distributed as follows: very often (1/10); often (1/100, less than 1/10); infrequently (1/1000, less than 1/100); rarely (1/10 000, less than 1/1000), very rarely (less than 1/10 000), frequency unknown (not enough data to estimate the frequency of development). Within each group, adverse reactions are presented in descending order of importance. Infectious diseases: often - local skin infections regardless of etiology (in particular, but not limited to, herpes eczema Kaposi, folliculitis, infection caused by the virus Herpes simplex, other infections caused by viruses of the family Herpes viridae). On the part of metabolism and nutrition: often - intolerance to alcohol (facial flushing or symptoms of skin irritation after drinking alcohol). On the part of the nervous system: often - paresthesia, hyperesthesia. On the part 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 use; often - a feeling of warmth, redness, pain, irritation, rash in the area of use; frequency is unknown - swelling in the application area. For the entire period of observation of the drug, isolated cases of rosacea, malignancy (skin and other types of lymphomas, skin cancer) were reported.
Overdose
In the local application of cases of overdose was noted. When ingested, it is necessary to take generally accepted measures, which include monitoring the vital functions of the body and monitoring the general condition. Stimulation of vomiting or gastric lavage are not recommended.
Interaction with other drugs
Tacrolimus is not metabolized in the skin, which eliminates the risk of drug interactions in the skin, which can affect its metabolism. Sincesystemic 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) with simultaneous use with Tacropic is unlikely, but cannot be completely excluded from patients with extensive lesions and / or erythroderma. The effect of Tacropic on the effectiveness of vaccination has not been studied. However, due to the potential risk of diminishing efficacy, vaccination should be carried out before using the ointment or 14 days after the last use of Tacropic. In the case of live attenuated vaccine, this period should be extended to 28 days, otherwise the use of alternative vaccines should be considered. The simultaneous use of tacrolimus with conjugated vaccine against Neisseria meningitidis serotype C in children from 2 to 11 years 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 the drug Tacropic with other external preparations, systemic corticosteroids and immunosuppressants has not been studied.
special instructions
The drug Tacropic cannot be used in patients with congenital or acquired immunodeficiencies or in patients who are taking immunosuppressive drugs. During the application of Tacropic ointment, it is necessary to avoid exposure of the skin to the sun, tanning visits, ultraviolet rays B or A therapy in combination with psoralen (PUVA therapy). Tacropic should not be used to treat lesions that are considered potentially malignant or premalignant. For 2 hours, no emollients can be used on the skin areas on which Tacropic was applied. The efficacy and safety of using the drug Tacropic in the treatment of infected atopic dermatitis has not been evaluated. If there are signs of infection before prescribing the drug Tacropic, appropriate therapy should be carried out. Use of the drug Tacropic may be associated with an increased risk of developing a herpetic infection. If there are signs of herpes infection, it is necessary to individually assess the ratio of the benefits and risks of using the drug Tacropic. In the presence of lymphadenopathy, it is necessary to examine the patient before starting therapy and observe him during the period of use 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. It is necessary to avoid getting the drug into the eyes and mucous membranes (in case of accidental ingestion of ointment, it is necessary to carefully remove and / or rinse with water). It is not recommended to apply Tacropic ointment under occlusive dressings and wear thick, air-tight clothing. Also, as with the use of any other local medicinal product, patients must wash their hands after applying the ointment, except when the ointment is applied to the area of the hands for therapeutic purposes. In children aged 2 to 11 years, it was shown that treatment with tacrolimus ointment 0.03% against the background of vaccination with the conjugated vaccine against Neisseria meningitidis serotype C does not affect the primary response to vaccination, induction of the T-cell immune response and the formation of immune memory. Impact on the ability to drive motor vehicles and control mechanisms Research on the effect of the drug on the ability to drive and the speed of reaction when working with complex equipment that requires increased attention, was not conducted. The drug Tacropic is used externally and there is no reason to believe that it can affect the ability to drive a car and work with mechanisms.