Tacropic, ointment 0.1% 15 g

Tacrolimus belongs to the group of calcineurin inhibitors. It binds to the specific cytoplasmic protein immunophilin (FKBP12), which is the cytosolic receptor for calcineurin (FK506). This results in the formation of a complex including tacrolimus, FKBPI2, calcium, calmodulin and calcineurin, which leads to inhibition of calcineurin phosphatase activity.

This makes dephosphorylation and translocation of nuclear factor of activated T cells (NFAT), necessary for initiation of transcription of genes encoding the production of key cytokines for the T-cell immune response (IL-2 and interferon-gamma), impossible.

In addition, tacrolimus inhibits transcription of genes encoding production of cytokines such as IL-3, IL-4, IL-5, granulocyte-macrophage colony-stimulating factor (GMSF) and tumor necrosis factor (TNFα), which are involved in the initial stages of T-lymphocyte activation.

In addition, tacrolimus inhibits release of inflammatory mediators from mast cells, basophils and eosinophils and decreases expression of FcεRI (high-affinity surface receptor for immunoglobulin E) on Langerhans cells, which leads to reduction of their activity and presentation of antigen to T-lymphocytes.

The tacrolimus ointment does not affect collagen synthesis and thus does not cause skin atrophy.

Indications

Active ingredient

Composition

How to take, the dosage

The treatment should be started with application of 0.03% ointment Tacropik® twice a day. Duration of treatment according to this scheme should not exceed three weeks. Later the frequency of application is reduced to once a day and treatment is continued until the lesions are completely cleared.

Application in adults and adolescents 16 years and older

Treatment should begin with 0.1% Tacropic® twice daily and continue until lesions are completely clear. As the symptoms improve, the frequency of application of the 0.1% ointment may be reduced and the use of 0.03% Tacropic® ointment may be switched to. If symptoms recur, resume treatment with Tacropic® 0.1% ointment twice daily.

If the clinical picture allows, an attempt should be made to reduce the frequency of use or use a lower dosage of 0.03% Tacropic® Ointment.

The use in the elderly (65 years and older)

There are no particular uses in the elderly. Usually there is an improvement within one week after the beginning of therapy. If there are no signs of improvement after two weeks of therapy, a change in therapy regimen should be considered.

The treatment of exacerbations

Tacropic® can be used for short-term or long-term repeated courses of therapy. Treatment of affected skin areas is carried out until clinical manifestations of atopic dermatitis have completely disappeared. As a rule, improvement is observed within the first week of treatment.

If signs of improvement are not seen within two weeks of starting the ointment, other options for further treatment should be considered. Treatment should be resumed at the first signs of an aggravation of atopic dermatitis.

Prevention of exacerbations

To prevent exacerbations and increase duration of remission in patients with a history of frequent (more than 4 times per year) exacerbations, maintenance therapy with Tacropic® is recommended.
The appropriateness of maintenance therapy is determined by the efficacy of the preceding therapy according to the standard regimen (2 times a day) for not more than 6 weeks.

In maintenance therapy, Tacropic® ointment should be applied twice a week (e.g., Monday and Thursday) to the areas of skin commonly affected by exacerbations.

The interval between applications should be at least 2 to 3 days.

In adults and adolescents 16 years of age and older, 0.1% Tacropic® ointment and in children (2 years of age and older) 0.03% Tacropic® ointment are used. If signs of an exacerbation appear, switch to the usual treatment regimen with Tacropic® ointment (see section “Treatment of exacerbations”).

After 12 months of maintenance therapy, the clinical course should be evaluated and a decision made as to whether to continue prophylactic use of Tacropic®. In children, the drug should be temporarily discontinued to evaluate clinical course and then consider whether continuation of maintenance therapy is necessary.

Interaction

Tacrolimus is not metabolized in the skin, which eliminates the risk of drug interactions in the skin that may affect its metabolism. Since systemic absorption of tacrolimus when used in the form of an ointment is minimal, interactions with CYP3A4 isoenzyme inhibitors (including erythromycin, itraconazole, ketoconazole, diltiazem) when used concomitantly with the drug Tacropic® is unlikely, but cannot be completely excluded in patients with extensive lesions and/or erythroderma.

The effect of Tacropic® on vaccine efficacy has not been studied. However, because of the potential risk of reduced efficacy, vaccination should be carried out before starting the ointment or 14 days after the last use of Tacropic®. If a live attenuated vaccine is used, this period should be extended to 28 days, otherwise alternative vaccines should be considered.

The concomitant use of tacrolimus with Neisseria meningitidis serotype C conjugate vaccine in children from 2 to 11 years of age has no effect on the initial vaccination response, immune memory formation, or the humoral and cellular immune response.

The possibility of co-administration of Tacropic® with other external agents, systemic GCS and immunosuppressants has not been studied.

Special Instructions

The drug Tacropic® should not be used in patients with congenital or acquired immunodeficiencies or in patients who are taking immunosuppressive drugs.

When using Tacropic® ointment, avoid exposing the skin to sunlight, visiting a tanning bed, UVB or A light therapy in combination with psoralen (PUVA therapy).

The drug Tacropic® should not be used to treat lesions that are considered to be potentially malignant or precancerous.

The areas of skin where Tacropic® was applied must not be treated with emollients for 2 hours.

The efficacy and safety of Tacropic® in the treatment of infected atopic dermatitis has not been evaluated. If there is evidence of infection, appropriate therapy should be given before prescribing Tacropic®.

The use of Tacropic® may be associated with an increased risk of herpetic infection. If there are signs of herpetic infection, the benefit-risk ratio of Tacropic® should be individually evaluated.

If lymphoadenopathy is present, the patient should be evaluated before initiating therapy and monitored during use. If there is no apparent cause of lymphadenopathy or if symptoms of acute infectious mononucleosis are present, Tacropic® should be discontinued.

Contacting the drug in the eyes and on the mucous membranes should be avoided (if the ointment is accidentally touched, it should be carefully removed and/or washed with water).

The application of Tacropic® ointment under occlusive dressings and wearing tight, airtight clothing is not recommended.

As with any topical medication, patients should wash their hands after applying the ointment unless the ointment is applied to the hand area for a therapeutic purpose.

In children between 2 and 11 years of age, treatment with 0.03% tacrolimus ointment against Neisseria meningitidis serotype C conjugate vaccine has not been shown to affect the initial vaccine response, induction of the T-cell immune response, or formation of immune memory.

Influence on driving and operating machinery

There have been no studies on the effect of the drug on driving ability and on reaction time when operating complex machinery requiring increased attention. Tacropic® is used topically, and there is no reason to believe that it may have an effect on driving and operating machinery.

Contraindications

Tacroldimus is largely metabolized in the liver, and although its concentration in the blood when applied topically is very low, in patients with decompensated hepatic insufficiency the ointment is used with caution.

Caution should be exercised when using Tacropic® ointment in patients with extensive skin lesions, long-term courses, especially in children.

Side effects

The most common adverse reactions are skin irritation symptoms (burning and itching sensation, redness, pain, paraesthesia and rash) at the application site.

In general, these are mild and go away within the first week of treatment.

Alcohol intolerance (redness of the face or symptoms of skin irritation after drinking alcohol) is common.

Patients using Tacropic® have an increased risk of folliculitis, acne, and herpetic infection.

In terms of frequency, adverse reactions are categorized as follows: very common (≥1/10); common (≥1/100, < 1/10); infrequent (≥1/1000, < 1/100); rare (≥1/10 000, < 1/1000), very rare (< 1/10 000), frequency unknown (not enough data to estimate frequency of development). Within each group, adverse reactions are presented in descending order of significance.

Infectious diseases: frequently, local skin infections regardless of etiology (in particular, but not limited to, Kaposi’s herpetic eczema, folliculitis, infection caused by Herpes simplex virus, other infections caused by viruses of the Herpes viridae family).

From metabolic and nutritional side: often – alcohol intolerance (facial hyperemia or symptoms of skin irritation after drinking alcohol).

Nervous system side: often – paresthesias, hyperesthesia.

Skin and subcutaneous tissues: frequent – folliculitis, itching; infrequent – acne.

General disorders and disorders at the site of administration: very common – burning and itching in the area of application; common – sensation of heat, redness, pain, irritation, rash in the area of application; infrequent unknown – edema in the area of application.

A solitary cases of rosacea and malignization (cutaneous and other types of lymphoma, skin cancer) have been reported during the entire period of drug monitoring.

Overdose

There have been no cases of overdose with topical administration.

In case of ingestion, common measures should be taken, which include monitoring of vital body functions and observation of the general condition.

Stimulation of vomiting or gastric lavage is not recommended.

Similarities