PROTOPIC OINTMENT 0.1% 10G

Composition

100 g of ointment contains 0.1 g of tacrolimus (in the form of tacrolimus monohydrate);
Excipients: white soft paraffin, liquid paraffin, propylene carbonate, white beeswax, solid paraffin.

Release form

Ointment for external use.

Packaging

Tuba 10

Mechanism of action

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, 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 initiating transcription of genes encoding the production of cytokines (IL-2 and interferon-gamma) that are key to the T-cell immune response. 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 (HMXF) and tumor necrosis factor (TNF-a), which take part in the initial stages 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 the expression of FcεRI (high-affinity surface receptor for immunoglobulin E) on Langerhans cells, which leads to a decrease in their activity and the presentation of antigen by T-lymphocytes. Tacrolimus ointment does not affect the synthesis of collagen and, thus, does not cause skin atrophy.

Indications

Protopic ointment is used at a dosage of 0.1% in adults for the 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.

Contraindications

Hypersensitivity to tacrolimus, to excipients, to macrolides.

Use during pregnancy and lactation

Do not use Protopic in patients with genetic defects of the epidermal barrier, such as Netherton syndrome, as well as in generalized erythroderma due to the risk of a progressive increase in systemic absorption of tacrolimus.

The use of Protopic ointment at 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

Protopic is largely 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 is used with caution.

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

Special notes

At a temperature not higher than 25 ° С.

Dosage and administration

For adults, Protopic ointment is applied with 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. Do not apply the drug to the mucous membranes and under occlusive dressings.

Treatment should begin with the use of 0.1% Protopic ointment twice a day and continue until complete elimination of the lesions. As you improve, you can reduce the frequency of applying 0.1% ointment or switch to using 0.03% Protopic ointment. In the case of recurrence of the symptoms of the disease, treatment should be resumed with 0.1% Protopic ointment twice a 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% Protopic ointment.

Use in the elderly (65 years and older)

Features of use in the elderly are absent.

Usually, improvement is observed within one week of the start of therapy.

If there are no signs of improvement on the background of therapy within two weeks, consideration should be given to changing the therapeutic tactics.

Exacerbations treatment

Protopic ointment can be used for short or long periods 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.

Exacerbation prevention

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, it is recommended supportive therapy with Protopic ointment. The feasibility of prescribing maintenance therapy is determined by the effectiveness of previous treatment according to the standard regimen (2 times a day) for no more than 6 weeks.

With maintenance therapy, Protopic 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% Protopic ointment is used. In case of signs of exacerbation, it is necessary to proceed to the usual regimen of treatment with Protopic ointment (see the 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 Protopic Ointment. 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 skin irritation symptoms (burning sensation and itching, redness, pain, paresthesia and rash) at the site of application. As a rule, they are mild or slight and disappear within the first week after starting treatment.

Alcohol intolerance often occurs (facial flushing or skin irritation symptoms after drinking alcohol).

In patients using Protopic ointment, there is an increased risk of developing folliculitis, acne and herpes infection.

According to the 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, adverse reactions are presented in descending order of importance.

General disorders and local reactions

Very frequent: burning and itching at the site of application.

Frequent: sensation of heat, redness, pain, irritation, rash at the site of use

Infections

Frequent: herpes infection (herpes simplex of the face and lips, varicelliform Kaposi rash).

Skin and subcutaneous tissue

Frequent: folliculitis, itching.

Infrequent: acne.

Nervous system

Frequent: paresthesias, hyperesthesia.

Metabolism and nutrition

Frequent: alcohol intolerance (facial flushing or symptoms of skin irritation after drinking).

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

Drug interaction

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

Since the systemic absorption of tacrolimus when used in the form of an ointment is minimal, interaction with inhibitors of CYP3A4 (erythromycin, itraconazole, Ketoconazole, diltiazem, etc.) when used simultaneously with Protopic ointment is unlikely, but cannot be completely excluded in patients with extensive lesions and / or erythroderma.

The effect of Protopic ointment 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 Protopic ointment. 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 possibility of joint use of Protopic ointment with other external preparations, systemic glucocorticosteroids and immunosuppressants has not been studied.

Overdose

In the local application of cases of overdose was noted.

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

Stimulation of vomiting or gastric lavage are not recommended.

Storage conditions

At a temperature not higher than 25 ° С.