Protopic ointment 0.03%, 30 g

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

For adults and children over 2 years old, ProtopicЃ ointment 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.
Application in children (2 years of age and older) and adolescents under 16 years of age
Treatment should be started with the application of 0.03% ProtopicЃ 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.
Use in adults and adolescents 16 years of age and older
Treatment should begin with the application of 0.1% ProtopicЃ 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 or switch to using 0.03%
ProtopicЃ ointment . In case of recurrence of symptoms of the disease, treatment with 0.1% ProtopicЃ ointment should be resumed 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% ProtopicЃ ointment.
Use in the elderly (65 years and older)
There are no peculiarities of use 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
ProtopicЃ ointment 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 frequent (more than 4 times a year) exacerbations of the disease in history, maintenance therapy with ProtopicЃ ointment 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, ProtopicЃ ointment should be applied 2 times a week (for example, on Monday and Thursday) on the skin areas usually affected during exacerbations.
The time interval between 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 children (2 years and older) - 0.03% ProtopicЃ ointment. If signs of exacerbation appear, you should switch to the usual regimen of therapy with ProtopicЃ ointment (see 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 ProtopicЃ ointment.In children, to assess the clinical dynamics, the drug should be temporarily discontinued and then the need to continue maintenance therapy should be considered.

100 g of ointment contains 0.03 g of tacrolimus (in the form of tacrolimus monohydrate);
excipients: soft white paraffin, liquid paraffin, propylene carbonate, white beeswax, hard paraffin.

Hypersensitivity to tacrolimus, to excipients, to macrolides.
Pregnancy and breastfeeding.
ProtopicЃ should not be used in patients with genetic defects of the epidermal barrier, such as Netherton's 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.

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

Trade name : PROTOPIKЃ

International non-proprietary name : Tacrolimus

Dosage form : Ointment for external use.

Description
Ointment with a uniform consistency from white to slightly yellowish.

Composition
100 g of ointment contains 0.03 g or 0.1 g of tacrolimus (in the form of tacrolimus monohydrate);
excipients: soft white paraffin, liquid paraffin, propylene carbonate, white beeswax, hard paraffin.

Pharmacotherapeutic group:
anti-inflammatory agent for topical use.

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 phosphatase 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 FceRI (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.
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 Distribution in the body. 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 released into the systemic circulation, tacrolimus is extensively metabolized in the liver by CYP3A4.
Excretion. With repeated topical application of tacrolimus ointment, the half-life is 75 hours in adults and 65 hours in children.

Indications for use
ProtopicЃ ointment is used at a dosage of 0.03% and 0.1% in adults and only 0.03% in children from 2 to 16 years old for the treatment of atopic dermatitis (moderate and severe) in 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.
Pregnancy and breastfeeding.
ProtopicЃ should not be used in patients with genetic defects of the epidermal barrier, such as Netherton's 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.

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

Dosage and administration For
adults and children over 2 years of age, ProtopicЃ ointment 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.
Application in children (2 years of age and older) and adolescents under 16 years of age
Treatment should be started with the application of 0.03% ProtopicЃ 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.
Use in adults and adolescents 16 years of age and older
Treatment should begin with the application of 0.1% ProtopicЃ 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 or switch to using 0.03%
ProtopicЃ ointment . In case of recurrence of symptoms of the disease, treatment with 0.1% ProtopicЃ ointment should be resumed 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% ProtopicЃ ointment.
Use in the elderly (65 years and older)
There are no peculiarities of use 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
ProtopicЃ ointment 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 frequent (more than 4 times a year) exacerbations of the disease in history, maintenance therapy with ProtopicЃ ointment 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, ProtopicЃ ointment should be applied 2 times a week (for example, on Monday and Thursday) on the skin areas usually affected during exacerbations.
The time interval between 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 children (2 years and older) - 0.03% ProtopicЃ ointment. If signs of exacerbation appear, you should switch to the usual regimen of therapy with ProtopicЃ ointment (see 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 ProtopicЃ ointment.In children, to assess the clinical dynamics, the drug should be temporarily discontinued and then the need to continue maintenance therapy should be considered.

Side effects
The most common adverse reactions are symptoms of skin irritation (burning and itching sensation, 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 (flushing of the face or symptoms of skin irritation after drinking alcohol) is common.
Patients using ProtopicЃ ointment have an increased risk of developing folliculitis, acne and herpes infection.
According to the frequency of occurrence, adverse 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 decreasing order of importance.
General disorders and local reactions
Very common: burning and itching at the site of application.
Frequent: sensation of warmth, redness, pain, irritation, rash in the area of ??application.
Infections
Frequent: herpes infection (herpes simplex of the face and lips, varicelliform rash of Galoshes).
Skin and subcutaneous tissue
Frequent: folliculitis, itching.
Infrequent: acne.
Nervous system
Frequent: paresthesia, hyperesthesia.
Metabolism and dietary habits
Frequent: alcohol intolerance (flushing of the face or symptoms of skin irritation after drinking alcohol).
Over the entire period of observation of the drug, isolated cases of rosacea, malignancy (skin and other types of lymphomas, skin cancer) were recorded.

Overdose
When applied topically, cases of overdose were not observed.
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 drugs
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, interaction with CYP3A4 inhibitors (erythromycin, itraconazole, ketoconazole, diltiazem, etc.) when used simultaneously with ProtopicЃ 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 reduced efficacy, vaccination must be carried out before using the ointment or 14 days after the last use of Protopic ointment. If a live attenuated vaccine is used, this period should be extended to 28 days, otherwise alternative vaccines should be considered.
The possibility of joint use of ProtopicЃ ointment with other external drugs, systemic glucocorticosteroids and immunosuppressants has not been studied.

Special instructions
Protopic ointment should not be used in patients with congenital or acquired immunodeficiencies or in patients who are taking immunosuppressive drugs.
When using ProtopicЃ ointment, avoid exposure to the sun's rays, visiting a solarium, UV B or A therapy in combination with psoralen (PUVA therapy).
Protopic ointment should not be used to treat lesions that are considered potentially malignant or precancerous.
Do not use emollients on the skin areas where ProtopicЃ ointment has been applied for 2 hours.
The efficacy and safety of using ProtopicЃ ointment in the treatment of infected atopic dermatitis has not been evaluated. If there are signs of infection, appropriate therapy is necessary before the appointment of ProtopicЃ ointment. The use of Protopic ointment may be associated with an increased risk of developing herpes infection. In the presence of signs of herpes infection, the ratio of the benefits and risks of using Protopic should be individually assessed.
In the presence of lymphadenopathy, it is necessary to examine the patient before starting therapy and observe him during the period of application of the ointment. In the absence of an obvious cause of lymphadenopathy or in the presence of symptoms of acute infectious mononucleosis, it is necessary to stop using Protopic ointment.
It is necessary to avoid getting the ointment in the eyes and on the mucous membranes (in cases of accidental contact, the ointment must be carefully removed and / or rinsed with water).
It is not recommended to apply ProtopicЃ 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.

Release form
Ointment for external use 0.03% and 0.1%.
10, 30 or 60 grams of ointment for external use in plastic tubes.
1 tube with instructions for use in a cardboard box.

Storage
conditions Store at a temperature not exceeding 25 ? —. Keep out of the reach of children.

Shelf life is
3 years. Do not use the drug after the expiration date indicated on the package.

Terms of dispensing
By prescription.