Protopik, 0.03% ointment 30 g

Protopik is a calcineurin inhibitor. The drug binds to the cytoplasmic protein immunophilin, which is a cytosolic receptor for calcineurin.

This creates a whole complex that includes tacrolimus, calcium, calcineurin, immunophilin and calmodulin.

This causes inhibition of the phosphatase activity of calcineurin, which prevents dephosphorylation and translocation of the nuclear factor of activated T cells, which is needed to initiate transcription of genes encoding the production of cytokines important for the T-cell immune response.

The active ingredient of the ointment also inhibits the transcription of genes that encode the production of IL-3, IL-4, IL-5 (cytokines). In addition, it inhibits:

< ul> < li>GMKSF and TNF-α, which are involved in T-lymphocyte activation;

< li>reduction of FcεRI expression on Langerhans cells (leading to a decrease in their activity);

< li>release of inflammatory mediators from mast cells, eosinophils and basophils.

This remedy does not cause atrophy of the skin.

Indications

For adults, 0.03% and 0.1% Protopic® ointment is used, for children from 2 to 16 years old – 0.03% ointment.

– treatment of atopic dermatitis (moderate and severe forms) in case of insufficient response of patients to traditional methods of treatment or the presence of contraindications to them.

Pharmacological effect

Protopic is a calcineurin inhibitor. The drug binds to the cytoplasmic protein immunophilin, which is a cytosolic receptor for calcineurin.

Due to this, a whole complex is created, which includes tacrolimus, calcium, calcineurin, immunophilin and calmodulin.

This causes inhibition of the phosphatase activity of calcineurin, which prevents the dephosphorylation and translocation of nuclear factor of activated T cells, which is needed to initiate transcription of genes encoding the production of cytokines important for the T-cell immune response.

The active substance of the ointment also inhibits the transcription of genes that encode the production of IL-3, IL-4, IL-5 (cytokines). In addition, it inhibits:

GMCSF and TNF-α, involved in the activation of T-lymphocytes;
decreased expression of FcεRI on Langerhans cells (leads to a decrease in their activity);
release of inflammatory mediators from mast cells, eosinophils and basophils.

This product does not provoke skin atrophy.

Special instructions

Protopic ointment should not be used in patients with congenital or acquired immunodeficiencies or in patients taking immunosuppressive drugs.

When using Protopic® ointment, it is necessary to avoid skin exposure to sunlight, visiting a solarium, or therapy with UV B or A rays in combination with psoralen (PUVA therapy).

Protopic ointment should not be used to treat lesions that are considered potentially malignant or premalignant.

For 2 hours, do not use emollients on the skin areas to which Protopic® ointment was applied.

The effectiveness and safety of Protopic® ointment in the treatment of infected atopic dermatitis has not been evaluated. If there are signs of infection, appropriate therapy is necessary before prescribing Protopic® ointment.

The use of Protopic ointment may be associated with an increased risk of developing herpes infection. If there are signs of herpetic infection, the benefit-risk ratio of using Protopic should be individually assessed.

If lymphadenopathy is present, it is necessary to examine the patient before starting therapy and monitor him during the period of application of the ointment. If there is no obvious cause of lymphadenopathy or if symptoms of acute infectious mononucleosis are present, you should stop using Protopic ointment.

It is necessary to avoid contact of the ointment with the eyes and mucous membranes (in cases of accidental contact, the ointment must be thoroughly removed and/or rinsed with water).

It is not recommended to apply Protopic® ointment under occlusive dressings and to wear tight, airtight clothing.
Just as with any other topical medication, patients should wash their hands after applying the ointment, unless the ointment is applied to the arm area for medicinal purposes.

Active ingredient

Tacrolimus

Composition

Active substance:

tacrolimus

Excipients:

soft white paraffin;

liquid paraffin;

propylene carbonate;

white beeswax;

paraffin paraffin

Contraindications

Hypersensitivity to tacrolimus, to excipients, to macrolides.
Pregnancy and breastfeeding.

Protopic should not be used in patients with genetic defects of the epidermal barrier, such as Netherton’s syndrome, as well as 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, and at a dosage of 0.03% in children under 2 years of age.

With caution

Protopic® is largely metabolized in the liver, and although its concentration in the blood when applied externally is very low, the ointment is used with caution in patients with decompensated liver failure. Caution must be exercised when using Protopic® ointment in patients with extensive skin lesions, especially long-term courses, and in children.

Side Effects

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

As a rule, they are moderate and disappear within the first week after the start of treatment.
Alcohol intolerance (facial flushing or skin irritation symptoms after drinking alcohol) is common.

Patients using Protopic® ointment have an increased risk of developing folliculitis, acne and herpetic infections.

According to the frequency of occurrence, adverse reactions are divided into very frequent (>1/10), frequent (>1/100, 1/1,000, <1/100). Within each group, adverse reactions are presented in descending order of importance.General disorders and local reactions
Very common: burning and itching at the application site.
Common: feeling of warmth, redness, pain, irritation, rash in the area of ​​application.
Infections
Frequent: herpetic infection (herpes simplex of the face and lips, varicelliform rash Galoshes).

Skin and subcutaneous tissue
Frequent: folliculitis, itching.
Uncommon: acne.
Nervous system
Frequent: paresthesia, hyperesthesia.

Metabolism and nutritional habits
Common: alcohol intolerance (facial flushing or symptoms of skin irritation after drinking alcohol).
During the entire period of observation of the drug, isolated cases of rosacea and malignancy (skin and other types of lymphomas, skin cancer) were recorded.

Interaction

Tacrolimus is not metabolized in the skin, eliminating the risk of drug interactions in the skin that could affect its metabolism.

Because systemic absorption of tacrolimus when used in ointment form is minimal; interaction with CYP3A4 inhibitors (including erythromycin, itraconazole, ketoconazole, diltiazem) when used simultaneously with Protopic ointment is unlikely, but cannot be completely excluded in patients with large areas of 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 effectiveness, vaccination must be carried out before starting to use 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 combined use of Protopic® ointment with other external drugs, systemic corticosteroids and immunosuppressants has not been studied.

Overdose

When used externally, no cases of overdose were 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. Inducing vomiting or gastric lavage is not recommended.

Storage conditions

At a temperature not exceeding 25 °C

Shelf life

3 years

Manufacturer

Netherlands