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

In adults, 0.03% and 0.1% Protopik® ointment is used; in children from 2 to 16 years of age – 0.03% ointment.

The treatment of atopic dermatitis (moderate and severe forms) when patients have insufficient response to traditional methods of treatment or have contraindications to these methods.

Active ingredient

Composition

Active substance:

Tacrolimus

Associates:

Paraffin soft white;

liquid paraffin;

propylene carbonate;

beeswax white;

hard paraffin.

How to take, the dosage

Interaction

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

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

The effect of Protopik® ointment on vaccine efficacy has not been studied. However, because of the potential risk of reduced efficacy, vaccination should be carried out before the start of ointment use or 14 days after the last use of Protopik® ointment.

If live attenuated vaccine is used, this period should be extended to 28 days, otherwise alternative vaccines should be considered.
The possibility of co-administration of Protopik® ointment with other external agents, systemic GCS and immunosuppressants has not been studied.

Special Instructions

Contraindications

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

Protopik® should not be used in patients with genetic defects of the epidermal barrier, such as Netherton’s syndrome, and in generalized erythroderma due to the risk of progressive increase in systemic absorption of tacrolimus.

The use of Protopik ointment in a dose of 0.1% is contraindicated in children and adolescents under 16 years of age, and in a dose 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 topically is very low, the ointment is used with caution in patients with decompensated hepatic insufficiency. Caution should be exercised when using Protopik® ointment in patients with extensive skin lesions, especially long-term courses, and in children.

Side effects

Overdose

If ingested, common measures should be taken which include monitoring of vital body functions and observation of the general condition. Induction of vomiting or gastric lavage is not recommended.

Similarities