Protopic - 14 reviews, instructions for use

Pharmacodynamics and pharmacokinetics

Protopic is a calcineurin . 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:

GM-CSF 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

Absorption into the systemic circulation when applied topically is minimal. Systemic absorption depends on the area of the lesion. It shrinks as the symptoms of dermatitis .

The active substance Protopica is not biotransformed in the skin. Upon penetration into the systemic circulation, it is broken down in the liver.

With prolonged local use of the drug, the half-life is 65 hours in children and 75 hours in adult patients.

Analogs

If Protopic is intolerant, the doctor replaces it with analogues - Tacrolimus, Advagraf, Prograf. Akrustal and Elidel cream have similar therapeutic properties.

The cheapest structural analogue of an immunosuppressant for topical use is Wingraf. This is a generic version of Protopica, that is, a product with lower quality auxiliary ingredients.

Contraindications

This product should not be used if:

significant violations of the epidermal barrier ;
breastfeeding;
pregnancy;
children under two years of age;
children under 16 years of age (cream 0.1%);
hypersensitivity to the components of the drug.

The drug is prescribed with caution to people with decompensated liver failure , as well as extensive lesions of the skin.

Protopic ointment - side effects

During treatment, doctors prohibit sunbathing not only in the open sun, but also in solariums, as this can cause an undesirable reaction. You need to adhere to this prohibition for another 10 days after the end of the course. It is acceptable to expect side effects if treatment with Protopic ointment is extended over a long period.

Characteristic symptoms:

inflammation of the hair follicles;
itching and redness of the skin;
burning;
poor sensitivity of the dermis;
herpes with and without blisters;
alcohol intolerance;
decrease in pressure;
shortness of breath, cough;
inflammation of the digestive organs;
problems with the liver, gall bladder;
hearing loss;
elevated temperature;
metabolic disease.

Side effects

symptoms of skin irritation at the site of application may appear as adverse reactions They are usually characterized by a moderate degree of severity and disappear within a week after starting therapy.

In addition, there may be alcohol intolerance and an increased likelihood of developing folliculitis , herpetic infections and acne . The following side effects also occur:

feeling of warmth at the site of application;
itchy skin;
paresthesia;
hyperesthesia.

In rare cases, cases of rosacea and malignancy .

Expert opinion

Lyudmila Sheveleva, pharmacist

Protopic is an effective ointment for the treatment of severe skin lesions with pathologies of allergic etiology. It is well absorbed by the skin and exhibits therapeutic activity relatively quickly. But you always need to take into account the mechanism of action of the drug, aimed at suppressing local immunity. In this condition, the likelihood of bacteria and fungi viruses penetrating into inflamed tissues is increased. It is often necessary to prescribe drugs to patients to inhibit pathogenic microorganisms. To prevent skin infection, you should try not to scratch it. Before carrying out the treatment procedure, it is necessary to wash your hands and treat them with antiseptic solutions.

Instructions for use of Protopik (Method and dosage)

The instructions for Protopic indicate that the cream should be applied externally. It should be applied to the affected area of the skin, but not to the mucous membranes and under occlusive dressings.

Children 2-16 years old need to use 0.03% ointment 2 times a day. The maximum duration of treatment is 3 weeks. In the future, if necessary, the frequency of use should be reduced to 1 time per day. Therapy continues until all lesions are eliminated.

Instructions for use of the ointment for adults and adolescents recommend starting the course of treatment with the use of 0.1% cream 2 times a day until all lesions disappear. As the disease passes, you can reduce the frequency of use or switch to 0.03% cream. If manifestations of the disease return, therapy with 0.1% ointment should be resumed twice a day. When the clinical picture allows, it is necessary to use the drug less frequently or switch to 0.03% ointment.

As a rule, improvements are noticeable after a week of treatment. If they are absent within two weeks of therapy, the use of other agents should be considered.

During exacerbations, the ointment can be used short-term or long-term in the form of courses repeated at some intervals. It is necessary to lubricate the affected area of the skin until the symptoms of the disease completely disappear. Usually, improvement is noticeable after the first week of therapy. If the clinical manifestations of the disease have not decreased within two weeks, you should consider using other means.

To prevent exacerbations (if the patient experiences exacerbations of atopic dermatitis more than four times a year), maintenance therapy with ointment is acceptable. Directions for use: Apply to the affected area of skin twice a week. The interval between application is at least 2-3 days. Protopic is used if its effectiveness has previously been noticeable with a standard regimen of use.

For adults and children over 16 years old, 0.1% ointment is indicated, for children under 16 years old – 0.03% cream. If signs of exacerbation appear, it is necessary to switch to the standard regimen of use.

Maintenance therapy lasts 12 weeks, after which it is necessary to evaluate the clinical dynamics and decide whether to use this drug. In children, the medication should be temporarily discontinued.

Composition and release form

The Dutch manufacturer produces Protopic in the form of 1% and 0.03% thick white ointment with a slight yellowish tint. It is packaged in 10 g, 30 g and 60 g in plastic tubes with a screw cap. Secondary packaging is a cardboard white-blue or white-green box, which contains instructions for use.

The active ingredient of the drug is the immunosuppressant tacrolimus, which determines its therapeutic effectiveness. The auxiliary composition is represented by the following components:

propylene carbonate;
paraffins, hard, soft and liquid;
white beeswax.

Additional ingredients not only form a thick base of the product. The course of atopic dermatitis is always accompanied by severe itching. When scratching, a person injures the skin, which causes the development of severe infections.

Wax and a mixture of paraffins form a protective film on the surface of the epidermis. It is impermeable to pathogenic fungi, viruses and bacteria. At the same time, oxygen, necessary for the formation of healthy cells, easily penetrates through it.

Pharmacological properties

Protopic is a drug used to provide artificial immunosuppression (artificial suppression of immunity). Once tacrolimus is absorbed into the skin, it binds to cytosolic proteins. The resulting complexes accumulate in tissues affected by dermatitis, and then are gradually released from them. This mechanism of action provides a long-term immunosuppressive effect of the drug:

the process of competitive inhibition of calcineurin is launched. It is the only known serine-threonine phosphatase in calcium-calmodulin control. It is the key regulator of the immune system;
the transmission of signals is blocked, in response to which the production of T-lymphocytes (killer cells) increases;
the production of interleukin-2, interleukin-3, and γ-interferon is suppressed.

During treatment with Protopic, acute and chronic inflammatory reactions are stopped. Swelling resolves, pain, burning , and severe itching disappear. The blood supply to damaged tissues with nutrients gradually improves, promoting their restoration.

Reviews about Protopika

Reviews about Protopic ointment can be found in a variety of ways. As a rule, those who have already tried this remedy on themselves report that it helped them. However, very often there are reports that when using the cream, severe itching, pain, redness and other undesirable manifestations on the skin appeared.

In addition, on forums people often ask whether this drug is hormonal or not. Patients with atopic dermatitis are afraid of side effects that may occur with prolonged use of this drug. Experts rush to reassure them - the medicine is not hormonal. However, like corticosteroid hormones , it can negatively affect immunity .

Reviews of Protopic report that the product helps in an average week. There are, however, also negative opinions. Such reviews about Protopic are left by those for whom it was not effective. These people suffered from adverse reactions on the skin, but did not notice the effect of the ointment. Also, some patients express concern that this drug may cause cancer.

Features of the drug

Protopic ointment has only one indication for use - atopic dermatitis . This disease develops in early childhood and remains with a person for life. It is very difficult to treat with medication. If the use of glucocorticosteroids and non-steroidal anti-inflammatory drugs is ineffective, doctors prescribe Protopic.

The ointment is a powerful immunosuppressant that reduces the activity of the immune system. It is its inadequate reaction to allergic agents that causes the appearance of symptoms of atopic dermatitis. In response to their introduction into the body, the immune system triggers the production of bioactive substances to destroy them. And they, in turn, provoke the development of inflammation, which cannot be stopped even with hormonal agents.

The use of Protopic suppresses the aggression of the immune system by reducing the production of antibodies and leukocytes.

Protopica price, where to buy

The cream can be found in many, including foreign pharmacies. The price of Protopik 0.1% is about 1,600 rubles. And you can buy 0.03% ointment for an average of 1,500 rubles. This price of Protopic is too high for many. Therefore, patients are often interested in analogues of this drug. However, the cost of most of them is as high as the price of Protopic ointment.

Online pharmacies in RussiaRussia
Online pharmacies in UkraineUkraine

ZdravCity

Protopic ointment for external use.
approx. 0.1% 10gAstellas Ireland Co. LTD RUB 625 order
Protopic ointment for external use. approx. 0.03% 30gAstellas Ireland Co. LTD
RUB 1,581 order
Protopic ointment for external use. approx. 0.1% 30gAstellas Ireland Co. LTD
RUB 1,669 order

Pharmacy Dialogue

Protopic (0.1% ointment 10g)Astellas Pharma
RUB 633 order
Protopic (0.1% ointment 30g)Astellas Pharma
RUB 1,544 order
Protopic (0.03% ointment 30g)Astellas Pharma
RUB 1,447 order

Pharmacy24

Protopic 0.03% 10 g ointment
384 UAH. order
Protopic 0.1% 10 g ointment
384 UAH order

Indications for use

If drugs with synthetic analogues of hormones produced by the adrenal glands are powerless, Protopic is prescribed. It is the drug of last choice in the treatment of atopic dermatitis because it suppresses local immunity. The ointment is included in therapeutic regimens at any stage of the pathology:

acute, manifested by red spots, nodular rashes, swelling and profuse peeling;
chronic, which is characterized by thickening of the skin, the formation of cracks on the soles and elbows.

The drug is also effective at the stage of formation of erosions, including weeping ones. The official instructions mention the only indication for the use of the ointment - atopic dermatitis.

We recommend

Akriderm GK cream for the treatment of dermatitis

special instructions

Protopic should not be used in patients taking immunosuppressants, as well as those who suffer from congenital or acquired immunodeficiency.

When using Protopik and Protopik analogues, you should not visit solariums. You should avoid exposing your body to sunlight, and you should not perform procedures with UV rays.

Protopic is strictly prohibited from being applied to areas of the skin whose lesions are defined as malignant. Within 2 hours after applying Protopic, emollient ointments and creams should not be applied to these areas of the skin. After using the ointment, be sure to wash your hands.

Interaction with other drugs

The instructions for Protopic indicate that the drug is not metabolized in the skin.

It is possible to simultaneously apply Protopic with drugs such as ketoconazole, erythromycin, diltiazem, itraconazole if the patient has a severe disease of large areas of the skin or erythroderma is recorded.

To date, there have been no medical studies that would confirm the effect of the ointment on the vaccination process. However, despite this, vaccination may become less effective when using Protopic. To avoid such results, it is carried out before using the ointment or 2 weeks after its use. If a patient is receiving a live attenuated vaccine, this process should begin 28 days after the last day of using Protopic. If this interval cannot be maintained, another vaccine must be used.

Numerous experiments confirm that children from 2 to 11 years old can be applied to the skin with Protopic and simultaneously administered a conjugate vaccine.

The reaction of the human body to the simultaneous use of Protopic with other ointments intended for external use, as well as immunosuppressants, is not known.