Protopic - dermatological ointment with anti-inflammatory effect for the treatment of atopic dermatitis.
The medicine does not affect the state and production of collagen, so it does not provoke atrophic changes in the skin. The ointment is intended for external treatment of atopic dermatitis of moderate and severe forms.
When applied topically, Protopic is minimally absorbed into the systemic circulation, its concentration in the blood remains negligible. With repeated use of the ointment, the half-life of the active ingredient is: in adults - 75 hours, in children - 65 hours.
Clinical and pharmacological group
Pharmacy sales terms
It is released on prescription.
How much does Protopic ointment cost in pharmacies? The average price is at the level of 700 rubles.
Release form and composition
Dosage form - ointment for external use of 0.03% and 0.1%: homogeneous, from white to slightly yellowish color (in plastic tubes of 10, 30 and 60 g, 1 tube in a carton box).
- Active substance: tacrolimus (in the form of monohydrate), in 1 g of ointment - 0.3 or 1 mg.
Auxiliary components: liquid paraffin, white paraffin soft, solid paraffin, beeswax white, propylene carbonate.
Protopic is an anti-inflammatory ointment, the effect of which is determined by the properties of its main substance, tacrolimus. The compound has the ability to cause reactions that suppress the production and functioning of calcineurin.
At the same time, tacrolimus neutralizes the activity of substances that ensure the activation of t-lymphocytes at the initial stage, blocks the release of inflammatory mediators from mast cells, as well as the release of basophils and eosonophils.
The components of tacrolimus ointment do not affect the synthesis of collagen, and therefore do not provoke a negative change in the dermis.
Indications for use
Why help? Protopic is a remedy for the treatment of moderate to severe atopic dermatitis in case of insufficient effectiveness of traditional methods of treatment or the presence of contraindications to their use.
Protopic ointment is contraindicated:
- With lamellar ichthyosis.
- It is forbidden to apply 0.1% Protopic ointment to children aged 2-16 years.
- It is strictly forbidden to apply to children under 2 years.
- In reviews to Protopik said that the ointment is prohibited to use during pregnancy and lactation.
- It should not be used if the patient has Netherton's syndrome or other genetic skin diseases.
- If the skin reacts poorly to ointment.
- If patients have hypersensitivity to the main and auxiliary components of the drug.
Patients with liver failure, very large skin lesions, children, as well as those patients who have been using this drug for a long time need additional consultation.
Use during pregnancy and lactation
There is no scientifically confirmed data on the danger or safety of Protopic during pregnancy and breastfeeding. However, it is known that Tacrolimus penetrates the placental barrier. Therefore, the appointment of the drug to pregnant women is recommended only in cases where the benefit to the mother exceeds the risk to the fetus. If the drug was still prescribed to a pregnant woman, then the general condition of the newborn baby and the function of its kidneys should be monitored.
Tacrolimus is excreted in breast milk. Therefore, when prescribing this drug to a nursing mother, breastfeeding is stopped.
Dosage and method of use
The instructions for use indicate that Protopic is applied externally, applying a thin layer to the affected areas of the skin.
The ointment can be used on any parts of the body, including on the face and neck, as well as in areas of skin folds. It is not recommended to apply the agent under occlusive dressings and mucous membranes.
Children from 2 to 16 years old should apply 0.03% ointment 2 times a day. With this frequency of application, the duration of treatment should not exceed 21 days. In the future, the multiplicity of application is reduced to 1 time per day and continue therapy until all lesions are eliminated.
Adults and adolescents over 16 years old are recommended to apply 0.1% ointment 2 times a day, the treatment lasts until complete cleansing of the lesions. With improved condition, the frequency of use is reduced or 0.03% ointment is used. If signs of disease recur, 0.1% therapy is resumed with the drug twice a day. But at the first opportunity (taking into account the clinical picture), the multiplicity of intake is reduced or transferred to a lower dosage (0.03%).
As a rule, improvements are noted already 7 days after the start of the course. In the absence of the expected result during the 14 days of therapy, it is necessary to consider the question of the expediency of using Protopic.
Features of use of the drug in elderly patients (65 years and older) are missing.
With exacerbations of atopic dermatitis, it is permissible to apply the remedy short-term or long-term in the form of periodically repeated courses. Treatment continues until the symptoms of the lesion disappear. If the therapeutic effect is not observed within 2 weeks from the beginning of the use of the ointment, you should consider the use of other drugs. Therapy is resumed at the first manifestations of exacerbation.
For prolongation of the period of remission and prevention of exacerbations (with the development of the latter more than 4 times a year), it is recommended to conduct maintenance therapy with Protopic. The drug is prescribed only in the case of effective previous treatment according to the standard scheme of its use (2 times a day) in a period not exceeding 6 weeks.
With maintenance therapy on the skin areas, usually affected by exacerbations, the ointment is applied 2 times a week. The interval between application should be at least 2-3 days. Adults and adolescents over the age of 16 use 0.1% ointment, children from 2 years and older -0.03%.
In the event of symptoms of exacerbation, switch to a normal dosing regimen. Upon completion of 12 months of maintenance treatment, it is required to evaluate the clinical dynamics and decide on the feasibility of further prophylactic use of the ointment.
In children, the use of the drug is temporarily canceled to assess the clinical dynamics and determine the need to continue maintenance treatment.
Against the background of therapy with Protopic ointment, the development of negative reactions from various organs and systems is possible, these include:
- Skin and subcutaneous tissue - inflammation of the hair follicles (folliculitis), itching of the skin, its redness, burning sensation, less common is acne in the area of application of the drug.
- Peripheral nervous system - a violation of the sensitivity of nerve endings (paresthesia, manifested by tingling sensations) and a decrease in skin sensitivity (hypesthesia in the form of numbness).
- Infectious complications - herpes infection, accompanied by the appearance of burning and small bubbles filled with clear liquid (vesicles).
- General reactions and metabolism - alcohol intolerance, which consists in hyperemia (redness) of the skin of the face, heat and burning sensation after drinking alcohol.
In post-marending studies, isolated cases of rosacea (rosacea), as well as malignancy (malignant degeneration) of the cells of the affected skin with the development of cancer, skin lymphoma, were reported. The appearance of signs of negative reactions is the reason for the termination of the use of Protopic ointment and treatment to a doctor.
Cases of overdose with external use were not noted.
If the drug got inside, you need to monitor vital functions and monitor the general condition of the patient. Avoid vomiting or gastric lavage.
Immunosuppressive therapy increases the risk of malignant neoplasms. It is recommended to limit insolation and ultraviolet radiation, wear appropriate clothing, use sunscreen with a high protection factor.
In the initial post-transplantation period, the following parameters should be regularly monitored: blood pressure, ECG, neurological status and state of vision, fasting blood glucose level, electrolyte concentration (especially potassium), indicators of hepatic and renal function, hematological parameters, coagulogram, proteininemia level. In the presence of clinically significant changes, correction of immunosuppressive therapy is necessary.
During the period of use of tacrolimus, the use of herbal preparations containing St. John's wort (Hypericum perforatum), as well as other herbal remedies that may cause a decrease (change) in the concentration of tacrolimus in the blood and adversely affect the clinical effect of tacrolimus, should be avoided.
In diarrhea, the concentration of tacrolimus in the blood may vary significantly; when diarrhea appears, careful monitoring of tacrolimus concentrations in the blood is necessary.
The simultaneous use of cyclosporine and tacrolimus should be avoided, and caution should be exercised when treating patients with tacrolimus who have previously received cyclosporine.
When using tacrolimus described cases of cardiomyopathy - ventricular hypertrophy or hypertrophy of the septum of the heart. In most cases, myocardial hypertrophy was reversible and was observed at tacrolimus concentrations in the blood that were higher than recommended. Other risk factors are: the presence of previous heart disease, the use of corticosteroids, arterial hypertension, renal and hepatic dysfunction, infections, hypervolemia, edema. Patients who are at high risk and receive intensive immunosuppressive therapy, before and after transplantation (after 3 and 9-12 months), should undergo echocardiographic and ECG monitoring. If anomalies are detected, consideration should be given to reducing the dose of tacrolimus or replacing it with another immunosuppressant.
Tacrolimus may cause prolongation of the QT interval. When treating patients with a diagnosed congenital long QT interval syndrome or suspicion of such a condition, special care should be taken.
Patients receiving immunosuppressants have an increased risk of opportunistic infections (caused by bacteria, fungi, viruses, protozoa). Among these infections, nephropathy associated with the BK virus, as well as progressive multifocal leukoencephalopathy (PML) associated with the JC virus is noted. Such infections are often associated with profound suppression of the immune system and can lead to severe or fatal outcomes, which must be taken into account when conducting a differential diagnosis in patients who have signs of impaired renal function or neurological symptoms in the background of immunosuppressive therapy.
Patients treated with tacrolimus may develop post-transplant lymphoproliferative diseases (PTHL) associated with Epstein-Barr virus. With simultaneous use of the drug with anti-lymphocytic antibodies, the risk of PTLD increases. There is also evidence of an increase in the risk of PTLZ in patients with the Epstein-Barr virus capsid antigen. Therefore, before using tacrolimus in this group of patients, a serological study should be conducted for the presence of the Epstein-Barr capsid antigen. In the course of treatment, it is recommended to carry out thorough monitoring of the Epstein-Barr virus using the polymerase chain reaction (PCR). Positive PCR for Epstein-Barr virus can persist for months and is not in itself evidence of PTHD or lymphoma.
There are reports of the occurrence of reversible posterior encephalopathy syndrome with tacrolimus therapy. If a patient taking tacrolimus develops symptoms characteristic of reversible posterior encephalopathy (headache, mental disorders, convulsions, and visual impairment), then magnetic resonance imaging is necessary. With the confirmation of the diagnosis should be monitored blood pressure, the occurrence of seizures, as well as immediately stop the systemic administration of tacrolimus. If these measures are taken, this condition is completely reversible in most patients.
Tacrolimus is not metabolized in the epidermis, which eliminates the risk of drug interactions in the skin. 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 together with Protopic ointment is unlikely. However, it is not completely excluded, especially in patients with erythroderma and / or extensive lesions.
The effect of Protopic ointment on the effectiveness of vaccination has not been studied. Because of the potential risk of reducing the effectiveness of vaccination is carried out before the use of the ointment, or 14 days after the last use of the ointment. When using live attenuated vaccine, this period increases to 28 days.
The possibility of complex administration of Protopic ointment with other external preparations, immunosuppressants and systemic corticosteroids has not been studied.
We picked up some reviews of people who used Protopic ointment:
- Natasha. My friend's son has dermatitis. She was advised by the doctor to buy this ointment. I come to visit, and the baby is almost without any spots of these red ones. She used to smear him with me and healed very quickly. For the price it is, of course, a little expensive, but it is worth it. Money spent, but the quality result is guaranteed. The girlfriend is delighted, the child is happy and healthy!
- Sasha. In a child (5 years), atopic dermatitis, which is difficult to treat, has no improvement in diet, and so on. Hormonal ointments help, but this is a temporary effect. We have been using Protopic since last year, we have smeared it for several weeks last winter. Improvements are obvious. I try not to increase them. Now in the autumn they began to smear again, as the deterioration went, the protopic took off almost everything in 10 days, smeared it with a thin layer, but the last year's tube was over, a week without this ointment and redness again. Now I am buying a new tube, since this is the only thing that really helps.
- Vera. Protopik's treatment for my child was successful. The diagnosis was contact dermatitis, presumably on street sand. Smeared the affected places + took drops “Fenistil”, followed a diet. Some products may provoke further spread of dermatitis. For example, semolina and chicken broth. In the complex, improvement came in 5 days. The course took place in 10 days.
In general, reviews of Protopic ointment can be found very different. As a rule, those who have already tried this tool for themselves report that it has helped them. However, it is very often reported that when using the cream there was a strong itching, pain, redness and other undesirable manifestations on the skin.
Structural analogues of the active substance:
Before using analogues consult your doctor.
Storage conditions and shelf life
The shelf life of Protopic ointment is 3 years. It must be stored in the original factory packaging, out of the reach of children at air temperature not higher than + 25 ° C.