Protopic – action, indications, dosage and side effects

Proven content

Protopic is an immunosuppressive ointment, that is, it suppresses the immune system response. It is a preparation that is used primarily in the treatment of moderate and severe forms of atopic dermatitis. Protopic ointment is recommended for those patients who do not improve after treatment with corticosteroids. What are the indications and contraindications for using Protopic ointment? How to properly use and dose this ointment? Can there be side effects after using it? How much does Protopic ointment cost?

Protopic – general characteristics of the drug

Protopic is a medical preparation, available in the form of an ointment, with an immunosuppressive effect. The ointment can be purchased in two versions:

1. Protopic 0,03%ointment available on standard prescription (one gram of Protopic 0,03% ointment contains 0,3 mg of tacrolimus as tacrolimus monohydrate);
2. Protopic 0,1%Prescription proprietary ointment (0,1 gram of Protopic 1,0% ointment contains XNUMX mg of tacrolimus as tacrolimus monohydrate).

Protopic is a white to slightly yellowish ointment. It is available in tubes containing 10, 30 or 60 grams of ointment.

Protopic is an ointment for the topical treatment of atopic dermatitis, where the active substance is tacrolimus. This ointment is usually prescribed to patients who have not improved with corticosteroids.

The manufacturer of the Protopic ointment is LEO Pharma, i.e. an international Danish pharmaceutical concern founded in 1908. The company’s drugs are present in around 100 countries. The seat of the LEO Pharma concern is in Ballerup near Copenhagen. Medical products offered by LEO Pharma are mainly dermatological preparations. In 1945, LEO Pharma was the first producer of penicillin outside the United States and Great Britain.

How do corticosteroids work and how do they affect our body? Read: Corticosteroids

Protopic – composition and action

The active substance in Protopic ointment is tacrolimus. This ingredient is a powerful immunosuppressive drug. Tacrolimus is usually used to prevent organ rejection or to treat acute transplant rejection. In dermatology, tacrolimus is effective in the local treatment of atopic dermatitis.

Tacrolimus is an inhibitor of calcineurin. Calcineurin is a protein that activates the T cells of the immune system. The mechanism of action of the drug is based on binding to a specific cytoplasmic immunophilin and inhibition of calcium-dependent signal transduction cascades in T lymphocytes. Tacrolimus is effective in inhibiting the formation of cytotoxic lymphocytes, B-cell proliferation and the formation of lymphokines. The compound also inhibits the release of inflammatory mediators from skin mast cells, basophils and eosinophils.

Treatment of skin lesions caused by atopic dermatitis is associated with a reduction in the expression of the Fc receptor in Langerhans cells and the reduction of their activating effect on T lymphocytes. Topical application of the drug does not cause collagen synthesis in humans.

So how does Protopic work? Well, if a patient with atopic dermatitis comes into contact with an allergen, calcineurin will be activated in his body. This compound, in turn, activates the transcription factor, which stimulates the formation of T cells.

This process leads to the development of an immune response and, consequently, an inflammatory reaction, manifested by itching and red spots. Applying Protopic ointment to the affected area causes the active ingredient, tacrolimus, to take effect. Tacrolimus penetrates inside the cell, where it forms a complex with a special protein. This complex binds to calcineurin and inhibits its action. This stops the inflammatory reaction, which results in the reduction of the atopic skin lesion or its complete disappearance.

Protopic ointment also contains white petrolatum, liquid paraffin, propylene carbonate, white wax, solid paraffin, butylated hydroxytoluene (E321) and all-rac-α-tocopherol.

What are the causes and symptoms of atopic dermatitis? Read on: Atopic dermatitis

Protopic – absorption and elimination of the drug from the body

Single or multiple topical application of Protopic ointment in healthy patients does not significantly affect the general condition of the body. Absorption of the active substance in Protopic into the systemic circulation is low and systemic effects are virtually absent or negligible.

Conversely, skin absorption may be increased if Protopic is applied to large areas of the skin. However, it is worth remembering that the degree and speed of absorption of the drug decreases along with the improvement of the skin condition.

After repeated use of the ointment on the skin, the average duration of the active substance presence in the body is 75 hours for adults and 65 hours for children. If tacrolimus is administered orally, the drug is absorbed from the gastrointestinal tract and its maximum concentration occurs approximately 1-3 hours after taking the drug. The drug can also be given by infusion. In this situation, in the circulation, tacrolimus binds first to erythrocytes and in the second phase to over 98% to proteins, including albumin and acid glycoprotein.

This drug is metabolized primarily in the liver but also in the gut wall. It is excreted from the body in the form of metabolites in the faeces.

How to care for atopic skin? Read on: Atopic skin – characteristics, care and soothing

Protopic – indications

Protopic ointment is a preparation recommended primarily to those patients who previously used steroid drugs with negligible effect.

The indications for the use of Protopic ointment are:

1. treatment of moderate and severe exacerbations of atopic dermatitis in adults and adolescents over 16 years of age;
2. treatment of exacerbations of moderate and severe forms of atopic dermatitis in children after 2 years of age;
3. maintenance treatment of moderate to severe forms of atopic dermatitis to avoid relapse and prolong periods without relapse.

How is atopic dermatitis manifested in babies? Check: Atopic dermatitis in infants (AD) – causes, symptoms, treatment

Protopic – contraindications

Despite its effectiveness, Protopic ointment cannot be used by every patient suffering from atopic dermatitis. This ointment cannot be used in people who have been diagnosed with hypersensitivity to tacrolimus, macrolide antibiotics or any of the auxiliary components of the ointment.

What are macrolide antibiotics and how do they work? Check: Macrolides

Protopic – precautions

The manufacturer of Protopic ointment in the package leaflet indicates the precautions to be taken when using this preparation.

When using Protopic ointment, remember that:

1. while using the ointment, sun and ultraviolet radiation from the solarium should be avoided. The skin should not be exposed to the sun, but also the treatment with the use of UVB or UVA rays should not be used. Patients should minimize exposure to the sun, use radiation protection products, and cover their skin with appropriate clothing;
2. the ointment should not be applied to the skin if the lesions may be cancerous or precancerous;
3. if a new lesion occurs on the treated skin while using the drug, you should immediately consult your doctor;
4. Patients with a skin barrier defect such as Netherton’s syndrome, ichthyosis or erythroderma should not use Protopic. These medical conditions increase the absorption of the drug;
5. long-term use of the drug on extensive skin lesions, especially in children, must be under the constant supervision of a doctor. After 12 months, the physician’s evaluation should consider stopping ointment treatment in children;
6. in patients after organ transplantation, long-term use of the drug may increase the risk of developing lymphoma and skin malignancies; 
7. the ointment should not be used by people with congenital or acquired immunodeficiency or using other immunosuppressive drugs;
8. Any infections at the treatment site should be cleared before starting Protopic ointment. Patients with atopic dermatitis are prone to superficial skin infections;
9. treatment with Protopic may be associated with an increased risk of folliculitis and herpes simplex skin infection;
10. Do not apply emollients to the same area within 2 hours of applying Protopic ointment;
11. contact of the ointment with the eyes or mucous membranes should be avoided;
12. occlusive dressings should not be applied;
13. ointment should be used with caution in patients with hepatic insufficiency.

What is UV radiation and how can I protect my skin against it? Check: UV radiation

Protopic – use and dosage

The correct use and dosage of Protopic ointment is always determined by a physician experienced in the diagnosis and treatment of atopic dermatitis. When using Protopic ointment, it is very important to distinguish between two ointment strengths: Protopic 0,03% and Protopic 0,1%.

For the treatment of the acute phase of atopic dermatitis, the ointment may be used for short periods or intermittently for long periods. This ointment should not be used for a long time without breaks.

Treatment with Protopic is usually initiated after previous unsuccessful corticosteroid therapies. Use Protopic until the lesions have completely cleared or become benign.

Dosage of Protopic ointment:

1. adults and adolescents over 16 years of age – Use Protopic 0,1% twice a day initially until the lesion has cleared. If the clinical condition improves, the frequency of application of the ointment should be reduced or the preparation should be changed to a lower potency, i.e. Protopic 0,03%. Improvement usually occurs about a week after the first application of the ointment. If there is no improvement, consult a doctor who will probably suggest a different treatment direction;
2. children from 2 to 16 years of age – only a weaker ointment, Protopic 0,03%, is used. The drug should not be used in children under 2 years of age.

If your doctor decides to continue your treatment and use Protopic ointment:

1. adults and adolescents over 16 years of age – Protopic 0,1% ointment should be used. To prevent disease worsening, use the ointment once a day, two days a week, e.g. on Tuesday and Friday. Always leave a 2-3 day break between applying the ointment dose. After one year of treatment, the physician should assess the patient’s condition and decide whether to continue or terminate maintenance treatment. If the disease recurs, treatment with the ointment should be restarted twice a day;
2. children from 2 to 16 years of age – only a weaker ointment, Protopic 0,03%, is used. The drug should not be used in children under 2 years of age.

Correct application of Protopic ointment is to apply a thin layer of the product to the affected area of ​​the skin. The ointment can be used on any part of the body, including the face, neck and bends. The ointment should not be applied to the mucous membranes.

When is it worth reaching for Mediderm cream? Check: Mediderm – application, composition, properties, leaflet, opinions

Protopic – side effects

The use of Protopic ointment may cause side effects in patients. In clinical trials, about 50% of patients indicated side effects of using the ointment.

In every case after authorization of a medicinal product, it is important to report any suspected adverse reactions so that the benefit / risk balance of the medicinal product can be monitored.

The general classification of the frequency of adverse body reactions (ADRs) is based on the following principles: very common (≥1 / 10), common (≥1 / 100 to <1/10), uncommon (≥1 / 1 to <000/1), rare ( ≥100 / 1 to <10 / 000), very rare (<1 / 1), not known (cannot be estimated from the available data).

The following side effects may occur with Protopic treatment:

1. very common (≥1 / 10) – burning and pain at the application site, itching at the site of application of the ointment;
2. common (≥1 / 100 to <1/10) - local skin infection (herpetic eczema, folliculitis, herpes simplex skin infection, herpes simplex infection, herpes virus infection, Kaposi's pox disease), alcohol intolerance, paraesthesia and dysaesthesia, pruritus, application site warmth, application site erythema, application site pain, application site irritation, application site paraesthesia, application site rash;
3. uncommon (≥1 / 1 to <000/1) - acne;
4. frequency not known (frequency cannot be estimated from the available data) – herpes infection of the eye, rosacea, lentigo, swelling at the injection site, increased drug concentration in tests.

What are allergic skin diseases? Check: Allergic skin diseases

Protopic – interactions with cosmetics and other drugs

Before using Protopic, always tell your doctor about the ointments you are using and the medications you are taking. Protopic ointment may interact with some medical preparations.

Among the significant interactions with other drugs, the following are indicated:

1. Protopic i Prevymis – these medicines contain tacrolimus and letermovir. Taking these drugs at the same time may increase the side effects of tacrolimus;
2. Protopic i Humira, Amgevita, Solymbic – these drugs contain tacrolimus and adalimumab. Both ingredients reduce the body’s ability to fight bacterial, viral and fungal infections. Their simultaneous use increases the risk of infections and inflammations of various organs, which may be severe and even threaten the patient’s health and life;
3. Protopic i Amikin, Amikacin B.Braun, Biodacyna Ophthalmicum – these drugs contain tacrolimus and amikacin. The use of these preparations at the same time increases the risk of symptoms of their negative effects on the kidneys. If you notice nausea, vomiting, reduced or increased amount of urine, discoloration of the urine, weakness, swelling, high blood pressure, consult your doctor.
4. Protopic i Olumiant – these drugs contain tacrolimus and baricitinib. Simultaneous use of these drugs reduces the body’s ability to fight bacterial, viral and fungal infections. The patient is at increased risk of serious infections and inflammations;
5. Protopic and Cimzia – these medicines contain tacrolimus and certolizumab. They reduce the body’s ability to fight bacterial, viral and fungal infections. This exposes the body to serious infections and inflammation;
6. Protopic i Sandimmun, Ikervis, Equoral – these drugs contain tacrolimus and cyclosporine. Their simultaneous use leads to an increase in side effects, as well as a significant increase in the risk of kidney damage;
7. Protopic i Naproxen Glaxo, Apranax Roche, Anapran Ec – these drugs contain naproxen and tacrolimus. Their simultaneous use increases the risk of side effects on the kidneys, as well as hypertension and edema;
8. Protopic i Ketoprofenum Fastum, Ketospray Forte, Ketoprofen Lgo – these drugs contain tacrolimus and ketoprofen. Their simultaneous use increases the risk of side effects on the kidneys, as well as hypertension and edema;
9. Protopic i Ketozol, Sinazol, Nizoral — Ir – these drugs contain tacrolimus and ketoconazole. Concomitant use of these preparations may increase the undesirable effects of tacrolimus. You may notice heart problems, headache, dizziness, muscle convulsions and tremors, blurred vision, photophobia, diarrhea, nausea, vomiting, abdominal pain, skin rash, weakness and insomnia;
10. Protopic i Tribiotic, Polibiotic, Cicatrex – these drugs contain tacrolimus and bacitracin. Concomitant use of the preparations may increase the risk of negative effects on the kidneys.

It is also worth remembering that when using Protopic ointment, you should avoid the consumption of citrus fruits and, above all, limit the consumption of grapefruit and grapefruit juice. These fruits increase the concentration of the drug in the body, which increases the risk of side effects.

What interactions are there between popular drugs? Check: Dangerous interactions

Protopic and alcohol consumption

You should not drink alcohol while using Protopic. Simultaneous use of the ointment and alcohol consumption may cause side effects in the form of flushing, skin irritation, and the feeling of heat.

What drugs can not be combined with alcohol? Check: Eight drugs that are better not to be combined with alcohol

Protopic and pregnancy and breastfeeding

Protopic ointment is not recommended for use in pregnant women, unless it is essential for the health of the woman, and the effects of treatment far outweigh possible side effects. The effect of the active substance on the fetus is unknown.

The use of Protopic ointment is also not recommended during breast-feeding as oral tacrolimus passes into breast milk.

Can drugs be used during pregnancy? Check: Pregnancy and medications

Protopic — cena preparatu

The price of Protopic ointment may differ depending on the town or pharmacy from which we obtain the drug, as well as the size of the tube and the strength of the ointment. The average price of Protopic ointment is:

1. Protopic ointment; 0,03%; 10 g – about PLN 60;
2. Protopic ointment; 0,03%; 30 g – about PLN 150;
3. Protopic ointment; 0,1%; 10 g – about PLN 60;
4. Protopic ointment; 0,1%; 30 g – about PLN 140.

What is eczema? How is it recognized and treated? Check: Eczema – causes, types, symptoms, treatment. Diet and home remedies for eczema

Before use, read the leaflet, which contains indications, contraindications, data on side effects and dosage as well as information on the use of the medicinal product, or consult your doctor or pharmacist, as each drug used improperly is a threat to your life or health. Do you need a medical consultation or an e-prescription? Go to halodoctor.pl, where you will get online help – quickly, safely and without leaving your home.