Buy Tacropic ointment 0.03% 15 g packaging
  • Buy Tacropic ointment 0.03% 15 g packaging

Tacrolimus

Akrikhin
1927 Items
2019-09-19
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$55.00
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Clinical Pharmacology

Tacrolimus belongs to the calcineurin inhibitor group. It binds to a specific cytoplasmic protein immunophilin (FKBP12), which is a cytosolic receptor for calcineurin (FK506). As a result, a complex is formed, including tacrolimus, FKBPI2, calcium, calmodulin and calcineurin. which leads to inhibition of the phosphatase activity of calcineurin. This makes it impossible to dephosphorylate and translocate the nuclear factor of activated T-cells (NFAT), necessary for initiating transcription of genes encoding the production of cytokines (IL-2 and interferon-gamma) that are key to the T-cell immune response. In addition, tacrolimus inhibits the transcription of genes encoding the production of cytokines such as IL-3, IL-4, IL-5, granulocyte-macrophage colony-stimulating factor (GMXF) and tumor necrosis factor (TNF-α). who are involved in the initial stages of T lymphocyte activation. In addition, under the influence of tacrolimus, inhibition of the release of inflammatory mediators from mast cells, basofyuv and eosinophils occurs, as well as a decrease in the expression of Fc? RI (high affinity surface receptor for immunoglobulin E) on Langerhans cells, which leads to a decrease in their activity and presentation of antigen T-lymphocytes .

Tacrolimus ointment does not affect the synthesis of collagen and, thus, does not cause skin atrophy.

Pharmacokinetics:

Absorption. Topical administration of tacrolimus to the systemic circulation is minimal. In most patients with atopic dermatitis (in adults and children), both with a single application and with repeated use of 0.03% and 0.1% tacrolimus ointment, its plasma concentration was <1.0 ng="" ml="" systemic="" absorption="" depends="" on="" the="" area="" of="" lesion="" and="" decreases="" as="" clinical="" manifestations="" atopic="" dermatitis="" disappear="" cumulation="" drug="" with="" prolonged="" use="" up="" to="" 1="" year="" in="" children="" adults="" was="" not="" observed="" p="">

Distribution. Due to the fact that systemic absorption of tacrolimus ointment is low, a high ability to bind to plasma proteins (more than 98.8%) is considered clinically insignificant.

Metabolism. Tacrolimus is not metabolized in the skin. When released into the systemic circulation, tacrolimus is extensively metabolized in the liver by the CYP3A4 isoenzyme.

Derivation. With repeated topical application of tacrolimus ointment, the half-life is 75 hours in adults and 65 hours in children.

Indications

For systemic use: prevention and treatment of liver allograft and kidney rejection in adult patients. Treatment of allograft rejection, resistant to standard modes of immunosuppressive therapy in adult patients.

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

Composition

Per 100 g:

tacrolimus 30 mg.

Excipients: macrogol 400 - 10 g, liquid paraffin - 20 g, white soft petrolatum - 5 g, emulsion wax - 10 g, disodium edetate - 0.05 g, preservative Euxyl PE 9010 (phenoxyethanol 90%, ethylhexylglycerol 10%) in terms of Phenoxyethanol - 0.45 mg, purified water - up to 100 g

Tacrolimus is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Tacropic Akrikhin Russia ointment
Protopic Astellas Netherlands ointment
Prograf Astellas Netherlands capsules

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Tacrolimus

Dosage and Administration

Adults and children over 2 years old Tacropic® Apply a thin layer to the affected skin. The drug can be used on any parts of the body, including the face and neck, in the area of ​​skin folds. Do not apply the drug to the mucous membranes and under occlusive dressings.

Use in children (2 years and older) and adolescents up to 16 years

Treatment should begin with applying 0.03% Tacropic ointment® 2 times / day. The duration of treatment according to this scheme should not exceed 3 weeks. In the future, the frequency of use is reduced to 1 time / day, the treatment continues until the lesions are completely cleared.

Use in adults and adolescents 16 years and older.

Treatment must begin with the use of 0.1% Tacropic ointment® 2 times / day and continue until complete purification of lesions. As you improve, you can reduce the frequency of applying 0.1% ointment or switch to using 0.03% Tacropic ointment®. In the event of recurrence of the symptoms of the disease, treatment with 0.1% Tacropic ointment® 2 times / day. If the clinical picture allows, an attempt should be made to reduce the frequency of use of the drug, or use a lower dosage - 0.03% Tacropic ointment®.

Use in the elderly (65 years and older)

Features of use in the elderly are absent. Usually, an improvement is observed within 1 week after the start of therapy. If there are no signs of improvement during therapy for 2 weeks, consideration should be given to changing the therapeutic tactics.

Exacerbations treatment

Drug tacropic® can be used briefly or long in the form of periodically repeated courses of therapy. Treatment of the affected skin is carried out until the clinical manifestations of atopic dermatitis disappear completely. As a rule, improvement is observed during the first week of treatment. If signs of improvement are not observed within two weeks of the start of the use of the ointment, other options for further treatment should be considered. Treatment should be resumed at the first signs of exacerbation of atopic dermatitis.

Exacerbation prevention

For the prevention of exacerbations and an increase in the duration of remission in patients with frequent (more than 4 times a year) exacerbations of the disease in history, supportive therapy with Tacropic is recommended.®.

The feasibility of prescribing maintenance therapy is determined by the effectiveness of previous treatment according to the standard regimen (2 times / day) for no more than 6 weeks.

With maintenance therapy Tacropic ointment® should be applied 2 times a week (for example, on Monday and Thursday) on the skin that is usually affected by exacerbations.

The time interval between the application of the drug should be at least 2-3 days.

In adults and adolescents 16 years and older, 0.1% Tacropic ointment is used.®, babies (2 years and older) - 0.03% Tacropic ointment®. When signs of exacerbation appear, proceed to the usual regimen of Tacropic ointment therapy.® .

After 12 months of maintenance therapy, it is necessary to evaluate the clinical dynamics and decide whether to continue the prophylactic use of Tacropic.®. In children, to evaluate the clinical dynamics, the drug should be temporarily discontinued and then the need to continue maintenance therapy should be considered.

Adverse reactions

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

As a rule, they are moderately expressed and disappear within the first week after the start of treatment.

Alcohol intolerance often occurs (facial flushing or skin irritation symptoms after drinking alcohol).

In patients using the drug Tacropic®, there is an increased risk of developing folliculitis, acne and herpes infection.

According to the frequency of occurrence, undesirable reactions are distributed as follows: very often (≥1 / 10); often (≥1 / 100,

Infectious diseases: often - local skin infections, regardless of etiology (in particular, but not limited to, herpes eczema Kaposi, folliculitis, infection caused by the virus Herpes simplex, other infections caused by viruses of the family Herpes viridae).

On the part of metabolism and nutrition: often - intolerance to alcohol (facial flushing or symptoms of skin irritation after drinking alcohol).

On the part of the nervous system: often - paresthesia, hyperesthesia.

On the part of the skin and subcutaneous tissues: often - folliculitis, itching; infrequently - acne.

Common disorders and disorders at the injection site: very often, burning and itching in the area of ​​use; often - a feeling of warmth, redness, pain, irritation, rash in the area of ​​use; frequency is unknown - swelling in the application area.

For the entire period of observation of the drug, isolated cases of rosacea, malignancy (skin and other types of lymphomas, skin cancer) were reported.

Contraindications

- serious violations of the epidermal barrier, in particular, Netherton syndrome, lamellar ichthyosis, skin manifestations of the graft-versus-host reaction, as well as generalized erythroderma (due to the risk of increasing systemic absorption of tacrolimus);

- children's age up to 2 years (for 0.03% ointment);

- children's and teenage age up to 16 years (for 0.1% ointment);

- pregnancy;

- breastfeeding period;

- hypersensitivity to tacrolimus, auxiliary components of the drug, macrolides.

Carefully

Tacrolimus is largely metabolized in the liver, and although its concentration in the blood when used topically is very low, in patients with decompensated liver failure, the ointment should be used with caution.

Care must be taken when using Tacropic ointment.® in patients with extensive skin lesions, long courses, especially in children.

Drug interactions

Tacrolimus is not metabolized in the skin, which eliminates the risk of drug interactions in the skin, which can affect its metabolism. Since systemic absorption of tacrolimus when used in the form of an ointment is minimal, interaction with inhibitors of the CYP3A4 isoenzyme (including erythromycin, itraconazole, ketoconazole, diltiazem), while using with Tacropic® unlikely, but cannot be completely excluded in patients with extensive lesions and / or erythroderma.

Effect of Tacropic® on the effectiveness of vaccination has not been studied. However, due to the potential risk of reduced efficacy, vaccination should be carried out before using the ointment or 14 days after the last use of Tacropic.®. In the case of live attenuated vaccine, this period should be extended to 28 days, otherwise the use of alternative vaccines should be considered.

The simultaneous use of tacrolimus with conjugated vaccine against Neisseria meningitidis serotype C in children from 2 to 11 years does not affect the primary response to vaccination, the formation of immune memory, as well as the humoral and cellular immune response.

The possibility of joint use of the drug Tacropic® with other external drugs, systemic corticosteroids and immunosuppressants has not been studied.

Pregnancy and Lactation

Use of the drug during pregnancy and lactation is contraindicated.

Application for violations of the liver

Special instructions

Drug tacropic® should not be used in patients with congenital or acquired immunodeficiencies or in patients who are taking immunosuppressive drugs.

While applying Tacropic ointment® It is necessary to avoid exposure of the skin to the sun's rays, a visit to the solarium, UV or B therapy in combination with psoralen (PUVA therapy).

Drug tacropic® should not be used to treat lesions that are considered potentially malignant or premalignant.

Within 2 hours on the skin areas on which the drug Tacropic was applied®, do not use emollients.

Efficacy and safety of using the drug Tacropic® in the treatment of infected atopic dermatitis not evaluated. If there are signs of infection before prescribing the drug Tacropic® appropriate therapy is needed. Use of the drug Tacropic® may be associated with an increased risk of herpes infection. If there are signs of herpes infection, you should individually assess the balance between the benefits and the risk of using the drug Tacropic.®.

In the presence of lymphadenopathy, it is necessary to examine the patient before starting therapy and observe him during the period of use of the drug. In the absence of an obvious cause of lymphadenopathy or in the presence of symptoms of acute infectious mononucleosis, use of the drug Tacropic should be discontinued.®.

It is necessary to avoid getting the drug in the eyes and mucous membranes (in case of accidental ingestion of ointment, it is necessary to carefully remove and / or rinse with water).

It is not recommended to apply Tacropic ointment® under occlusive dressings and wear tight airtight clothing.

Also, as with the use of any other local medicinal product, patients should wash their hands after applying the ointment, unless the ointment is applied to the area of ​​the hands for therapeutic purposes.

It has been shown that in children aged 2 to 11 years, treatment with 0.03% tacrolimus ointment against the background of vaccination with the conjugated vaccine against Neisseria meningitidis serotype C does not affect the primary response to vaccination, induction of the T-cell immune response and the formation of immune memory.

Influence on ability to drive motor transport and control mechanisms

Studies on the effect of the drug on the ability to drive a car and on the speed of reaction when working with complex equipment that requires increased attention have not been conducted. Drug tacropic® it is used externally and there is no reason to believe that it can affect the ability to drive and work with machinery.

Overdosage

In the local application of cases of overdose was noted.

When ingested, it is necessary to take generally accepted measures, which include monitoring the vital functions of the body and monitoring the general condition.

Stimulation of vomiting or gastric lavage are not recommended.

  • Brand name: Tacropic
  • Active ingredient: Tacrolimus
  • Manufacturer: Akrikhin
  • Country of Origin: Russia

Studies and clinical trials of Tacrolimus (Click to expand)

  1. Microangiopathic hemolytic anemia complicating FK506 (tacrolimus) therapy
  2. De novo malignancies after liver transplantation using tacrolimus-based protocols or cyclosporine-based quadruple immunosuppression with an interleukin-2 receptor antibody or antithymocyte globulin
  3. A Quantitative Study of in vitro Hepatic Metabolism of Tacrolimus (FK506) Using Secondary Ion and Matrix-assisted Laser Desorption/Ionization Mass Spectrometry
  4. Immunosuppressive effect of combination schedules of brequinar with leflunomide or tacrolimus on rat cardiac allotransplantation
  5. Simvastatin-tacrolimus and simvastatin-cyclosporin interactions in rats
  6. Effect of oral itraconazole on the pharmacokinetics of tacrolimus in a hematopoietic stem cell transplant recipient with CYP3A5*3/*3
  7. Immunosuppression-induced leukoencephalopathy from tacrolimus (FK506)
  8. Could a herpesvirus mimic tacrolimus-induced leukoencephalopathy?
  9. Efficacy of tacrolimus in rheumatoid arthritis patients who have been treated unsuccessfully with methotrexate: A six-month, double-blind, randomized, dose-ranging study
  10. Tacrolimus in rheumatoid arthritis patients receiving concomitant methotrexate : A six-month, open-label study
  11. Efficacy and safety of tacrolimus in patients with rheumatoid arthritis: A double-blind trial
  12. In vivo mechanisms for the inhibition of T lymphocyte activation by long-term therapy with tacrolimus (FK-506)
  13. Treatment of antisynthetase-associated interstitial lung disease with tacrolimus
  14. Evaluation of the effect of candesartan cilexetil on the steady-state pharmacokinetics of tacrolimus in renal transplant patients
  15. Influence of rabeprazole and lansoprazole on the pharmacokinetics of tacrolimus in relation to CYP2C19, CYP3A5 and MDR1 polymorphisms in renal transplant recipients
  16. Bottom-up modeling and simulation of tacrolimus clearance: prospective investigation of blood cell distribution, sex and CYP3A5 expression as covariates and assessment of study power
  17. Randomized clinical trial of the effect of microemulsion cyclosporin and tacrolimus on renal allograft fibrosis
  18. Randomized clinical trial of daclizumab induction and delayed introduction of tacrolimus for recipients of non-heart-beating kidney transplants
  19. Study of the effect of Wuzhi tablet (Schisandra sphenanthera extract) on tacrolimus tissue distribution in rat by liquid chromatography tandem mass spectrometry method
  20. Synergistic effects of a novel nanoporous stent coating and tacrolimus on intima proliferation in rabbits
  21. Particle debris from a nanoporous stent coating obscures potential antiproliferative effects of tacrolimus-eluting stents in a porcine model of restenosis
  22. Real world safety and efficacy of the Janus tacrolimus-eluting stent: Long-term clinical outcome and angiographic findings from the tacrolimus-eluting stent (TEST) registry
  23. ChemInform Abstract: Discovery and Development of a Novel Immunosuppressant, Tacrolimus Hydrate
  24. Cyclosporine: Advantages versus Disadvantages vis-a-vis Tacrolimus

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