Equoral

The medicine Ekvoral belongs to the pharmacological series of antineoplastic immunomodulatory drugs. The main active ingredient is cyclosporine, which is a polypeptide with 11 amino acids in its composition.

Indications Equoral

Cyclosporine is a powerful immunosuppressant. It has a positive effect on transplanted organs - in particular, on the skin, heart, lungs, bone marrow, kidneys. Due to this, Ekvoral is successfully used before and after organ transplant surgery, as the drug helps improve the engraftment of the transplant and prolongs its service life.

In addition to surgical interventions, Ekvoral is used:

• in endogenous uveitis (mid-posterior localization, as well as in Behcet's disease);
• in nephrotic syndrome;
• in severe cases of rheumatoid arthritis;
• in severe cases of psoriasis;
• in severe cases of atopic dermatitis.

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Release form

Ekvoral is produced in the form of soft capsules with different dosages:

• 25 mg each – yellowish capsules with a gelatin shell and oily liquid inside;
• 50 mg each – gelatin capsules with an ocher tint, with an oily liquid inside;
• 100 mg each – brownish capsules with oily contents.

Each capsule has an inscription indicating the dosage of the drug, as well as a logo - an hourglass.

Ekvoral is packaged with 10 capsules in a blister plate. A cardboard box contains 5 such plates.

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Pharmacodynamics

The active ingredient of the drug Ekvoral is cyclosporine, a polypeptide with 11 amino acids in its composition. Cyclosporine is a powerful immunosuppressant that inhibits the course of cellular reactions, including immune processes in relation to the transplant. At the cellular level, Ekvoral inhibits the formation and release of lymphokines - for example, interleukin-2, which is a growth factor for T-lymphocytes.

The active ingredient of Ekvoral fixes lymphocytes in the quiet phase G0 or G1 of the cell cycle, and also inhibits antigen-dependent release of lymphokines by stimulated T-lymphocytes. Available information indicates that the drug can affect lymphocytes in a reversible and specific manner. It does not have a depressing effect on hematopoiesis (like cytostatics), does not change the functionality of phagocytes. Patients who are treated with Ekvoral are less susceptible to infections than those taking other immunosuppressants.

A positive effect from taking Ekvoral has been recorded in the treatment of various pathologies and conditions that are considered autoimmune.

Ekvoral also demonstrates effectiveness in the treatment of steroid-dependent nephrosyndromes in pediatrics.

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Pharmacokinetics

After internal use of Ekvoral capsules, the maximum content of the active ingredient in the blood can be observed for 60-120 minutes. Complete oral bioavailability is from 20 to 50%.

When taking Ekvoral against the background of a special low-fat diet, a decrease in AUC and maximum concentration by 13 and 33%, respectively, is observed. The proportion between the recommended dosage and exposure is linear in the range of the therapeutic dose. The range of AUC and maximum concentration values can be about 15%. The medicinal liquid in the form of a solution and elastic capsules are considered bioequivalent.

The drug is distributed in an average volume of 3.5 l per kg. Approximately 40% is determined in plasma, about 5-6% in lymphocyte cells, about 8-10% in granulocytes, and about 50% in erythrocytes. The connection with plasma proteins is approximately 90%.

The active ingredient cyclosporine is metabolized to about 15 metabolites. These processes occur primarily in the liver.

The drug component is excreted with bile, and only up to 6% is excreted with urine.

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Dosing and administration

The therapeutic regimen based on taking Ekvoral depends on the indications and is determined by the doctor on an individual basis. The selection of the initially effective dose, as well as its correction, is carried out taking into account the dynamics of tissue engraftment or pathology. In addition, the concentration of the active component in the blood serum, which is determined daily, is also important.

Ekvoral capsules are intended for internal use. The required dose is swallowed without crushing and washed down with liquid. Usually the daily amount of the drug is divided into two doses.

Adult patients receive intravenous injections of Ekvoral in the amount of 3 to 5 mg/kg of body weight per day before bone marrow transplantation. After that, they receive the same dosage for the next 14 days, and only then switch to maintenance administration of Ekvoral capsules.

In organ transplantation, a single injection of Ekvoral in the amount of 3-5 mg/kg of body weight is used several hours before the surgical intervention, after which the medication is administered daily for 14 days in the same dosage. The maintenance dose of the drug is 0.7-2 mg per day.

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Use Equoral during pregnancy

There are no full-fledged studies on the possibility of taking Ekvoral during pregnancy and breastfeeding. It is believed that women who have taken the drug have an increased risk of premature labor.

When taking the drug by nursing women, there is a risk of developing serious side effects in the breastfed baby.

For these reasons, treatment with the drug during the periods listed is not recommended. The exception is taking the drug for vital indications.

Contraindications

Ekvoral is not prescribed if you are prone to allergies to the components of the drug.

Do not use Ekvoral in the following situations:

• in severe uncontrolled arterial hypertension;
• in the acute phase of infectious diseases;
• in the presence of malignant neoplasms;
• in case of persistent disorders of renal function (exception: nephrotic syndrome).

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Side effects Equoral

During the entire period of treatment with Ekvoral, the following side effects may occur:

• a feeling of pressure in the epigastric region, loss of appetite, sometimes nausea and vomiting, diarrhea, liver pain, swelling of the mucous membrane of the gums;
• periodic headaches, numbness and cramps in the limbs;
• increased blood pressure;
• renal dysfunction;
• elevated levels of uric acid and potassium in the blood;
• increased hair growth, transient menstrual irregularities;
• feeling of weakness and muscle spasm;
• slight anemia;
• redness of the eyes, loss of visual acuity, allergic reactions.

If side effects are persistent or increasing, it makes sense to consider the possibility of reducing the dosage of Ekvoral.

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Overdose

There is little data on Ekvoral overdose. Internal use of up to 10 g of the drug can lead to minor clinical manifestations - vomiting, fatigue, headaches, increased heart rate, and sometimes - renal dysfunction. However, accidental ingestion of large amounts of the drug by infants has provoked the development of serious signs of intoxication.

If an overdose is suspected, the doctor prescribes symptomatic therapy and supportive measures. Immediately after taking a large dose of the drug, the gag reflex should be induced and the stomach should be washed out.

Hemodialysis and hemoperfusion are considered to be ineffective.

Interactions with other drugs

The combination of Ekvoral and potassium-based medications increases the risk of hyperkalemia.

Combination with aminoglycosides, ciprofloxacin, trimethoprim and non-steroidal anti-inflammatory drugs can lead to impaired renal function, and with colchicine or lovastatin - to increased muscle pain.

The effect of Ekvoral can be enhanced by: erythromycin, ketoconazole, verapamil, doxycycline, contraceptive pills, methylprednisolone, amiodarone, fluconazole, allopurinol, etc.

The effects of Ekvoral are weakened by: sleeping pills, carbamazepine, rifampicin, orlistat, St. John's wort-based medications, phenytoin, sulfadimidine, griseofulvin, etc.

The combined use of Ekvoral and prednisolone is not recommended.

In addition, doctors do not recommend the following combinations with Ekvoral:

• diuretics - may cause kidney dysfunction;
• doxorubicin - its toxicity increases;
• methotrexate - increases the risk of nephrointoxication and increased blood pressure;
• melphalan - increases the risk of developing renal insufficiency;
• teniposide - its toxicity increases;
• enalapril - possible increase in signs of renal failure;
• nifedipine - increases gingival hyperplasia;
• diclofenac - increases the risk of transient renal impairment;
• ACE inhibitors, aminoglycosides, cephalosporins, ciprofloxacin, trimethoprim, antiviral agents - increase the degree of nephrotoxicity of Ekvoral;
• cilastatin - may cause signs of neurointoxication;
• Immunosuppressants – increase the risk of infections and lymphoproliferations.

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Storage conditions

Ekvoral is stored at a temperature of no more than +30°C, in the original packaging, out of the reach of children. The medicine cannot be frozen, otherwise it will lose its medicinal properties.

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Shelf life

Equor can be stored for up to 3 years.

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