Ekvoral

Medicinal product Ecwral belongs to the pharmacological series of antineoplastic immunomodulating medications. The main active ingredient is cyclosporin, which is a polypeptide with 11 amino acids in the composition.

Indications Ekvoral

Cyclosporine is a potent immunosuppressant. It positively affects the transplanted organs - in particular, the skin, heart, lung, bone marrow, kidneys. Due to this, Ecurolog successfully use before and after the operation of organ transplantation, as the drug improves the engraftment of the transplant and prolongs its useful life.

In addition to surgical interventions, Ekvoral uses:

• with endogenous uveitis (mid-back localization, as well as with Behcet's disease);
• with nephrotic syndrome;
• with a severe variant of rheumatoid arthritis;
• with severe psoriasis;
• with severe atopic dermatitis.

[1], [2], [3], [4]

Release form

Ecoral is produced in the form of soft capsules with different dosage:

• 25 mg - yellowish capsules with gelatinous coating and with oil fluid inside;
• 50 mg - gelatin capsules with a shade of ocher, with an oil liquid inside;
• 100 mg - brown 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 in 10 capsules in a blister plate. A cardboard box contains 5 such plates.

[5]

Pharmacodynamics

The active ingredient of the drug Ecvoral Ciclosporin is a polypeptide with 11 amino acids in the composition. Cyclosporine is a powerful immunosuppressive agent that inhibits the course of cell-type reactions, including immune processes in relation to the transplant. At the cellular level, Ecvoral inhibits the formation and release of lymphokines - for example, interleukin-2, which is a growth factor of t-lymphocytes.

Active ingredient Ecoraw fixes lymphocytes in the calm phase of the G0 or G1 cell cycle, and also inhibits the antigen-dependent release of lymphokines by stimulated t-lymphocytes. The available information indicates that the drug can affect lymphocytes in a turnaround and in a specific way. It does not exert a depressing effect on hemopoiesis (like cytostatics), it does not change the functionality of phagocytes. Patients undergoing treatment with the drug Ecvoral are less susceptible to infections than those taking other immunosuppressants.

The positive effect of taking Ecurol is fixed in the treatment of various pathologies and conditions that are considered autoimmune.

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

[6], [7], [8], [9], [10]

Pharmacokinetics

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

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

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

Metabolism of the active ingredient of cyclosporine proceeds with the formation of about 15 metabolites. These processes occur mainly in the liver.

Excretion of the drug component is carried out with bile, and only up to 6% is excreted with urinary fluid.

[11], [12], [13], [14], [15],

Dosing and administration

The therapeutic regimen based on the reception of Ecuoral is dependent on the indications and is determined by the doctor on an individual basis. Selection of the initially effective dose, as well as its correction, is performed 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, also has significance.

Capsules Ecwral are intended for internal reception. The necessary dose is swallowed, not crushing, and washed down with liquid. Usually the daily amount of the drug is divided into two doses.

Adult patients receive an intravenous injection of Ecvoral in an amount of 3 to 5 mg / kg of body weight per day before a bone marrow transplant. After that, they receive the same dosage for the next 14 days, and only then switch to the supporting capsule Ecvoral.

When organ transplantation is performed several hours before the surgery, a single dose of Ecvoral in the amount of 3-5 mg / kg of body weight is used, after which the medication is administered daily at the same dosage for 14 days. The supporting amount of the drug is 0.7-2 mg per day.

[20], [21]

Use Ekvoral during pregnancy

There are no full-fledged studies regarding the possibility of taking Eczoral during pregnancy and breastfeeding. It is believed that women who took the drug increased the risk of premature labor.

When taking the drug by lactating women, there is a risk of developing serious side effects in the infant.

For these reasons, medication treatment in these periods is not recommended. The exception is the taking of the drug according to vital indications.

Contraindications

 Ecoral is not prescribed with a tendency to allergy to the components of the drug.

Do not apply Ekvoral in the following situations:

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

[16], [17], [18]

Side effects Ekvoral

During the treatment period with the drug Ecvoral, the following side effects may occur:

• sensation of pressure in the epigastric region, deterioration of appetite, sometimes - nausea and vomiting, diarrhea, pain in the liver, swelling of the mucous gums;
• periodic headaches, numbness and cramps in the limbs;
• increased blood pressure;
• disorders of renal function;
• elevated levels of uric acid and potassium in the blood;
• increased hair growth, transient disorders of the menstrual cycle;
• sensation of weakness and spasm in muscles;
• small anemia;
• redness of the eyes, loss of vision, allergic manifestations.

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

[19]

Overdose

Data on the overdose of Ecoveral is not enough. Internal use of up to 10 g of medication can lead to insignificant clinical manifestations - vomiting, fatigue, headaches, increased heart rate, and sometimes - to a disorder of kidney function. Nevertheless, the occasional ingestion of a large number of drugs by infants provoked the development of serious signs of intoxication.

If you suspect an overdose, the doctor prescribes symptomatic therapy and supportive measures. Immediately after taking a large dose of medication, it is necessary to provoke a gag reflex and rinse the stomach.

Hemodialysis and hemoperfusion are considered ineffective.

Interactions with other drugs

The combination of Equal and potassium-based medicines increases the risk of hyperkalemia.

Combination with aminoglycosides, ciprofloxacin, trimethoprim and non-steroidal anti-inflammatory drugs can lead to impairment of renal function, and with colchicine or lovastatin - to an increase in pain in the muscles.

Strengthen the action Ekvoral can: erythromycin, ketoconazole, verapamil, doxycycline, contraceptive pills, methylprednisolone, amiodarone, fluconazole, allopurinol, etc.

Weaken the action of Ecoral: hypnotics, carbamazepine, rifampicin, orlistat, medicines based on St. John's wort, phenytoin, sulfadimidine, griseofulvin, etc.

It is not advisable to take Ecurol and Prednisolone together.

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

• diuretics - possibly disrupting the kidneys;
• doxorubicin - its toxicity increases;
• methotrexate - the risk of nephrointoxication and increased blood pressure increases;
• melphalan - the risk of developing insufficient renal function is increased;
• teniposide - its toxicity is increased;
• enalapril - possibly an increase in signs of renal insufficiency;
• nifedipine - increased gingival hyperplasia;
• diclofenac - increases the risk of a transient disorder of kidney function;
• drugs-ACE inhibitors, aminoglycosides, cephalosporins, ciprofloxacin, trimethoprim, antiviral agents - increase the degree of nephrotoxicity Ecvoral;
• cilastatin - may lead to signs of neurointoxication;
• immunosuppressants - increase the risk of infection and lymphoproliferation.

[22], [23], [24], [25], [26]

Storage conditions

The eclog is stored at a temperature of no more than + 30 ° C, in the original packaging, outside the area of children's access. Freeze the medicine can not, otherwise it will lose its healing properties.

[27]

Shelf life

You can store the ecorail for up to 3 years.

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