Ecoral, 50 mg capsules 50 pcs

Ecoral has an immunosuppressive effect.

At the cellular level it suppresses formation and release of lymphokines, including IL-2 (T-lymphocyte growth factor). It blocks lymphocytes in the resting state in G0 or G1 phase of the cell cycle and inhibits antigen-dependent release of lymphokines by activated T-lymphocytes. All these data indicate that cyclosporine acts on lymphocytes specifically and reversibly.

It does not inhibit hematopoiesis and does not affect the function of phagocytic cells.

Pharmacokinetics

After oral administration, Cmax in blood is noted between 1 and 6 h, with bioavailability averaging 30% (20-50%) and increasing with increasing dose and duration of treatment. Absorption decreases after liver transplantation, liver disease or gastrointestinal pathology (diarrhea, vomiting, intestinal obstruction).

It is intensively bound to proteins and blood-forming elements (concentration in whole blood is 2-9 times higher than in plasma). Protein binding is 90% (mainly with lipoproteins). It is distributed mainly outside the bloodstream: 33-47% in plasma, 4-9% in lymphocytes, 5-12% in granulocytes, 41-58% in erythrocytes. After oral administration Tmax in plasma is 1.5-3.5 hours. Intensively metabolized in liver by cytochrome P4503A, to a lesser extent in gastrointestinal tract and kidneys with formation of 15 identified metabolites. It is excreted with the bile; 6% of the administered dose is excreted with the urine. It is excreted with breast milk.

The T1/2 in adults is 19 h, in children 7 h, regardless of dose or route of administration.

Indications

Transplant versus host reaction (TGR) – prevention and treatment; autoimmune diseases.

Transplant-related indications: Sulidic organ transplantation (prevention of graft rejection after allogeneic kidney, liver, heart, combined heart-lung, lung, or pancreas transplantation; treatment of graft rejection in patients previously receiving other immunosuppressants; bone marrow transplantation (prevention of graft rejection after bone marrow transplantation, prevention and treatment of RTPX.

Non-transplant indications: Endogenous uveitis (active, vision-threatening middle and posterior uveitis of noninfectious etiology if conventional therapy is unsuccessful or leads to severe adverse reactions), Behcet’s uveitis with recurrent bouts of inflammation affecting the retina; Nephrotic syndrome (steroid-dependent and steroid-resistant forms in remission); rheumatoid arthritis (severe forms), psoriasis (severe forms when systemic therapy is required).

Active ingredient

Composition

How to take, the dosage

Ingestion. Ekoral capsules should be swallowed whole with water. The daily dose is divided into two doses. The following dose ranges of Ecoral are only recommendations. Blood concentration of cyclosporine should be monitored. Based on the results, determine the dose needed to achieve the desired level of cyclosporine concentration in different patients.

In adults undergoing a bone marrow transplant on the day before transplant, Ekoral is given intravenously at a dose of 3-5 mg per kg of weight per day, then continues at the same dose for 2 weeks and then switches to maintenance therapy in capsules.

In case of organ transplantation, 4-12 hours before the operation the drug is prescribed once in a dose of 3-5 mg per kg of body weight, then for 1-2 weeks after the operation the drug Ekoral is prescribed daily in the same dose, then the dose is gradually reduced until a maintenance dose of 0.7-2 mg per kg of weight per day is reached.

Interaction

Cytochrome P450 inducers or inhibitors may decrease or increase the blood concentration of cyclosporine.

Drugs that decrease the concentration of cyclosporine: barbiturates, carbamazepine, phenytoin, nafcillin, sulfadimidine (when administered by IV); rifampicin, octreotide, probucol, orlistat; drugs containing St. John’s wort (Hypericum perforatum); troglitazone.

Drugs that increase the concentration of cyclosporine: Some antibiotics – macrolides (mainly erythromycin and clarithromycin); ketoconazole, fluconazole, itraconazole, diltiazem, nicardipine, verapamil, metoclopramide, oral contraceptives, danazol, methylprednisolone (high doses); allopurinol, amiodarone, cholic acid and its derivatives.

The oral administration of erythromycin should be avoided (increases the blood concentration of cyclosporine). If, due to lack of alternative therapy, erythromycin is prescribed, it is recommended to carefully monitor the blood concentration of cyclosporine, renal function and the presence of side effects of cyclosporine.

Caution should be exercised when concomitant administration of drugs with nephrotoxic effects, such as: aminoglycosides (including aminoglycosides (including gentamicin and tobramycin), amphotericin B, ciprofloxacin, vancomycin, trimethoprim (+ sulfamethoxazole), NSAIDs (including diclofenac, naproxen, sulindac), melphalan.

Vaccination may be less effective during treatment with cyclosporine; live, attenuated vaccines should be avoided.

Combined use with nifedipine may lead to more severe gingival hyperplasia than cyclosporine monotherapy.

May significantly increase the bioavailability of diclofenac (probably due to decreased metabolism) with possible development of reversible renal dysfunction.

May decrease clearance of digoxin, colchicine, lovastatin and prednisolone, leading to increased toxic effects, particularly muscle pain, weakness, myositis and, rarely, rhabdomyolysis.

Special Instructions

The data on the experience of using the drug in the elderly are quite limited, but to date, no abnormalities have been reported in patients taking the drug at the recommended dose.

If a patient has increased BP and creatinine levels (greater than 30% of baseline) during treatment with cyclosporine, the dose should be reduced by 25-50%.

If side effects cannot be controlled or if there is severe renal impairment, the drug should be stopped.

Contraindications

Side effects

In the first week of use of Ecoral, a burning sensation on the skin of the extremities may occur.

After organ transplantation the most frequent occurrences are: hypertrichosis, tremor, impaired renal function and liver dysfunction, gum hypertrophy, GI disorders (anorexia, nausea, vomiting); dose-dependent and reversible increase in serum creatinine, urea, bilirubin, liver enzymes (careful monitoring of parameters and carrying out correction of cyclosporine dosing is necessary).

Hypertension is the most common in heart transplants; this side effect is less common in kidney transplants.

Bone marrow transplants most commonly cause gastrointestinal disturbances, tremors, hypertrichosis, and facial edema. Swelling and seizures have been reported in children.

The adverse reactions are mild and usually resolved with dosage reduction of Ecoral.

Overdose

To date there are no data on overdose with the drug and there is limited experience with overdose with other cyclosporines.

Symptoms: Renal dysfunction, which is probably reversible and disappears after discontinuation of the drug.

Treatment: general supportive measures when indicated. The drug can only be eliminated from the body with non-specific measures, including gastric lavage, because hemodialysis and hemoperfusion with activated charcoal are ineffective.

Pregnancy use

Experience with the use of cyclosporine in pregnant women is limited.

The data obtained in post-transplant patients show that treatment with cyclosporine increases the risk of adverse effects on the course and outcome of pregnancy.

Breastfeeding should be discontinued if Ekoral is to be prescribed.

Similarities