Ecoral - Instructions For Use, Price, Analogs, Capsules 25 Mg

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Ecoral

Ecoral: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Equoral

ATX code: L04AD01

Active ingredient: cyclosporin (ciclosporin)

Manufacturer: AIVEX Pharmaceuticals s. R. about. (Czech Republic), Teva Check Industries s. R. about. (Czech Republic)

Description and photo update: 2018-21-11

Prices in pharmacies: from 3370 rubles.

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Ecoral is an immunosuppressive drug.

Release form and composition

Ekoral's dosage forms:

• capsules: soft gelatinous, shell with an opaque structure, in three doses: 25 mg - yellow, oval, size 12.5 by 8 mm, on the shell the image of a double triangle and marking "25 mg", 50 mg - brownish-yellow colors, oblong, size 21 by 8 mm, on the shell the image of a double triangle and marking "50 mg", 100 mg each - brown, oblong, size 26 by 8 mm, on the shell the image of a double triangle and marking "100 mg"; the contents of the capsule are oily transparent liquid from yellow-brown to yellow color (10 pcs. in blisters or blisters, in a cardboard box 5 packages or blisters);
• oral solution 10%: clear oily liquid from yellow-brown to yellowish color (50 ml in glass vials of dark color, in a plastic case 1 bottle complete with a dispenser, in a cardboard box 1 case).

1 capsule Ekoral contains:

• active substance: cyclosporine - 25 mg, 50 mg or 100 mg;
• auxiliary components: polyglyceryl (3) oleate, D, L-alpha-tocopherol, polyglyceryl (10) oleate, macrogol glyceryl hydroxystearate, ethyl alcohol;
• shell: glycerol 85%, gelatin, titanium dioxide, glycine, sorbitol solution.

In addition, in addition to the shell:

• Ekoral capsules 25 mg and 50 mg: iron oxide yellow;
• capsules Ecoral 100 mg: iron oxide brown.

1 ml of solution contains:

• active substance: cyclosporine - 100 mg;
• auxiliary components: polyglyceryl (3) oleate, ethyl alcohol, macrogol glyceryl hydroxystearate, polyglyceryl (10) oleate.

Pharmacological properties

Pharmacodynamics

Ecoral is a powerful immunosuppressive drug that is a cyclic polypeptide of 11 amino acids.

The mechanism of action of cyclosporin A at the cellular level is due to the suppression of the formation and release of interleukin-2 (T-lymphocyte growth factor) and lymphokines. By blocking resting lymphocytes in the G ₀ or G ₁ phase _{of the} cell cycle, the drug inhibits the antigen-dependent release of lymphokines by activated T-lymphocytes. The specific effect of cyclosporine on lymphocytes is reversible, it does not inhibit hematopoiesis, does not affect the function of phagocytic cells.

Pharmacokinetics

After oral administration, the maximum concentration of cyclosporine in the blood is reached after 1-6 hours. The bioavailability of the drug is dose-dependent, increases with increasing dose and treatment period, on average it is 30%.

After liver transplantation, in case of impaired liver function or gastrointestinal pathologies (ileus, diarrhea, vomiting), the absorption of the drug decreases.

Binding to blood corpuscles and proteins is intense, the concentration level of cyclosporine in whole blood exceeds the plasma content by 2-9 times.

90% of the accepted dose of Ekorala binds to proteins, mainly lipoproteins.

Cyclosporin is excreted in breast milk.

Distribution: blood plasma - 33–47%, lymphocytes - 4–9%, erythrocytes - 41–58%, granulocytes - 5–12%. The maximum concentration in blood plasma is reached after 1.5–3.5 hours.

It is metabolized with the formation of 15 metabolites in the gastrointestinal system, kidneys and most intensively in the liver with the help of the P450 3A enzyme.

The half-life, regardless of the dose and dosage form of Ekorala, is: adults - 19 hours, children - 7 hours.

It is excreted to a greater extent with bile, through the kidneys - only 6% of the dose taken.

Indications for use

• transplantation of solid organs: prevention of graft rejection after allogeneic transplantation of kidney, liver, heart, lung, pancreas, heart-lung complex; treatment of transplant rejection in patients who have previously received other immunosuppressive drugs;
• prevention of graft rejection after bone marrow transplantation, prevention and treatment of graft versus host disease (GVHD);
• uveitis of non-infectious (endogenous) etiology of the middle and posterior region of the eye (in the absence of a therapeutic effect or the development of severe adverse reactions from conventional treatment);
• Behcet's uveitis (with recurrent attacks of inflammation affecting the retina);
• nephrotic syndrome (steroid-dependent and steroid-resistant), the development of which is due to the pathology of the glomeruli: membranous glomerulonephritis, nephropathy of minimal changes, segmental and focal glomerulosclerosis - to achieve remission, its support, as well as to maintain remission achieved by glucocorticosteroids with the purpose of subsequent use of glucocorticosteroid therapy;
• severe forms of psoriasis - if it is necessary to use systemic therapy or the impossibility of using traditional therapy;
• severe forms of atopic dermatitis - in the absence of a therapeutic effect from traditional methods of treatment or the impossibility of their use;
• a severe form of rheumatoid arthritis of high activity - with the ineffectiveness of antirheumatic drugs or the impossibility of their use.

Contraindications

• malignant neoplasms, precancerous skin diseases;
• acute phase of infectious diseases;
• chicken pox;
• shingles (Herpes Zoster);
• severe liver failure;
• uncontrolled arterial hypertension;
• hyperkalemia;
• malabsorption syndrome;
• breast-feeding;
• individual intolerance to the components of the drug.

In addition, the use of Ecoral for the treatment of diseases not associated with transplantation, with severe renal dysfunction (with the exception of nephrotic syndrome and renal dysfunction of an acceptable degree) is contraindicated.

During pregnancy, the use of Ekorala is indicated only in exceptional cases when, according to the doctor, the expected therapeutic effect for the mother exceeds the potential threat to the fetus.

Since the experience of using cyclosporine in children with atopic dermatitis, endogenous uveitis and psoriasis is limited, it is not recommended to prescribe a drug for the treatment of these diseases in this category of patients.

Ekoral should be prescribed with caution to elderly patients.

Ekorala instructions for use: method and dosage

The solution and capsules are taken orally.

The capsules should be swallowed whole and washed down with water.

The daily dose of Ekorala should be divided into 2 doses.

Recommended dosage:

• transplantation of solid organs: the daily dose for monotherapy is 10–15 mg per 1 kg of patient weight. Reception begins 12 hours before surgery and continues for 7-14 days after organ transplant. Then, taking into account the concentration of cyclosporine in the blood, the dose is gradually reduced to a maintenance dose, which is 2–6 mg per 1 kg of body weight per day. The daily dose for three-component, four-component combination therapy, including glucocorticosteroids (GCS), is 3–6 mg per 1 kg of body weight. Dose adjustment in the course of combined treatment should be made taking into account the level of cyclosporine in the blood, the dynamics of blood pressure and indicators of the concentration of urea, serum creatinine;
• bone marrow transplantation: the initial daily dose is 12.5 mg per 1 kg of the patient's body weight. Dividing it into 2 equal shares, the reception begins 24 hours before the operation and continues for 90-180 days after it as maintenance therapy. Then the dose is gradually reduced over 365 days until Ekoral is completely canceled;
• endogenous uveitis (to achieve remission): the initial daily dose is 5 mg per 1 kg of body weight. Taking capsules or solution is continued until signs appear that confirm the absence of an active inflammatory process and an improvement in visual acuity. If necessary, it is possible to increase the dose for a short period up to 7 mg per 1 kg of body weight per day. In the absence of the desired effect against the background of monotherapy with Ecoral, the use of GCS, including prednisolone at a dose of 0.2-0.6 mg per 1 kg of body weight, is indicated to stop an attack of inflammation or achieve an initial remission. For maintenance therapy it is necessary to use the lowest effective dose, which is determined by slowly decreasing the initial dose;
• nephrotic syndrome (to achieve remission): the initial daily dose for adults is 5 mg per 1 kg of body weight, for children - 6 mg per 1 kg of body weight (in 2 divided doses). The initial dose for functional disorders of the kidneys should not be higher than 2.5 mg per 1 kg of body weight per day. If monotherapy does not allow achieving an adequate therapeutic response, including in steroid-resistant patients, concomitant administration of low doses of oral corticosteroids is indicated. If there is no effect after using Ecoral within 90 days, the therapy should be canceled;
• rheumatoid arthritis: the initial daily dose is 3 mg per 1 kg of body weight. If the effect is insufficient after 42 days of therapy and with good tolerance, the dose can be gradually increased, but not more than up to 5 mg per 1 kg of body weight per day. The course of treatment is 84 days. The dose of maintenance therapy is selected individually, taking into account the tolerability of the drug. For combination therapy, the initial daily dose of Ecoral is 2.5 mg per 1 kg of body weight, if necessary, it can be gradually increased. Simultaneous use for 7 days is indicated with methotrexate in the absence of the effect of its monotherapy. When combined with corticosteroids and / or non-steroidal anti-inflammatory drugs (NSAIDs), they should be used in low doses;
• psoriasis (for the induction of remission): the initial daily dose is 2.5 mg per 1 kg of body weight. Given the variability of the disease, the dose should be selected individually. In the absence of effect while taking the initial dose after 30 days of treatment, the daily dose can be gradually increased, but not more than up to 5 mg per 1 kg of body weight per day. If, after 42 days of treatment at a dose of 5 mg per 1 kg of body weight per day, it is not possible to stop inflammation, Ekoral should be discontinued. Prescribing a dose of 5 mg per 1 kg of body weight per day as an initial dose can only be used in patients in serious condition. Taking into account the individual characteristics of the course of the disease, after achieving remission, the drug is canceled or maintenance therapy is prescribed at a dose of no more than 5 mg per 1 kg of body weight per day. In the treatment of the next relapse, the appointment of an effective dose of the previous course is indicated;
• atopic dermatitis: the initial daily dose is from 2.5 mg to 5 mg per 1 kg of body weight. A wide range of dose variability allows for an individual selection of the optimal effective dose. In addition, in the absence of the desired response after 14 days of taking the drug at a dose of 2.5 mg per 1 kg of body weight per day, a quick transition to the maximum daily dose is possible - 5 mg per 1 kg of body weight. After achieving a clinical response, the dose of Ecoral should be reduced gradually, up to its complete cancellation. The course of treatment is continued until the skin is completely cleared, usually it is 56 days. Supportive therapy with good tolerance of the drug can last up to 365 days.

Side effects

• neoplasms: rarely - basal cell carcinoma, skin papilloma, squamous cell carcinoma of the skin, Bowen's disease, lymphoproliferative pathologies (including lymphoma); very rarely - melanoma, seborrheic keratosis;
• infections: often - infection of the upper and / or lower respiratory tract (including bronchiolitis), cytomegalovirus infection, urinary tract infection; infrequently - herpes, candidiasis, sepsis;
• from the lymphatic system and blood: infrequently - thrombocytopenia, anemia; rarely - hemolytic uremic syndrome, microangiopathic anemia;
• from the digestive system: often - diarrhea, abdominal pain, gingival hyperplasia, nausea, vomiting, anorexia; infrequently - an increase in the serum level of bilirubin and the activity of hepatic transaminases; rarely - pancreatitis;
• from the nervous system: very often - headache, migraine, tremor; often - paresthesia; infrequently - convulsions, sleep disturbances, encephalopathy, confusion, lethargy, disorientation, psychomotor agitation, cortical blindness, visual impairment, paresis, cerebellar ataxia, coma; rarely - motor polyneuropathy; very rarely - edema of the optic nerve head (including edema of the optic papilla);
• on the part of the cardiovascular system: very often - an increase in blood pressure (BP);
• dermatological reactions: often - hypertrichosis; infrequently - skin rash of allergic genesis;
• from the genitourinary system: very often - impaired renal function; rarely - gynecomastia, dysmenorrhea;
• from the musculoskeletal and connective tissue: often - muscle spasms, myalgia; rarely - myopathy, muscle weakness;
• laboratory parameters: very often - hyperlipidemia; often - hyperuricemia, hypomagnesemia, hyperkalemia, hypercholesterolemia; rarely - hyperglycemia;
• others: often - feeling tired; infrequently - edema, weight gain.

Side effects in most cases are dose-dependent and reversible. With different clinical indications for taking Ecoral, their spectrum is generally the same, the frequency of development and the severity may vary.

Overdose

Symptoms: reversible renal dysfunction.

Treatment: symptomatic therapy, including timely gastric lavage. The use of hemodialysis and hemoperfusion using activated carbon is not effective.

special instructions

Ecoral should only be prescribed by a doctor who has experience in immunosuppressive therapy. Treatment should be accompanied by careful monitoring of the patient's condition, including blood pressure measurement, regular complete physical examination, monitoring of serum creatinine levels, kidney and liver function indicators. In case of deviations from the norm, a decrease in the dose of cyclosporine may be required. In patients after transplantation, it is necessary to determine the concentration of cyclosporine in the blood plasma.

Patients who have undergone organ transplant or bone marrow transplantation during the period of taking the drug should be observed only in specialized medical institutions with appropriate laboratory equipment.

During the period of Ekoral's use, a generally accepted control of the concentration of cyclosporin in the blood is required in order to accurately determine the individual dose of the drug, which allows to achieve the desired level of concentration of cyclosporin.

Do not consume grapefruit or grapefruit juice 1 hour before taking the drug.

During the treatment period, exposure to direct sunlight, ultraviolet radiation, photochemotherapy should be avoided.

Immunosuppressive drugs, including cyclosporine, increase the risk of developing malignant neoplasms, especially of the skin. The likelihood of their development largely depends on the duration of taking Ecoral and the degree of immunosuppression.

Given the high risk of developing infections (fungal, bacterial, parasitic or viral infection) and their potential danger to the patient's life, it is necessary to carry out concomitant effective preventive and therapeutic measures, especially in patients with prolonged use of combined immunosuppressive therapy.

Since the clinical condition of the patient is characterized by both the content of cyclosporine in the blood, serum or plasma, and various clinical and laboratory parameters, all factors should be taken into account when determining the dosage regimen.

The reason for the cancellation of Ecoral is the development of uncontrolled arterial hypertension.

It is not recommended to prescribe the drug for the treatment of diseases not associated with transplantation, for infectious pathologies that do not lend themselves to adequate therapy.

In case of skin lesions in patients with psoriasis, which is not typical for psoriasis, as well as if a precancerous or malignant disease is suspected, a biopsy should be performed before starting treatment with Ecoral.

Skin diseases caused by Staphylococcus aureus are not among the absolute contraindications for the use of cyclosporine, but require the mandatory appointment of concomitant antibiotic therapy.

Influence on the ability to drive vehicles and complex mechanisms

Due to the risk of developing adverse reactions from the nervous system, which can affect the patient's ability to drive vehicles and perform other potentially hazardous activities, caution should be exercised during treatment.

Application during pregnancy and lactation

Since the experience of using cyclosporine during gestation is limited, the use of Ecoral is indicated only in cases where, in the doctor's opinion, the expected therapeutic effect for the mother exceeds the potential threat to the fetus.

It should be borne in mind that against the background of the use of immunosuppressive drugs, including cyclosporine, the risk of preterm birth increases before the gestation period is less than 37 weeks.

If it is necessary to use Ekorala during lactation, breastfeeding should be discontinued.

Pediatric use

The experience of using cyclosporine in children with atopic dermatitis, endogenous uveitis, psoriasis is limited, therefore, it is not recommended to prescribe Ekoral for the treatment of these diseases in childhood.

With impaired renal function

According to the instructions, Ecoral is contraindicated for the treatment of diseases not related to transplantation, with severe renal dysfunction (with the exception of nephrotic syndrome and renal dysfunction of an acceptable degree).

For violations of liver function

The use of the drug is contraindicated in case of severe liver failure.

Use in the elderly

It is recommended to use the drug with caution in elderly patients, they need especially careful monitoring of renal function.

The use of Ekorala for the treatment of psoriasis in elderly patients is indicated only for disabling forms of the disease under close monitoring of renal function.

Drug interactions

With the simultaneous use of Ekoral:

• rifampicin, barbiturates, oxcarbazepine, phenytoin, carbamazepine, nafcillin, probucol, sulfadimidine for intravenous administration, octreotide, orlistat, ticlopidine, terbinafine, sulfinpyrazone, bosentan, containing St.
• erythromycin, clarithromycin and azithromycin (macrolide antibiotics), ketoconazole, itraconazole, fluconazole, voriconazole, nicardipine, metoclopramide, diltiazem, verapamil, oral contraceptives, high doses of methylprednisolone, danazoluvic acid, imbodarone HIV proteases, nefazodone, colchicine increase the level of cyclosporine in the blood plasma;
• aminoglycosides (tobramycin, gentamicin), amphotericin B, ciprofloxacin, vancomycin, trimethoprim, sulfamethoxazole, diclofenac, sulindac, naproxen, ranitidine, cimetidine, melphalan, methotrexate, tacrolimus should be used carefully and other drugs that increase the risk of nephrotoxicity;
• bezafibrate, fenofibrate and other derivatives of fibric acid in patients after transplantation can cause significant renal dysfunction;
• nifedipine increases the likelihood of developing gingival hyperplasia;
• lercanidipine increases its total concentration in blood plasma by 3 times and the total concentration of cyclosporine by 21%;
• aliskiren and other drugs that are a substrate for glycoprotein significantly increase their plasma level;
• digoxin, prednisolone, colchicine, statins, etoposide reduce their clearance, increasing the risk of increased toxic effects;
• lovastatin, simvastatin, atorvastatin, pravastatin, fluvastatin can contribute to the development of muscle toxicity, which is manifested by muscle pain, weakness, myositis, rhabdomyolysis;
• everolimus, sirolimus significantly increase the level of their concentration in blood plasma;
• potassium preparations, potassium-sparing diuretics, angiotensin-converting enzyme (ACE) inhibitors, angiotensin II receptor antagonists increase the risk of hyperkalemia;
• repaglinide increases the risk of hypoglycemia;
• grapefruit juice, fatty foods help to increase the bioavailability of cyclosporine.

Vaccination with live attenuated vaccines is not recommended during cyclosporine therapy, as their effectiveness may be reduced.

Analogs

Ecoral's analogues are: Sandimmun, Tacrolimus, Consupren, Cyclosporin, Orgasporin, Panimun Bioral, Restasis, Cyclopren.

Terms and conditions of storage

Keep out of the reach of children.

Store at temperatures up to 25 ° C in a dark place.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Ecoral

A few reviews about Ecoral give both positive and negative assessments of the drug. One part of patients indicates the absence of undesirable reactions, influence on the test results. Another part reports nausea and vomiting, worsening liver function tests during therapy, the appearance of edema, acute nephrotoxicity.

Ecoral price in pharmacies

The price of Ecoral 25 mg per pack containing 50 capsules varies within 995–1030 rubles. You can buy 50 capsules at a dosage of 50 mg for about 1,355 rubles. The cost of 50 capsules of 100 mg each can be 2685–3200 rubles.

Ecoral: prices in online pharmacies

Drug name Price Pharmacy

Ecoral 100 mg soft capsules 50 pcs. 3370 RUB Buy

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!