Orgasorin® (Orgasporin®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceCyclosporinCyclosporin
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    • Dosage form: & nbspcapsules
    Composition:

    Composition per one capsule:

    Active substance:

    Cyclosporin

    25 mg

    50 mg

    100 mg

    Excipients:

    Propylene glycol caprylate

    90 mg

    180 mg

    360 mg

    Glyceryl monocaprylate

    3.5 mg

    7 mg

    14 mg

    Macrogol glycerol hydroxy stearate

    91.4 mg

    182.8 mg

    365.6 mg

    Propylene glycol

    28.6 mg

    57.2 mg

    114.4 mg

    Macrogol and glycerides of corn oil esters

    34 mg

    68 mg

    136 mg

    Alpha-tocopherol acetate

    0.5 mg

    1 mg

    2 mg

    Capsule shell composition:

    Gelatin

    27 mg

    77 mg

    131 mg

    Glycerol

    12 mg

    35 mg

    61 mg

    Methylparahydroxybenzoate

    0.05 mg

    0.14 mg

    0.24 mg

    Propyl parahydroxybenzoate

    0.01 mg

    0.03 mg

    0.06 mg

    Purified water

    22 mg

    65 mg

    111 mg

    Description:

    Dosage of 25 mg. Spherical soft gelatin capsules from light yellow to brown color with a transparent shell. The contents of the capsules are a clear, oily liquid of light yellow color.

    Dosage of 50 and 100 mg. Oblong soft gelatin capsules from light yellow to brown with a transparent coating. The contents of the capsules are a clear, oily liquid of light yellow color.

    Pharmacotherapeutic group:Immunosuppressive remedy
    ATX: & nbsp

       

    Pharmacodynamics:

    Immunosuppressive agent, a cyclic polypeptide consisting of 11 amino acids. Suppresses the development of cell-type reactions, including allograft immunity, delayed-type cutaneous hypersensitivity, allergic encephalomyelitis, Freund's adjuvant-mediated disease, graft-versus-host disease, and T-lymphocyte-dependent antibody production. At the cellular level, it blocks the resting lymphocytes in the G phases0 or G1 cell cycle and suppresses the antigen-triggered production and secretion of cytokines (including interleukin-2, T-lymphocyte growth factor) by activated T lymphocytes. It acts on lymphocytes reversibly.Does not suppress hemopoiesis and does not affect the functioning of phagocytic cells.

    Pharmacokinetics:

    Bioavailability - 30%, increases with increasing dose and duration of treatment. Absorption decreases after liver transplantation, with liver diseases or pathology of the gastrointestinal tract (diarrhea, vomiting, paralytic intestinal obstruction). Intensively binds to proteins and shaped elements of blood (concentration in whole blood is 2-9 times higher than in plasma). The connection with plasma proteins is 90% (mainly with lipoproteins). It is distributed mainly outside the bloodstream; is present in plasma -33-47%, in lymphocytes - 4-9%, in granulocytes - 5-12%, in erythrocytes - 41-58%. Time to reach the maximum concentration in the plasma - after 1,5-3,5 h after oral intake.

    Metabolised in the liver, to a lesser extent in the wall of the gastrointestinal tract and kidneys. In the metabolism of the drug, isozymes CYP3A4, CYP3A5 and CYP3A7 are involved. It is excreted with bile; kidneys - 6% of the administered oral dose (0.1% - unchanged). T1/2 -19 h (10-27 h) in adults and 7 h (7-19 h) - in children, regardless of dose or route of administration. Excreted in breast milk. It is not excreted during hemodialysis.

    Indications:

    In combination with other immunosuppressive drugs and glucocorticosteroids - to prevent rejection reactions in bone marrow transplantation, kidney, liver, heart, combined cardiopulmonary graft, lung or pancreas.

    Autoimmune diseases, endogenous uveitis (active, eye-threatening uveitis of the middle or posterior region of the eye of non-infectious etiology, if conventional therapy does not result or leads to severe side effects), Behcet's uveitis (with recurrent attacks of inflammation affecting the retina); atopic dermatitis (in severe form, in cases when systemic therapy is indicated); nephrotic syndrome (in remission, steroid-dependent and steroid-resistant form); psoriasis (severe persistent course, insufficient response to systemic treatment); rheumatoid arthritis (severe forms of active course in cases when classical slow-acting antirheumatic drugs are ineffective or their use is impossible).

    Contraindications:

    Hypersensitivity (including polyoxyethylated castor oil).

    For indications not related to transplantation: malignant neoplasms, precancerous skin diseases; lactation period; Children's age up to 3 years (for this dosage form); children's age (for the treatment of psoriasis, rheumatoid arthritis and atopic dermatitis).

    Carefully:

    Chicken pox (currently or recently transferred, including recent contact with the patient), Varicella zoster (risk of generalization of the process) and other viral diseases, renal and / or hepatic insufficiency, hyperkalemia, hypertension, infections, malabsorption syndrome.

    Pregnancy and lactation:

    Teratogenic effects of cyclosporine in animals have not been revealed. However, studies on use in pregnant women have not been carried out, so the possibility of using the preparation of Orgasporin® in pregnancy should be limited only to those cases when the expected benefit for the mother justifies the potential risk to the fetus. Cyclosporin penetrates into breast milk, so breast-feeding mothers should stop breastfeeding.

    Dosing and Administration:

    Inside: for adults with a solid organ transplant treatment should be started 12 hours before the operation in a dose of 10-15 mg / kg, divided into 2 doses.Within 1-2 weeks after surgery - daily, at the same dose and then gradually reduce the dose (5% per week) until the maintenance - 2-6 mg / kg per day. When administered in combination with corticosteroids or other immunosuppressants using lower doses (3-6 mg / kg per day during the initial phase of treatment).

    In bone marrow transplantation: the day before transplantation and for 2 weeks, administered in a daily dose of 12.5-15 mg / kg, then pass to a maintenance therapy dose of about 12.5 mg / kg per day (in violation absorption may require higher oral doses or a switch to intravenous administration). Supportive treatment continues for at least 3-6 months (preferably 6 months), after which the dose was gradually reduced so that 1 year after transplant treatment was discontinued. In some patients, after the cessation of treatment, a rejection reaction develops, in which case the treatment should be resumed.

    When endogenous uveitis, to induce remission - an initial daily dose of 5 mg / kg, in one or more steps, until remission of inflammation and improvement of visual acuity. In severe cases, the dose can be increased to 7 mg / kg per day for a limited period.In the course of maintenance therapy, the dose should be slowly reduced to the lowest effective dose, which during the remission period should not exceed 5 mg / kg per day.

    In nephrotic syndrome, to induce remission - in a daily dose of 5 mg / kg, provided that there is no decrease in kidney function (except for cases of proteinuria). For patients with impaired renal function, the initial daily dose should not exceed 2.5 mg / kg. If monotherapy with the preparation of Orgasporin® fails to achieve the desired effect, it is possible to combine with small doses of glucocorticosteroids, inside. If after 3 months of treatment no positive effect is observed, therapy should be discontinued. For maintenance treatment, the dose should be slowly reduced to a minimum effective dose.

    With rheumatoid arthritis for the first 6 weeks of treatment, the daily dose is 3 mg / kg in 2 divided doses. In case of insufficient effect, the daily dose can be gradually increased under the condition of satisfactory tolerability (not more than 5 mg / kg per day). The course of treatment is up to 12 weeks. For maintenance therapy, the dose should be selected individually, depending on the tolerability (can be prescribed in combination with small doses of glucocorticosteroids and / or non-steroidal anti-inflammatory drugs).

    In psoriasis, for induction of remission, the daily dose is 2.5 mg / kg in 2 divided doses. In severe cases, when rapid effect is required, the initial daily dose may be 5 mg / kg. If it was not possible to achieve an adequate effect when administered at a daily dose of 5 mg / kg for 6 weeks, the drug should be discontinued. The dose for maintenance treatment of psoriasis should be minimally effective (should not exceed 5 mg / kg per day). Atopic dermatitis - the initial dose of 2.5 mg / kg per day. In severe cases, the dose may be increased to 5 mg / kg per day. When a positive result is achieved, the dose should be gradually reduced to a complete cancellation. Children over the age of two years are prescribed in the same doses as adults at a rate of 1 kg of body weight.

    Side effects:

    From the urinary system: renal dysfunction, nephropathy, interstitial fibrosis, hematuria.

    From the cardiovascular system: increased blood pressure (often asymptomatic), arrhythmias.

    From the side of the central nervous system and the peripheral nervous system: headache, tremor, paresthesia, hyperesthesia, epileptic syndrome, retardation,disorientation, agitation, sleep disturbance, impaired consciousness, visual disorders, encephalopathy, motor disorders, edema of optic discs.

    From the digestive system: anorexia, nausea, vomiting, diarrhea, gingival hyperplasia, abdominal pain, impaired liver function, increased activity of "liver" transaminases, hyperbilirubinemia, pancreatitis.

    On the part of the hematopoiesis system: anemia, thrombocytopenia.

    From the side of metabolism: hyperlipidemia, hyperuricemia, hyperkalemia, hypomagnesemia, hyperglycemia.

    From the musculoskeletal system: short-term muscle spasms, muscle weakness, myopathy.

    From the endocrine system: Dysmenorrhea, amenorrhea, gynecomastia, hypertrichosis.

    Allergic reactions: skin rash, respiratory distress syndrome; "tides" of blood to the skin of the face and upper body, bronchospasm, lowering blood pressure, tachycardia, in severe cases - shock, the occurrence of which is associated with polyoxyethylated castor oil.

    Other: weakness, fatigue, edematous syndrome, weight gain, burning in the hands and feet; against a background of microangiopathic hemolytic anemia and renal insufficiency - hemolyticuremic syndrome.

    Lymphoproliferative diseases after transplantation: lymphoma, malignant skin diseases.

    Overdose:

    Symptoms: impaired renal function.

    Treatment: if there are indications, symptomatic therapy is performed. The drug is practically not excreted from the body during hemodialysis and hemoperfusion with the use of activated charcoal. It is necessary to reduce the dose by 25-50% in patients who, on the background of treatment, have an increase in blood pressure, hypercreatininaemia (more than 30% of the initial value). If it is not possible to control the side effect or if the kidney function is severely impaired, the drug is canceled.

    Interaction:

    Strengthens the action of quinidine, theophylline, valproic acid. When treating with cyclosporin, excess intake of potassium ions in the body (with food, with potassium-containing drugs) should be avoided, and potassium-sparing diuretics, potassium-containing penicillins, heparin, angiotensin converting enzyme inhibitors, beta-adrenoblockers, cardiac glycosides should not be prescribed. When cyclosporine is used in conjunction with other immunosuppressive drugs (azathioprine, chlorambucil, glucocorticosteroids, cyclophosphamide, mercaptopurine) there is a risk of developing excessive immunosuppression, which can lead to increased sensitivity to infections and the development of lymphoproliferative diseases.

    Increases the risk of developing nephrotoxicity of aminoglycosides, amphotericin B, fluoroquinolones, melphalan, colchicine, trimethoprim, non-steroidal anti-inflammatory drugs (it is necessary to reduce the dose of both drugs). Reduces the clearance of prednisolone, treatment with high doses of prednisolone may increase the concentration of cyclosporine in the blood.

    Allopurinol, bromocriptine, cimetidine, clarithromycin, androgens, estrogens, danazol, diltiazem, some macrolide antibiotics (including, erythromycin and josamycin), doxycycline, oral contraceptives, propafenone, some blockers of "slow" calcium channels (including verapamil, diltiazem, nicardipine), miconazole, fluconazole, itraconazole, ketoconazole, HIV protease inhibitors, metoclopramide, grapefruit juice can increase the concentration of cyclosporin (inhibition of the isoenzyme CYP3 A), increasing the risk of hepatitis and nephrotoxicity.Inductors P450 isoenzyme CYP3A (barbiturates, carbamazepine, phenytoin, metamizol sodium, benzodiazepine derivatives, aminoglutethimide, estrogen-gestagenic drugs, progesterone, isoniazid, rifampicin, nafcillin, and sulfadimidine and trimethoprim) accelerate the metabolism of cyclosporine (dose adjustment is necessary).

    Statins (lovastatin and simvastatin) increase the risk of rhabdomyolysis and acute renal failure.

    Colchicine increases the risk of developing myalgia and weakness; nifedipine - gingival hyperplasia. Non-steroidal anti-inflammatory drugs (indomethacin, diclofenac, naproxen) increase the risk of kidney failure and gilercalemia. Non-steroidal anti-inflammatory drugs can potentially reduce the amount of glomerular filtration, their addition or increase in dose should be accompanied by strict control of kidney function (especially at the initial stages of treatment). Activated carbon, metoksalen, trioksalen, PUVA-therapy (combined therapeutic effect on the skin of medicinal substances of plant origin - psoralens (photosensitizer, agent,which increases the sensitivity of the skin to light) and soft long-wave ultraviolet rays, is used in the treatment of psoriasis) increase the risk of developing malignant skin tumors.

    During treatment with cyclosporine, vaccination may be less effective (use of live attenuated vaccines should be avoided).

    Special instructions:

    The spectrum of side effects is generally the same for different indications, although the frequency and severity of side effects may vary. In patients who undergone transplantation, due to a higher dose and longer duration of treatment, side effects may occur more frequently and be more pronounced than in patients with other indications. Orgosporin® should be used by physicians with experience of conducting immunosuppressive therapy and have the ability to provide adequate monitoring of the patient, including regular complete physical examination, blood pressure measurement and monitoring of laboratory safety indicators. Patients treated with Orsporin® are less likely to be infected than those who receive therapy with other antidepressants.In patients who underwent liver transplantation, to determine the concentration of the preparation of Orgasporin® in order to select doses that provide sufficient immunosuppressive effect, specific monoclonal antibodies should be used or a parallel determination using both specific and nonspecific monoclonal antibodies. In the process of treatment with the preparation of Orgasporin® systematic monitoring of the functional state of the kidneys and liver is shown, control of blood pressure; ions of potassium and magnesium in plasma (especially in patients with impaired renal function); concentration of urea, creatinine, uric acid, bilirubin, "liver" enzymes, amylase and lipids in blood serum (before treatment and after 1 month of treatment). If the increase in the concentration of lipids, urea, creatinine, bilirubin, "liver" enzymes in the blood has a persistent character, should reduce the dose of the drug Orgasorin®. In the case of the development of hypertension, it is necessary to initiate antihypertensive treatment.

    Effect on the ability to drive transp. cf. and fur:

    During the treatment period, care must be taken when driving vehicles and other potentially hazardous speciesactivities that require increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:Soft capsules.
    Packaging:

    10 capsules per contour cell package. For 10 or 50 capsules in a plastic jar. A bag (container) with silica gel is placed in a jar. Each jar, or 1, or 5 contour squares, together with the instruction for use, is placed in a bundle.

    Storage conditions:

    In dry, the dark place at a temperature of no higher than 25 C.

    Keep out of the reach of children.

    Shelf life:

    2 years. Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-001676
    Date of registration:16.09.2011
    Expiration Date:Unlimited
    The owner of the registration certificate:MIR-FARM, LLC MIR-FARM, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp11.06.2017
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