Orgasporin

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

Orgasporin: instructions for use and reviews

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

Latin name: Orgasporin

ATX code: L04AD01

Active ingredient: cyclosporin (Ciclosporin)

Manufacturer: LLC Pharmasintez-Tyumen (Russia); Obninsk Chemical-Pharmaceutical Company CJSC (Russia)

Description and photo update: 2019-23-10

Orgasporin is an immunosuppressive drug.

Release form and composition

The drug is produced in the form of capsules: gelatinous, with a transparent soft shell, from light yellow to brown, in a dosage of 25 mg - spherical, in a dosage of 50 mg and 100 mg - oblong; the contents of the capsules are an oily transparent liquid mass of light yellow color (10 pcs. in blisters, in a cardboard box 1 or 5 packs; 10 or 50 pcs. in polymer cans, a cardboard box of 1 can. Each pack also contains instructions on the use of Orgasporin).

One capsule contains:

active substance: cyclosporine - 25, 50 or 100 mg;
auxiliary components: propylene glycol caprylate (propanediol monocaprylate), glyceryl monocaprylate (caprylic acid monoglyceride), propylene glycol, macrogol glyceryl hydroxystearate 40 (hydrogenated castor oil polyoxyl 40), alpha-tocopherol glycerol and acetate oil, macrogol
capsule shell: gelatin, methyl parahydroxybenzoate, glycerol, propyl parahydroxybenzoate, purified water.

Pharmacological properties

Pharmacodynamics

Orgasporin is an immunosuppressive drug containing, as an active component, cyclosporin, which is a cyclic polypeptide consisting of 11 amino acids.

The mechanism of action of the drug is associated with the ability of cyclosporin at the cellular level to block lymphocytes resting in the G0 or G1 phase of the cell cycle, and to suppress antigen-triggered production and secretion of interleukin-2, T-lymphocyte growth factor and other cytokines activated by T-lymphocytes. The substance acts reversibly on lymphocytes.

Suppressing the development of cell-type reactions such as immunity against allograft, delayed-type cutaneous hypersensitivity, allergic encephalomyelitis, graft-versus-host reaction (GVHD) caused by the administration of Freund's adjuvant adjuvant-induced arthritis, T-lymphocyte-dependent formation of non-antibodies inhibits hematopoiesis and does not affect the functioning of phagocytic cells.

Pharmacokinetics

After oral administration, the maximum plasma concentration of cyclosporine is reached after 1.5-3.5 hours. Its bioavailability, on average, remains 30% and increases with increasing dose, as well as the duration of the course of treatment. In patients after liver transplantation, with liver disease or pathologies of the gastrointestinal tract (vomiting, diarrhea, paralytic intestinal obstruction), the absorption of the drug decreases.

Plasma protein binding (mainly lipoproteins) at 90%. Because of the intense connection with proteins and blood cells, the concentration of cyclosporine in whole blood is 2–9 times higher than in plasma. It is distributed mainly outside the bloodstream. Plasma contains 33 to 47% of the dose, lymphocytes 4–9%, erythrocytes 41–58%, granulocytes 5–12%.

It is metabolized with the participation of isoenzymes CYP3A4, CYP3A5 and CYP3A7, to a greater extent in the liver, a small part in the wall of the gastrointestinal tract and kidneys.

Regardless of the dose or route of administration, the half-life (T _1/2) of cyclosporin in adults averages 19 hours, in children - from 7 to 19 hours. 6% of the received oral dose is excreted through the kidneys, the rest is excreted in the bile. Cyclosporin is excreted in breast milk. With hemodialysis, it is not displayed.

Indications for use

In transplantation, Orgasporin is used for the transplantation of solid organs such as kidneys, liver, heart, combined cardiopulmonary transplant, lungs or pancreas, in order to prevent the rejection of allografts. The drug is also prescribed for the treatment of transplant rejection in patients who have previously received other immunosuppressants.

In bone marrow transplantation, the indication for the use of Orgasporin is:

the period after bone marrow transplant - for the prevention of transplant rejection;
GVHD (graft-versus-host disease) - for therapy and prevention.

Autoimmune diseases not related to organ transplant for which it is recommended to take Orgasporin:

uveitis: endogenous uveitis (active phase of vision-threatening uveitis of the middle or posterior region of the eye of non-infectious etiology) - if there is no therapeutic effect from conventional treatments or they cause severe adverse reactions in the patient; Behcet's uveitis (with relapses of inflammation affecting the retina);
psoriasis: the most severe forms that do not respond to traditional systemic therapy, or when it is not effective enough;
nephrotic syndrome: steroid-dependent and steroid-resistant in adults and children (due to minimal change nephropathy, focal and segmental glomerulosclerosis, membranous glomerulonephritis, leading to glomerular pathology), provided that previous therapy with cytostatics was not effective enough or led to the development of severe side effects reactions. It is prescribed exclusively for the treatment of patients whose renal function indicators are at least 50% of the norm. Orgasporin is used to induce / maintain remission, as well as to maintain remission induced by the use of glucocorticosteroids in order to ensure the possibility of their cancellation
rheumatoid arthritis: severe forms of active rheumatoid arthritis, the previous therapy of which with basic DMARDs (disease-modifying antirheumatic drugs) was ineffective or led to the development of severe adverse reactions;
atopic dermatitis: severe forms of the disease when previous treatment was not effective enough or caused severe side effects that require systemic treatment.

Contraindications

Absolute contraindications for the appointment of Orgasporin:

malabsorption of sucrose-isomaltose, food intolerance to fructose, galactosemia (sorbitol is included in the capsules);
lactation period;
children's age up to three years (this dosage form);
established intolerance to polyoxyethylated castor oil, hypersensitivity to cyclosporine and / or any other ingredient of the drug.

Absolute contraindications for the treatment of conditions / diseases not related to transplantation:

impaired renal function (except for patients with moderate nephrotic syndrome);
NCAH (uncontrolled arterial hypertension);
infectious diseases resistant to appropriate therapy;
malignant tumors, precancerous skin diseases.

Additional absolute contraindications for psoriasis therapy:

severe impairment of hepatic function;
long-term methotrexate therapy;
simultaneous PUVA (psoralen-ultraviolet) therapy or ultraviolet therapy (also contraindicated in atopic dermatitis);
the combined use of other immunosuppressants (retinoids, methotrexate, etc.).

Orgasporin should be used with caution in patients with chickenpox (including recent or contact with a patient), Varicella zoster and other viral or infectious diseases, renal and / or hepatic failure, arterial hypertension, hyperkalemia, malabsorption syndrome, during pregnancy.

Orgasporin, instructions for use: method and dosage

Orgasporin capsules are taken orally.

The cyclosporin dose ranges given below are to be considered approximate. For the purpose of their correction, patients are provided with control of the plasma concentration of cyclosporine by an enzyme-linked immunosorbent assay using monoclonal antibodies.

Recommended dosage:

transplantation of solid organs in adults: monotherapy - taking Orgasporin should be started 12 hours before the operation at a dose of 10-15 mg per 1 kg of patient weight (mg / kg), divided into 2 doses. After the operation, treatment is continued at the same dose, taking it daily for 7-14 days. Then they begin to gradually (by 5% in 7 days) decrease it until the maintenance dose is reached - 2–6 mg / kg per day. As part of combination therapy with other immunosuppressants or GCS - in the initial phase of treatment, the use of a reduced dose of Orgasporin is indicated - 3–6 mg / kg per day;
bone marrow transplantation: at a daily dose of 12.5–15 mg / kg, the intake starts from the day before the transplant and continues for 14 days after it. Then the patient is transferred to supportive therapy, the dose is selected individually, taking into account the subjective degree of absorption of the drug. The usual maintenance dose is about 12.5 mg / kg per day. In patients with impaired absorption, it is possible to use higher doses of cyclosporine or switch to dosage forms for intravenous (IV) administration. The duration of the course of maintenance therapy should be at least 90 days, optimally 180 days. Then the maintenance dose is gradually reduced at a rate that will ensure that Orgasporin is discontinued by the end of the first year after the transplant. If, after discontinuation of cyclosporine, the patient develops a rejection reaction,treatment must be resumed;
endogenous uveitis: induction of remission - from 5 to 7 mg / kg per day (once or divided into several doses) for a period sufficient to relieve inflammation and improve visual acuity. Maintenance therapy should be carried out at the lowest effective dose that can be achieved by gradually reducing the starting dose. During the period of remission of the disease, the dose should not exceed 5 mg / kg per day;
nephrotic syndrome: induction of remission - 5 mg / kg per day, including patients with proteinuria. The initial daily dose for impaired renal function is not more than 2.5 mg / kg per day. If monotherapy with Orgasporin does not allow achieving the desired therapeutic effect, the combined use of the drug with small doses of oral forms of GCS is indicated. In the absence of a positive effect after 90 days of taking the drug, treatment should be discontinued. For maintenance therapy, use the minimum effective dose;
rheumatoid arthritis: 1.5 mg / kg 2 times a day for the first 42 days. In the absence of a sufficient effect, patients with satisfactory tolerance are shown a gradual increase in the daily dose, which should not exceed 5 mg / kg per day. The duration of the course of treatment is up to 84 days. The dose of maintenance therapy is selected individually, taking into account the tolerability of Orgasporin. Perhaps the appointment of cyclosporine in combination with low doses of GCS and / or non-steroidal anti-inflammatory drugs (NSAIDs);
psoriasis: induction of remission - 2.5 mg / kg per day, divided into 2 doses. In severe cases of the disease, for a quick effect, you can increase the initial daily dose to 5 mg / kg. If treatment at a daily dose of 5 mg / kg for 42 days does not give an adequate response, the use of Orgasporin should be discontinued. The dose of maintenance therapy should be the minimum effective, and not more than 5 mg / kg per day;
atopic dermatitis (adults and children over the age of three): the initial dose is 2.5 mg / kg per day, in severe cases, up to 5 mg / kg per day. After achieving a positive result, it is gradually lowered until it is completely canceled.

If the dosage regimen of Orgasporin with taking capsules in the morning and in the evening in equal doses is not effective enough, especially in patients with low body weight, it is possible:

In the morning and evening, take different doses of the drug.
Change the dosage form of the drug using cyclosporine in the form of an oral solution.

Side effects

on the part of the cardiovascular system: increased blood pressure (BP), arrhythmias;
from the urinary system: nephropathy, functional disorders of the kidneys, hematuria, interstitial fibrosis;
from the nervous system: sleep disturbance, headache, lethargy, agitation, paresthesia, hyperesthesia, disorientation, epileptic syndrome, impaired consciousness, tremor, movement disorders, visual disturbances, edema of the optic nerve discs, encephalopathy;
from the digestive system: nausea, vomiting, gingival hyperplasia, abdominal pain, diarrhea, anorexia, liver dysfunction, pancreatitis, increased liver transaminase activity, hyperbilirubinemia;
from the hematopoietic system: thrombocytopenia, anemia;
from the side of metabolism: hyperkalemia, hyperlipidemia, hyperuricemia, hypomagnesemia, hyperglycemia;
from the musculoskeletal system: muscle weakness, short-term muscle spasms, myopathy;
from the endocrine system: gynecomastia, hypertrichosis, dysmenorrhea, amenorrhea;
from the immune system: allergic reactions, including skin rash, respiratory distress syndrome; with hypersensitivity to polyoxyethylated castor oil - bronchospasm, rush of blood to the skin of the upper body and face, lowering blood pressure, tachycardia, up to shock;
others: fatigue, weakness, weight gain, edema syndrome, burning sensation in the hands and feet; against the background of renal failure and microangiopathic hemolytic anemia - the development of hemolytic-uremic syndrome;
lymphoproliferative pathologies (in patients who underwent transplantation): malignant skin diseases, lymphoma.

Overdose

An overdose of cyclosporine may result in impaired renal function.

In this condition, the appointment of symptomatic therapy is recommended. The use of hemodialysis and hemoperfusion using activated charcoal for elimination of cyclosporine from the body is practically ineffective. If during treatment there is an increase in blood pressure, hypercreatininemia (exceeding the initial value by more than 30%), then it is necessary to reduce the dose of the drug by 25-50%. In case of severe renal dysfunction or inability to control the side effect, Orgasporin is canceled.

special instructions

Orgasporin should be prescribed by a doctor with experience in immunosuppressive therapy. Treatment should be accompanied by close monitoring of the patient's condition, including measurement of blood pressure, regular complete physical examination and monitoring of laboratory parameters. Systematic monitoring of the functional state of the liver and kidneys, potassium and magnesium ions in plasma (especially with impaired renal function), the level of serum concentration of urea, uric acid, creatinine, bilirubin, hepatic enzymes, amylase and lipids is shown. It should be started before using the drug and continued after 1 month of treatment. If there is a persistent increase in the concentration in the blood of creatinine, lipids, urea, bilirubin or liver enzymes, then the dose of the drug should be reduced. With the development of arterial hypertension, it is necessary to begin its treatment.

In cases of using Orgasporin for various indications, the spectrum of undesirable effects is generally the same, only their frequency and severity can vary, depending on the dose and duration of treatment. Therefore, after transplantation, side effects are more pronounced and occur more often than when using the drug for other indications.

Against the background of the use of Orgasporin, patients are less susceptible to infections compared to treatment with other antidepressants.

For dose selection in patients undergoing liver transplantation, it is recommended to use specific monoclonal antibodies or to carry out parallel determination using specific and non-specific monoclonal antibodies.

Influence on the ability to drive vehicles and complex mechanisms

During the period of treatment with Orgasporin, patients should be careful when engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions, including driving and complex mechanisms.

Application during pregnancy and lactation

During pregnancy, the use of cyclosporine is allowed in exceptional cases when the expected therapeutic effect for the mother fully justifies the potential threat to the fetus.

The use of Orgasporin capsules during lactation is contraindicated, therefore, if it is necessary to prescribe the drug, breastfeeding should be discontinued.

Pediatric use

It is contraindicated to prescribe Orgasporin to children under the age of three years, as well as for the treatment of psoriasis and rheumatoid arthritis in children over three years old.

For children over the age of three, cyclosporine is prescribed in doses as for adult patients, calculated for 1 kg of body weight.

With impaired renal function

Orgasporin should be used with caution in patients with renal insufficiency.

For violations of liver function

Orgasporin should be used with caution in patients with hepatic impairment.

Drug interactions

With the simultaneous use of Orgasporin with other medicinal substances / preparations, their pharmacological interaction with cyclosporin is possible:

quinidine, theophylline, valproic acid: when interacting with cyclosporine, the effectiveness of these agents increases;
potassium-sparing diuretics, angiotensin-converting enzyme inhibitors, potassium preparations and potassium-containing agents (cardiac glycosides, angiotensin-converting enzyme inhibitors, beta-blockers, heparin, potassium-containing penicillins, potassium-sparing diuretics should be avoided in the body: potassium-sparing diuretics should be avoided in the body: with the listed drugs;
GCS, azathioprine, chlorambucil, mercaptopurine, cyclophosphamide: concomitant therapy with other immunosuppressants contributes to the development of excessive immunosuppression, which may result in increased sensitivity to infections and the occurrence of lymphoproliferative diseases;
NSAIDs, aminoglycosides, amphotericin B, melphalan, colchicine, fluoroquinolones, trimethoprim: when combined with these drugs, the likelihood of developing their nephrotoxicity increases, therefore it is necessary to reduce the dose of both drugs;
prednisolone: the clearance of prednisolone decreases, possibly an increase in the concentration of cyclosporine in the blood when combined with high doses of prednisolone;
allopurinol, bromocriptine, clarithromycin, cimetidine, androgens, estrogens, diltiazem, danazol, some macrolide antibiotics (including erythromycin, josamycin), oral contraceptives, doxycycline, propafenone, slow calcium channel blockers (including diltiazemiltiazem), nauketazem, miconazole, itraconazole, HIV protease inhibitors (human immunodeficiency virus), metoclopramide, as well as grapefruit juice: it should be borne in mind that when combined with each of these agents, the risk of increased plasma concentration of cyclosporine and the occurrence of nephro- and hepatotoxicity increases;
metamizole sodium, barbiturates, phenytoin, carbamazepine, benzodiazepine derivatives, aminoglutethimide, progesterone, estrogen-progestogen agents, isoniazid, rifampicin, nafcillin, trimethoprim, sulfadimidine: as inducers of the isoenzyme CYP3A, the cytochrome ₄₅₀ agents accelerate the cytochrome metabolism; dosing the latter;
lovastatin, simvastatin: the combination with these statins increases the risk of acute renal failure and rhabdomyolysis;
colchicine: concomitant therapy with colchicine increases the likelihood of developing weakness and myalgia;
nifedipine: the risk of developing gingival hyperplasia increases when cyclosporine is combined with nifedipine;
indomethacin, naproxen, diclofenac: these drugs increase the risk of renal failure and hyperkalemia. It should be borne in mind that the combination with NSAIDs can potentially cause a decrease in the value of glomerular filtration, therefore, when adding or increasing their dose, it is necessary to carefully monitor renal function, especially at the initial stage of treatment;
trioxalen, methoxalen, activated carbon, PUVA therapy: the risk of developing skin malignant neoplasms increases.

In addition, during the period of treatment with Orgasporin, vaccination is less effective; it is recommended to avoid the use of live attenuated vaccines.

Analogs

Orgasporin analogs are Cyclosporin Hexal, Cyclosporin Sandoz, Panimun Bioral, Restasis, Sandimmun, Sandimmun Neoral, Ekoral, etc.

Terms and conditions of storage

Keep out of the reach of children.

Store at temperatures up to 25 ° C, protected from moisture and light.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Orgasporin

Currently, there are not enough reviews about Orgasporin from patients and specialists to assess its safety and effectiveness.

The drug is a generic drug of a domestic production of a well-known original drug developed by a foreign pharmaceutical company. It is rarely found on sale (in Moscow pharmacies there are from 10 to 100 proposals). Patients most often prefer not to take risks and prefer the original, despite the higher cost, if they have the opportunity.

The price of Orgasporin in pharmacies

Registered prices for Orgasporin, included in the list of vital and essential medicines (VED), capsules of 50 pcs. packaged:

dosage 25 mg - 770 rubles;
dosage of 50 mg - 1500 rubles;
dosage 100 mg - 2915 rubles.

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, 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!