Universal reference book for medicines
Product name: ORGASPORIN ® (ORGASPORIN)

Active substance: ciclosporin

Type: Immunosuppressive drug

Manufacturer: MIR-PHARM (Russia) manufactured Obninsk Chemical and Pharmaceutical Company (Russia)
Composition, form of production and packaging
Capsules
spherical, soft gelatinous, from light yellow to brown color with a transparent shell;
the contents of the capsules are a clear, oily liquid of light yellow color.
1 caps.

cyclosporin 25 mg

Excipients: propylene glycol caprylate (propanediol monocaprylate), glyceryl monocaprylate (caprylic acid monoglyceride), polyoxyl 40 hydrogenated castor oil (macrogol glycerol hydroxy stearate 40), propylene glycol, macrogol glycerol linoleate,? -tocopherol acetate.

The composition of the capsule shell: gelatin, glycerol, methyl parahydroxybenzoate, propyl parahydroxybenzoate, purified water.

5 pieces.
- blisters (10) - packs of cardboard.
10 pieces.
- plastic cans (1) - packs of cardboard.
Capsules oblong, soft gelatinous, from light yellow to brown color with a transparent membrane;
the contents of the capsules are a clear, oily liquid of light yellow color.
1 caps.

cyclosporin 50 mg

- "- 100 mg

Excipients: propylene glycol caprylate (propanediol monocaprylate), glyceryl monocaprylate (caprylic acid monoglyceride), polyoxyl 40 hydrogenated castor oil (macrogol glycerol hydroxy stearate 40), propylene glycol, macrogol glycerol linoleate,? -tocopherol acetate.

The composition of the capsule shell: gelatin, glycerol, methyl parahydroxybenzoate, propyl parahydroxybenzoate, purified water.

5 pieces.
- blisters (10) - packs of cardboard.
10 pieces.
- plastic cans (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

The product description was approved by the manufacturer for the 2009 print edition.

PHARMACHOLOGIC EFFECT

The immunosuppressive drug is a cyclic polypeptide consisting of 11 amino acids.

Suppresses the development of cell-type reactions, including allograft immunity, delayed-type skin reactions, allergic encephalomyelitis, Freund's adjuvant-mediated disease, graft-versus-host disease, and T-lymphocyte-dependent antibody production.

At the cellular level, it blocks lymphocytes in the G 0 or G 1 phase of the cell cycle and suppresses the antigen-dependent production and secretion of cytokines (interleukin-2, T-lymphocyte growth factor) by activated T lymphocytes.

Ciclosporin acts on the lymphocytes reversibly.
Does not suppress hemopoiesis and does not affect the function of phagocytes.
PHARMACOKINETICS

Suction

C max in plasma is achieved through 1.5-3.5 h after ingestion.
Bioavailability is 30% and increases with increasing dose and duration of treatment.
Distribution

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%.
Excreted in breast milk.

Metabolism

Metabolised in the liver, to a lesser extent in the wall of the digestive tract and kidneys.
In the metabolism of the drug, isozymes CYP3A4, CYP3A5 and CYP3A7 are involved.
Excretion

It is excreted mainly with bile, with urine 6% of the dose taken inward (0.1% in unchanged form) is excreted.
T 1/2 in adults - 19 hours (10-27 hours), in children 7 hours (7-19 hours), regardless of dose or route of administration. It is not excreted during hemodialysis.
Pharmacokinetics in special clinical cases

Absorption of cyclosporine decreases with liver disease or gastrointestinal pathology.

INDICATIONS

Transplantation

- prevention of rejection reaction in the transplantation of bone marrow, kidney, liver, heart, combined cardiopulmonary graft, lung or pancreas (in combination with other immunosuppressants and GCS);

- prevention and treatment of the disease "graft versus host";

- transplant rejection in patients who previously received other immunosuppressants.

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 produce results or leads to serious side effects), Behcet uveitis (with recurrent attacks of inflammation affecting the retina);

- severe forms of atopic dermatitis, when systemic therapy is required;

- Nephrotic syndrome (remission, steroid-dependent and steroid-resistant form);

- psoriasis (with severe persistent flow, with insufficient response to traditional therapy);

- rheumatoid arthritis (severe forms of active course in cases when classical antirheumatic drugs are ineffective or their use is impossible).

DOSING MODE

Adults with transplantation of solid organs should be treated 12 hours prior to surgery at a dose of 10-15 mg / kg divided into 2 doses.
Within 1-2 weeks after the operation, the drug is prescribed daily, at the same dose, after which the dose is gradually reduced (by 5% per week) until the maintenance dose reaches 2-6 mg / kg / day. When administered in combination with SCS or other immunosuppressive drugs, lower doses (3-6 mg / kg / day at the initial stage of therapy) are used.
In bone marrow transplantation, the drug is prescribed on the day preceding the operation and within 2 weeks after the operation at a daily dose of 12.5-15 mg / kg, then go on maintenance therapy at a dose of about 12.5 mg / kg / day (with an impaired absorption, the drug inside at higher doses or the transition to an IV injection).Supportive treatment continues for at least 3-6 months (preferably 6 months), after which the dose is gradually reduced so that treatment is discontinued after 1 year after transplantation.
In some patients, after the cessation of treatment, a rejection reaction develops, in which case therapy should be resumed.
With endogenous uveitis, to achieve remission, the drug is administered at an initial daily dose of 5 mg / kg in 1 or more doses until the signs of active inflammation disappear and visual acuity is improved.
In cases that are difficult to treat, the dose may be increased to 7 mg / kg / day for a short period. During maintenance therapy, the dose should be slowly reduced to the lowest effective dose, which should not exceed 5 mg / kg / day during the remission period.
In nephrotic syndrome, to achieve remission, the recommended daily dose is 5 mg / kg with normal renal function.
In patients with impaired renal function, the initial dose should not exceed 2.5 mg / kg / day. If monotherapy with Orgosporin fails to achieve the effect, it is recommended that it be combined with oral GCS in low doses. 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.
In rheumatoid arthritis during the first 6 weeks of treatment, the recommended dose is 3 mg / kg / day in 2 divided doses.
In case of insufficient effect, the daily dose can be gradually increased, if tolerability permits, but should not exceed 5 mg / kg. The course of treatment is 12 weeks. For maintenance therapy, the dose should be selected individually, depending on the tolerability of the drug (can be given in combination with low doses of GCS and / or NSAIDs).
In psoriasis, in order to induce remission, the recommended dose is 2.5 mg / kg / day in 2 divided doses.
In severe cases, when a 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 / day).
Atopic dermatitis, the initial dose is 2.5 mg / kg / day.
In severe cases, the dose can be increased to 5 mg / kg / day. When a positive result is achieved, the dose should be gradually reduced to a complete cancellation.
Children over the age of 2 years are prescribed in the same doses as adults at a rate of 1 kg of body weight.

SIDE EFFECT

On the part of the urinary system: a violation of kidney function, nephropathy, interstitial fibrosis, hematuria.

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

From the central nervous system and peripheral nervous system: headache, tremor, paresthesia, hyperesthesia, epileptic syndrome, inhibition, disorientation, agitation, sleep disturbance, impaired consciousness, visual disorders;
rarely - edema of the optic discs.
On the part of the digestive system: anorexia, nausea, vomiting, diarrhea, gingival hyperplasia, abdominal pain, impaired liver function;
rarely - pancreatitis.
From the hemopoietic system: anemia, thrombocytopenia.

From the side of metabolism: hyperlipidemia, hyperuricemia, hyperkalemia, hypomagnesemia;
rarely - hyperglycemia.
From the musculoskeletal system: short-term muscle spasms;
rarely - muscle weakness, myopathy.
From the endocrine system: dysmenorrhea, gynecomastia, hypertrichosis.

Allergic reactions: skin rash, respiratory distress syndrome;
blood rushes to the skin of the face and upper body, bronchospasm, lowering of blood pressure, tachycardia; in severe cases - shock. The occurrence of allergic reactions may be due to the presence in the preparation of polyoxyethylated castor oil.
Other: fatigue, edematous syndrome, weight gain, burning in the hands and feet.

Lymphoproliferative diseases after transplantation: lymphoma, malignant skin diseases.

CONTRAINDICATIONS

- malignant neoplasms and precancerous skin diseases;

- the period of lactation (breastfeeding);

- Children's age up to 1 year;

- Children's age (for the treatment of psoriasis and rheumatoid arthritis);

- Hypersensitivity to the components of the drug (including polyoxyethylated castor oil).

Caution should be given to the preparation with varicella (currently existing or recently transferred, including recent contact with the patient), shingles (due to the risk of generalization of the process), and other viral diseases, kidney and / or liver failure, hyperkalemia, hypertension , infectious diseases, malabsorption syndrome.

PREGNANCY AND LACTATION

Adequate and well-controlled studies in pregnant women have not been conducted, therefore, do not use Orgasorin in pregnancy, except when the expected benefit for the mother justifies the potential risk to the fetus.

Contraindicated use of the drug during breastfeeding.

APPLICATION FOR FUNCTIONS OF THE LIVER

With caution should prescribe the drug for kidney failure


APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With caution should prescribe the drug for liver failure


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 the use in a higher dose and longer duration of treatment, side effects can occur more often 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, measurement of blood pressure and monitoring of laboratory indicators.

In the treatment with Orgasorin, systematic monitoring of the functional state of the kidneys and liver, control of blood pressure, potassium and magnesium ions in plasma (especially in patients with impaired renal function), urea, creatinine, uric acid, bilirubin, liver enzymes, amylase and lipids in serum (before treatment and after 1 month of treatment).
If the increase in the concentration of lipids, urea, creatinine, bilirubin, hepatic trannaminases in the blood is persistent, reduce the dose of Orgasporin.
Patients receiving treatment with Orgasporin are less prone to infections than those receiving therapy with other immunosuppressants.

In patients who underwent liver transplantation, specific monoclonal antibodies should be used to determine the concentration of Orgosporin for the purpose of selecting doses giving a sufficient immunosuppressive effect or to perform a parallel determination using both specific and nonspecific monoclonal antibodies.

OVERDOSE

Symptoms: impaired renal function.

Treatment: if necessary, conduct symptomatic therapy.
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).
In the case of hypertension, it is necessary to start antihypertensive treatment.
If it is not possible to control the side effect or if the kidney function is severely impaired, the drug should be discontinued.

DRUG INTERACTION

With the simultaneous use of Orgasporin enhances the action of quinidine, theophylline, sodium valproate.

In the treatment with Orgosporin, 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, ACE inhibitors, beta-adrenoblockers, cardiac glycosides should not be prescribed.

When using the Organosporin together with other immunosuppressive drugs (azathioprine, chlorambucil, glucocorticoids, cyclophosphamide, mercaptopurine), there is a risk of developing excessive immunosuppression, which can lead to increased sensitivity to infections and the development of lymphoproliferative diseases.

Orgasorin with simultaneous application increases the risk of developing nephrotoxicity aminoglycosides, amphotericin B, fluoroquinolones, melphalan, colchicine, trimethoprim, NSAIDs (it is necessary to reduce the dose of both drugs).

Orgasporin reduces the clearance of prednisolone, the use of prednisolone in high doses can 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 slow calcium channel blockers (including verapamil, diltiazem, nicardipine), miconazole, fluconazole, itraconazole, ketoconazole, HIV protease inhibitors, metoclopramide, grapefruit juice with simultaneous application with Orgasporin may increase the concentration of cyclosporin (inhibition of the isoenzyme CYP3A) by increasing the rice
to the occurrence of hepato- and nephrotoxicity.
Inductors of the isoenzyme CYP3A (barbiturates, carbamazepine, phenytoin, metamizole sodium, benzodiazepine derivatives, aminoglutethimide, estrogen-progestogen, progesterone, isoniazid, rifampicin, nafcillin, and sulfadimidine and trimethoprim) accelerate the metabolism of cyclosporine (dose adjustment is necessary).

Statins (lovastatin and simvastatin) with simultaneous application with Orgasporin increase the risk of rhabdomyolysis and acute renal failure.

With simultaneous application with Orgasorin colchicine increases the risk of developing myalgia and weakness;
nifedipine - gingival hyperplasia.
NSAIDs (indomethacin, diclofenac, naproxen) with simultaneous application with Orgasporin increase the risk of kidney failure and hyperkalemia.
NSAIDs can potentially reduce the amount of glomerular filtration, their addition or increase in dose should be accompanied by strict control of the kidney function (especially at the initial stages of treatment).
With the simultaneous use of activated carbon, metoxaline, trioxalene, PUVA-therapy (psoriasis) with Orgasporin, the risk of developing malignant skin tumors increases.

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

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. The drug should be stored in a dry, protected from light, inaccessible to children at a temperature of no higher than 25 C. Shelf life - 2 years.

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