Cyclosporine

When ATH:
L04AD01

Pharmacological action.
Immunosuppressive.

Application.

Kidney transplant, liver, hearts, light, pancreas (Prevention of transplant rejection, treatment response rejection), bone marrow (prevention of rejection reaction, prevention and treatment of graft versus host disease); acute non-infectious uveitis, vision-threatening, Behcet's uveitis with recurrent inflammation and retinal involvement, chronic glomerulonephritis, accompanied by the development of nephrotic syndrome, highly active rheumatoid arthritis, psoriasis, severe forms of atopic dermatitis.

Contraindications.

Hypersensitivity (incl. a polyoxyethylated castor oil), malignant neoplasms, serious infectious disease, impaired renal and / or liver function, arterial hypertension, hyperuricemia, hyperkalemia, pregnancy, lactation.

Pregnancy and breast-feeding.

Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

Side effects.

Acute and chronic renal failure, interstitial renal fibrosis, arterial hypertension, tremor, weakness, headache, paresthesia, seizures, myopathy, abnormal liver function, pancreatitis, nausea, vomiting, anorexia, abdominal pain, a feeling of heaviness in the epigastric region, diarrhea, giperplaziya right, fluid retention, reversible dysmenorrhea and amenorrhea, hypertryhoz, thrombocytopenia, anemia, hyperkalemia, hyperuricemia, increased susceptibility to infections.

Cooperation.

Melphalan increases toxicity, diltiazem, nikardipin, verapamil, beta-blockers, fluconazole, imidazole derivatives, glucocorticoids, macrolides - plasma level. Increases the risk of myopathy and rhabdomyolysis when prescribing lipid-lowering drugs (HMG-CoA reductase), renal dysfunction - against the background of aminoglycosides, amphotericin B, Trimethoprim, co-trimoxazole, ciprofloxacin, some cephalosporins, NSAIDs, propafenone. Phenytoin, Carbamazepine, barbiturates, benzodiazepines, aminoglutethimide, estrogen-progestational drugs, progesterone, rifampicin, Isoniazid, metamizole sodium weaken the effect - accelerate elimination. Enhances the action of quinidine, teofillina, sodium valproate, as well as potassium preparations and potassium-sparing diuretics (increased likelihood of hyperkalemia).

Overdose.

Symptoms: vomiting, drowsiness, headache, tachycardia, severe renal insufficiency.

Treatment: stimulation of vomiting and gastric lavage (in the first hours after oral administration), maintaining vital functions; dialysis and hemoperfusion with activated charcoal are ineffective.

Dosing and Administration.

Inside, I /. The daily dose is divided into 2 admission. The solution for intravenous infusion is prepared time, diluting the concentrate with isotonic sodium chloride solution or 5% glucose solution in the ratio 1:20–1:100; administered within 2-6 hours. The initial dose is 3-5 mg / kg per day. IV applications are considered optimal at the initial stage of treatment of patients with bone marrow transplant.. The oral solution can be diluted in a glass (but not plastic) a glass of cold chocolate drink, milk, fruit juice (excluding grapefruit), coca cola, mix well and drink immediately. The capsules should be swallowed whole. When transplanting organs - by mouth at a dose of 10-15 mg / kg 4-12 hours before the operation, once, and then in this daily dose for 1-2 weeks; in the future, the dose is gradually reduced to a maintenance (usually 2-6 mg / kg). For autoimmune diseases - by mouth in a daily dose of 2.5-5 mg / kg (excluding endogenous uveitis, in which for a short time it is possible to increase the daily dose to 7 mg / kg).

Precautions.

Treatment should be carried out in a specialized hospital by doctors, with sufficient experience in immunosuppressive therapy. It will be appreciated, that against the background of cyclosporine, the predisposition to lymphoproliferative malignant neoplasms increases, therefore, before its appointment, it is necessary to decide, how much the expected beneficial effect justifies the risk of undesirable effects. Use during pregnancy is permissible only under strict indications.. Since there is a possibility of developing anaphylactoid reactions with intravenous administration, prophylactic intake of antihistamines is advisable, and the fastest possible transfer of the patient to oral medications. It is recommended to select the dose depending on the content in the blood.. After kidney transplantation, the plasma level is determined within the first 2 weeks. 2 times a week, for 3-6 weeks - 1 once a week, with outpatient supervision - 1 once every 2-3 months. Regular monitoring of plasma creatinine concentration is necessary - an increase may indicate a rejection reaction, or about nephrotoxicity and require (in the latter case) dose reduction: on 25% with an increase in creatinine by more than 30% starting from, and 50%, if its level doubles; when the dose is reduced during 4 weeks does not lead to a decrease in creatinine, cyclosporine is canceled. Blood pressure monitoring is recommended, blood potassium, Uric acid, bilirubin, transaminases, lipid profile, during the treatment period, immunization with live attenuated vaccines is contraindicated. In the treatment of autoimmune diseases, the lack of adequate positive results through 3 month indicates the need to stop treatment.

Cautions.

It is advisable to use glass containers for the preparation of the infusion solution..

Cooperation