Ciclosporin

Chemical name

[R-[R*,S*-(E)]]-Циклич.(L-алан ил-D-аланил-N-метил-L-ле��цил-N-метил-L-лейцил-N-м етил-L-валил-3-гидрокси -N,4-диметил-L-2-амино-6-о��теноил-L-альфа-аминоб��тирил-N-метилглицил-N-��етил-L-лейцил-L-валил-N- метил-L-лейцил)

Gross

C62-H111-N11-O12

Of drugs

The drugs-immunodepressivne. Specific and reversible ingibiruet G_0 and G_1 phase cell cycle immunocompetent cells, especially T-helperov, stifles education and a way out of the cells interleikina-2 and its binding to specific receptors. Violate differentiation and proliferatiou cells involved in the divestiture трансплантата.Достат��чно quickly and completely absorbed in the digestive tract. Time to C_max after oral admission ranges from 1 to 6 pm Absolute bioavailability - 20-50%. Linking plasma proteins (mostly lipoproteinami) - about 90%. Distributed mainly outside blood bed, though found in erythrocytes, granoulozitah, Lymphocytes. Apparent volume of 3.5 l / mm In the liver, with the participation of zitohrom P450-zawisimoy monooksigenazna system gidrauxiliruetsa and N-demetiliruetsa. All metabolites (15) contain intaktnuu starting peptidnuu basis, some remains weak immunosupressus activity. T_1/2 ranges from 6.3 hours to 20.4 hours Write mainly jelchew, in the urine found about 6% rate, less than 1% in unchanged Vide.povshaet (especially in combination with prednisolone and azatioprinom) survival after transplantation trupna kidneys and reduces the frequency krizov exclusion and reactions "to the transplant house." Endangering the safety of allogeneic transplants skin, heart, lungs and other organs. Effective in bone marrow, heavy Chronic ulcerative disease of non-conventional treatments revmatoidnom arthritis.

Indications

Transplant kidneys, liver, heart, lung, pancreas (prevention of transplant rejection and treatment rejection reactions), bone marrow (prevention rejection reactions, prevention and treatment of disease to the transplant master "); Acute neinfekiy uveit threatening blindness, uveit Behceta with recurring inflammation and involvement in the retina, chronic glomerulonefrit accompanied by the development of nefroticski syndrome rheumatoid arthritis with a high degree of activity, psoriasis, severe atopic dermatitis.

Contraindications

Гиперчувствительност ь (including the �олиоксиэтилированно��у castorovomu Oil), malignant neoplasms, severe infectious diseases, disorders of the kidneys and / or liver, arterial hypertension, giperuriquemia, giperkaliemia, pregnancy, breast-feeding (at the time of treatment deleted).

Side-Effects

Acute and chronic kidney failure, intersticialny fibrosis kidneys, arterial hypertension, tremor, weakness, headache, parestesia, apnoea seizures, miopatia violation of the liver, pancreatitis, nausea, vomiting, anorexia, pain in the abdomen, the feeling of gravity in the epigastralna, diarrhoea, giperplazia gums whose fluid in the body, obratimaya dismenorea and amenorea, gipertrihoz, thrombocytopenia, anemia, giperkaliemia, giperuriquemia, increased susceptibility to infections.

Specific guidance

The homemade infuzing solution to the glass containers.

Patient interaction

Melfalan increases toxicity, diltiazem, nikardeepin, verapamil, beta-adrenoblokatora, flukonazol, derivatives imidazola, glukokortikoida, makrolida-level plasma. Increases risk myo rabdomioliza and in the appointment of lipid drugs (G-koa-reduktaza inhibitors), of the kidney-a aminoglikozidov, amfoteritina B trimetoprima, ko-trimoksazola, ciprofloxacin, some zefalosporinov, NPVS, propafenon. Phenytoin, carbamazepine, barbiturates, benzodiazepine derivative, aminoglutetimid, estrogen-gestagenne preparations progesterone, rifampicin, isoniazid, metamizol sodium weaken effect - eliminatiu up. Do the hinidina, theofillina, valproata sodium, and potassium products and kalisberegath dioretikov (more likely giperkaliemii).

Overdosing

Symptoms : vomiting, drowsiness, headache, tachycardia, severe renal Nedostaternsti.lechenie : stimulation vomiting scene and stomach (in the first hours after oral admission), the maintenance of the vital functions; Dialysis and gemoperfuzia with activated carbon ineffective.

Precautions

Treatment should be carried out in a specialized medical practitioners with sufficient experience immunodepressantami therapy. It should be borne in mind that, against the background of cyclosporine more predisposed to limfoproliferative novoobrazovaniam memories, and before his appointment to the extent expected useful to justify the risk of unwanted effects. Use during pregnancy can be done only on the strict condition. Because there is a likelihood of anaphylactoidnykh reactions with in / in the introduction, appropriate prophylactic administration antigistaminnah funds, and the most rapid transfer of the patient to lekforma pill. The pre-dose, depending on the content in the blood. After transplantation of kidneys plasma set for the first two weeks, twice a week, from 3 to 6 weeks, once a week, and out-patient health care, every 2-3 months. There is a need for regular monitoring of plasma creatinine Improvement can be demonstrated by the reaction of exclusion, or nefrotoksicescom action and demand (in the latter case) reduction rate : 25% increase in creatinine more than 30% of the baseline, and 50% if the level of increase by half; Reducing the dose for 4 weeks does not lead to lower creatinine, ciclosporin overturned. The monitoring AD content in the blood potassium, uric acid, cium, transaminaz, lipid profile, in the period of treatment contraindicated immunization living weakened vaccines. In therapy mediated diseases lack of adequate positive results in a 3-points to the need for stopping treatment.

Dosing and Administration

Inside, in / 386/1989 Daily dose is divided into two reception. R-r for in / Infusion in preparing ex tempore, lemons concentrate izotoniceski solution of sodium chloride or 5% glucose solution in the ratio 1:20-1:100; Give a 2-6 pm Initial dose-3-5 mg / kg per day. In / in the application are best at the initial stage of treatment for patients with transplants bone marrow. Solution for admission into the mix is in a glass (not plastic) glass of cold chocolate drink, milk, fruit juice (with the exception of grapefruit), Cola, a well-mixed, and immediately drink. Capsule should swallow whole. In organ transplants, in the interior of the dose of 10-15 mg / kg for 12 hours before the operation once, and then in the daily dose over 1-2 weeks; Further dose gradually reduce to support (typically 2-6 mg / kg). In autoimmune diseases, in the interior of a daily dose of 2.5-5 mg / kg (with the exception of endogenous uweita where for a short time can raise the daily intake to 7 mg / kg).

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