Cyclosporine

Циклоспорин Drug photo

The description is actual on 17.01.2015

  • Latin name: Cyclosporin
  • ATH code: L04AD01
  • Active ingredient: Cyclosporine (Ciclosporin)
  • Producer: Ltd. Okasa pharma, India

Structure

One capsule of Cyclosporine contains 50, 100 or 25 mg of active ingredient.

One ml of drug contains 100 mg of cyclosporine + excipients.

The concentrate for intravenous administration contains on 50 or 650 mg of active component in one milliliter.

Release form

Medicine is let out in the form of capsules of a different dosage, in blister strip packagings on 10 pieces, in cardboard packs on 5 packagings.

Also drug is issued in the form of solution for intravenous pricks in ampoules on 1 or 5 ml.

Pharmacological action

Immunodepressive.

Pharmacodynamics and pharmacokinetics

Cyclosporine A possesses the expressed immunodepressive effect. Drug suppresses ability of an organism to resist to the foreign bodys getting into a body prolongs the term of a survival of fabrics and bodies for change.

Active ingredient oppresses products of antibodies, slows down reactions T-helperov, selectively and reversibly changes function of lymphocytes. There is it thanks to oppression of synthesis of lymphokines and processes of their linkng with specific receptors.

It should be noted that medicine does not oppress processes of a hemopoiesis and does not influence activity of a phagocytal link of immune system.

At reception of tablets process of absorption happens in intestines. Biological availability makes about 30%. The maximum concentration of drug in plasma is reached within one or five hours. Distribution of medicine is carried out mainly on fabrics and bodies. A small amount of drug is found in erythrocytes, lymphocytes and granulocytes. Cyclosporine gets into breast milk.

Drug will actively be transformed, has about 15 metabolites. The elimination half-life makes 19 hours for adults and about 7 h for children. Medicine with bile and urine is removed.

Indications to use

Means is appointed:

  • for treatment and prevention of rejection after operations of an organ transplantation and fabrics (kidneys, a liver, marrow, heart, lungs, a pancreas, etc.);
  • at autoimmune diseases (an endogenous uveitis, Bekhchet's uveitis with inflammatory recurrence);
  • for prevention and treatment of reactions like "transplant against the owner";
  • at a nephropathy of the minimum changes, a focal or segmented glomerulosclerosis, a hymenoid glomerulonephritis before cancellation of glucocorticosteroids or for remission maintenance;
  • for treatment of severe forms of a pseudorheumatism if use of other medicines is impossible;
  • at psoriasis, atopic dermatitis (in hard cases, as a part of complex therapy).

Contraindications

Drug is contraindicated to reception in the presence of reactions of hypersensitivity to its components.

Side effects

Are possible:

  • headache, fatigue, spasms, tremor, paresthesias, inflammation of muscles;
  • nausea, diarrhea or lock, vomiting, abdominal pains, pancreatitis, increase of level of liver enzymes;
  • increase of arterial pressure, thrombopenia and leukopenia, anemia;
  • vision disorders, problems with coordination of movements, encephalopathy;
  • problems in work of kidneys, up to intersticial fibrosis at long reception.

Are seldom shown: dysmenorrhea, acne, puffiness, hirsutism, active growth of hair, increase in weight, insufficiency of magnesium, hyperpotassemia, lipidemia.

Application instruction of Cyclosporine (Way and dosage)

Medicine is taken inside or intravenously, depending on a form of release and a disease.

The dosage is selected individually. Reception of such amount of drug which would have desirable therapeutic effect is considered the most optimum, without causing serious side reactions.

Has the right to appoint means the doctor, it is desirable the having experience of therapy by similar drugs.

The instruction on Cyclosporine A

The initial daily dosage makes from 3 to 5 mg on weight kg (intravenously) or from 10 to 15 mg on kg of the weight (tablet). Then the dosage is gradually reduced.

For treatment of a pseudorheumatism and other autoimmune diseases appoint 3 mg to weight kg, 2 times a day, the first 1,5 months. Then the dosage can be increased or lowered gradually. The maximum daily dosage – 5 mg on kg. Treatment duration – no more than 3 months.

At psoriasis appoint 2,5 mg to the weight kg distributed on 2 receptions. In especially hard cases, it is possible to increase an initial dosage to 5 mg by kg.

For treatment of atopic dermatitis the initial dosage is appointed on 2, by mg % for kg a day. It is possible to increase it to 5 mg by kg. After achievement of desirable effect the dosage is reduced to full cancellation.

The instruction on solution for introduction intravenously

The drug is administered kapelno, slowly, having dissolved in glucose or isotonic solution.

At organ transplantation, in 4-12 hours before operation appoint drug injections. The dose which is picked up by the specialist is entered before operation and continued within 14 days later. Further it is recommended to transfer the patient to reception of the tableted medicine form.

The concentrate of cyclosporine is parted with glucose or isotonic solution and use not later, than in 2 days after cultivation.

During treatment it is recommended to make every day analyses on Cyclosporine level in blood.

Overdose

At overdose strengthening of side effects, including disturbances in work of kidneys can be observed. Disturbances are reversible.

At overdose by tablets during the first hours it is necessary to wash out a stomach.

Apply symptomatic therapy, the hemodialysis and hemoperfusion are inefficient.

Interaction

Increase in nephrotoxicity of Cyclosporine at a combination to Amiodaronum, Aminoglycosides, Amphotericinum was observed In, by Trimethoprimum, Co-Trimoksazol, Ciprofloxacin, NPVS and Melphalanum.

Drug level in a blood plasma considerably increases at a combination to Diltiazem, Verapamil, nikardipiny, Flukonazoly, the beta adrenoblockers derivative of an imidazole, glucocorticosteroids, macroleads.

At a drug combination to inhibitors of GMG-KOA-reduktazy the risk of development of a myopathy and rabdomioliz increases.

Under the influence of Phenytoinum, barbiturates, Carbamazepine, derivative Benzodiazepine, Aminoglutetimid, Progesterone, estrogen and gestagen, Rifampicin, Metamizole sodium, the Isoniazid there is an acceleration of elimination and decrease in efficiency of Cyclosporine.

Drug strengthens Teofilin's action, kaliysberegayushchy diuretics, Quinidine, Valproatum of sodium, potassium drugs.

Terms of sale

According to the recipe.

Storage conditions

To store far from children, in the cool dark place.

Period of validity

2 years.

Special instructions

During treatment means recommends to make periodic control of level of potassium and lipids in plasma, functions of a liver and kidneys.

At emergence of a lipidemia it is recommended to lower amount of the fats arriving with food and to lower a means dosage, at hypertensia – hypotensive therapy.

During treatment by means it is impossible to make vaccination.

Analogs of Cyclosporine

Coincidence on the ATH code of the 4th level:

The closest analogs: Sandimmun, Orgasporin, Takrolimus, Advagraf, Takrosel, Pro-count.

Section: Immunity increase
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