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Cyclosporine

Systems	General systemic
Category	Immunosupressant

Pharmacokinetics

It is given both orally as well as parenterally. Absolute oral bio-availablity is 20-50%. The plasma protein binding is 90%. The plasma half life is 6 hours. The drug is metabolised mainly in the liver ( 99%), and is excreted in the bile.

Indications

Cyclosporine is one of the most effective drugs for prevention and treatment of organ transplantation rejection reactions. It is routinely used in patients with renal, hepatic or cardiac transplantation. It is started orally 12 hours before the transplant and continued for 6 or more months thereafter.When graft rejection has started, it is preferably given I.V because oral bio-availability is low.

Routes of Administration and Dosage

Oral dose in adults or children with transplant rejection is based on the body weight. Initially start with 12 to 15 milligrams (mg) per kilogram (kg) per day and after a period of time the dose may be reduced to 5 to 10 mg per kg per day. Parentral dose in adults or children with transplant rejection is based on the body weight and is 2 to 6 mg per kg per day.

Contra Indications

Cyclosporine is contraindicated during breast feeding and in patients with hypersensitivity.

Precautions

Special precaution should be taken during pregnancy,renal or hepatic impairment and in patients with infections

Interactions

May occur with the following: Amiloride, Spironolactone, Triamterene: Both cyclosporine and these drugs increase the amount of potassium in the body, hence hyperkalemia may occur. Androgens, Cimetidine, Danazol, Diltiazem, Erythromycins, Estrogens, Ketoconazole : May potentiate the effects of cyclosporine by increasing the amount of the drug in the body. Azathioprine, Chlorambucil, Corticosteroids, Cyclophosphamide, Mercaptopurine : There may be an increased risk of infection and cancer because both cyclosporine and these drugs decrease the body's immune response. Lovastatin : May increase the risk of renal disorders.

Brand Names

Immusol (Dabur), Imusporin (Cipla), Panimum Bioral (Panacea), Sandimmum conc (Novartis), Sandimmum Neoral (Novartis)