It is a cyclic polypeptide containing 11 amino acids. It is a potent immunosuppressive agent, which in animals prolong survival of allogenic transplants involving skin, heart, kidney, pancreas, bone marrow, small intestine and lung. The effectiveness of cyclosporine is due to specific and reversible inhibition of immunocompetent lymphocytes in the Go or G phase of the cell cycle.
||Orally used for prevention of graft rejection after kidney, liver, heart, lung, pancreas. By IV infusion used in bone marrow transplant.
Warnings - Cyclosporine when used in higher doses can cause hepatotoxicity and nephrotoxicity. Vaccinationus are less effective with its use.
|Safety Profile :
||Elderly, thyrotoxicosis, renal or hepatic diseases and acute myocardial infection.
|Adverse Effects :
||Hypertension, renal dysfunction hirsutism, acne, tremor, convulsions Gum hyperplasia, Diarrhoea, parasthesias, Flushing, leucopenia, hepatotoxicity and abdominal discomfort.
|Drug Interactions :
||Nephrotoxicity is potentiated by Vancomycin, Trimethoprim with Sulfamethoxazole, Aminoglycosides, Melphalan, Amphotericin B, Azapropazon, Diclofenac, Ketoconazole, Cimetidine, Ranitidine and Tracolimus.
Blood levels of cyclosporine are increased by Nicardipine, Verapamil, Ketoconazole, Fluconazole, Itraconazole, Danazole, Bromocriptine, Metoclopramide, Erythromycin and Methylprednisolone. Blood levels of cyclosporine are decreased by Rifampicin, Phenytoim, Phenobarbitol and Carbemazepine.
||Orally (First dose is given in the amount of 10-15 mg/kg/ 4-12 hours before transplantation. This dose is continued daily for 1-2 weeks after which a maintenance dose of 2-6 mg/kg/day is continued)
I.V.inf : Starting dose one day before the transplantation. 3-5 mg/kg/day. Continue for 2 weeks after transplant. Then oral maintenance dose of 12.5mg./kg/day in two divided doses for six month to a year.
||Not less than 99%.