This is a powerful immunosuppressant which appears to act specifically on lymphocyte, mainly helper T-cells. It has little effect on bone marrow but marked nephrotoxicity.

Indications: prevention of graft rejection following bone marrow, kidney, liver, pancreas, heart, and heart-lung transplantation, and for prophylaxis and treatment of graft-versus-host disease. Because of risk of anaphylaxis, IV infusion should only be used where oral ingestion is not feasible in immediate post-operative period or where gastro-intestinal absorption is impaired. Such patients should be switched to oral therapy as soon as possible.

Cautions: increased susceptibility to infections and lymphomas especially when administered with the immunosuppressive agents due to over suppression; avoid during pregnancy, breast-feeding: or with systemic nephrotoxic antibiotics; avoid other immunosuppressant except cortico-steroids; monitor liver and kidney functions.

Contra-indications: uncontrolled hypertension; uncontrolled infections, and malignancy; renal impairment.

Side effect: hepatic and renal impairment; tremor, gastrointestinal disturbances, hypertrichosis; gum hyperplasia; hyperkalaemia; occasionally facial oedema, hypertension, fluid retention, and convulsion; serum creatinine, bilirubin, and liver enzymes may be increased; burning sensation in hands and feet during first week of oral administration.

Dose: Orally should be given 4-12 hours prior to transplantation as a single dose of 15mg/kg. By IV injection it should be given 4-12 hours prior to transplantation as a single IV dose of 5-6mg/kg/day. This daily single dose is continued postoperatively until the patient can tolerate the soft gelatin capsules or oral solution.