This is a potent macrolide immunosuppressant derived from Streptomyces tsukabaensis, and has actions similar to those of cyclosporine.

Indications: prophylaxis organ rejection in patients receiving allogenic liver or kidney transplants. Used in conjunction with adrenal corticosteroids.

Cautions: Cardiomyopathy has been reported in children given tacrolimus after transplantation. Patients should be monitored carefully by echocardiography for hypertrophic changes; dose reduction or discontinuation should be considered if these occur. Monitor visual status, blood glucose, hematological and neurological parameters.

Contra-indications: hypersensitivity to macrolides; hypersensitivity (risk of anaphylaxis) to polyoxyl 60 hydrogenated castor oil, which is present in the injection; avoid concurrent use with cyclosporine (additive nephrotoxicity).

Side Effects: include gastrointestinal disturbances like dyspepsia, and inflammatory & ulcerative disorders; hepatic dysfunction, jaundice, bile duct and gall bladder abnormalities; hypertension; cardimyopathy.

Dose: 100 – 300 mcg/kg daily in 2 divided doses orally; or by IV infusion over 24 hrs. 10 – 50 mcg/kg.