Version June 2024
| Drug | Dosing | Target levels | Major toxicities |
| Calcineurin inhibitors | |||
| Cyclosporine | 4 to 8 mg/kg/day in 2 divided doses, titrated to keep target 12-hour trough levels | 0 to 6 weeks: 275 to 375 ng/mL 6 to 12 weeks: 200 to 350 ng/mL 3 to 6 months: 150 to 300 ng/mL >6 months: 150 to 250 ng/mL | Renal insufficiency Hypertension Dyslipidemia Hypokalemia and hypomagnesemia Hyperuricemia Neurotoxicity (encephalopathy, seizures, tremors, neuropathy) Gingival hyperplasia Hirsutism |
| Tacrolimus | 0.05 to 0.1 mg/kg/day in 2 divided doses, titrated to keep target 12-hour trough levels | 0 to 2 months: 10 to 15 ng/mL 3 to 6 months: 8 to 12 ng/mL >6 months: 5 to 10 ng/mL | Renal dysfunction Hypertension Hyperglycemia and diabetes mellitus Dyslipidemia Hyperkalemia Hypomagnesemia Neurotoxicity (tremors, headaches) |
| Cell cycle agents | |||
| Azathioprine | 1.5 to 3.0 mg/kg/day, titrated to keep WBC at or slightly above 3000/mm3 | None | Bone marrow suppression Hepatitis (rare) Pancreatitis Malignancy |
| Mycophenolate mofetil | 1000 to 1500 mg/day twice daily | Mycophenolic acid (MPA): 2 to 5 mcg/mL | Gastrointestinal disturbances (nausea, gastritis, and diarrhea) Leukopenia |
| Mycophenolate sodium | 720 to 1080 twice daily | None | Fewer gastrointestinal disturbances compared with mycophenolate mofetil Leukopenia |
| Proliferation signal inhibitors | |||
| Sirolimus | 1 to 3 mg/day, titrated to keep therapeutic 24-hour trough levels | 4 to 12 ng/mL when used in combination with a CNI
8 to 14 ng/mL when used as part of a CNI-free regimen
Target ranges vary depending upon the assay used, so clinicians should use the reference range for the assay used at their institutions. | Oral ulcerations Hypercholesterolemia and hypertriglyceridemia Poor wound healing Lower extremity edema Pulmonary toxicities (pneumonitis, alveolar hemorrhage) Leukopenia, anemia, and thrombocytopenia Potentiation of CNI nephrotoxicity |
| Everolimus | 1.5 mg/day in 2 divided doses | 3 to 8 ng/mL when used in combination with a CNI 6 to 10 ng/mL when used as part of a CNI-free regimen | Similar to sirolimus |
| Corticosteroids | |||
| Prednisone | 1 mg/kg/day in 2 divided doses, tapered to 0.05 mg/kg/day by 6 to 12 months
(Prednisone is typically administered after 24 hours of treatment with methylprednisolone immediately following transplantation.) | None | Weight gain Hypertension Hyperlipidemia Osteopenia Hyperglycemia Poor wound healing Salt and water retention Proximal myopathy Cataracts Peptic ulcer disease Growth retardation |
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