| Cyclosporine |
Calcineurin inhibitor; binds cyclophilin. Blocks T-cell activation (prevents IL-2 transcription). |
Nephrotoxicity, gingival hyperplasia, hirsutism. |
Both calcineurin inhibitors are highly nephrotoxic. |
| Tacrolimus |
Calcineurin inhibitor; binds FKBP. Blocks T-cell activation (prevents IL-2 transcription). |
Similar to cyclosporine (nephrotoxic), but no gingival hyperplasia/hirsutism. Risk of diabetes. |
Highly nephrotoxic. |
| Sirolimus |
mTOR inhibitor; binds FKBP. Blocks T-cell activation/B-cell differentiation (prevents response to IL-2). |
"Pansirtopenia", insulin resistance, hyperlipidemia. Not nephrotoxic. |
Kidney "sir-vives". Synergistic with cyclosporine. Drug-eluting stents. |
| Basiliximab |
Monoclonal antibody; blocks IL-2R. |
Edema, hypertension, tremor. |
- |
| Azathioprine |
Antimetabolite precursor of 6-mercaptopurine. Inhibits lymphocyte proliferation (blocks nucleotide synthesis). |
Pancytopenia. |
6-MP degraded by xanthine oxidase; toxicity ↑ by allopurinol. |
| Mycophenolate |
Reversibly inhibits IMP dehydrogenase (purine synthesis). |
GI upset, pancytopenia, invasive CMV infection. |
Less nephrotoxic. |
| Glucocorticoids |
Inhibit NF-κB. Induce T cell apoptosis. |
Cushing syndrome, osteoporosis, diabetes, avascular necrosis. |
Demargination of WBCs causes artificial leukocytosis. Adrenal insufficiency if stopped abruptly. |