Immunosuppressants |
Medication | Clinical Use | Mechanism of Action | Adverse Effects |
Cyclosporine | Rheumatoid arthritisPsoriasisTransplant rejection prophylaxis | Calcineurin inhibitor whichimpairs IL-2 production and releaseimpairs IL-2-induced T-cell activation | Nephrotoxicity NeurotoxicityHirsutismGingival hyperplasiaHypertensionHyperlipidemia |
Tacrolimus (FK506) | Transplant rejection prophylaxis | Calcineurin inhibitor via binding with intracellular FKBP-12 protein whichimpairs IL-2 production and releaseimpairs IL-2-induced T-cell activation | NephrotoxicityNeurotoxicity↑ risk of diabetes |
Sirolimus (Rapamycin) | LymphangioleiomyomatosisRenal transplantation prophylaxis | mTOR inhibitor via binding with intracellular FKBP-12 protein which↓ cytokine-induced T-cell proliferation | PancytopeniaHyperlipidemia EdemaInsulin resistance |
Basiliximab | Renal transplantation prophylaxis | Targets the α-chain of the IL-2 receptor complex whichis expressed on activated T-cells | EdemaTremorHypertension |
Azathioprine | Rheumatoid arthritisRenal transplantationInflammatory bowel disease | A precursor of 6-mecaptopurine whichinhibits purine nucleotide synthesis incorporates itself into the cell’s DNA and halts replication | Pancytopenia |
Mycophenolate mofetil | Organ transplantationLupus nephritis | Inosine monophosphate dehydrogenase (IMPDH) inhibitor which impairs guanosine nucleotide synthesis | Gastrointestinal upsetPancytopeniaHypertension |
Corticosteroids | A number of autoimmune and inflammatory disorders | NF-κB inhibitorInduces T-cell apoptosis | HyperglycemiaOsteoporosisCushing syndromeAdrenocortical atrophyPeptic ulcersCataractsAvascular necrosisPsychosis |