Immunosuppressive Drugs

5212017mdstep1immunotargetsofimmunosuppressants
Snapshot
A 36-year-old woman presents to the emergency department with worsening weakness and decreased visual acuity of the right eye. She reports that her symptoms progressively worsened over the course of a week and after developing an upper respiratory infection. Medical history is significant for multiple sclerosis (MS) treated with rituximab. Physical examination is significant for 2/5 strength in the lower extremities and an afferent pupillary defect appreciated in the right eye. Magnetic resonance imaging of the brain and spine shows new enhancing lesions when compared to prior imaging. After further evaluation, it was determined she had an MS exacerbation. She is started on intravenous methylprednisolone.
Immunosuppressants
Immunosuppressants
MedicationClinical UseMechanism of ActionAdverse Effects
Cyclosporine Rheumatoid arthritisPsoriasisTransplant rejection prophylaxisCalcineurin inhibitor whichimpairs IL-2 production and releaseimpairs IL-2-induced T-cell activationNephrotoxicity NeurotoxicityHirsutismGingival hyperplasiaHypertensionHyperlipidemia
Tacrolimus (FK506) Transplant rejection prophylaxisCalcineurin inhibitor via binding with intracellular FKBP-12 protein whichimpairs IL-2 production and releaseimpairs IL-2-induced T-cell activationNephrotoxicityNeurotoxicity↑ risk of diabetes
Sirolimus (Rapamycin)LymphangioleiomyomatosisRenal transplantation prophylaxismTOR inhibitor via binding with intracellular FKBP-12 protein which↓ cytokine-induced T-cell proliferationPancytopeniaHyperlipidemia EdemaInsulin resistance
BasiliximabRenal transplantation prophylaxisTargets the α-chain of the IL-2 receptor complex whichis expressed on activated T-cellsEdemaTremorHypertension
Azathioprine Rheumatoid arthritisRenal transplantationInflammatory bowel diseaseA precursor of 6-mecaptopurine whichinhibits purine nucleotide synthesis incorporates itself into the cell’s DNA and halts replicationPancytopenia 
Mycophenolate mofetilOrgan transplantationLupus nephritisInosine monophosphate dehydrogenase (IMPDH) inhibitor which impairs guanosine nucleotide synthesisGastrointestinal upsetPancytopeniaHypertension
CorticosteroidsA number of autoimmune and inflammatory disordersNF-κB inhibitorInduces T-cell apoptosisHyperglycemiaOsteoporosisCushing syndromeAdrenocortical atrophyPeptic ulcersCataractsAvascular necrosisPsychosis