Updated: 1/29/2019

Immunosuppressants

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Snapshot
  • A 40-year-old woman presents to the emergency department with worsening lower extremity 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 a urinary tract infection. Medical history is significant for multiple sclerosis treated with rituximab. Physical examination is significant for 1/5 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 hyperintense lesions. She is started on intravenous methylprednisolone.
Immunosuppressants
 
Immunosuppressants
Medication
Clinical Use
Mechanism of Action Adverse Effects
Cyclosporine 
  • Rheumatoid arthritis
  • Psoriasis
  • Transplant rejection prophylaxis
  • Calcineurin inhibitor impairs
    • IL-2 production and release
    • IL-2-induced T-cell activation
  • Nephrotoxicity
  • Neurotoxicity
  • Hirsutism
  • Gingival hyperplasia
  • Hypertension
  • Hyperlipidemia
Tacrolimus (FK506)
  • Transplant rejection prophylaxis
  • Calcineurin inhibitor via binding with intracellular FKBP-12 protein which impairs
    • IL-2 production and release
    • IL-2-induced T-cell activation
  • Nephrotoxicity
  • Neurotoxicity
  • ↑ risk of diabetes
Sirolimus (Rapamycin)
  • Lymphangioleiomyomatosis
  • Renal transplantation prophylaxis
  • mTOR inhibitor via binding with intracellular FKBP-12 protein which
    • ↓ cytokine-induced T-cell proliferation
  • Pancytopenia
  • Hyperlipidemia 
  • Edema
  • Insulin resistance
Basiliximab
  • Renal transplantation prophylaxis
  • Targets the α-chain of the IL-2 receptor complex which is expressed on activated T-cells
  • Edema
  • Tremor
  • Hypertension
Azathioprine
  • Rheumatoid arthritis
  • Renal transplantation
  • Inflammatory bowel disease
  • A precursor of 6-mecaptopurine which
    • incorporates itself into the cell's DNA and halts replication
  • Pancytopenia 
  • Hepatotoxicity
Mycophenolate mofetil
  • Organ transplantation
  • Lupus nephritis
  • Inosine monophosphate dehydrogenase (IMPDH) inhibitor which
    • impairs guanosine nucleotide synthesis
  • Gastrointestinal upset
  • Pancytopenia
  • Hypertension
  • Hyperglycemia
Corticosteroids
  • A number of autoimmune and inflammatory disorders
  • NF-κB inhibitor
  • Induces T-cell apoptosis
  • Hyperglycemia
  • Osteoporosis
  • Cushing syndrome
  • Adrenocortical atrophy
  • Peptic ulcers
  • Cataracts
  • Avascular necrosis
  • Psychosis

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