Updated: 8/8/2017

Immunosuppressants

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Immunosuppressants Drug Introduction
  • Immunosuppressants medications can be broken down into the following categories
    • corticosteroids
    • calcineurin Inhibitors
    • monoclonals
    • antimetabolites
    • others
Immunosuppressants Drug Table
 
Corticosteroids
Name Mechanism of Action  Key Indication  Key Toxicity
Prednisone
  • Glucocorticoid receptor agonist
  • Phospholipase A2 inhibitor → ↓ COX expression
  • NFκB inhibitor
  • Adrenal insuffiency
  • Asthma
  • Autoimmune disease
    • to achieve immunosuppression
  • Organ transplantation
  • Certain hematologic cancers
  • Drug-induced Cushing-like symptoms
  • Hyperglycemia
  • Osteoporosis
  • Mood alterations
Calcineurin Inhibitors
Cyclosporine
  • Calcineurin inhibitor via cyclosporine-cyclophilin complex
  • Organ transplantation
  • Certain autoimmune diseases
  • Nephrotoxicity
  • Neurotoxicity
  • Hypertension
  • Gingival hyperplasia
  • Hirsutism
FK506 (tacrolimus)
  • Calcineurin inhibitor via FK506 immunophilin
  • Prophylaxis for organ transplant rejection
  • Nephrotoxicity
  • Neurotoxicity
  • Hypertension
Monoclonals
OKT3 (muromonab)
  • CD3 receptor monoclonal antibody
  • Allograft rejection
  • Pyrexia
  • Diarrhea
Basiliximab
  • CD25 subunit of IL-2 receptor antibody
  • Renal transplant rejection
  • Hypertension
  • Edema
  • Hypercholesterolemia
  • Hyperglycemia
  • Hyperuricemia
  • Hypophosphatemia
Antimetabolites
Azathioprine
  • Precursor to 6-mercaptopurine
    • leads to inhibition of lymphocytic proliferation
      • perhaps by inhibiting nucleotide synthesis
  • Transplant rejection prophylaxis
  • Autoimmune diseases
  • Pancytopenia
  • Increased toxicity when used with allopurinol
Mycophenolic acid
  • Inosine monophosphate dehydrogenase inhibitor
    • Cytostatic effect on lymphocytes
      • lymphocytes do not have enzymes involved in salvage pathway, and thus why they are preferentially affected
  • Transplant rejection
  • GI distrubances
  • Pancytopenia
  • CMV infection
  • Less nephro- and neurotoxic
Others
Rapamune (sirolimus)
  • mTOR inhibitor
    • via sirolimus-FK506 complex
  • Impairs lymphocyte response to IL-2 activation
  • Kidney transplant prophylaxis
  • Pancytopenia
  • Insulin resistance
  • Hyperlipidemia

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