Updated: 12/31/2021

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
      • Name
      • Mechanism of Action
      • Key Indication
      • Key Toxicity
      • 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
      • Name
      • Mechanism of Action
      • Key Indication
      • Key Toxicity
      • 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
      • Name
      • Mechanism of Action
      • Key Indication
      • Key Toxicity
      • 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
      • Name
      • Mechanism of Action
      • Key Indication
      • Key Toxicity
      • 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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