Common drug interactions of concern with immunosuppressants

What are the common drug interactions of concern with immunosuppressants?

The major drug interactions involve the CNIs (cyclosporine, tacrolimus) and drugs that are metabolized through the cytochrome p450-3A4 system 

Classes of Immunosuppressive Drugs Used in Kidney Transplantation

  • A. Glucocorticoids
  • B. Small molecule drugs
    • 1. Immunophilin-binding drugs a
      • a. Calcineurin inhibitors (cyclosporine, tacrolimus)
      • b. Mammalian target of rapamycin inhibitors (sirolimus, everolimus)
    • 2. Inhibitors of nucleotide synthesis
      • a. Purine synthesis (inosine monophosphate dehydrogenase) inhibitors (mycophenolate mofetil, mycophenolic acid
      • b. Pyrimidine synthesis inhibitors (Leflunomide)
    • 3. Anti-metabolites (Azathioprine)
  • C. Protein drugs
    • 1. Antibody-depleting agents against T cells, B cells, or both
      • a. Polyclonal antibody (thymoglobulin)
      • b. Monoclonal antibody (muromonab)
    • 2. Non-depleting antibodies (basiliximab)
    • 3. Fusion drugs (Belatacept)
    • 4. Intravenous immune globulin

a Immunophilin is an intracellular protein that, when bound to calcineurin inhibitors, will engage calcineurin.

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