Immunosuppressants (Cyclosporine, Mycophenolate, Tacrolimus)

Musculoskeletal Drugs
  1. Azathioprine
  2. Corticosteroids
  3. Sulfasalazine
  4. TNF Inhibitors
  5. Immunosuppressants (Cyclosporine, Mycophenolate, Tacrolimus)
  6. Acetaminophen
  7. NSAIDs
  8. Colchicine
  9. Allopurinol
  10. Rasburicase
  11. Dantrolene
  12. Muscle Relaxants
  13. Bisphosphonates: Alendronate, Risedronate


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Key Points

  • Immunosuppressants
    • Drug Names
      • Cyclosporine
      • Tacrolimus
      • Mycophenolate
      • Sirolimus
    • Mechanism
      • Multiple mechanisms
        • Cyclosporine and tacrolimus act as calcineurin inhibitors
          • Inhibits T cell differentiation and activation
        • Mycophenolate acts to inhibit IMP dehydrogenase, reducing immune cell differentiation and proliferation
        • Sirolimus acts to inhibit mTOR, needed for T-cell signaling
    • Clinical Use
      • Prevent organ transplant rejection
        • Immunosuppressants are the standard of care after receiving foreign organ transplants
      • Anti-inflammatory
        • May be used to treat severe refractory autoimmune diseases (e.g. rheumatoid arthritis, psoriasis)
        • This use case is less common due to severe immunosuppression and side effects
    • Side Effects and Adverse Reactions
      • Avoid grapefruit juice
        • Grapefruit juice increases drug levels of cyclosporine, tacrolimus, and sirolimus, and can lead to toxicity
      • Immunosuppression
        • Increased risk of infection
        • Do not receive live vaccines
        • Avoid large crowds
        • Immunosuppression also increases risk for developing cancer due to loss of immune surveillance
      • Gingival hyperplasia (cyclosporine)
      • Hirsutism (cyclosporine)
        • Increased hair growth
      • Hypertension (cyclosporine)
      • Kidney toxicity (cyclosporine, tacrolimus)