Immunosuppressants (Cyclosporine, Mycophenolate, Tacrolimus)

Summary

The immunosuppressants are drugs that include cyclosporine, tacrolimus, and mycophenolate. These drugs work by suppressing or weakening the immune system, and are used in the clinical setting to prevent organ transplant rejection. In rare cases, these drugs may also be used as anti-inflammatory agents to treat autoimmune diseases. Patients taking immunosuppressants should avoid grapefruit juice, since grapefruit juice can increase the risk of drug toxicity. As with all immunosuppressants, one major side effect to keep in mind is an increased risk for infection. Other side effects of cyclosporine include gingival hyperplasia or overgrowth of the gums of the mouth, hirsutism referring to increased hair growth, hypertension, and kidney failure.

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)