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Flashcards in Immunology Deck (5)
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1
Q

Cyclosporine

A
  • Mech: binds cyclophilins. inhibits calcineurin -> blocks differentiation and activation of T cells -> prevent production of IL-2 and its receptor
  • Clinical use: suppresses organ rejection after transplantation, selected autoimmune d/os
  • Toxicity: nephrotoxicity, HTN, hyperlipidemia, hyperglycemia, tremor, gingival hyperplasia, hirsutism
2
Q

Tacrolimus (FK-506)

A
  • Mech: similar to cyclosporine. binds FK-binding protein -> inhibits calcineurin and IL-2 secretion
  • Clinical use: potent immunosuppressive used in organ transplant recipients
  • Toxicity: similar to cyclosporine, exc no gingival hyperplasia or hirsutism
3
Q

Sirolimus (rapamycin)

A
  • Mech: binds FK binding protein 12 -> inhibits mTOR -> inhibits IL-2 induced activation and proliferation of T and B cells
  • Clinical use: immunosuppression after KIDNEY transplantation in combo with cyclosporine and corticosteroids, also used in drug-eluting stents
  • Toxicity: hyperlipidemia, thrombocytopenia, leukopenia
4
Q

Azathioprine

A
  • Mech: antimetabolite precursor of 6-MP that interferes with metabolism and synthesis of nucleic acids (6-MP blocks de novo purine synthesis). toxic to proliferating lymphocytes
  • Clinical use: KIDNEY transplantation, autoimmune d/os (inc glomerulonephritis and hemolytic anemia)
  • Toxicity: BM suppression. active metabolite mercaptopurine metabolized by xanthine oxidase -> toxic effects may be increased by allopurinol (XO inhibitor)
5
Q

Muromonab-CD3 (OKT3)

A
  • Mech: monoclonal Ab that binds CD3 (epsilon chain) on surface of T cells. blocks cellular interaction with CD3 protein responsible for T-cell signal transduction
  • Clinical use: immunosuppression after KIDNEY transplantation, steroid-resistant cardiac and hepatic transplant patients, deplete T cells from donor BM prior to transplant
  • Toxicity: cytokine release syndrome (anaphylactoid and CNS Sx), hypersensitivty reaction