Immunosuppresants (Pharm) Flashcards
MOA of Cyclosporine
Binds to cyclophilins forming a complex that inhibits Calcineurin.
This complex prevents production of IL-2 and its receptor, thus blocking T cell differentiation/activation
Conditions for which you give Cyclosporine
Post-transplant organ rejection suppression
What are signs of toxicity of Cyclosporine?
Nephrotoxicity
Hyper: -TENSION, -LIPIDEMIA, -GLYCEMIA, -HIRSUTISM, PLASIA of gums
Tremor
MOA of Tacrolimus (FK-506)
Binds to FK-binding protein, inhibiting Calcineurin and secretion of IL-2, thus preventing production of IL-2 and its receptor, thus blocking T cell differentiation/activation
Conditions for which you give Tacrolimus (FK-506)
Post-transplant organ rejection suppression
What are signs of toxicity of Tacrolimus (FK-506)?
Nephrotoxicity
Hyper: -TENSION, -LIPIDEMIA, -GLYCEMIA,
Tremor
MOA of Sirolimus (Rapamycin)
Inhibits mTOR
Inhibits T-cell proliferation in response to IL-2
Conditions for which you give Sirolimus (Rapamycin)
Post-kidney transplant immunosuppression IN COMBINATION with Cyclosporine and Corticosteroids
Drug-eluting stents
What are signs of toxicity of Sirolimus (Rapamycin)?
Hyperlipidemia
Thrombocytopenia
Leukopenia
MOA of Azathioprine
6MP precursor metabolite that interferes with metabolism and synthesis of nucleic acids
(especially toxic to proliferating LYMPH)
Conditions for which you give Azathioprine
Post-kidney transplant immunosuppression
Glomerulonephritis and Hemolytic anemia
What are signs of toxicity of Azathioprine?
Bone marrow suppression
What medicine can increase the toxic effects of Azathioprine?
Allopurinol.
The active metabolite of Azathioprine is metabolized by the same enzyme that metabolizes Allopurinol (Xanthine Oxidase)
MOA of Muromonab CD3 (OKT3)
Binds to CD3 on T cell surface and blocks T cell signal transduction
Conditions for which you give Muromonab CD3 (OKT3)
Post-kidney transplant immunosuppression
