Immunology-Pharmacology Flashcards
What is Cyclosporine?
A calcineurin inhibitors that binds cyclophilin and blocks T cell activation by preventing IL-2 transcription for use in transplant rejection prophylaxis, psoriasis, and rheumatoid arthritis
What are the AEs of cyclosporine?
Nephrotoxicity (highly), HTN
hyperlipidemia
neurotoxicity
gingival hyperplasia
hirsutism
What is tacrolimus (FK506)?
a calcinueron inhibitor that binds Fk506 binding protein (FKBP) and blocks T cell activation by preventing IL-2 transcription mainly for use as a transplant rejection prophylatic
What are the AEs of Tacrolimus?
Similar to cyclosporine but with additional increased risk of diabetes and neutrotoxicity
no ginigival hyperplasia or hirsutism
What is Sirolimus (Rapamycin)?
an mTOR inhibitor that binds FKBP and blocks T cell activation and B cell differentiation by preventing the response to IL-2 for primary use as a kidney transplant rejection prophylatic (synergistic with cyclosporine)
What are the main AEs of Sirolimus (Rapamycin)?
Anemia, thrombocytopenia, leukopenia,
insulin resistance
hyperlipidemia
NOT NEPHROTOXIC
What is Daclizumab and Basiliximab?
MABs that bind to and block IL-2R for kidney transplant rejection prophylaxis
What are the main AEs of Daclizumab and Basiliximab?
Edema, HTN, and tremor
What is Azathioprine?
Antimetabolite precursor for 6-MP that inhibits lymphocyte proliferation for use in transplant rejection and autoimmune diseases
What are the main AEs of Azathioprine?
Leukopenia, anemia, and thrombocytopenia
6-MP is broken down by ______
xanthine oxidase so increased toxicity with allopurinol
How do glucocorticoids work?
Inhibit NF-kB to suppress both B and T cell function by decreasing transcription of many cytokines
What are some AEs of glucocorticoids?
Hyperglycemia
osteoporosis
central obesity/Iatrogenic Cushing syndrome
muscle breakdown
psychosis
acne
HTN
cataracts
avascular necrosis
What are the main uses of Aldesleukin (recombinant IL-2)?
renal cell carcinoma, melanoma METS
What are the main uses of Epoietin Alfa (recombinant EPO)?
Anemias (esp. in renal failure)