Immunology--Pharmacology Flashcards
cyclosporine moa
calcineurin inhibitor (calcineurin dephosphorylates NFAT allowing it to translocate to nucleus and activate transcription); binds cyclophilin and blocks T cell activation by preventing IL2 transcription
cyclosporine toxicity
nephrotoxic, HTN, HLD, hyperglycemia, tremor, hirsutism, gingival hyperplasia
cyclosporine uses besides transplants
psoriasis, rheumatoid arthritis
tacrolimus moa
calcineurin inhibtor, binds FK506 binding protein (FKBP), blocks T cell activation by preventing IL-2 transcription
tacrolimus toxicity
nephrotoxic, increased risk of diabetes and neurotoxicity; unlike cyclosporine: no gingival hyperplasia or hirsutism
sirolimus (rapamycin) moa
binds FKBP and inhibits mTOR, blocks T cell activation and B cell differentiation by preventing IL2 signal transduction;
sirolimus tox?
anemia, thrombocytopenia, leukopenia, insulin resistance, hyperlipidemia, NOT nephrotoxic
sirolimus is synergistic with..?
cyclosporine
Basiliximab moa, tox?
monoclonal ab blocks IL-2R; edema, hypertension, tremor
azathioprine moa
antimetabolite precursor of 6-MP, inhibits lymphocyte proliferation by blocking nucleotide synthesis
azathioprine tox?
leukopenia, anemia, thrombocytopenia
do not combine azathioprine with..?
allopurinol; 6MP degraded by xanthine oxidase;
azathioprine is also used for..?
RA, crohns, glomerulonephritis, other autoimmune stuff
glucocorticoids moa?
inhibit NFkappaB, suppress both B and T cell function by decreasing transcription of many cytokines
glucocorticoid tox?
hyperglycemia, osteoporosis, central obesity, muscle breakdown, psychsis, acne, HTN, cataracts, peptic ulcers; iatrogenic cushings
