Immunosuppression drugs Flashcards
mechanism of glucocorticoids in immunosuppression
bind/inhibit NF-kB;
prevent many cytokines from forming – inhibits T and B cell function
mTOR inhibitors
sirolimus everolimus
my Tortoise even sings!
azathioprine mechanism
metabolized to 6-mercaptopurine antagonizes purine metabolism and may inhibit synthesis of DNA, RNA
what IS meds are favored in pregnancy?
cyclosporine,
tacrolimus
azathioprine
prednisone
induction agents
ATG
alemtuzumab - CD52 Ab
basiliximab - IL2 Ab
antimetabolite agents
azathioprine
mycophenolate mofetil(MMF)
belatacept
blocks costimulation!
targets B7 on APCs and blocks CD28 mediated T-cell costimulation
mTOR inhibitor mechanism
sirolimus, everolimus
bind FKBP, then bind mTOR/inactivate it prevent cell cycle progression; cause apoptosis
cyclosporine toxicities
hirsutism
gingival hyperplasia
hyperlipidemia
hyperuricemia, gout
HTN
nephrotoxic
azathioprine adverse effects
myelotoxic - thrombo/leukopenia
UV radiation sensitive
Allopurinol decreases breakdown of 6MP which cane increase toxicities
mTOR inhibitor adverse effects
proteinuria(from apoptosis)
hyperlipidemia
oral ulcers
anemia
thrombocytopenia, leukopenia
not nephrotoxic
tacrolimus toxicities
nephrotoxic
neurotoxic
hyperglycemia - diabetes risk
no gingival hyperplasia or hirsutism like cyclosporine
calcineurin inhibitors
cyclosporine - binds cyclophilin and inhibits calcineurin
tacrolimus - binds FKBP1 and inhibits calcineurin
no calcineurin activity means no IL2 production – no T cell differentiation
what do you give for rejection therapy?
solumedrol/prednisone taper
thymoglobulin
IVIG
mycophenolate mofetil mechanism
inhibits inosine monophosphate dehydrogenase – blocks de novo purine synthesis
hurts cells that cant utilize salvage pathway(lymphocytes)
metabolized to mycophenolic acid – active drug