Immunopharmacology Flashcards
inhibits MTOR
inhibits T lymphocyte activation and proliferation downstream of IL 2
sirolimus
evorlimus
MOA: cones to FKBP 12, which inhibits a protein kinase; inhibitor of MTOR blocks cell cycle progression at the G1 - S phase transition
sirolimus
evorlimus
Uses: prophylaxis of organ transplant rejection in combo with calcineurin inhibitor and glucocorticoids
1st line drug to prevent renal transplant rejection
sirolimus
evorlimus
SE: dose dependent increase in S cholesterol and TAGs, hyperglycemia, *BM depression: thrombocytopenia
sirolimus
evorlimus
more potent then cyclosporine
MOA: binds to immunophilin (FK506 BP 12), then complex forms (FKBP 12, Ca, Calmodulin)
tacrolimus
uses: prophylaxis of solid organ allograft rejection
ADR: hyperglycemia, nephrotoxicity, HTN
tacrolimus
1) forms a complex with cyclophilin
2) complex inhibits calcineurin phosphatase activity
3) prevents NFAT dephosphorylation so NFAT doesn’t enter the nucleus, transcription NOT activated
cyclosporine - calcineurin inhibitor
Uses: organ transpant, RA, psoriasis
cyclosporine
ADR: renal dysfunction, HTN, hyperlipidemia, hyperglycemia
cyclosporine
drugs increasing cyclosporine levels
Ca ch blockers, p450 inhibitors
drugs decreasing cyclosporine levels
p450 inducers
enhanced renal toxicity
cyclosporine and tacrolimus
reversibly inhibits of IMPDH
inhibitor if de novo synthesis (guanine)
indicted for prophylaxis of transplant
use din combo with glucocorticoids and calcineurin inhibitor
SE: reversible BM depression (neutropenia)
mycophenolate
bind to CD25 on t cells
inhibit IL 2 induced T cell activation
dacliximab
basiliximab
causes T cell depletion
can cause cytokine storm
antithymocyte globulin