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
used in RA and crohns
bind to TNF
infliximab
adalimumab
use din kidney transplant
CD3 receptor
induces rapid internalization of the T cell receptor
muromonab
fusion protein, mimics TNF receptor to bind to free TNF or men bound TNF
used in RA and crohns dz
etanercept
restores depressed immune fxn of b and T cells
adjunct therapy with 5 FU after surgical resection on px with colon cancer
levamisole
used in tx for px with erythema nodosum leprosum and in multiple myeloma
thalidomide
carcinoma in situ of the urinary bladder
bacillus calmette guerin
used when fetal RBCs are known or suspected of an Rh negative mother unless the fetus is known also to be Rh negative
use at 28 wks of pregnancy and within 72 hrs after delivery
Rho D immune globulin
rhesus dz if child born
hydrops fetalis fetus in utero
