Immunopharmacology Flashcards
Acute rejection defined as
rejection that occurs 24 hours to several weeks following organ transplantation
Adrenocortical steroids used for
induction and maintenance of immunosuppression
What do adrenocortical steroids do?
reduce circulating lymphocyte levels, block lymphocyte activation required for antigen presentation, and block T-cell proliferation
Name an alkylating agent
cytotoxic drug cyclophosphamide (VERY TOXIC)
Inhibitors of de novo purine synthesis
azathiprine and 6-mercaptopurine (1st gen)
mycophenolate mofetil and inosine 5’ monophosphate deydrogenase inhibitor (2nd gen)
methotrexate is in which class of immunosuppressants
inhibitor of de novo purine synthesis
inhibitors of de novo pyrimidine synthesis inhibit which enzyme
dihydroorotate dehydrogenase
Cyclosporine and tacrolimus are drugs used for
the induction and maintenance of immunosuppression
block T-cell signaling pathways that stimulate IL-2
Cyclosporine associates with
calcineurin and inhibits its phosphatase activity
prevents translocation of NFAT family of transcription factors
limiting factor for the use of cyclosporine
renal toxicity
Tacrolimus
macrolide antibiotic
100X more potent than cyclosporine
Tacrolimus binds
to cytoplasmic protein FK506-binding protein 12 - creates a complex that inhibits the phosphatase activity of calcineurin
Sirolimus inhibits
calcineurin by binding FKBP12 and mTOR
Belatacept
targeted immunosuppressant drug for the replacement of calcineurin inhibitors over time
Belatacept inhibits
CD28-mediated T cell costimulation by binding to CD80 and CD86 on antigen presenting cells