Immunosuppressant Drugs Flashcards
Prednisolone
Corticosteroid
Cell Traffic
redistributes immune cells outside of vascular space
prevent neutrophil adhesion to endothelium
inhibit chemotactic factor
Cell Function
interferes with macrophage antigen processing
blocks lymphokines activity
inhibits Fc receptor binding
adverse effects- acute adrenal insufficiency on withdrawal and cushings syndrome
Contraindicated with present infection
Azathioprine
Inhibits De Novo and salvage pathway for DNA synthesis
used to inhibit rejection of transplant and autoimmune diseases
side effect- GI, hepatic toxicity and bone marrow suppression
Cyclophosphamine
Crosslinks DNA to kill replicating and non-replicating cells
suppresses humoral immunity greater then T-cells
only used to treat autoimmune disease
Methotrexate
inhibits dihydrofolate reductase which inhibits De Novo DNA sythesis
used for autoimmune diseases
adverse effect- hepatic toxicity
Mycophenolate Mofetil
prodrug
inhibits IMP dehydrogenase which inhibits De Novo but NOT salvage pathway for DNA
helps target lymphocytes because they only use De Novo pathway
used for autoimmune and prevent transplant rejection
adverse effects- infection, anemia, leukopenia
No not use in pregnant women
Cyclosporine
Blocks synthesis and activation of IL-2
Binds to Cyclophilin and inhibits Calcineurin which blocks NFAT needed for IL-2 prodiction
used to prevent organ rejection with transplants
by blocking IL-2 it prevents T-cell helper prolifertion
Adverse effect- nephrotoxicity
Tacrolimus
Blocks synthesis and activation of IL-2
Binds to FKBP and inhibits Calcineurin which blocks NFAT needed for IL-2 prodiction
used to prevent organ rejection with transplants
by blocking IL-2 it prevents T-cell helper prolifertion
more potent than Cyclosporine
Sirolimus
Inhibits IL-2 Cascade to block T-cell activation
Bind FKBP-12 which binds to mTOR and blocks its ability to progress the cell cycle (G1->S)
Used to prevent organ rejection with transplants
