Immunosupressants Flashcards
Inhibit enzyme in purine synthesis through inhibition of inosine monophosphate dehydrogenase
Mycophenalte motefil (MMF)
Mycophenolate sodium (MPS)
Mycophenolate motefil
Anti-proliferative
Inhibits purine synthesis: inhibits inosine monophosphate dehydrogenase
More selective and effective vs azathioprine
Blocks T-cell and B-cell proliferation
Prevents smooth muscle proliferation - also beneficial in preventing chronic rejection
Non-specific blockade of nucleic acid synthesis
Azathioprine
Non-specific
Azathioprine
Anti-proliferative
Blocks nucleic acid synthesis
Non-specific: affects all rapidly dividing cells
i.e. T cells undergoing clonal expansion
Inhibit T cell activation by inhibiting IL-2 gene transcription
Calcineurin inhibitors
Ciclosporin
Tacrolimus
Ciclosporin and Tacrolimus
Both drugs are calcineurin inhibitors and fungal products
Inhibit T cell activation by blocking IL-2 gene transcription
–> inhibit cytotoxic T cell generation
Both nephrotoxic - requiring blood level monitoring as nephrotoxicity is level-dependent
Macrolide antibiotic that blocks mTOR
Rapamycin (sirolimus)
Blocks mTOR
Rapamycin
Macrolide antibiotic
Blocks protein-designated mammalian target of rapamycin (mTOR)
–> inhibition reduces cytokine-dependent cellular proliferation at G1 to S phase of cell division cycle
–> thereby blocking T-cell activation
Non-nephrotoxic
Impairs wound healing
Anti-IL-2R
Basiliximab
Daclizumab