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Immunosupresants - Coggle Diagram
Immunosupresants
Glucocorticoids
Prednisone
Methylprednisolone
Dexamethasone
Inhibitors of calcineurin
Tacrolimus
MOA
Binds to FKBP-12
inhibition of calcineurin
inhibition of Nuclear factor of activated T-cells activation (NFAT)
↓ IL-2 TRANSCRIPTION factor
↓ activation of T cells
Indications
transplant allograft rejection prophylaxis for solid organs
10-100x more potent than CsA (but more nephrotoxic and neurotoxic
psoriasis
rescue therapy in patients with rejection episodes despite therapeutic levels of cyclosporine
preferred calcineurin inhibitor
Side effects
Nephrotoxic
Neurotoxic
increase risk of diabetes
increase risk of malignancy
increase risk of infection
hypertension
Diabetogenic
DOES NOT affect uric acid of LDL cholesterol
increased risk of secondary tumors and opportunistic infections
Interactions
not recommended concomitant use of tacrolimus with cyclosporine or sirolimus
coadministration with cyclosporine: synergistic nephrotoxicity (delay 24 h when switching)
Cyclosporine A
MOA
Anti- TNF-a antibodies
Infliximab
Adalimumab
mTORinhibitors
Sirolimus
IMDH/IMPDH inhibitor
Mycophenolate mofetil
Inhibition of dihydrofolate reductase
Methotrexate
antimetabolite precursor of 6-mercaptopurine
Azathioprine
Chimeric
Rituximab