Immunomodulatory Drugs Flashcards
Cyclosporine (CsA)
Calcineurin inhibitor. Inhibits activation of CD4+ and CD8+ T cells. Binds with cyclophilin, this complex inhibits calcineurin and stops IL-2 transcription. DMARD for RA. CYP3A4 metabolism, 3A4 inhibition leads to decreased CsA clearance and increased activity.
Tacrolimus
Fujimycin. Calcineurin inhibitor, much more potent than cyclosporine with less nephrotoxicity. Used in transplant rejection, GVHD.
Sirolimus
Rapamycin. Inhibits mTOR, blocks protein synthesis triggered by IL-2. As effective as CsA for renal transplant but NO NEPHROTOXICITY. Causes anemia, thrombocytopenia. Not for lung or liver transplants.
Mycophenylate Mofetil (MMF)
Hydrolized to MPA in liver, this stops de novo purine synthesis. Most T and B cell purine synth is denovo, not salvage. Combined with CsA/tacrolimus in kidney/liver transplants to allow reduced calcineurin inhibitor dose and reduce nephrotoxicity.
Azathioprine
Purine analog, disrupts de novo purine synth and stops transcription. Combined with calcineurin inhibitors to reduce rejection and treat severe RA.
Methotrexate
Folate analog, competes for and competitively inhibits dihydrofolate reductase.
Sulfasalazine
Scavenges ROS produced by neutrophils thereby diminishing their damaging effects. Sulfa-scavenger.
Penicillamine
Prevents IL-1 generation and collagen maturation, treats RA. PenicIL kILls IL-1. IL IL IL.
Chloroquine
Stops lysosomal processing and antigen presentation, decreases T-cell activation. Anti-malarial drug, combined with methotrexate and sulfasalazine to treat RA.
Leflunamide
Inhibits dihydroorotate dehydrogenase, blocking pyrimidine synthesis. Left-rotation, lefl. blocks rotate.
Daclizumab
CD-25. Targets CD-25 on IL-2 receptor, thereby inhibits IL-2 mediated T-cell activation.
Basilixumab
CD-25. Targets CD-25 on IL-2 receptor, thereby inhibits IL-2 mediated T-cell activation.
Infliximab
TNF-α. Increased infection susceptibility. TNF-α: AEI: Adalimumab, Etanercept, Infliximab.
Etanercept
TNF-α. Increased infection susceptibility. TNF-α: AEI: Adalimumab, Etanercept, Infliximab.
Adalimumab
TNF-α. Increased infection susceptibility. TNF-α: AEI: Adalimumab, Etanercept, Infliximab.
Abatacept
Immunoglobulin against CTLA4, treats RA.
Muromonab
CD3. Targets CD3, treats rejection in heart, liver, kidney transplants. Not given prophylactically, only given after rejection is seen.
Anakinra
IL-1R, treats RA. Increased risk of infections, as with pretty much all the mAb’s.
Tocilizumab
IL-6R. Treats RA, increased infection risk.
Rituximab
CD 20, treats RA. B cell depleting Ab.
Natalizumab
VLA4, blocks T cell migration to site of infection. Crohn’s disease and multiple sclerosis. High risk of progressive multifocal leukoencephalopathy (PML).
IV Immunoglobulin
Pooled Ig’s of healthy donors, confers passive immunity and has anti-inflammatory effect.
Fingolimod
Prevents lymphocytes from leaving the lymph nodes by binding to sphingosine-1 phosphate receptors. Treats MS. Risk of fatal infections since T cells can’t leave the lymph node to fight infection.
IFN-β
Treats MS.
Epoetin alfa
Stimulates RBC production, treats anemia.
Darbepoetin alfa
Hopefully the same as epoetin alfa.
Filgastrim
Stimulates neutrophil proliferation, maturation, and migration.
Belimumab
BAFF, depletes B cells. Treats SLE.
