Immunosuppressants/Immunomodulators Flashcards
Drugs that are non-selective COX1/2 inhibitors
Aspirin; Naproxen, Ibuprofen, Nabumetone, Indothemacin, Ketorolac
Drugs that are COX-2 selective Inhibitors
Celecoxib, Rofecoxib
5-Lioxygenase Inhibitors
Zileuton
Leukotriene Receptor Antagonists
Montelukast, Zafirlukast
Transcriptional activators of Lipocortin
(weakest) Hydrocortisone, Prednisone, Methylprednisolone, Dexamethasone (strongest)
Calcinuerin Inhibitors
Cyclosporin, Tacrolimus
Transcriptional inhibitors of cytokine production
Calcinuerin inhibitors, corticosteroids, jak/stat inhibitors
JAK/STAT Inhibitor example
Tofacitinib
Cytokinase antibodies (binds directly to TNF antibody)
Adalimumab; Infliximab; Etanercept (artifical)
Cytokine antibodies (Binds directly to IL-5)
Mepolizumab
Cytokine antibodies (Binds directly to IL-6)
Toclizumab
DNA Synthesis inhibitors classes for leukocyte proliferation
Purine Synthesis inhibitors, Folate synthesis inhibs, rUMP synthesis
Types of Purine synthesis inhibitors
Azathioprine, Mycophenolate
Types of Folate synthesis inhibitors
Methotrexate
Types of rUMP synthesis inhibitors
Leflunomide
mTOR inhibitors
Sirolimus
Cytokine receptor antibodies (binds to the CD20 receptor)
Rituximab
Cytokine receptor antibodies (binds to IgE on Bcell)
Omalizumab
Cytokine receptor antibodies (Binds to eosinophils)
Benralizumab
Cytokine receptor antibodies (Binds to IL-2 receptor of T-cell)
Basiliximab
Cytokine receptors antibodies (Binds to IL-1 receptor)
Anakinra
Mechanism of mTOR Inhibitors
In T-cells, Sirolimus +FKBP inhibits mTOR in the cell inhibiting proliferation of genes
Mechanism of azathiorpine
2 mechanisms: It can be converted to meTIMP, a direct inhibitor of purine synthesis by binding one of the enzymes needed for purines(Primary therapeutic effect). Or it can also be converted to a derivative of GTP, which would kill the daughter T-cell if taken into the DNA.
Mechanism of methotrexate synthesis inhibitors
Inhibits DHFR
Mechanism of JAK/STAT Inhibs
Prevents association of JAK and STAT, which is part of the intracellular signalling process when IL-2 binds to the outside receptor.
Mechanism of Calcineurin inhibitors
Inhibits the signalling intermedium calcinuerin, which helps transmit signals to the nucleus which would have otherwise produced IL-2.
Mechanism of Mycophenolate
Inhibits Inosine monophosphate dehydrogenase, which is an enzyme used in production of GTP