Immuno-modulating Drugs Flashcards
(36 cards)
MOA of the glucocorticoids/corticosteroids
Bind intracellular hormone receptors preventing activation leading to inhibition of the synthesis of the eicosanoids
-which are used to make prostaglandins, thromboxanes, lipoxins, and leukotrienes; each contributes to inflammation
Main indications for corticosteroids.
Autoimmune disease or reactions
-ITP, AIHA, acute glomerulonephritis
Transplant
-renal, heart, liver, bone marrow
What are the toxic side effects of corticosteroids?
Osteoporosis
Hyperglycemia
Adrenal Insufficiency (negative feedback of hypothalamic-pituitary axis)
Peptic Ulcers
MOA of Cyclosporine
Binds and inhibits cyclophilin in the T cell cytoplasm preventing released of IL-2, IL-3, and INF-gamma
Indications for Cyclosporine
Solid organ transplant
Graft vs. Host Disease (with methotrexate)
Why does cyclosporine have many drug-drug interactions?
It is metabolism by CYP3A4, along with many other drugs, mainly Calcium channel blockers and antifungals
Name a major drug that increases the activity of CYP3A4 decreasing the 1/2 life of Cyclosporine.
Carbamazepine
Major toxic side effect of cyclosporine
Induces Tissue Growth Factor Beta (TGF-B) with chronic use. Leads to tumor invasion and metastasis
ex. lymphomas, Kaposi sarcoma
MOA of Tacrolimus
Binds Immunophilin FK binding protein (IFKBP)
-immunophilins are general immune proteins, cyclophilin is an immunophylin that cyclosporine specifically inhibits. Tacrolimus inhibits multiple immunophilins and is much more potent
Indications for Tacrolimus
Stem Cell transplant (more than solid organ)
Prophylaxis of Graft vs. Host disease (with methotrexate)
MOA of Sirolimus
Inhibits mTOR which inhibits T cell response to cytokines
Binds and inhibits action of Immunophilin FKBP-12
-no inhibition of calcineurin
What is calcineurin?
In order for a T cell to be activated cyclophilin (the thing that cyclosporine inhibits) must bind with calmodulin (calcium binding protein) to form calcineurin. The complex is a phosphatase enzyme that activates T cells.
Main indication of Sirolimus.
Stem Cell Transplant
Prophylaxis of Graft vs. Host disease (with methotrexate)
Major toxicity of Sirolimus
Myelosuppression
MOA of Mycophenolate Mofetil
Inosine Monophosphate Dehydrogenase Inhibitor
- an enzyme for use in synthesis of GTP needed protein production
- may be a possible target for cancer chemotherapy
Main indication for Mycophenolate Mofetil
Suppress the immune system in graft rejection
Indication for Muromonab CD3
Autoimmune disorders and transplant management
Indication for IVIG
Autoimmune disorders, HIV, bone marrow transplant
Indication for RhD Immune Globuilin Micro-Dose
Rhogam
Hemolytic disease of Newborns
What is the one requirement for Monoclonal Abs to function?
The target of the therapy must have receptors that bind to the MAbs
MOA and indication for Alemtuzumab
Binds CD 52 on malignant WBCs
Treats B cell lymphoma/leukemia or T cell cancer
Toxicity of Alemtuzumab
WBCpenias
-so patients are normally also on antibiotics to prevent infection
MOA and indication for Bevacizumab
binds VEGF and prevents it from binding to its receptor
Used in colorectal cancer to prevent angiogenesis in tumors. Doesn’t work on already established tumors so it is often given in combination
Toxicity of Bavacizumab
Hemorrhage and wound healing problems so not used within a month before or after surgery
