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42 Cards in this Set
- Front
- Back
- 3rd side (hint)
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What do Cyclosporine, Tacrolimus, and Sirolimus do?
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Inhibit Cytokine Production and function
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What are Azathioprine (Imuran) and Mycophenolate mofetil (CellCept)?
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they are cytotoxic agents
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What are Antithymocyte globulin (ATG), muromonab-CD3 (Orthoclone OKT3) and Basiliximab (Simulect)
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Antibodies
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What are Predisone (Deltasone) and Methylprednisolone (Solu-Medrol)
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Corticosteroids
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What type of dru is Thalidomide?
Why was it taken off the market? |
a sedative used in erythema nodosum leprosum and anemia due to myelodysplastic syndrome
taken off the market because of severe side effects |
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How do immunosuppressives work generally?
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they prevent the proliferation and synthesis of lymphoid cells
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When are immunosupressives generally used?
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During organ transplantation, auto immune diseases and isoimmune disorders?
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What are the general side effects of immunosuppressives?
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you are self inducing an immune comprimised state so you will see increased infections from bacteria, virus, fungi, and increased neoplasms and lymphomas
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What is the major drug for organ transplantation>
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cyclosporin and other combinations
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What is the drug of choice for autoimmune diseases?
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predisone
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How do Cyclosporine and Tacrolimus work?
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When an antigen presenting cell shows a T cell it's antigen it starts a cycle in the cell that will ultimately cause it to proliferate and set off the immune response, the TCR-APC complex increases calcium which activates calcineurin wich activates the cell to make IL-2, but these drugs bind to Calcineurin and inhibit IL-2 formation?
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How are Tacrolimus and Cyclosporine different?
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Cyclosporine uses cyclophilin
while, Tacrolimus uses FK-binding protien, both of these proteins then inhibit Calcineurin |
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What is one important factor about the pharmokinetics of Cyclosporine that would effect it's drug contraindications?
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It is broken down by CYP3A4
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Other that being used for organ trasplants, what are some other used for Cyclosporine?
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used in combination with corticosteroid, for severe recalcitrant psoriasis, and severe Rheumatoid arthritis
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What does Phenolobitol, phenytoin and refampin do to Cyclosporine metabolism?
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they increase it's metabolism
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What do cimetadine, grapefruit juice, and ketoconazole to to Cyclosporine metabolism?
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they decrease it, due to inhibiting the CYTP450 enzyme and possibly increasing it to toxic levels
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What is the risk of using NSAIDS and Gentamicin with Cyclosporines?
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Increase the chances of nephrotoxicity
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Is Tacrolimus less or more potent than Cyclosporine?
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100X more potent
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What is Tacrolimus especially used for?
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rescue therapy for organ graft rejection unresponsive to cyclosporine,
atopic dermatitis psoriasis |
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What is better and what is worse about the side effects of Tacrolimus in compared to Cyclosporine?
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It doesn't cause hypertension, but the possibility of nephrotoxicity is increased, as well as headach, insomnia, tremor, seizures and hallucinations
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What do Sirolimus and Cyclosporine's MOA have in common and where are they different?
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both drugs inhibit IL-2 production thereby decreaseing T cell proliferation, but whil Cyclosporine and Tacrolimus do it by binding Calcieurin, Sirolimus doesn it by binding nTOR
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What two drugs are macrolides and immunosupppressives?
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sirolimus and tacrolimus
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Which of the three cytokine inhibitors is also a potent inhibitor of B cell proliferation?
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Sirolimus (think serum- serolimus)
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How are Axathioprine and 6-MP alike?
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Azathioprine is converted into 6-MP within the red blood cell which makes it safer because it will act more locally
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What does Azathioprine inhibit? And what other kind of potent effect does it have?
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Azathiprine inhibits DNA/RNA synthesis and has potent anti-inflammatory effects
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What are the clinical uses of Azathioprine?
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used in organ transplants along with cyclosporines and prednisone, and used with Rheumatoid arthritis and systemic lupus and other autoimmuned disorders
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What are the side effects of Azathioprine?
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mild leukopenia, NV, fever, alopenecia, and risk of infection (alopecia)
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What does mycophenolate mofetil and mycophenolate sodium inhibit?
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inosine monophosphate dehydrogenase (GMP) (precursor for nucleic acid synthesis) and de novo synthesis of purines, thus suppressing B and T cell proliferation
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What is mycophenolate hydrolyed to in VIVO?
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MPA mycophenolic acid
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What are some possible side effects of Mycophenolate?
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mild leukopenia, NVD, GI hemmorhage, increased infections
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How do antacids and Cholestyramine (Questran) effect Mycophenolate?
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They decrease it's absorption
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How can Antilymphocytic globulin be used to suppress the immune system?
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Act to bind and decrease the number of peripheral T-Lymphocytes
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When would you use antilymphocytic globulin and what are possible side effects?
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you would use them for organ transplants and because they are a foreign protien they might cause flu like symptoms such as fever, chill, skin rash, and serum sickness
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How does Muromonab CD3 Monoclonal antibody (Orthoclone OKT3) suppress the immune system?
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this is a mouse antibody that selectively binds to CD3 glycoprotein on T lymphocytes and immediately depletes them
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What are the clinical uses of CD3 Monoclonal antibody?
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emergency use in acute rejection of liver and heart transplants after steroid use has failed, and used to deplete the T cells from donor bone marrow prior to transplant
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what are the side effects of Muromonab CD3?
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flue like illness, shock, anaphylaxis, high fever, seizures, encephalopathy, cerebral edema, headache, increased infections and neoplasms
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the side effects are probably why it is only used in extreme situations
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How does Masiliximab work?
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It binds the Interlukin-2 and therefore is immunesupprsive
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muro means...
zu means... xi means... |
muro- from mouse
zu- from human xi means from both |
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What is an advantage to using Basaliximab?
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it has very few side effects because it is a partly human protein
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we love basil,it is good for us because it is like us
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How do the anti-inflammatory corticosteroids work? (5 things)
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inhibit the inflammatory response by inhibiting the production of inflammatory mediators and cytokines, decrease chemotaxis and phagocytic activity of neutrophils and monocytes,
lower IgG levels |
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What are the clinical uses for Corticosteroids?
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with the other immunosuppresives for transplantation, for immune disorders, allergic reactions, bronchial asthma
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Adverse reactions of Corticosteroids?
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increased infections, adrenal suppressions, GI bleeding, delayed wound healing, osteoporosis, Cushing's Habitus
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