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42 Cards in this Set

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