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43 Cards in this Set
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Azathioprine
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Inhibits PRPP synthase, PRPP amidotransferase and the salvage pathway of purines-->blocking both de novo and salvage pathways
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Azathioprine is converted to what nucleotide that inhibits the creation of purine nucleotides?
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Azathiprine-->6-mercaptopurine (6-MP)--> 6-thioinsosinic acid-->Thiouric acid
The 6-thioinosinic-->Thiouric acid will not give rise to gout. |
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This is an indescrimately cytotoxic immunosuppressive that acts as an antimetabolite, therefore hitting dividing cells only (CCS). This drug is sued to prevent graft rejection.
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Azathioprine
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What are the adverse affects of azathioprine?
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-Bone marrow suppression
-Leukopenia -Hyperuricemia(?) *remember there won't be anemia b/c this drug is inhibiting synthesis of NEW blood cells, not destruction of existing ones. |
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Why is hyperuricemia a side effect of azathioprine? Didn't we say it makes Thiouric acid and doesn't cause gout? Whats goin on?
-Can we give a rescue agent? |
Don't forget that Azathioprine is killing many other cells in the body, which causes a spillage of purines. These will react with xanthine oxidase and create uric acid
Rescue agent is allopurinol |
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Mercaptopurine
How does it work? |
Prevents de novo purine synthesis by blocking PRPP synthetase, which also inhibits the salvage pathway.
Eventually, mercaptopurine will kill cells spilling purines into the body that interact with XO to form gout causing uric acid. SO, we give allopurinol to reduce the gout. ****Allopurinol is preferred by XO so you may get mercaptopurine toxicity, may need to reduce mercaptopurine. |
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Allopurinol and mercaptopurine when given together?
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Keeps urica cids low but results in toxic mercaptopurine levels, b/c allopurinol is the preferred occupant of xantine oxidase, so mercaptopurine cannot be oxidized by this enzyme
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What are the uses of cyclosporine?
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1.) organ transplantation and treatment of graft vs. host dz in BM transplants.
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How does cyclosporine work?
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cyclosporine blocks CYP-A which prevents dephosphorylation of NFAT thus preventing its translocation across the nucleus. If NFAT cannot get in, no IL-2 is secreted, preventing T cell proliferation
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When do you give cyclosporine and is it toxic?
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HIGHLY nephrotoxic so we developed a way to allow kidney transplant patients to gain complete function before giving the drug to them (2 weeks later).
Toxicity: nephrotoxic and gingival hyperplasia |
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Sirolimus
What is it used for? |
Sirolimus-eluting stents have been approved to reduce stenosis
Binds mammalian kinase or mTOR* |
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Sirolimus MOA
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combines with FKBP-12 and forms a complex that inhibits mTOR, which is a key enzyme in the cell cycle progression. It blocks the response of T cells to cytokines and inhibits B cell proliferation
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Mycophenolate mofetil
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Prophylaxis of kidney, liver and heart rejection and for Lupas
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Mycophenolate MOA
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It inhibits Inhibits inosine monophosphate dehydrogenase which is an important enzyme in de novo Guanine NT synthesis; B and T cells are HIGHLy dep on this pathway.
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What are the lymphotoxic drugs?
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1.) ALG
2.) Immune globulin 3.) Rho D 4.) Muromanab CD3 5.) Asparanginase 6.) Steroids |
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This lymphotoxic drug is raised in horses to human lymphocyte preparations and used for prophylaxis to prevent rejection following kidney transplant
Its MOA is to bind to T lymphocytes causing them to be destroyed by complement |
Antilymphocytic globulin (ALG)
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This lymphotoxic drug is rasied to human thymocytes in rabits and used in acute renal transplant rejection crises!
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Antithymocytic globulins
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This lymphotoxic drug is given to Rhesus negative moms with R+ babies to prevent hemolytic disease of the newborn.
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Rho (D) immunoglobulin
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This lymphotoxic drug is a polyclonal human antibody used for passive immunization in autoimmune diseases and Kawasaki's disease?
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Immune Globulin IV
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This lymphotoxic drug is a monoclonal antibody to CD3 surface molecules of thymocytes and used for acute renal allograft regection crisis especially when the rejection is resistant to corticosteroid treatment
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Muromonab
**can cause cytokine release syndrome |
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What are the drugs that selectively act on a subpopulation of immunocompetant cells?
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-cyclosporine
-Tacrolimus -Sirolimus -Mycophenolate mofetil |
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This drug prevents IL secretion by inhibiting the dephosphorylation of NFAT.
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-cyclosporine
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Tacrolimus (macrolide antibiotic)
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Used like cyclosporine but it is also used topically to treat atopic dermatitis and is NOT NEARLy as nephrotoxic as cyclosporine; 10-100x more potent than cyclosporine
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This drug is 10-100x more potent than cyclosporine and is often used to rescue graft rejection in very early stages.
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Tacrolimus
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This is not nephrotoxic and works by blocking a key enzyme for G1-->S phase progression.
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Sirolimus
***binds FKBP and inhibits mTOR (mammalian kinase) |
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Name the drugs that targer inflammatory cytokines or their receptors
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1.) Etanercept
2.) Infliximab 3.) Daclizumab |
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Which drug targeting cytokines binds to TNF-alpha and acts as a receptor? Also Tx: RA
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Entanercept
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This drug targeting cytokine also binds to TNF-alpha and prevents the cytokine from binding to ITS receptors. Tx: Chrohn's disease and RA w/ methotrexate.
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Infliximab
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This drug neutralizes the biological activity of TNF alpha and inhibits the binding of TNF-alpha to its receptor.
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Infliximab
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This drug targeting cytokines brinds to the IL-2 receptor on T cells preventing activation of the CD4 Th cells. Tx: of acute rejection following kidney heart or liver transplants.
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Daclizumab
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Levamisole
-What does it stimulate? -Use with what 2 other drugs? -Uses/Treatment? |
stimulates maturation/proliferation of T cells
-Used w 5-FU and leucovorin -Tx: Dukes stage C colon cancer Tx: It is also an antiparasitic drug |
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Bacillus Calmette-Guerin (BCG).
-Tx: |
Used as a non-specific immunostimulant for bladder cancer
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Cytokines immunostimulants:
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-Interferons
Interferon alpha Interferon beta Interferon gamma b Interluekins aldesleukin Oprelvekin Colony stimulating factors 1.)Filgrastim 2.) Sargramostim 3.) Epoetin 4.) Thrombopoetin |
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cytokines drugs
Interferons alpha, beta and gamma What are the treatments of each? |
Alpha: Hep B &C
Beta: MS Gamma: Chronic granulomatous disease |
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Cytokine drugs:
-Interleukin Aldesleukin |
Form of IL-2 that promotes production of NK cells
Tx: adjunct in metastatic renal cell carcinoma |
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cytokine drugs:
Interluekin groups; what are the two drugs? |
Aldesleukin and Oprelvekin
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Cytokine drugs: interluekin group; what is oprelvekin?
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A recombinent form of IL 11
Tx: thrombocytopenia |
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Cytokine drugs: colony stimulating factors; what are they? (4)
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Filgrastim
Sargramostim Epoetin-alpha (erythropoetin) Thrombopoetin |
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Cytokine drugs; colony stimulating factors;
1.) Filgrastim: |
*Granulocyte stimulator: stimulates CFU-G
-->increases neutrophil production!!! Used to stimulate bone marrow recovery during chemo!! |
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Cytokine drugs; colony stimulating factors
2.) Sargramostim |
Derived from yeast and stimulates granulocytes and macrophage.
Used to promote myeloid recovery in patients with high dose chemo |
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Cytokine drugs
-colony stimulating Erythropoetin |
stimulates RBC's
---make sure you take with lots of iron to treat anemia ADV: heart and liver toxic!! |
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Which colony stimulating immunostimulant drug is contraindicated in patients with heart failure and yeast hypersensitivity?
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Sargramostim
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Cytokine drug; colony stimulating
Thrombopoetin |
selectivly stimulates megakaryocytopoiesis ie increases platelets
used in hastening platelet recovery in patients undergoing stem cell transplantation |