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43 Cards in this Set

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Azathioprine
Inhibits PRPP synthase, PRPP amidotransferase and the salvage pathway of purines-->blocking both de novo and salvage pathways
Azathioprine is converted to what nucleotide that inhibits the creation of purine nucleotides?
Azathiprine-->6-mercaptopurine (6-MP)--> 6-thioinsosinic acid-->Thiouric acid

The 6-thioinosinic-->Thiouric acid will not give rise to gout.
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.
Azathioprine
What are the adverse affects of azathioprine?
-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.
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
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.
Allopurinol and mercaptopurine when given together?
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
What are the uses of cyclosporine?
1.) organ transplantation and treatment of graft vs. host dz in BM transplants.
How does cyclosporine work?
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
When do you give cyclosporine and is it toxic?
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
Sirolimus
What is it used for?
Sirolimus-eluting stents have been approved to reduce stenosis

Binds mammalian kinase or mTOR*
Sirolimus MOA
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
Mycophenolate mofetil
Prophylaxis of kidney, liver and heart rejection and for Lupas
Mycophenolate MOA
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.
What are the lymphotoxic drugs?
1.) ALG
2.) Immune globulin
3.) Rho D
4.) Muromanab CD3
5.) Asparanginase
6.) Steroids
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)
This lymphotoxic drug is rasied to human thymocytes in rabits and used in acute renal transplant rejection crises!
Antithymocytic globulins
This lymphotoxic drug is given to Rhesus negative moms with R+ babies to prevent hemolytic disease of the newborn.
Rho (D) immunoglobulin
This lymphotoxic drug is a polyclonal human antibody used for passive immunization in autoimmune diseases and Kawasaki's disease?
Immune Globulin IV
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
Muromonab
**can cause cytokine release syndrome
What are the drugs that selectively act on a subpopulation of immunocompetant cells?
-cyclosporine
-Tacrolimus
-Sirolimus
-Mycophenolate mofetil
This drug prevents IL secretion by inhibiting the dephosphorylation of NFAT.
-cyclosporine
Tacrolimus (macrolide antibiotic)
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
This drug is 10-100x more potent than cyclosporine and is often used to rescue graft rejection in very early stages.
Tacrolimus
This is not nephrotoxic and works by blocking a key enzyme for G1-->S phase progression.
Sirolimus
***binds FKBP and inhibits mTOR (mammalian kinase)
Name the drugs that targer inflammatory cytokines or their receptors
1.) Etanercept
2.) Infliximab
3.) Daclizumab
Which drug targeting cytokines binds to TNF-alpha and acts as a receptor? Also Tx: RA
Entanercept
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.
Infliximab
This drug neutralizes the biological activity of TNF alpha and inhibits the binding of TNF-alpha to its receptor.
Infliximab
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.
Daclizumab
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
Bacillus Calmette-Guerin (BCG).
-Tx:
Used as a non-specific immunostimulant for bladder cancer
Cytokines immunostimulants:
-Interferons
Interferon alpha
Interferon beta
Interferon gamma b
Interluekins
aldesleukin
Oprelvekin
Colony stimulating factors
1.)Filgrastim
2.) Sargramostim
3.) Epoetin
4.) Thrombopoetin
cytokines drugs
Interferons alpha, beta and gamma
What are the treatments of each?
Alpha: Hep B &C
Beta: MS
Gamma: Chronic granulomatous disease
Cytokine drugs:
-Interleukin
Aldesleukin
Form of IL-2 that promotes production of NK cells

Tx: adjunct in metastatic renal cell carcinoma
cytokine drugs:
Interluekin groups; what are the two drugs?
Aldesleukin and Oprelvekin
Cytokine drugs: interluekin group; what is oprelvekin?
A recombinent form of IL 11

Tx: thrombocytopenia
Cytokine drugs: colony stimulating factors; what are they? (4)
Filgrastim
Sargramostim
Epoetin-alpha (erythropoetin)
Thrombopoetin
Cytokine drugs; colony stimulating factors;
1.) Filgrastim:
*Granulocyte stimulator: stimulates CFU-G
-->increases neutrophil production!!!

Used to stimulate bone marrow recovery during chemo!!
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
Cytokine drugs
-colony stimulating
Erythropoetin
stimulates RBC's
---make sure you take with lots of iron to treat anemia

ADV: heart and liver toxic!!
Which colony stimulating immunostimulant drug is contraindicated in patients with heart failure and yeast hypersensitivity?
Sargramostim
Cytokine drug; colony stimulating
Thrombopoetin
selectivly stimulates megakaryocytopoiesis ie increases platelets

used in hastening platelet recovery in patients undergoing stem cell transplantation