- binds cyclophilin A in T cells - complex binds to calcineurin - inhibits synthesis of cytokines (IL2), protooncogenes, and cytokine receptors (IL-2R) - Increase production of transforming growth factor B-(TGF-B)

Immunopharmacology Flashcards by Bina Malapur

primary or secondary immune response which one is more easily and effectively affected

primary

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when does immunosuppressive therapies work the best

used before rather then after exposure

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name 3 clinical uses for immosupressive drugs

organ transplantation
Selective immunosuppression - Rh
autoimmune disease

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name 2 limitations to therapy

increase risk of infection

- increase risk of lymphomas and related cancers

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Cyclosporine inhibits what

Calcineurin

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MOA for Cyclosproine

binds cyclophilin A in T cells
complex binds to calcineurin
inhibits synthesis of cytokines (IL2), protooncogenes, and cytokine receptors (IL-2R)
Increase production of transforming growth factor B-(TGF-B)

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Cyclosporine is selective for what lymphocyte

T lymphocytes

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what is cyclosporine used for

prevention and treatment of organ rejection

- autoimmune disorders

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what is the toxicity for Cyclosporin

nephrotoxicity

hypertension

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Tacrolimus (FK506) inhibits what

Calcineurin

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MOA of Tacrolimus

binds FK506 binding protein-12 (FKBP)

-inhibits calcinerurin and calcineurin mediated events

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difference between Tacrolimus and Cyclosporine

tacrolimus more potent

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what is the toxicity for Tacrolimus

Nephrotoxicity
neurotoxicity
hypertension
diabetes

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Sirolimus and Everolimus MOA

binds to FKBP

does not inhibit calcineurin
inhibits mTor

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what is the role of mTor

kinase for T cell proliferation

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Where does Sirolimus/Everolimus block the T cell cycle

G1 to S phase

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Toxicities for Sirolimus and Everolimus

Not nephrotoxic

increase cholesterol and triglycerides in serum

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Glucocorticoid MOA

unclear, inhibit T-cell proliferation, T-dependent immunity, and expression of genes encoding cytokines

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what is the use for Glucocorticoid

prevent organ rejection

autoimmune disease

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What are the cytotoxic drugs

Azathioprine

Mycophenolate mofeitl

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What is the MOA for Azathioprine

6-MP metabolites inhibit purine biosynthesis, then inhibits DNA synthesis, inhibits T cell proliferation

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What is Azathioprine used for

prevention of organ transplant rejection

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what is the drug interaction for Azathioprine

Allopurinol is given, then reduce Azathioprine

Allopurinol inhibits Xanthine oxidase
Xanthine oxidase catabolizes Azathioprine metabolites

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what is the toxicity for Azathioprine

bone marrow supression
leukopenia
thrombocytopenia
anemia

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Mycophenolate mofetil MOA

prodrug converted to MPA

role of MPA

reversible inhibitor of IMPDH | -inhibits guanine nucleotide synthesis

What is Mycophenolate mofetil used for

prophylaxis of transplant reject

What is Mycophenolate Mofetil toxicity

GI effects | leukopenia

What should you not take Mycopheonolate mofetil with

antacids

Antithymocyte globulin (ATGAM) MOA

binds to circulating T lymphocytes which induces lymphonpenia and decreases T-cell function

what is antithymocyte globulin (ATGAM) used for

prevent and treat acute allograft rejection

what is the toxicity for antithymyocyte globulin ( ATGAM)

serum sickness nephritis chills, fever, rash

Muromonab-CD3 (Orthoclone) MOA

induces internalization of T cell receptor complex, reduces T cell circulating

How is Muromonab-CD3 made

mouse monoclonal antibody against CD3 glycoprotein

what is the toxicity for Muromonab-CD3

cytokine release syndrome anaphylactic reactions CNS toxicity increased risk for infections and malignancy

Daclizumab/Basiliximab

bind IL-2 receptor on T cells - inhibit T-cell activation - prophylaxis of acute rejection in renal transplantation

Alemtuzumab ( Campath -1H)

binds CD52 glycoprotein on B cells and T cells, monocytes, macrophages, NK cells - induces lympholysis - Chronic lymphocytic leukemia CLL

Efalizumab

binds CD2a subunit of leukocyte function associated LFA-1, which inhibits T cell adhesion and activation

what does Efalizumab treat

prevent organ transplant rejection | treat psoriasis

Tocilizumab

binds IL-6 receptors, inhibits IL-6 actions

what is Tocilizumab used to treat

juvenile rheumatoid arthritis | increase risk of infection

Rituximab

binds CD20 on B lymphocytes | induces B lymphocyte lyses

what is Rituximab used to treat

chronic lymphoid leukemia non-Hodgkin's lymphoma rheumatoid arthritis

What are the anti-TNF drugs

Infliximab Adalimumab etanercept

What is Infliximab

mouse-human chimeric monoclonal antibody

Adalimumab

humanized monoclonal antibody

Etanercept

fusion of protein consisting of ligand binding domain of TNF receptor fused to IgG1 fragment

What is the MOA for Anti-TNF drugs

bing TNF and neutralizes TNF activities

what are Anti-TNF drugs used for

rheumatoid arthritis psoriasis crohn's disease

what is the toxicity for anti-TNF drugs

increased risk for infection, lymphomas

name 2 fusion proteins

Afefacept | Abatacept/Belatacept

Alefacept

LFA-3IgG1 fusion protein binds CD2 on T cells - inhibits interaction between LFA-3 and CD2 - inhibits T cell activation

what is Alefacept used for

psoriasis

Abatacept/Belatacept

CTLA4-IgG1 fusion proteins that bind CD8 and CD 86 on APC cells -inhibits CD80/CD86 an CD28 on t-cell -inhibits co-stimulatory pathway

what is Abatacept used to treat

juvenile idiopathic arthritis | rheumatoid arthritis

What is Belatacept used for

prevent organ transplant rejection

name 2 natureal adjuvants

immune globulins | Bacillus Calmette-Geurin ( BCG ) vaccine

what is immune globulins

contains all immunoglobulin subclasses to provide passive immunity

when are immune globulins used

prevent measles, hep A, tetanus, hemolytic diseases

Bacillus Calmette-Guerin ( BCG ) vaccine

viable attenuated strain of Mycobacterium bovis; muramyl dipeptide is active part - stimulates NK and T cell activity

what is BCG vaccine used for

bladder cancer

what is the toxicity for BCG

severe hypersensitivity reactions and shock can develop

What are 3 immunostimulants synthetic agents

Levamisole Isoprinosine Thalidomide

Levamisole

anthelminic agent inhibits T supressor cells - used in colon cancer

Isoprinosine

Increase NK cell cytotoxicity and activity of T-cell and monocytes

Thalidomide

decreases circulating TNF-alpha

what is the contraindiction in Thalidomide

pregnant due to teratogenic properties

name 3 cytokines

interferone alpha interleukin - 2 (Proleukin) Granulocyte colony stimulating factors

interferon alpha activates

activates macrophages, T-lymphocytes, NK T cells

interferon alpha treats what

Hep B and C

what is toxicities for Interferons alpha

flu like symptoms and boxed warning regarding development of pulmonary hypertension

Interleukin -2 (Proleukin) MOA

activates cellular immunity

what is IL2 (Proleukin) used for

metatstic melonoma renal cell carcinoma AIDS patients

toxicity of IL2 ( proleukin)

severe hypotension and life threatenting cardiovascular toxicity

what is dose limiting in IL2

pulmonary edema ( capillary leak syndrome)

Granulocyte colony stimulating factors (G-CSFs) - myeloid growth factor

stimulate increases in the number of granulocytes and monocytes -reduce neutropenia