Exam 4; Immunosuppressants Flashcards by Courtney Kast

All of the immunosuppressants carry an increased risk of this

infection

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Many immunosuppressants cause an increased risk of this

malignancy

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What are four immunosuppressants that affect T cell activation

atgam
antithymocyte globulin
abatacept
belatacept

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This agent that affects T cell activation can be used to treat acute renal transplant (polyclonal antibodies)

antithymocyte globulin

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This agent that affects T cell activation bind to and inhibits CD80 and CD86; used to treat RA

abatacept

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This agent that affects T cell activation binds to CD80 and CD86, is used in renal transplant and causes an increase in malignancies

belatacept

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How can you tell which drug is a monoclonal antibody

it ends in -mab

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The middle (Li or Tu) of a monoclonal antibody drug signifies what

target
Li = immune cell
Tu = tumor cell

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How can you tell the source of a monoclonal antibody drug

Xi = chimeric source
Zu = humanized
U = fully human
O = fully mouse

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Which source of a monoclonal antibody is the most antigenic

Xi = chimeric (foreign with human)
O = fully mouse

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Natalizumab is what kind of monoclonal antibody

immune cell = Li

humanized = zu

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What is the mechanism behind natalizumab

binds to alpha integrins on the CD4 cell and other immune cell

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What disease is natalizumab linked with

progressive multi-focal leukoenephalopathy (PML)

fatal viral CNS disease

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Tocilizumab is what kind a monoclonal antibody

immune cell = Li

fully human = U

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What is the mechanism behind tocilizumab

bind to IL-6 receptors; T, B, and macrophages

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Ustekinumab is what kind of monoclonal antibody

immune cell = Li

fully human = U

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What is the mechanism behind ustekinumab

binds to IL-12 and IL-23

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Which condition is ustekinumab designed to treat

psoriasis

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What condition is tocilizumab designed to treat

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What conditions are natalizumab designed to treat

Crohn’s and MS

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What is the mechanism behind etanercept

binds to TNF itself (binds to an interleukin)

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What is the route of administration of etanercept

given subQ

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What is different about etanercept that the other agents that bind to TNF

it is not a monoclonal antibody

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What disorder is entanercept used to treat

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Infliximab is what kind of monoclonal antibody

chimeric = Xi | immune cell = Li

What is the mechanism behind infliximab

it binds to TNF

What disorder is imfliximab used to treat

RA and Crohn's

What are two side effects of infliximab

can induce an immune response | if given IV, the infusion can cause itching, hypotension, and fever

What is the concern with taking infliximab if you have a pre-existing condition

a pre-existing infection with a fungus or TB will flare up

Adalimumab is what kind of monoclonal antibody

immune cell = Li | fully human = U

What is the mechanism behind adalimumab

binds to TNF

What is certolizumab used to treat

RA and Crohn's

What is golumumab used to treat

RA ulcerative colitis psoriatic arthritis

What is the mechanism behind anakinra

blocks the IL-1 receptor

What condition is anakinra used to treat

What is the method of administration of anakinra

subQ

What other medications should anakrina be used with and NOT used with

use with other immunosuppressants like methotrexate, but not with TNF inhibitors

What is the mechanism behind rilonacept

binds to IL-1 molecule

This was the first drug that allowed transplantation to work properly

cyclosporine

What conditions is cyclosporine used for now

transplantation psoriasis dry eye

What is the mechanism behind cyclosporine

inhibits calcineurin phosphatase (ENZYME INHIBITOR) preventing the NFAT complex which prevents activation of the gene for IL-2, IL-3, and TNF

What is cyclosporine metabolized by

P450

What are the side effects of cyclosporine

``` nephrotoxicity hepatotoxicity hypertrichosis (hair growth) gingival hyperplasia increase in cholesterol hypertension ```

What is the mechanism behind tacrolimus

binds the FK binding protein (FKBP) which inhibits calcineuron phosphatase

Which is more efficacious, cyclosprine or tacrolimus

tacrolimus

What are the side effects of tacrolimus

nephrotoxicity neurotoxicity alopecia diabetes

What is tacrolimus metabolized by

P450

What is the mechanism of glucocorticoids

through the cell membrane → bind to receptor → receptor dimerizes → complex then binds with GC receptor element on DNA

What is the mechanism behind sirolimus and everolimus

bind to FKBP inhibit a kinase required for binding of IL-2 decrease in cytokine production

What are the side effects of sirolimus and everolimus

renal toxicity | lung toxicity

What is the mechanism behind basilixumab

blocks the IL-2 receptor

What other drug is basilixumab used with

cyclosporine

What are some conditions to watch for with someone taking basilixumab

hypersensitivity reaction; hypotension bronchospasm pulmonary edema

What is the mechanism behind tofacitinib

janus kinase inhibitor; inhibits the signal pathway of cytokines and ILs presents the activation of Signal Transducers and Activators of Transcription (JAK STAT)

What are the side effects of tofacinitinib

increase infection and malignancy

What kind of drug is azathioprine

pro-drug

What disorders is azathioprine used to treat

transplantation RA Crohn's

What is the mechanism behind azathioprine

since it is a prodrug, it is converted to 6-mercaptopurine which inhibits the synthesis of purines; inhibit T cell replication

What are the side effects of azathioprine

bone marrow depression leading to; megalobalstic anemia throbocytopenia leukopenia

What conditions are mycophenolate mofetil used to treat

transplantation and lupus

What is the mechanism behind mycophenolate mofetil

inhibits the enzyme inosine monophosphate dehydrogenase; inhibiting the synthesis of guanosine

What are the side effect of mycophenolate mofetil

``` bone marrow depression leading to; megalobalstic anemia throbocytopenia leukopenia as well as GI destruction ```

This is the drug of choice for early treatment of RA, is disease modifying so it will stop the progression of RA

methotrexate

What is the mechanism of methotrexate

inhibits dihydrofolate reductase inhibiting mammalian cell division inhibits a lot of folic acid dependent processes

What is dihydrofolate reductase necessary for?

the synthesis of dihydro-folic acid and tetrahydrofolic acid

What type of drug is leflunomide

prodrug that is converted to teriflunomide

What is the mechanism behind teriflunomide and leflunomide

inhibitors of pyrimidine synthesis | inhibiting the enzyme dihydro-orotate dehydrogenase

What are the side effects of leflunomide and teriflunomide

diarrhea | teratogen

How does leflunomide and teriflunomide affect P450

inhibits P450

This drug was first developed as a treatment for malaria

hydroxychloroquine

What is the mechanism of hydrochloroquine

taken up my macrophages and concentrated in macrophage lysosome which interferes with macrophage processing of antigens

What are the side effects of hydrooxychloroquine

GI dysfunction severe dermatitis irreversible retinal damage

Exam 4; Immunosuppressants Flashcards

(72 cards)