Lecture 3 - Drugs for Autoimmune Disease Flashcards by Indy P

Entercept

immunosuppresant

useful for many rheumatic syndromes
thought to be less effective against IBDs compared to other TNF alpha inhibitors

MOA:
TNF - alpha blocking agent
fusion protein (fusion of TNF receptor and Fc domain of IgG) that neutralizes TNF alpha

SE:
activation of latent TB
increased opportunistic infections
avoid in pts with recent malignancies

less immunogenic than other TNF-alpha blocking agents

often combined with other traditional DMARDs (methotrexate, azathioprine, cyclosporine)

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What is the MOA of etancercept?

TNF - alpha blocking agent 
fusion protein (fusion of TNF receptor and Fc domain of IgG) that neutralizes TNF alpha

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What are the SE of entanercept?

activation of latent TB
increased opportunistic infections
avoid in pts with recent malignancies

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Adalimumab

immunosuppressant

useful for RA, ulcerative colitis, Crohn’s disease

MOA: TNF-alpha blocking agent
human monoclonal antibody that neutralizes TNF -alpha

SE:
activation of latent TB
increased opporuntistic infection
avoid in pts with recent malignancies

associated with basal cell and squamous cell skin cancers

often combined with other traditional DMARDs

concurrent therapy with methotrexate to prevent antibody formation against adalimumab

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What is the indication for adalimumab?

immunosuppressant

useful for RA, ulcerative colitis, Crohn’s disease

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What is the MOA of adalmumab?

TNF-alpha blocking agent

human monoclonal antibody that neutralizes TNF -alpha

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What are the SE of adalmumab?

activation of latent TB
increased opporuntistic infection
avoid in pts with recent malignancies

associated with basal cell and squamous cell skin cancers

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Infliximab

immunosuppresant

useful for RA, UC, Crohn’s disease

MOA:
TNF alpha blocking agent
chimeric human/mouse monoclonal antibody that neutralizes TNF-alpha

SE:
activation of latent TB
increased opportunistic infections
avoid in pts with recent malignancies

often combined with other traditional DMARDs

concurrent therapy with methotrexate to prevent antibody formation against infliximab

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What is the indication for infliximab?

immunosuppresant

useful for RA, UC, Crohn’s disease

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What is the MOA of infliximab?

TNF alpha blocking agent

chimeric human/mouse monoclonal antibody that neutralizes TNF-alpha

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What are the SE of infliximab?

activation of latent TB
increased opportunistic infections
avoid in pts with recent malignancies

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Tocilizumab

immunosuppressant

used for RA in pts unresponsive to TNF alpha inhibitors

MOA:
humanized monoclonal antibody that neutralizes IL-6 receptor on immune cells

SE:
activation of latent TB
increased opportunistic infections
GI perforation

suppression of IL-6 receptor can lead to induction of CYP2C9, 2C19, @d6, 3A4
plasma levels of drugs metabolized by these enzymes are typically decreased by tocilizumab

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What is the indication for tocilizumab?

immunosuppressant

used for RA in pts unresponsive to TNF alpha inhibitors

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What is the MOA for tocilizumab?

humanized monoclonal antibody that neutralizes IL-6 receptor on immune cells

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What are the SE of tocilizumab?

activation of latent TB
increased opportunistic infections
GI perforation

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Rituximab

immunosuppressant

used for RA in pts unresponsive to TNF alpha inhibitors

MOA:
B-cell depletor

humanized monoclonal antibody against CD20 on the surface of B-cells

SE: 
Increased opportunistic infections
increased viral infections
Hep B reactivation 
NOT associated with TB activation

may harm fetus

infusion reactions - treat with corticosteroids

often given in conjunction with methotrexate

also used to treat non-Hodgkin’s lymphoma and CLL

What is the indication for etanercept?

immunosuppresant

useful for many rheumatic syndromes
thought to be less effective against IBDs compared to other TNF alpha inhibitors

What is the indication for rituximab?

immunosuppressant

used for RA in pts unresponsive to TNF alpha inhibitors

also used to treat non-Hodgkin’s lymphoma and CLL

What is the MOA of rituximab?

B-cell depletor

humanized monoclonal antibody against CD20 on the surface of B-cells

What are the SE of rituximab?

Increased opportunistic infections
increased viral infections
Hep B reactivation
NOT associated with TB activation

may harm fetus

infusion reactions - treat with corticosteroids

Abatacept

immunosuppressant

used for RA in pts unresponsive to TNF - alpha inhibitors

MOA:
fusion protein that neutralizes the costimulatory ligand CD80/86 on antigen presenting cells; thus preventing T cell activation

SE:
test for latent TB (but no clear association with activation of latent TB), increased opportunistic infection
increased incidence of lung cancer and lymphomas

What is the indication for abatacept?

immunosuppressant

used for RA in pts unresponsive to TNF - alpha inhibitors

What is the MOA of abatacept?

fusion protein that neutralizes the costimulatory ligand CD80/86 on antigen presenting cells; thus preventing T cell activation

What are the SE of abatacept?

test for latent TB (but no clear association with activation of latent TB), increased opportunistic infection
increased incidence of lung cancer and lymphomas

Methotrexate

immunosuppressant for : organ transplant useful for many rheumatic syndromes can be combined with biologics MOA: folic acid analog; inhibits dihydrofolate reductase (DHFR), which prevents formation of tetrahydrofolate, a cofactor for thymidylate, purine and amino acid synthesis SE: myelosuppression given to pts to decrease antibody formation against biologic therapies

What is the indication for methotrexate?

immunosuppressant for : organ transplant useful for many rheumatic syndromes can be combined with biologics

What is the MOA of methotrexate?

folic acid analog; inhibits dihydrofolate reductase (DHFR), which prevents formation of tetrahydrofolate, a cofactor for thymidylate, purine and amino acid synthesis

What are the SE of methotrexate?

myelosuppression

Hydroxychloroquine

useful for many rheumatic syndromes can be combine with biologics MOA: weak base; neutralizes acid environment of lysosomes to inhibit processing of citrullinated proteins by acid hydrolases consequently, peptide presentation by MHC class 2 molecules on surface of antigen presenting cells is inhibited SE: HA, Nausea, diarrhea serious adverse reactions include allergic reaction; difficulty breathing; swelling of face, lips, tongue, or throat also antimalarial agent

What are the indications for hydroxychloroquine?

useful for many rheumatic syndromes can be combine with biologics also antimalarial agent

What is the MOA of hydroxychloroquine?

``` weak base; neutralizes acid environment of lysosomes to inhibit processing of citrullinated proteins by acid hydrolases consequently, peptide presentation by MHC class 2 molecules on surface of antigen presenting cells is inhibited ```

What are the SE of hydroxychloroquine?

HA, Nausea, diarrhea serious adverse reactions include allergic reaction; difficulty breathing; swelling of face, lips, tongue, or throat