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Drugs > Autoimmune Drugs ( Lupus + RA) > Flashcards

Autoimmune Drugs ( Lupus + RA) Flashcards

1
Q

Anakinra

A

(Kineret)
• Antagonist of IL-1 receptor
FDA approved for RA but not terribly effective

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2
Q

Tumor Necrosis Factor (TNF) Inhibitors

A 
• Pro-inflammatory cytokine
• Produced by macrophages
Reduces joint inflammation and damage to joints
Etenercept (Enbrel)  -not monoclonal Ab
Adalimumab (Humira) 
Certolizumab (Cimzia) 
Golimumab (Simponi) 
Infliximab (Remicade)
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3
Q

Infliximab

A

Remicade

Chimeric monoclonal Ab directed against TNF

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4
Q

Simponi

A

Golimumab

Human monoclonal Ab directed against TNF

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5
Q

Corticosteroids

methylprednisolone

A

Decrease inflammation
Cytokine signaling
Inhibit INF-alpha
Weight gain ( moon face, buffalo hump, abdominal striae), bone health (osteoporosis, avascular necrosis), DM, infection risk, mood

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6
Q

Arava

A

Leflunomide
Inhibition of dihydroorotate dehydrogenase -> inhibit pyrimidine synthesis -> reduction of lymphocytes
Prodrug (oral)(enterohepatocyte circulation = long half life) [LOWEST effectivity]
reduction of lymphocytes
Diarrhea, cytopenia, liver toxicity
TERATOGEN
DMARDS

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7
Q

Certolizumab

A

Cimzia

Fab fragment of monoclonal Ab directed against TNF

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8
Q

Abatacept

A

Orencia
Binds CD80/86 on antigen presenting cells (APCs) blocking the interaction of CD28 between APCs and T cells
• Result is that T cells cannot be activated
T cells are at the “center” of pathogenesis
subcutaneous and intravenous
TEROTAGEN

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9
Q

Cyclophosphamide

A

(Cytoxan )
Phosphoramide mustard:
Attaches an alkyl group to DNA -> cell apoptosis
Apoptosis of cells ( ab? Of cell not apoptosising right?)
chemo
Nausea, hair loss, cytopenia, secondary malignancy

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10
Q

Hydroxychloroquine

A 
Interfere with self Ag presentation 
MHC processing blocked via 
*lysosomal acidification block 
	- Acid dependent protease cleaving TLR, cant cleave 
	- Prevent TLR binding to epitopes
Takes 3-6 months to work 
Immune modulatory=
No risk of infection
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11
Q

CellCept

A

Mycophenolate mefetil
Decrease proliferation of B/T cells
Inhibits inosine monophosphate dehydrogenase -> reduced guanine monophosphate for purine synthesis devo nova pathway ( used by B/T cell in proliferation)
Diarrhea, cytopenia

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12
Q

Rituximab

A

• Monoclonal antibody directed against CD20 antigen on B lymphocytes
• Result is depletion of B cells
But not existing plasma cells (do not have CD20)
Initial researchers surprised rituximab works as well as it does for RA as current understanding does not place B cells as most prominent player
Intravenous
TEROTAGEN

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13
Q

Plaquenil

A

Hydroxychloroquine
Oral [LOWEST]
• Inhibits activity of toll like receptors (innate immune system)
Inhibits acidification of lysosomes ultimately interfering with antigen processing
Rare retinal toxicity
DMARDS

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14
Q

Cytoxan

A

Cyclophosphamide
Phosphoramide mustard:
Attaches an alkyl group to DNA -> cell apoptosis
Apoptosis of cells ( ab? Of cell not apoptosising right?)
chemo
Nausea, hair loss, cytopenia, secondary malignancy

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15
Q

Mycophenolate mefetil

A

(CellCept)
Decrease proliferation of B/T cells
Inhibits inosine monophosphate dehydrogenase -> reduced guanine monophosphate for purine synthesis devo nova pathway ( used by B/T cell in proliferation)
Diarrhea, cytopenia

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16
Q

Triple Therapy

A

Methotrexate
Hydroxychloroquine
Sulfasalazine

17
Q

Orencia

A

Abatacept
Binds CD80/86 on antigen presenting cells (APCs) blocking the interaction of CD28 between APCs and T cells
• Result is that T cells cannot be activated
T cells are at the “center” of pathogenesis
subcutaneous and intravenous
TEROTAGEN

18
Q

Cimzia

A

Certolizumab

Fab fragment of monoclonal Ab directed against TNF

19
Q

Azathioprine

A

(Imuran)
Purine analog that inhibits purine synthesis
Inhibition of DNA/RNA = lower T/B cells
Result: reduced cell proliferation particularly leukocytes
Decreased function of B and T-cells
Cytopenia, hepatotoxicity, rash

20
Q

• Tofacitinib

A 
Xeljanz
• Inhibits Janus kinase (JAK) enzymes
• Inhibition of JAKs prevents cytokine/growth factor mediated gene expression and intracellular activity of immune cells
Targeted synthetic DMARD
TEROTAGEN
21
Q

Xeljanz

A 
Tofacitinib 
• Inhibits Janus kinase (JAK) enzymes
• Inhibition of JAKs prevents cytokine/growth factor mediated gene expression and intracellular activity of immune cells
Targeted synthetic DMARD
TEROTAGEN
22
Q

Humira

A

Adalimumab

Human monoclonal Ab directed against TNF

23
Q

Enbrel

A

Etenercept
TNF inhibitor
NOT monoclonal Ab.
Fusion protein of Fc portion of IgG that binds to TNF receptor and prevents it from interacting w/ cell surface receptors

24
Q

Tocilizumab

A

(Actemra)
• Humanized monoclonal antibody targeting IL-6 receptor
• Reduces inflammation and joint damage
Subcutaneous or intravenous versions
*Cytopenia, Cell toxicity, bowel perfusion TEROTAGEN

25
Q

Golimumab

A

Simponi

Human monoclonal Ab directed against TNF

26
Q

Etenercept (Enbrel)

A

(Enbrel)
TNF inhibitor
NOT monoclonal Ab.
Fusion protein of Fc portion of IgG that binds to TNF receptor and prevents it from interacting w/ cell surface receptors

27
Q

Leflunomide

A

(Arava)
Inhibition of dihydroorotate dehydrogenase -> inhibit pyrimidine synthesis -> reduction of lymphocytes
Prodrug (oral)(enterohepatocyte circulation = long half life) [LOWEST effectivity]
reduction of lymphocytes
Diarrhea, cytopenia, liver toxicity
TERATOGEN
DMARDS

28
Q

Imuran

A

Azathioprine
Purine analog that inhibits purine synthesis
Inhibition of DNA/RNA = lower T/B cells
Result: reduced cell proliferation particularly leukocytes
Decreased function of B and T-cells
Cytopenia, hepatotoxicity, rash

29
Q

Adalimumab

A

Humira

Human monoclonal Ab directed against TNF

30
Q

Methotrexate

A

Oral or subacute
Inhibition of dihydrofolate reductase = decrease synthesis of purine + pyrimidines
Increase adenosine release from cell
• Decrease DNA synthesis, repair, replication
Dampen cellular inflammation
Need to take Folate
Oral OR subcutaneous weekly
Oral ulcers, GI side effects: nausea, cytopenia, Liver toxicity, TERATOGEN
Oral or subacute
DMARDS

31
Q

Actemra

A

Tocilizumab
• Humanized monoclonal antibody targeting IL-6 receptor
• Reduces inflammation and joint damage
Subcutaneous or intravenous versions
*Cytopenia, Cell toxicity, bowel perfusion TEROTAGEN

32
Q

Sulfasalazine

A

Sulfapyridine is active moiety but exact mechanism of action has not been identified
Oral
rash, GI upset, hepatotoxicity, cytopenias
Sulfa allergy = no drug

33
Q

Remicade

A

Infliximab

Chimeric monoclonal Ab directed against TNF

34
Q

(Kineret)

A

Anakinra
• Antagonist of IL-1 receptor
FDA approved for RA but not terribly effective

35
Q

Belimumab

A

Inhibits Autoantibody production/ B cell function
Blocks BAFF/Blys
(B-cell activating factor blocker)

Drugs (2 decks)

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