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Disease Modifying Anti-rheumatic Drugs Flashcards

1
Q

What drugs are first choice for RA tx?

A

NSAIDs- rapid onset and efficacy

  • provides anti-inflammation and pain relief but does not alter disease progression
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2
Q

What drug can be given for pain relief in addition to an NSAID for RA treatment?

A

acetaminophen

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3
Q

What drug complexes with NF-kB and AP-1 transcription factors causing indirect immunosuppression?

A

glucocorticoids (prednisone)

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4
Q

What can create RA and relieve pain an inflammation while waiting for DMARD effects?

A

glucocorticoids

  • treated RA flares and other autoimmune diseases
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5
Q
  • Lymphocytopenia
  • Monocytopenia due to redistribution
  • neutrophilia
  • eosinophila
  • PLA2 blockade (decreases eicosanoid synthesis)
A

Glucocorticoids

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6
Q

What can happen if glucocorticoids are stopped abruptly?

A

Death

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7
Q

How long should glucocorticoids be used?

A

less than 6 months

  • glucocorticoids should not be used chronically because of adverse side effects
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8
Q

-cept indicates..

A

fusion of a receptor to the Fc part of human IgG1

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9
Q

-mab indicates…

A

a monoclonal antibody

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10
Q

-ximab indicates…

A

indicates a chimeric mAb

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11
Q

zumab indicates..

A

a humanized mAb

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12
Q

-umab indicates…

A

indicates a human mAb origin

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13
Q

What DMARD is an inhibitor of dihydrofolate reductase and can cause a thymineless death with loss of TH4 when used as an antiproliferative to treat cancer?

A

Methotrexate

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14
Q

What DMARD undergoes polyglutamation and accumulates in cells over multiple weeks and thymidylate synthase and AICAR transformylase?

A

Methotrexate

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15
Q

Methotrexate causes AICAR accumulation leading to adenosine efflux to exert what effects?

A

anti-inflammatory (reduced B and T cell activity)

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16
Q

What DMARD is effective in 80% of patients and is faster than other DMARDs yielding effects evident in 3-6 weeks?

A

Methotrexate

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17
Q

What drug is a first choice for RA due to its relative safety, low cost, and extensive use?

A

Methotrexate

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18
Q

How often is methotrexate administered and how?

A

RA treatment administered once per week wither oral or injected

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19
Q

Weekly folate supplements should be taken with what drug?

A

methotrexate - low doses are used for immunosupressin and well-tolerated

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20
Q

What are methotrexate toxicities?

A
  • bone marrow suppression
  • hepatic fibrosis
  • GI ulceration
  • pneumonitis
  • fetal death
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21
Q

What DMARD is a lipophilic weak base that can easily go through plasma membranes and accumulate in lysosomes to raise the pH of the lysosomes?

A

Hydroxychloroquine

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22
Q

What RA drug can safely be used in pregnancies?

A

Hydroxychloroquine — also used to treat malaria

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23
Q

What DMARD can cause retinal damage?

A

hydroxychloroquine — low doses carry little risk

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24
Q

What drug can be used to treat ra alone or in combo with hydroxycholorquine and/or methotrexate as a triple therapy?

A

Sulfasalazine

25
Can sulfasalazine be used in pregnancy?
seems okay but less studied
26
What is the most common reason sulfasalazine is discontinued?
GI side effects- N/V, diarrhea, abdominal pain
27
What drug can cause pruritus, rash and urticaria?
Sulfasalazine- sulfa drug run! @Lauren
28
What RA drug inhibits mitochondrial enzyme dihydroorotate dehydrogenase to block the synthesis of rUMP?
Lefunomide
29
What are the effects of leflunomide?
inhibition of T cell proliferation - also blocks leukocyte adhesion and NF-kB activation
30
What drug is a second choice that would be used alternatively to methotrexate?
Leflunomide - can also be used in combo with methotrexate, sulfasalazine or hydroxyquine
31
What biologic DMARDs can be combined?
NONE!
32
When are TNF antagonists indicated?
- moderate to severe rheumatoid arthritis, given after traditional DMARDs have proven to be ineffective - often used in combination with methotrexate
33
What RA drug class poses a serious risk of developing serious infections and severe allergic reactions?
TNF antagonists! - bacterial sepsis, invasive fungal infections, hep B, TB -
34
What is Etanercept?
TNF inhibitor that is a fusion protein administered once or twice weekly subQ
35
What is Infliximab?
chimeric mAB against TNF that is administered intravenously every 6 weeks
36
What is Adalimumab?
recombinant fully human anti-TNF mAb administer subQ every 2 weeks
37
What is rituximab?
RA tx that targets CD20 on B lymphocytes
38
What RA tx causes profound B cell lymphocytopenia but maintains Ig Levels?
Rituximab- targets CD20 that isn't found on plasma cells so Ig is good
39
What will indicate a greater likelihood of responsiveness for Rituximab?
positive test for rheumatoid factor or anti-cyclic citrullinated peptide predicts greater responsiveness
40
How is rituximab administered?
by IV every 6 months
41
What can cause infusion related hypersensitivity?
Rituximab - also can cause SJS, Hep B reactivation, and PML
42
What drug for moderate to severe rheumatoid arthritis prevents CD28 from binding to counter- receptor CD80/CD86?
Abatacept hey bata bata bata 'cept you! fusion protein compromising CTLA-4 and Fc portion of IgG1 -used after TNG antagonist have failed and can be used in combo with non biological DMARDs
43
What does tocilizumab do?
Humanized anti human IL-6 receptor Ab - competes for membrane bound and soluble forms of human IL-6 receptor
44
What drug blocks IL-6 binding to its receptor and prevents JAK3 kinase signaling and also limits hepatic acute phase response activation of T cells, B cells, macrophages and osteoclasts
Tocilizumab That 'cili' JAK!!!
45
What RA drug can cause URI, and make the patient susceptible to life threatening reactions?
Tocilizumab?
46
What is tofacitinib?
JAK 3 antagonist - directly surpasses the production of IL-17 and IFN-gamma, and proliferation of IL17 cells
47
How is tofacitinib administered?
orally- unusual for DMARDS
48
What are warnings of tofacitinib?
Increased risk of malignancies and serious infections
49
What RA drug is a recombinant non-glycosylated version of human IL-1 receptor antagonist?
Anakinra
50
What does anakinra do?
Blocks the pro inflammatory activity of naturally occurring IL-1 on many cells including synovitis and cartilage degradation - use when no good rheumatoid arthritis response to non-biologic DMARS, considered less efficacious
51
What are toxicities of anakinra?
- increased risk of infection | - Hypersensitivity Rxn
52
What are the misc. drugs for pain and inflammation in RA?
1. NSAIDs 2. Acetaminophen 3. Glucocorticoids Treat the NAGging pain
53
``` Methotrexate hydroxychoroquine sulfasalazine leflunomide are what type of rheumatoid arthritis drugs? ```
Traditional non biologic disease modifying anti rheumatoid drugs (DMARDS)
54
Etanercept adalimumab infliximab are what type of RA drugs?
Biologic DMARDs- TNF alpha blockers
55
Rituxumab is what type of RA drug?
Biologic DMARD- B cell depletes (CD20 mAb)
56
Abatacept is what kind of RA drug?
Biological DMARD- T cell activation inhibitor
57
Tocilizumab is what kind of RA drug?
Biological DMARD IL-6 receptor mAb
58
What RA drug is Tofacitinib?
Biological DMARD: Jak-3 inhibitor
59
What kind of drug is anakinra?
Biological DMARD: Recombinant IL-1 antagonist

NMSP (14 decks)

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