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
Q

Can sulfasalazine be used in pregnancy?

A

seems okay but less studied

26
Q

What is the most common reason sulfasalazine is discontinued?

A

GI side effects- N/V, diarrhea, abdominal pain

27
Q

What drug can cause pruritus, rash and urticaria?

A

Sulfasalazine- sulfa drug run!

@Lauren

28
Q

What RA drug inhibits mitochondrial enzyme dihydroorotate dehydrogenase to block the synthesis of rUMP?

A

Lefunomide

29
Q

What are the effects of leflunomide?

A

inhibition of T cell proliferation

  • also blocks leukocyte adhesion and NF-kB activation
30
Q

What drug is a second choice that would be used alternatively to methotrexate?

A

Leflunomide

  • can also be used in combo with methotrexate, sulfasalazine or hydroxyquine
31
Q

What biologic DMARDs can be combined?

A

NONE!

32
Q

When are TNF antagonists indicated?

A
  • moderate to severe rheumatoid arthritis, given after traditional DMARDs have proven to be ineffective
  • often used in combination with methotrexate
33
Q

What RA drug class poses a serious risk of developing serious infections and severe allergic reactions?

A

TNF antagonists!

  • bacterial sepsis, invasive fungal infections, hep B, TB

-

34
Q

What is Etanercept?

A

TNF inhibitor that is a fusion protein administered once or twice weekly subQ

35
Q

What is Infliximab?

A

chimeric mAB against TNF that is administered intravenously every 6 weeks

36
Q

What is Adalimumab?

A

recombinant fully human anti-TNF mAb administer subQ every 2 weeks

37
Q

What is rituximab?

A

RA tx that targets CD20 on B lymphocytes

38
Q

What RA tx causes profound B cell lymphocytopenia but maintains Ig Levels?

A

Rituximab- targets CD20 that isn’t found on plasma cells so Ig is good

39
Q

What will indicate a greater likelihood of responsiveness for Rituximab?

A

positive test for rheumatoid factor or anti-cyclic citrullinated peptide predicts greater responsiveness

40
Q

How is rituximab administered?

A

by IV every 6 months

41
Q

What can cause infusion related hypersensitivity?

A

Rituximab

  • also can cause SJS, Hep B reactivation, and PML
42
Q

What drug for moderate to severe rheumatoid arthritis prevents CD28 from binding to counter- receptor CD80/CD86?

A

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
Q

What does tocilizumab do?

A

Humanized anti human IL-6 receptor Ab

  • competes for membrane bound and soluble forms of human IL-6 receptor
44
Q

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

A

Tocilizumab

That ‘cili’ JAK!!!

45
Q

What RA drug can cause URI, and make the patient susceptible to life threatening reactions?

A

Tocilizumab?

46
Q

What is tofacitinib?

A

JAK 3 antagonist

  • directly surpasses the production of IL-17 and IFN-gamma, and proliferation of IL17 cells
47
Q

How is tofacitinib administered?

A

orally- unusual for DMARDS

48
Q

What are warnings of tofacitinib?

A

Increased risk of malignancies and serious infections

49
Q

What RA drug is a recombinant non-glycosylated version of human IL-1 receptor antagonist?

A

Anakinra

50
Q

What does anakinra do?

A

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
Q

What are toxicities of anakinra?

A
  • increased risk of infection

- Hypersensitivity Rxn

52
Q

What are the misc. drugs for pain and inflammation in RA?

A
  1. NSAIDs
  2. Acetaminophen
  3. Glucocorticoids

Treat the NAGging pain

53
Q
Methotrexate 
hydroxychoroquine
sulfasalazine
leflunomide 
are what type of rheumatoid arthritis drugs?
A

Traditional non biologic disease modifying anti rheumatoid drugs (DMARDS)

54
Q

Etanercept
adalimumab
infliximab

are what type of RA drugs?

A

Biologic DMARDs- TNF alpha blockers

55
Q

Rituxumab is what type of RA drug?

A

Biologic DMARD- B cell depletes (CD20 mAb)

56
Q

Abatacept is what kind of RA drug?

A

Biological DMARD- T cell activation inhibitor

57
Q

Tocilizumab is what kind of RA drug?

A

Biological DMARD IL-6 receptor mAb

58
Q

What RA drug is Tofacitinib?

A

Biological DMARD: Jak-3 inhibitor

59
Q

What kind of drug is anakinra?

A

Biological DMARD: Recombinant IL-1 antagonist