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Pharmacology > Rheumatoid Arthritis & Gout > Flashcards

Rheumatoid Arthritis & Gout Flashcards

1
Q

Indomethacin class?

A

Non-selective NSAID (eliminate pain, reduce inflammation)

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2
Q

Indomethacin for?

A

RA, gout

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3
Q

Indomethacin side effetcs?

A

Gastric and duodenal ulcers

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4
Q

Naproxen class?

A

Non-selective NSAID (eliminate pain, reduce inflammation)

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5
Q

Naproxen for?

A

RA, gout

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6
Q

Naproxen side effects?

A

Gastric and duodenal ulcers

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7
Q

COX-2 inhibitor class?

A

Selective NSAID (eliminate pain, reduce inflammation)

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8
Q

COX-2 inhibitors are____conventional NSAIDs for RA?

A

Superseding

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9
Q

COX-2 inhibitor side effects?

A

Gastric and duodenal ulcers, but 50% less than traditional NSAIDs

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10
Q

Quinolines class?

A

DMARDs (antimalarials)

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11
Q

Quinoline mxn?

A

Reduce T-cell activation & chemotaxis

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12
Q

Quinoline for?

A

RA & SLE, for patients who no longer respond to NSAIDs or cannot tolerate other DMARDs

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13
Q

Glucocorticoids (Corticosteroids) class & mxn?

A

DMARDs; Inhibit Phospholipase A2 (inhibit release of arachidonic acid and formation of prostaglandins) + Inhibit cytokine production and prevent induction of COX-2

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14
Q

Glucocorticoids for?

A

RA, Acute Gouty Arthritis

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15
Q

Glucocorticoid side effects?

A

Cushingoid symptoms

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16
Q

Glucocorticoid timing?

A

Fast acting

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17
Q

Sulfasalazine class and mxn?

A

DMARD; likely inhibition of IL-1 and TNF-a release

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18
Q

Sulfasalazine for?

A

RA

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19
Q

Sulfasalazine side effects?

A

N/V, HAs, Skin rashes, neutropenia, 30% discontinue drug

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20
Q

Sulfasalazine timing?

A

Fast acting

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21
Q

Methotrexate class and mxn?

A

DMARD (immunosuppressive). Inhibits aminoimidazolecarboxamide transformylase (AICAR) and thimidylate sunthase, with secondary effects on PMN chemotaxis; Causes adenosine accumulation which inhibits inflammation

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22
Q

Methotrexate for?

A

RA

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23
Q

Methotrexate side effects?

A

Nausea, stomatitis, hepatotoxicity (rare)

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24
Q

Methotrexate timing?

A

Takes several to start working

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25
Q

Leflunomide class and mxn?

A

DMARD (immunosuppressive). Inhibits dihydroorotate dehydrogenase (DHODH) (RLenzyme in de novo pyrimidine synthesis). T-lymphocyte response to stimuli.

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26
Q

Leflunomide for?

A

RA

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27
Q

Leflunomide side effects?

A

Diarrhea, hepatotoxicity (slightly more toxic than MTX)

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28
Q

Leflunomide timing?

A

Takes several weeks to start working

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29
Q

Leflunomide a prodrug?

A

Yes, an oral prodrug

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30
Q

Etanercept class and mxn?

A

BRM, blocks binding of TNF to TNFR (fusion protein of 2 TNF receptors with Fc portion of IgG)

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31
Q

Etanercept for?

A

RA

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32
Q

Etanercept dosing?

A

Twice weekly SubQ inection

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33
Q

Infliximab class and mxn?

A

BRM, blocks binding of TNF to TNFR (chimeric mouse/human IgG)

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34
Q

Infliximab for?

A

RA

35
Q

Infliximab side effect?

A

Antigenic response to murine monoclonal Abs

36
Q

TNF inhibitors?

A

Etanercept, Infliximab, Adalimumab, Golimumab, Certolizumab

37
Q

Adalimumab mxn and class?

A

BRM, blocks binding of TNF to TNFR (fully human IgG)

38
Q

Adalimumab for?

A

RA

39
Q

Adalimumab dosing?

A

2 monthly injections

40
Q

Adalimumab side effects?

A

Fully human so no antigenic response

41
Q

Golimumab mxn and class?

A

BRM, blocks binding of TNF to TNFR

42
Q

Golimumab for?

A

RA

43
Q

Golimumab side effects?

A

Serious infections

44
Q

Certolizumab mxn and class?

A

BRM, blocks binding of TNF to TNFR

45
Q

Certolizumab for?

A

RA

46
Q

Certolizumab side effects?

A

Serious infections

47
Q

Quinolines efficacy and side effects?

A

Low side effects (except retinal damage with chloroquine), but low efficacy

48
Q

Non-selective NSAIDs?

A

Indomethacin, Naproxen

49
Q

Immunosuppressive DMARDs?

A

Methotrexate and Leflunomide

50
Q

DMARD that inhibits IL-1 and TNFa release?

A

Sulfasalazine

51
Q

IL-1 receptor antagonist?

A

Anakinra

52
Q

Anakinra for?

A

RA

53
Q

Anakinra timing?

A

Short (6 hr) half life, daily tx with high doses

54
Q

Il-6 receptor antagonist?

A

Tocilizumab

55
Q

Tocilizumab for?

A

RA

56
Q

Tocilizumab side effects?

A

Serious infections

57
Q

Rituximab class and mxn?

A

BRM, Anti-CD20 Ab, reducing circulating B cells

58
Q

Rituximab for?

A

RA refractory to TNFa inhibitors

59
Q

Rituximab side effects?

A

Infections, hypersensitivity reactions

60
Q

Abatacept mxn and class?

A

BRM, inhibits T-cell activation and induces T-cell apoptosis

61
Q

Abatacept for?

A

RA refractory to MTX or TNFa inhibitors

62
Q

Abatacept side effects?

A

HAs, infections

63
Q

Uricosuric agent?

A

Probenecid

64
Q

Probenecid mxn?

A

Uricosuric agent. Competes with urate at the anionic transport side of the renal tubule and inhibits urate reabsorption.

65
Q

Probenecid for?

A

Chronic tophaceous gout

66
Q

Probenecid side effects?

A

GI irritation, urate crystal mobilization and acute gouty arthritis, secretion of weak acids (penicillin) reduced

67
Q

For acute gouty arthritis?

A

NSAIDs, corticosteroids, colchicine

68
Q

Colchicine for?

A

Acute gouty arthritis

69
Q

Colchicine mxn?

A

Prevents tubulin polymerization and leads to inhibition of leukocyte migration, phagocytosis, and cytokine release

70
Q

Colchicine timing?

A

works in 12-24 hours

71
Q

Colchicine side effects?

A

N/V/D/Ab pain, Long-term use causes peripheral neuropathy and neutropenia, low therapeutic index

72
Q

Allopurinal mxn?

A

Reduce uric acid synthesis by inhibiting xanthine oxidase (competitive inhibitor. It is converted to alloxanthine by XO, which is a non-competitive inhibitor of XO.

73
Q

Allopurinol for?

A

Chronic tophaceous gout

74
Q

Allopurinol side effects?

A

Acute attacks of gouty arthritis early in tx due to mobilization of urate crystals, hypersensitivity, maculopapular rash in 2%

75
Q

Pegloticase is?

A

Recombinant stabilized uricase, converts uric acid to allantoin

76
Q

Pegloticase for?

A

Chronic tophaceous gout

77
Q

Non-purine, non-competitive antagonist of XO?

A

Febuxostat

78
Q

Useful if allopurinol is not tolerable?

A

Febuxostat

79
Q

Febuxostat for?

A

Chronic tophaceous gout

80
Q

Febuxotat side effects?

A

Nausea, rash, arthralgias

81
Q

Febuxostat is expensive?

A

Yes

82
Q

TNF inhibitor conjugated to PEG for stabilization?

A

Certolizumab

83
Q

“Classic” pharmacologic interventions for chronic gout?

A

Allopurinol, probenecid, febuxostat

84
Q

Concerns for febuxostat remain for?

A

Cardiovascular safety

Pharmacology (46 decks)

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