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Rheum Pharm > DMARDs > Flashcards

DMARDs Flashcards

1
Q

What do DMARDs have the ability to do?

A

Improve inflammatory symptoms and slow progression of joint erosion

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2
Q

What are the non-biological DMARDs?

A

They are the cornerstone of RA tx; MTX, Sulfasalazine, Leflunomide, Hydroxychloroquine

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3
Q

What is the MOA of MTX?

A

Immunosuppression by inhibition of AICAR transformylase; this means AICAR doesnt => FAICAR, increased AICAR blocks adenosine deaminase; increased Adenosine inhibits IL-1, TNF-a, IFN-g, lymphocyte proliferation, neutrophil chemotaxis, and histamine release

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4
Q

What is the metabolism/excretion of MTX?

A

MTX gets polyglutamated, which increases intracellular retention. Hepatic metabolism and enterohepatic recirculation (longer halflife); renal elimination

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5
Q

What are the ADEs of MTX?

A

Immunosup; blood dyscrasia; infxn; bleeding; contra-HIV and vaccination; pulm fib; CAT-X; malignant lymph; skin rxn; GI fox in pts with ulcerative colitis (esp w/ NSAID)

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6
Q

What do you monitor for in MTX?

A

CBC, LFT, Creatinine/BUM, Serum Uric Acid, Pregnancy tests

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7
Q

When is sulfasalazine used for?

A

For when NSAIDs provide inadequate response

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8
Q

What is the MOA of sulfasalazine

A

Metabolised into sulfapyridine and mesalamine by colonic bacteria = Mesalamine is anti-inf that inhibits PG and LT

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9
Q

What happens to sulfapyridine?

A

Acetylated in liver therefor slow acetylators can be affected

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10
Q

What is the elimination of sulfasalazine?

A

Renal

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11
Q

What are the ADEs of sulfasalazine?

A

Contra-hypersens to salicylates or sulfonamides, Fatal blood dyscrasias

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12
Q

What do you monitor for sulfasalazine?

A

CBC, LFT, Creatnine/BUM, Urinalysis

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13
Q

What is the MOA of Leflunomide?

A

Metabolized into A77 1726; this inhibits dihydroorotate dehydrogenase (DHODH) in mitochondria and catalyzes pyrimidine synthesis; This causes T/B cell cycle arrest; no Ig is made; Cytostatic at clinical dosing

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14
Q

What is the met/elim of Leflunomide?

A

Met into A77 1726 by CYPs and eliminated in feces

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15
Q

What are the ADE’s of Leflunomide?

A

Hepatitis (CYPs), contra-alcohol, immunodef, bone marrow dysplasia, infxn, CAT-X

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16
Q

What do you monitor with Leflunomide?

A

CBCs, LFTs, Pregnancy, Serum electrolytes

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17
Q

What is hydroxychlorquine prophylactially given for?

A

Malaria

18
Q

What is the MOA of hydrocychloroquine?

A

Increase intracellular vaculor pH and alters protein degradation by lysosome, macromolecule assemble in endosome, and proetin mod in golgi; MHC not assembled = down regulation in immune response to foreign and self antigens

19
Q

What is the met/elim of hydroxychloroquine?

A

Partial hepatic metabolism and then sow and extensive renal elim

20
Q

What are the ADEs of Hydroxychloroquine?

A

CNS tox (neuropathy, oto-, seizures), hepatits, blood dyscrasias; Contra-ocular dz

21
Q

What do you monitor with Hydroxychloroquine?

A

CBC and Opthalmic exams

22
Q

What are the biologic agents used for in treatment of RA dz?

A

Targeted Treatment; Adalimumab, Etanercept, Infliximab, Golimumab, Certolizumab pegol, Abatecept, Rituximab, Anakinra, Tocilizumab

23
Q

What are the ADEs/worries of ALL of the biologic agents used for the treatment of RA?

A

All cause immunosuppression, do not give any with an active infection, they increase infxn (especially respiratory in COPD/asthma), worry about Hep B/TB reactivation, NO live vaccines

24
Q

What is a specific ADE for all of the TNF-a blockers?

A

increase in malignancies

25
Q

What is the MOA of adalimumab?

A

TNF-a mAb, blocks interaction with p55 and p75

26
Q

What are the specific ADE’s for adalimumab?

A

CHF or hypotension/angina/dysrhythmia, a lupus like syndrome, and advice patient about save SC injection practice

27
Q

What is the MOA for etanercept?

A

TNF-a receptor-Ab fusion protein, p75 bound to IgG1 (inactivates TNF but does not affect production or serum levels)

28
Q

What are the specific ADE’s for etanercept?

A

Lupus like syndrome, advise patient about safe SC injection

29
Q

What is the MOA for Infliximab?

A

TNF-a Chimeric (mouse) maB (IgG-1k), binds soluble and transmembrane TNF-a and neutralzies

30
Q

What are the specific ADE’s for infliximab?

A

CHF/hypotension/angina/dysrhythmia, Lupus like syndrome and perform LFTs

31
Q

What is the MOA of Golimumab?

A

Human derived TNF-a antibody that binds soluble and transmembrane TNF-a and neutralizes

32
Q

What are the specific ADE’s for Golimumab?

A

CHF/hypotension/angina/dysrhythmia, LFTs, Advise about safe SC injection

33
Q

What is the MOA of Certolizumab pegol?

A

Fab fragment of humanized TNF-a that binds soluble and membrane bound TNF-a and neutralizes

34
Q

What are the specific ADE’s for Certolizumab pegol?

A

Blood dyscrasias, lupus like syndrome, advise about safe SC injection

35
Q

What is the MOA of abatacept?

A

CTLA4/IgG1 fusion protein that binds CD80 and CD86 which blocks CD28 from activating T-cells

36
Q

What are the specific ADE’s of abatacept?

A

Contains maltose which can mess with blood glucose test, advise about safe SC injection

37
Q

What is the MOA of Rituximab?

A

Chimeric (mouse-human) CD20/IgG1k mAb against B-lymphocyte CD20 receptor which will lyse B-cells, also sensitizes drug resistant human B-cell lymphoma cell lines to cytotoxic chemotherapy

38
Q

What are the specific ADE’s of Rituximab?

A

CHF/hypotension/angina/dysrhythmia, Blood dyscrasia, toxic epidermal necrolysis/SJS, Contraindicated in pregnancy

39
Q

What is the MOA of Anakinra?

A

IL1 receptor antagonist which inhibits IL1alpha and beta from binding to IL-1R1; decrease inflammatory response

40
Q

What are the specific ADE’s of Anakinra?

A

Blood dyscrasia, advise patient about safe SC injection

41
Q

What is the MOA of Tocilizumab?

A

IL-6 receptor inhibiting mAb that binds to soluble and membrane bound IL-6 receptors and inhibits signaling which decreases immune response regulator production

42
Q

What are the specific ADE’s of Tocilizumab?

A

Blood dyscrasia, LFTs (serum lipids too)

Rheum Pharm (9 decks)

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