DMARDs Flashcards

1
Q

Non-biological DMARDs

A

methotrexate, hydroxychloroquine, leflunomide, sulfasalazine

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2
Q

Methotrexate

A

Inhibits AICAR transformylase (catalyzes the last step in synthesis of inosine monophosphate). AICA riboside accumulates → inhibits adenosine deaminase → ↑ circulating adenosine → inhibition of lymphocyte proliferation, ↓ secretion of IL-1, IFN-gamma, TNF, ↑ secretion of IL-4, ↓ release of histamine, ↓ neutrophil chemotaxis

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3
Q

Side effects of methotrexate

A

Bone marrow suppression (do not use with HIV) & anemia.
Interstitial pneumonitis (can be fatal) & pulmonary fibrosis
Category X.
↑ risk of malignant lymphomas
Fatal derm rxns
GI toxicity, esp with NSAIDS and PUD/UC
↑ LFTs

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4
Q

Monitoring for methotrexate

A

CBC w/diff
LFTs
serum Cr/BUN
serum uric acid

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5
Q

Sulfasalazine

A

Metabolized to sulfapyridine & mesalamine by bacteria in colon.
Inhibits PG & LT production → anti-inflammatory

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6
Q

Side effects of sulfasalazine

A

↑ serum levels in poor acetylators
Contraindicated with hypersensitivity to salicylates or sulfonamide drugs
Rarely, fatal blood dyscrasias

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7
Q

Monitoring for sulfasalazine

A

CBC w/diff
LFTs
serum Cr/BUN
urinalysis

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8
Q

Leflunomide

A

Inhibits DHODH → enzyme in mitochondria that is important in pyrimidine synthesis. Arrests cell cycle in T and B cells and ↓ IG production

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9
Q

Side effects of Leflunomide

A

↑ uric acid excretion

Category X

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10
Q

Contraindications to leflunomide

A

Severe immunodeficiency, bone marrow dysplasia, uncontrolled infxn, pregnancy

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11
Q

Monitoring for leflunomide

A

CBC w/diff
LFTs
pregnancy
serum electrolytes

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12
Q

Hydroxychloroquine

A

↓ presentation of antigenic peptides on MCH class II molecules that stimulate CD4 T-cells

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13
Q

Side effects of hydroxychloroquine

A

Liver toxicity with hepatic disease or alcoholism
Blood dyscrasias
Contraindicated in ocular disease
CNS toxicity: polyneuritis, ototoxicity, seizures, neuromyopathy

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14
Q

Monitoring for hydroxychloroquine

A

CBCs

Ophthalmalogic exam

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15
Q

Abatacept

A

CTLA4/IgG Fc fusion protein

Binds CD80 & CD86 to prevent T-cell co-stimulatory signal from engaging with CD28/B7 on APCs.

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16
Q

Adalimumab

A

TNF-alpha monoclonal Ab

Prevents TNF-alpha from binding to p55 & p75 cell receptors

17
Q

Anakinra

A

IL-1 receptor antagonist

Competitively inhibits IL-1 binding to receptor

18
Q

Certolizumab pegol

A

Fab fragment of TNF-alpha Ab → neutralizes membrane-bound & soluble TNF-alpha

19
Q

Etancercept

A

Fusion protein of TNF receptor & IgG Fc

Inactivates TNF

20
Q

Golimumab

A

TNF-alpha Ab

Neutralizes soluble & membrane-bound TNF-alpha

21
Q

Infliximab

A

Mouse-human TNF-alpha MAb

Neutralizes soluble & membrane-bound TNF-alpha

22
Q

Rituximab

A

Mouse-human CD20 B-cell receptor MAb

Binds to membrane-bound CD20 receptor & causes immune cells to lyse B-cells

23
Q

Tocilizumab

A

IL-6 MAb

Inhibits signaling of IL-6 receptors. ↓ activation of TH17 cells & mø.

24
Q

Side effects of biological DMARDs

A

Immunosuppression → no live vaccines, don’t give to pts with active infections, careful with asthmatics & COPD
↑ risk of malignancies → esp the TNF-alpha inhibitors

25
Q

Biologics causing CHF or hypotension/angina/dysrhythmias

A

Adalimumab, Golimumab, Infliximab, Rituximab

26
Q

Biologics causing blood dyscrasias

A

Anakinra, certolizumab, rituximab, tocilimumab

Do routine CBCs

27
Q

Biologics causing a lupus-like syndrome

A

Adalimumab, certolizumab, entanercept, infliximab

28
Q

Biologics causing SJS or TEN

A

rituximab

29
Q

Complication with Abatacept IV

A

Contains maltose - may affect blood glucose tests

30
Q

Pregnancy tests recommended for which biologics

A

rituximab (IgG crosses placenta)

31
Q

LFTs recommended for which biologics

A

golimumab, infliximab, tocilimumab (also serum lipids)