E2: DMARDs Flashcards

1
Q

What are the toxicites of Gold salts?

A

Bone marrow damage, dermatitis, enterocolitis, jaundice, and peripheral neuropathy

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2
Q

What are the mediators of chronic inflammation?

A
  • Interleukins 1, 2, and 3
  • GM-CSF
  • TNF-a
  • interferons
  • PDGF
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3
Q

What are the effects of Gold salts?

A
  • Inhibitions of phagocytosis, uncouple oxidative phosphorylation and inhibit cellular respiration
  • prevent PG synthesis
  • suppress cellular immunity
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4
Q

What kind of drug is Aurothioglucose?

A

A Gold salt

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5
Q

What kind of drug is Penicillamine?

A

A cheating agent effective in RA and Wilson’s disease

-unknown mechanisms but similar to gold compounds

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6
Q

What are the adverse effects of Penicillamine?

A
  • Pruritis, rash, and alternation in taste
  • Thrombocytopenia, leukopenia, agranulocytosis
  • proteinuria, nephrotic syndrome
  • Lupus like Disease, pemphigus
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7
Q

What are the effects of Hydroxychloroquine?

A
  • Possess antihistamine, anticholinesterase, and antiprotease properties
  • inhibits PG synthesis
  • Inhibits biosynthesis of mucopolysaccharide
  • Inhibits response to chemotactic stimuli and phagocytosis
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8
Q

When does hydroxychloroquine concentrate in the body and why?

A

It has a high affinity for melanin so it is concentrated in the epidermis and retina

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9
Q

What are the toxicites associated with hydroxychloroquine?

A

Pruritis, hemolysis, ototoxicity, retinopathy, and peripheral neuropathy

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10
Q

What are the uses of sulfasalazine?

A
  • Used to treat RA

- just as effective as gold compounds and Penicillamine but with less side effects

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11
Q

Why does mesalamine have anti-inflammatory action?

A
  • inhibition of arachidonic acid metabolism by inhibition of Cyclooxygenase
  • inhibits leukotriene synthesis, possibly through inhibition of lipoxygenase
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12
Q

What are the toxicites of sulfasalazine?

A
  • GI disturbance, rash
  • Hepatitis and blood dyscrasias are rare
  • Monitoring for hepatitis and marrow suppression is recommended for 2-3 weeks during the first 3 months of treatment
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13
Q

What are the 5 anti TNFa drugs?

A
  • Infliximab
  • adalimumab
  • certolizumab
  • golimumab
  • etanercept
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14
Q

What are the two inhibitors of B cell differentiation and T cell activation?

A
  • Rituximab

- Abatacept

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15
Q

What are the 2 interleukin receptor antagonists?

A
  • Anakinra

- Tocilizumab

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16
Q

What is the MOA of Infliximab?

A
  • Chimeric IgG1k monoclonal antibody targeted against TNFa

- composed of human constant and murine variable regions

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17
Q

What is Infliximab used to treat and what drug is it often combined with?

A

-Combined with methotrexate to treat Crohns and RA

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18
Q

What are the contraindications of Infliximab?

A

Pregnancy, breast feeding, children, and infections

19
Q

What is the MOA of Adalimumab?

A
  • Recombinant human IgG1 monoclonal antibody
  • Has human derived heavy and light chain variable regions and human IgG1k constant reactions (100% human peptide sequences)
  • Specific for TNFa
20
Q

What are the uses of Adalimumab?

A

Approved as Monotherapy for treatment of RA

21
Q

What are the most common adverse effects of adalimumab?

A

-Influenza like symptoms, fatigue, headache, pruritis, and nausea/vomiting

22
Q

What is the MOA of Certrolizumab?

A
  • Humanized antibody that is a potent neutralizer of the TNFa
  • adverse effects similar to other TNFa binders
23
Q

What is the MOA of Golimumab?

A
  • Human derived monoclonal antibody with human derived variable and constant regions TNFa
  • Adverse effects similar to other TNFa binders
24
Q

What is the MOA of Etanercept?

A

-Dimeric fusion protein produced by recombinant produced by recombinant DNA technology, this protein consistent of extracellular ligand binding portion of the human 75 kilo dalton TNF receptor linked to the FC portion of the human IgG1

25
Q

What are the contraindications to Etanercept?

A

Bone marrow suppresion, breast feeding, children, DM, infection, sepsis, vaccination, varicella

26
Q

What is the MOA of Ritubximab?

A
  • A genetically engineered chimeric murine/human monoclonal antibody
  • Binds specifically to CD20, a B-lymphocyte differentiation antigen on. Pre-B and mature B lymphocytes
27
Q

What is the MOA of Abatacept?

A
  • Fully recombinant fusion protein categorized as a costimulatory or second signal blockers for T cell activation
  • Disturbs a key mechanism of inflammation and progressive ointment destruction in RA
28
Q

How is etanercept administered?

A

SubQ

29
Q

How are rituximab and abacept administed?

A

IV

30
Q

What are the two inhibitors

A

Leflunomide and Mycophenolate mofetil

31
Q

What is the MOA of Leflunomide?

A

Inhibits dihydroorotate dehydrogenase (DHODH), an enzyme located in cell mitochondria that catalyzes a key step in de novo pyrimidine

  • Secondary mechanism of action is inhibitionof cytokines and growth factor receptor associated with TK activity
  • Inhibits the induction of COX2
32
Q

What are the contraindications of Leflunomide?

A

Pregnancy, breast feeding, hepatic and renal failure

33
Q

What is the MOA of Mycophenolate Mofetil?

A

-a prodrug that inhibits lymphocyte purine synthesis by reversible and non competitively inhibiting the enzyme inosine monophosphate dehydrogenase

34
Q

What are the contraindications to Mycophenolate mofetil?

A

Active GI disease, diarrhea, pregnant, breast feeding, infections

35
Q

What is the MOA of anakinra?

A

-Recombinant non glycosylated form of the human interleukin-1 receptor antagonist

36
Q

What is the use of Anakinra?

A

RA patients experienced improvements of swollen and painful joints
-Given SubQ

37
Q

What are the contraindications to Anakinra?

A

Breast feeding, children, hypersensitivity reactions, renal disease

38
Q

What is the MOA of tocilizumab?

A
  • Humanized interleukin-6 receptor inhibiting monoclonal antibody
  • competes for IL-6 for binding to the IL-6 receptor
39
Q

What are the two Janus Kinase inhibitors?

A

Tofacitinib and Baricitinib

40
Q

What is the MOA of Tofacitinib?

A

-Primarily inhibits JAK1 and JAK3 and to a lesser extent, JAK2

41
Q

What is the use of Tafcitinib?

A

-For adults with moderately to severely active RA who have had an inadequate response or intolerance to methotrexate

42
Q

What is the MOA of Baricitinib?

A

-Oral JAK inhibitor, has greater affinity for JAK1 and JAK2 relative to JAK3

43
Q

What is the used of Baricitinib?

A
  • Indicated for the treatment of adult patients with moderately to severely active RA
  • may be used as monotherapy or in combination with methotrexate or other non-biologic DMARDs