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Flashcards in Drugs for RA Deck (24)
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1

What are the therapeutic goals for treating RA? 

  • Relieve pain
  • Reduce inflammation
  • Slow down or stop joint damage
  • Improve a person's sense of well being and ability to function 

2

Have minimal effect on progression of joint deformity 

Used in large doses for long duration of treatment 

Relieve symptom pain 

NSAIDs

3

What does DMARDs stand for? 

Disease-Modifying Anti-Rheumatics 

4

Inhibits the ability of TNF-a to bind to its receptor

Recombinant fusion protein 

Etanercept 

5

Pharmacokinetics of Etanercept. 

IV or subcut administration

Onset of action 1-2 weeks

Elimination half life > 3 days

6

Adverse effects of Etanercept

Injection site reactions
Increase risk of infections (screen for latent TB before beginning treatment and closely monitored during and after drug therapy) 

Lymphomas in children/adolescent patients 

7

What is etanercept therapeutically used for? 

Moderate to severe RA

Juvenile RA

Early stage

8

IgG monoclonal antibody (human) 

Binds to soluble AND transmembrane forms of TNF-a

Prevents TNF-a binding to its receptor 

Adalimumab 

9

How and how often is Adalimumab administered? 

Subq

Every other week 

10

Adverse effects of Adalimumab

Injection site reactions 

Increased risk of infections 

Lymphomas in children/adolescent patients

11

What are the therapeutic uses of Adalimumab? 

Active RA (moderate to severe); may be used alone or in combination with methotrexate or other DMARDs

Active juvenile idiopathic arthritis (moderate to severe); may be used alone or in combo with methotrexate 

12

How does Infliximab and Adalimumab differ from Etanercept in regards to binding TNF-a? 

Infliximab and Adalimumab can bind to both m-TNF and s-TNF, neutralizing their biologic activity -- may also induce apoptosis of the expressing cells

 

Etanercept also neutralizes s-TNF but does not bind to m-TNF or induce apoptosis of expressing cells 

13

Humanized antibody, binds to soluble and membrane bound IL-6 receptors 

Inhibits IL-6 mediated signaling via these receptors 

Tocilizumab

14

How often is Tocilizumab administered? 

IV every 4 weeks

SubQ every other week 

15

Adverse effects to Tocilizumab

Injection site reactions

Increased risk of infections

Alterations in lipid profile -- increases in total cholesterol, triglycerides, LDL, and/or HDL 

16

What is Tocilizumab therapeutically used for? 

Indicated for adult patients with moderatly to severely active RA who have had an inadequate reponse to one or more TNF antagonists

17

Janus kinase (JAK) inhibitor 

Tofacitinib

18

How is Tofacitinib metabolized? 

Administered orally

Metabolism mediated by CYP3A4 with minor contribution from CYP2C19

19

Adverse effects of Tofacitinib

Increase risk of infections

Increase in cholesterol

20

How is Tofacitinib therapeutically used? 

For treatment of moderately to severely active RA in patients who are unable to take methotrexate

 

May be used as monotherapy or in combo with methotrexate or other DMARDs 

21

Sites of action of drugs: 

1. Abatacept

2. Methotrexate and Leflunomide

3. Etanercept, Infliximab, Adalimumab

4. Anakinra and Tocilizumab

5. Glucocorticoids

 

1. Abatacept blocks co-stim of T cells

2. Methotrexate and Leflunomide inhibits the proliferation and activity of T and B cells

3. Etanercept, Infliximab and Adalimumab inactivate TNF-a 

4. Anakinra blocks the action of IL-1 and Tocilizumab inactivates IL-6

22

Blocks IL-1 Receptor

Anakinra

23

Inhibits T-cell activation

Abatacept

24

Antibody directed against CD20 antigen on B-lymphocytes

Rituximab