Drugs for Rheumatoid Arthritis

Question 1

anakinra

Answer 1

IL-1 receptor blocker

Question 2

how are adalimumab and etanercept different in mech?

Answer 2

• etanercept binds only soluble TNF-alpha
• adalimumab binds both soluble and transmembrane

Question 2

methotrexate

Answer 2

-DHFR inhibitor, inhibits folate dependent steps in purine synthesis to inhibit DNA synthesis

Question 3

etanercept

• mech
• therapeutic use
• adverse effects (3)

Answer 3

‘intercept TNF alpha’

• binds to soluble TNF-alpha
• used for RA
• side effects:
  1. injection site reactions
  2. increased risk of infections
  3. lymphoma in children

Question 4

tofacitinib

• mech
• use
• side effects –2

Answer 4

• JAK inhibitor
• used in active RA pts who had inadequate repsonse from methotrexate

adverse effects:

1. increase infection risk
2. increase in cholesterol

Question 5

Infliximab

Answer 5

TNF alpha inhibitor

Question 6

tocilizumab

• mech
• therapeutic use
• side effects (2)

Answer 6

• IL-6 receptor blocker. (both soluble and transmembrane)
• used for adult RA with poor response to TNF anatgonists

side effects:

1. injection site reactions
2. increase infection risk

Question 7

adalimumab

• mech
• therapeutic use
• adverse effects–3

Answer 7

• IgG that binds TNF-alpha (both soluble and transmembrane)
• active RA, juvenile idiopathic arthritis
• side effects:
  1. injection site reactions
  2. increased risk of infections
  3. lymphoma in children

Question 8

azathioprine

Answer 8

• prodrug to 6-MP
• purine antimetabolite to inhibit DNA synthesis

Question 9

DMARDs

Answer 9

disease-modifying anti-rheumatic drugs

-protein drugs that target cytokines and cell surface molecules

Question 10

abatacept

Answer 10

• inhibits T-cell activation by blocking the CD28/B7 costimulation of APCs on T cells.
• abatecept (which has CTLA-4) competes with B7 to bind CD28. This induces anergy.

Question 11

hydroxychloroquine

Answer 11

• mech not understood
• useful as oral tx for early RA
• long term toxicity: irreversible retinal damage

Question 12

leflunomide

Answer 12

-inhibits dihydroorotate DH (DHODH), an enzyme that produces UMP

Question 14

what drugs require the pt to be screened for latent TB infection and monitored while taking it? why?

Answer 14

• etanercept, adalimumab, infliximab
• as TNF-alpha inhibitor, the inflammatory response is reduced. This could allow a latent TB infection to relapse

Question 15

rituximab

Answer 15

-Ab against CD20 antigen of B-cells, inducing complement and destroying them