2- DMARDs

Question 1

What is the MOA for gold salts?

Answer 1

Inhibit phagocytosis, prevent PG synthesis

Question 2

What is the use for gold salts?

Answer 2

Supress cellular immunity

Question 3

What are the SEs of gold salts?

Answer 3

BM damage, enterocolitis

Question 4

What is the caution with use of Penicillamine?

Answer 4

HIGH incidence of SEs

(hematologic, renal, AI, ↑ risk > 65 yo)

Question 5

What is the use for Penicillamine?

Answer 5

Wilson’s disease, RA

Question 6

What type of properties does Hydroxychloroquine (Plaquenil) have?

Answer 6

Antihistaminic, anticholinesterase, antiprotease

(inhibits PG synthesis, stabilize lysosomes)

Question 7

What are the SEs for Hydroxychloroquine (Plaquenil)?

Answer 7

Hemolysis (G6PD def), ototoxicity

Question 8

What is the use for Sulfasalazine?

Answer 8

RA, better tolerated and less toxic

(but still not well tolerated)

Question 9

What are general contraindications to use of DMARD agents?

Answer 9

Breastfeeding, children, renal disease +/- infections

Question 10

What mediators of chronic inflammation are specifically identifed as DMARDs? (4)

Answer 10

Gold salts, Penicillamine, Hydroxychloroquine (Plaquenil), Sulfasalazine

Question 11

What mediators of chronic inflammation are identifed as agents acting on TNF-alpha? (5)

Answer 11

Infliximab (Remicade)

Adalimumab (Humira)

Certolizumab Pegol (Cimiza)

Golimumab (Simponi)

Etanercept (Enbrel)

Question 12

Which drug is a chimeric IgG1k monoclonal Ab targeting TNFa and is combined with Methotrexate?

Answer 12

Infliximab (Remicade)

Question 13

What is the use for Infliximab (Remicade)?

(TNF-alpha agent)

Answer 13

RA, Crohn’s Disease

(given IV)

Question 14

Which drug is a 100% HUMAN IgG1 monoclonal Ab targeting TNF-alpha?

Answer 14

Adalimumab (Humira)

(given subcutaneously)

Question 15

What is the use for Adalimumab (Humira)?

Answer 15

RA (monotherapy)

Question 16

Which drugs are humanized Abs targeting TNF-alpha?

Answer 16

Certolizumab Pegol (Cimiza)

Golimumab (Simponi)

Question 17

What drug is considered a “fake TNFa receptor” and is a dimeric fusion protein?

Answer 17

Etanercept (Enbrel)

(given subcutaneously)

Question 18

What are the contraindications to Etanercept (Enbrel)?

Answer 18

BM suppression, breastfeeding, children, DM, infection/ sepsis, live vaccines, current varicella infection

Question 19

What are the SEs of Infliximab (Remicade)?

Answer 19

HA, infusion reactions

Question 20

What are the SEs of Adalimumab (Humira)?

Answer 20

Rash, flu-like sxs, fatigue, HA

Question 21

What is a SE of Etanercept (Enbrel) aside from injection site rxn and infections?

Answer 21

Increased incidence of antibody formation

Question 22

What mediators of chronic inflammation are inhibitors of beta-cell differentiation and T-cell activation?

Answer 22

Rituximab

Abatacept

Question 23

What mediators of chronic inflammation are inhibitors of nucleic acid synthesis?

Answer 23

Leflunomide

Micophenolate Mofetil

Question 24

What mediators of chronic inflammation are interleukin receptor antagonists?

Answer 24

Anakinra

Tocilizumab

Question 25

What mediators of chronic inflammation are JAK inhibitors?

Answer 25

Tofacitinib Baricitinib

Question 26

What drug is a genetically engineered chimeric antibody, specifically **binds CD20** and is a B-lymphocyte differentiation antigen on **B cells**?

Answer 26

Rituximab (Rituxan) (given IV)

Question 27

What is the use for Rituximab (Rituxan)?

Answer 27

RA, relapsed/ refractory B-cell Non-Hodgkin Lymphoma (NHL)

Question 28

What drug is a **fully human** recombinant fusion protein that blocks **T cell** activation to disturb key mechanisms of inflammation and progressive joint destruction?

Answer 28

Abatacept (Orencia) (given IV, long half life)

Question 29

What is the use for Abatacept (Orencia)?

Answer 29

RA

Question 30

What drug **inhibits DHODH** and **inhibits induction of COX-2**?

Answer 30

Leflunomide (Arava) (oral admin, long half life)

Question 31

What are the SEs of Leflunomide (Arava)?

Answer 31

GI, immune suppression

Question 32

What are the contraindications of Leflunomide (Arava)?

Answer 32

Pregnancy, breastfeeding, hepatic failure, renal failure

Question 33

What drug inhibits lymphocyte purine synthesis and is a prodrug for the immunosuppressive agent MPA?

Answer 33

Mycophenolate Mofetil (Cellcept) (given oral or IV)

Question 34

Whare are the SEs of Mycophenolate Mofetil (Cellcept)?

Answer 34

Diarrhea, vomiting, GI bleeding

Question 35

What are the contraindications to Mycophenolate Mofetil (Cellcept)?

Answer 35

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

Question 36

What is the use for Mycophenolate Mofetil (Cellcept)?

Answer 36

RA, esp if resistant to Methotrexate

Question 37

What drug is a **human interleukin-1 receptor antagonist** (IL-1Ra) and takes 4-13 weeks to have an effect?

Answer 37

Anakinra (Kineret) (given subcutaneoulsy, eliminated renally)

Question 38

What is the use for Anakinra (Kineret)?

Answer 38

RA- improve swollen/ painful joints

Question 39

What drug is **human interleukin-6 receptor antagonist** (IL-6)?

Answer 39

Tocilizumab (Actemra)

Question 40

What drug **inhibits JAK1 and JAK 3** and is used in pts with mod-sev active RA who are intolerant to or have not had an adequate response to methotrexate?

Answer 40

Tofacitinib (Xeljanz) (given orally)

Question 41

What are the SEs of Tofacitinib (Xeljanz)?

Answer 41

Serious infections/ malignancy

Question 42

What drug inhibits **JAK1 and JAK2** and is used for the tx of mod-sev RA?

Answer 42

Baricitinib (Olumiant) (mono or combo therapy)

Question 43

What are the SEs of Baricitinib (Olumiant)?

Answer 43

Serious infection/ malignancy, thrombosis