DMARDs

Question 1

What are glucocorticoids usually used for in RA

Answer 1

Bridge agent while other DMARDs become effective

Question 2

What is the most popular DMARD

Answer 2

Methotrexate

Question 3

Pharmakokineteics of Methotrexate

Answer 3

Oral, or injection once per week (possible hepatotoxicity)

May take 4-6 weeks to become effective.

Question 4

Methotrexate MOAs (3)

Answer 4

1. “anti-metabolite” to inhibit purine synthesis (folate), side effects
2. Inhibits AICAR transformylase leading to increased adenosine release which is anti-inflammatory
3. Inhibits pyrimidine synthesis which inhibits proliferation of inflammatory cells

Question 5

Major side effect of Methotrexate

Answer 5

Hepatotoxicity

Question 6

Least effective of the DMARDs

Answer 6

Hydroxychloroquine

Question 7

Possible mechanism of hydroxychloroquine anti-inflammatory effects

Answer 7

altering cellular pH

Question 8

Pharmacokinetics of Hydroxychloroquine

Answer 8

Oral, once daily. Long half life (45 days)

Question 9

Clinical use of Hydroxychloroquine

Answer 9

often combined with other DMARDs

Question 10

Side effects of Hydroxychloroquine

Answer 10

Short term: GI and skin problems

Long term: retinal damage and decrease blood glucose.

Question 11

Which DMARDs can be used in pregnant patients

Answer 11

hydroxycholorquine

Question 12

Which DMARD is metabolized to a salicylate

Answer 12

Sulfasalazine

Question 13

What are the two metabolites of Sulfasalazine

Answer 13

salicylate and slufapyridine

Question 14

Which DMARD has a chance of blood dyscrasias, which can be fatal

Answer 14

Sulfasalazine

Question 15

What three drugs are part of triple drug therapy

Answer 15

Methotrexate, Hydroxychloroquine, Slufasalazine

Question 16

General properties of Leflunomide

Answer 16

inhibits pyrimidine synthesis, tyrosine kinases

inhibits T-cell proliferation and auto-antibody formation

Question 17

Which DMARD requires wash out before pregnancy

Answer 17

Leflunomine

Question 18

Which DMARD inhibits matrix metalloproteinases, including collagenase

Answer 18

Minocycline

Question 19

Biologic DMARD that is a subunit of the TNF receptor

Answer 19

Entercept

Question 20

Biologic DMARD that is a partially humanized mouse antibody against TNF

Answer 20

Infliximab

Question 21

Biologic DMARD that is a fully humanized antibody against TNF

Answer 21

Adalimumab

Question 22

What are the two biologic DMARDs that target immune cells directly and what are their targets

Answer 22

Abatacept targets T-cell activation

Rituximab is an antibody that inhibits B cell activation

Question 23

Which DMARD is most likely to cause eye damage

Answer 23

hydroxychloroquine

Question 24

Which DMARD can cause liver damage

Answer 24

Methotrexate