RA Pharmacology

Question 1

MOA: Prednisone

Answer 1

Acts on NF-kß and AP-1 to cause immunosuppression Activates Lipocortin which inhibits PLA2

Question 2

MOA: Methotrexate

Answer 2

Blocks Thymidylate Synthase –> accumulation of AICAR –> adenosine efflux –> adenosine activating GPCR –> anti-inflammatory effects

Question 3

MOA: Hydroxychloroquine

Answer 3

Weak base that increases pH in lysosomes preventing peptide loading onto MHC2

Question 4

MOA: Leflunomide

Answer 4

Blocks synthesis of ribonucleotides inhibiting T cell proliferation

Question 5

MOA: Etanercept

Answer 5

TNF inhibitor

Question 6

MOA: Infliximab

Answer 6

TNF inhibitor

Question 7

MOA: Adalimumab

Answer 7

TNF inhibitor

Question 8

MOA: Rituximab

Answer 8

Binds CD20 on B cells acting as opsonizing agent –> depletion of immature B cells –> decreased production of autoAb

Question 9

MOA: Abatacept

Answer 9

Prevents CD28 binding w/ CD80/86 preventing activation of T cells by APCs

Question 10

MOA: Tocilizumab

Answer 10

Anti-IL-6R IgG Ab limiting hepatic acute phase response

Question 11

MOA: Tofacitinib

Answer 11

JAK3 enzyme inhibitor

Question 12

MOA: Anakinra

Answer 12

Blocks pro-inflammatory activity of IL-1

Question 13

Clinical application: Prednisone

Answer 13

Relieve pain/inflammation until DMARD kicks in Tx for flare ups

Question 14

Clinical application: Methotrexate

Answer 14

1st choice for RA

Question 15

Clinical application: Hydroxychloroquine

Answer 15

Combined w/ MTX (safe in pregnancy)

Question 16

Clinical application: Sulfasalazine

Answer 16

Alone or combo (safe in pregnancy)

Question 17

Clinical application: Leflunomide

Answer 17

Last choice for RA

Question 18

Clinical application: Rituximab

Answer 18

Combo w/ MTX in pts w/ RA not responding to TNFi’s

Question 19

Clinical application: Abatacept

Answer 19

Moderate/Severe RA when TNFi’s fail

Question 20

Clinical application: Tocilizumab

Answer 20

Moderate/Severe RA when DMARDs and TNFi’s fail

Question 21

Clinical application: Tofacitinib

Answer 21

Moderate/Severe active RA

Question 22

Clinical application: Anakinra

Answer 22

Moderate/Severe RA

Question 23

Major SE’s: Hydroxychloroquine

Answer 23

Retinal damage

Question 24

Major SE’s: Leflunomide

Answer 24

Respiratory infection Reversible alopecia

Question 25

Major SE's: Abatacept

Answer 25

Serious infection

Question 26

Major SE's: Tocilizumab

Answer 26

URI

Question 27

Major SE's: Tofacitinib

Answer 27

Fatal/opportunistic infections Malignancy

Question 28

What drugs are in the Non-biologic DMARD category

Answer 28

MTX Hydroxychloroquine Sulfasalazine Leflunomide

Question 29

What drugs are in the Biologic DMARD category

Answer 29

Etanercept, Infliximab, Adalimumab Rituximab Abatacept Tocilizumab Tofacitinib Anakinra