Drugs for Autoimmune Disease Flashcards Preview

Pharmacology II - Exam 3 > Drugs for Autoimmune Disease > Flashcards

Flashcards in Drugs for Autoimmune Disease Deck (35):
1

What are the "Mab" (monoclonal antibody) and "Cept" (fusion) drugs on our list?

"Mab"s: infliximab (Remicaid), adalimumab (Humira), tocilizumab (Actemra), rituximab (Rituxan)

 

"Cept"s: etanercept (Enbrel), abatacept (Orencia)

2

What are some common side effects of biologics? 

Activation of latent TB (test for and treat TB first)

Opportunistic infections

Lymphomas

Infection site reactions

3

What are the indications for Etanercept? 

Rheumatic syndromes: decreases new erosions in joints

4

What is the MOA of etanercept? 

Fusion protein: fusion of  TNF alpha receptor and Fc domain of IgG1

Acts as a decoy receptor for TNF alpha so it cannot do its work

5

What is the ADME for etanercept? 

Administered SC q 2 weeks

often combined with non-biologic DMARDS 

6

What are the side effects of etanercept? 

increased antinuclear antibodies in 98% (can lead to SLE)

activation of latent TB

opportunistic infections

lymphoma

infection site reactions

 

NOTE: less immunogenic (patients less likely to develop antibodies to etanercept than other TNF alpha blockers)

7

What are the indications for infliximab and adalimumab? 

RA

Ulcerative Colitis

Crohn's Disease

8

What is the MOA of infliximab and adalimumab? 

Which is chimeric human/mouse? 

Monoclonal antibodies that bind TNF alpha and down regulate T-cells and macrophages

 

Infliximab is  chimeric human/mouse

Adalimumab is all human

 

9

What is the ADME for infliximab (Remicaid)? 

Administation: IV q 8 wks, often in combo with nonbiologic DMARDS

Patients often develop antibodies to Infliximab. 

Coadministation with methotrexate prevents this. 

10

What are the side effects of infliximab? 

Basal cell and squamous cell skin cancer

Nausea, HA, sinusitis, rash, cough

Injection site reaction

Activation of latent TB

Opportunistic infections

Lymphomas

11

What are the side effects of adalimumab (Humira)? 

Basal and squamous skin cancer

Lupus-like Sx (rare)

TB activation

Lymphoma

Infection site reaction

12

What is the MOA of Tocilizumab? 

Monoclonal antibody

that inhibits binding of IL-6 to its receptor

thereby blocking activation of JAK-STAT pathway,

decreasing transcription of pro-inflammatory proteins

13

What are the indications for tocilizumab? 

RA patients who are unresponsive to TNF alpha inhibitors

14

What is the ADME for tocilizumab? 

Administration: IV q 4-6 weeks

15

How does Tocilizumab affect the metabolism of other medications? 

IL-6 suppresses several CYPs in the liver,

so inhibition of IL-6 results in induction of CYPs

and increased metabolism of medications. 

Increase dosages accordingly. 

16

What are the side effects of tocilixumab? 

GI perforation

Neutropenia, thrombocytopenia

Opportunistic infections

Activation of latent TB

 

17

What is the MOA of rituximab? 

Humanized monoclonal antibody with selectivity for CD-20 on B-cells

Results in B-cell depletion

18

What are the indications for rituximab? 

RA patients unresponsive to TNF alpha inhibitors

Non-Hodgkin's lymphoma

Chronic Lymphocytic Leukemia (CLL)

19

What is the ADME of rituximab? 

Administration: IV q 2 weeks with methotrexate q 6 mo

20

What are the side effects of rituximab? 

Serious infections (Hep B reactivation, bacterial, fungal, not TB)

First dose infusion reaction (Tx with glucocorticoids)

Some cardiac events and death reported

C/I re pregnancy: wait 6 mo prior to conception! 

 

21

What is the MOA of abatacept? 

Fusion protein

Neutralizes co-stimulatory ligand CD80/86 on APCs

preventing binding to CD28 on T cells

preventing T cell activation

22

What are the indications for abatacept? 

RA refractory to TNF alpha inhibitors

23

What is the ADME for abatacept? 

Administration: IV on day 1, wk 2, wk 4, then q 4 wks

24

What are the side effects of abatacept? 

Serious infections 3%: no live vax til 3 mo after D/C

Lung cancer and lymphoma

Respiratory problems in patients with COPD

25

Which biologics would you prescribe for IBD? 

infliximab or adalimumab

26

Which biologics would you prescribe for NonHodgkin's Lymphoma? 

 

rituximab

27

Which biologics would you prescribe for Chronic Lymphocytic Leukemia? 

rituximab

28

Which biologics are TNF alpha inhibitors? 

etanercept

adalimumab

infliximab

29

Which biologics are IL-6 inhibitors? 

TocILizumab (it has an IL in its name)

30

Which biologics are B-cell depleters? 

rituximab

31

Which biologics block costimulation of T-cells? 

abatacept

32

What is the MOA of methotrexate? 

Folic acid analog 

that inhibits the formation of cofactors for synthesis of:

purine, amino acid and thymidylate 

33

What are the indications for methotrexate? 

Organ transplantation

Rheumatic syndromes

 

Combined with biologics

to inhibit antibody formation against them

34

What is the major side effect of methotrexate? 

myelosuppression

35