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

Drugs for Autoimmune Disease Flashcards

1
Q

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

A

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

“Cept”s: etanercept (Enbrel), abatacept (Orencia)

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2
Q

What are some common side effects of biologics?

A

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

Opportunistic infections

Lymphomas

Infection site reactions

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3
Q

What are the indications for Etanercept?

A

Rheumatic syndromes: decreases new erosions in joints

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4
Q

What is the MOA of etanercept?

A

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

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5
Q

What is the ADME for etanercept?

A

Administered SC q 2 weeks

often combined with non-biologic DMARDS

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6
Q

What are the side effects of etanercept?

A

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)*
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7
Q

What are the indications for infliximab and adalimumab?

A

RA

Ulcerative Colitis

Crohn’s Disease

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8
Q

What is the MOA of infliximab and adalimumab?

Which is chimeric human/mouse?

A

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

Infliximab is chimeric human/mouse

Adalimumab is all human

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9
Q

What is the ADME for infliximab (Remicaid)?

A

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

Patients often develop antibodies to Infliximab.

Coadministation with methotrexate prevents this.

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10
Q

What are the side effects of infliximab?

A

Basal cell and squamous cell skin cancer

Nausea, HA, sinusitis, rash, cough

  • Injection site reaction*
  • Activation of latent TB*
  • Opportunistic infections*
  • Lymphomas*
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11
Q

What are the side effects of adalimumab (Humira)?

A

Basal and squamous skin cancer

Lupus-like Sx (rare)

  • TB activation*
  • Lymphoma*
  • Infection site reaction*
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12
Q

What is the MOA of Tocilizumab?

A

Monoclonal antibody

that inhibits binding of IL-6 to its receptor

thereby blocking activation of JAK-STAT pathway,

decreasing transcription of pro-inflammatory proteins

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13
Q

What are the indications for tocilizumab?

A

RA patients who are unresponsive to TNF alpha inhibitors

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14
Q

What is the ADME for tocilizumab?

A

Administration: IV q 4-6 weeks

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15
Q

How does Tocilizumab affect the metabolism of other medications?

A

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.

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16
Q

What are the side effects of tocilixumab?

A

GI perforation

Neutropenia, thrombocytopenia

  • Opportunistic infections*
  • Activation of latent TB*
17
Q

What is the MOA of rituximab?

A

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

Results in B-cell depletion

18
Q

What are the indications for rituximab?

A

RA patients unresponsive to TNF alpha inhibitors

Non-Hodgkin’s lymphoma

Chronic Lymphocytic Leukemia (CLL)

19
Q

What is the ADME of rituximab?

A

Administration: IV q 2 weeks with methotrexate q 6 mo

20
Q

What are the side effects of rituximab?

A

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
Q

What is the MOA of abatacept?

A

Fusion protein

Neutralizes co-stimulatory ligand CD80/86 on APCs

preventing binding to CD28 on T cells

preventing T cell activation

22
Q

What are the indications for abatacept?

A

RA refractory to TNF alpha inhibitors

23
Q

What is the ADME for abatacept?

A

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

24
Q

What are the side effects of abatacept?

A

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

Lung cancer and lymphoma

Respiratory problems in patients with COPD

25
Q

Which biologics would you prescribe for IBD?

A

infliximab or adalimumab

26
Q

Which biologics would you prescribe for NonHodgkin’s Lymphoma?

A

rituximab

27
Q

Which biologics would you prescribe for Chronic Lymphocytic Leukemia?

A

rituximab

28
Q

Which biologics are TNF alpha inhibitors?

A

etanercept

adalimumab

infliximab

29
Q

Which biologics are IL-6 inhibitors?

A

TocILizumab (it has an IL in its name)

30
Q

Which biologics are B-cell depleters?

A

rituximab

31
Q

Which biologics block costimulation of T-cells?

A

abatacept

32
Q

What is the MOA of methotrexate?

A

Folic acid analog

that inhibits the formation of cofactors for synthesis of:

purine, amino acid and thymidylate

33
Q

What are the indications for methotrexate?

A

Organ transplantation

Rheumatic syndromes

Combined with biologics

to inhibit antibody formation against them

34
Q

What is the major side effect of methotrexate?

A

myelosuppression

35
Q
A

Pharmacology II - Exam 3 (5 decks)

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