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MSK/Rheum > Pharm-RA-DMARDs-Biologics > Flashcards

Pharm-RA-DMARDs-Biologics Flashcards

1
Q

What are the 9 biological DMARDs?

A
  1. Adalimumab
  2. Certolizumab Pegol
  3. Etanercept
  4. Golimumab
  5. Infliximab
  6. Abatacept
  7. Anakinra
  8. Rituximab
  9. Tocilizumab
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2
Q

Cytokines and Cytokine Receptors are expressed in what two forms?

A

Both membrane-bound and soluble forms

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3
Q

What two ways are soluble cytokines produced?

A

a. Secreted via vesicular fusion

b. Cleavage of transmembrane cytokines

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4
Q

T/F: once transmembrane cytokines bind their receptors, signaling can be bidirectional?

A

True

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5
Q

What are the 3 types of cytokine targeted therapies?

A
  1. mAbs (next question)
  2. Therapeutic soluble receptors: primarily target soluble cytokines (Etanercept)
  3. Receptor antagonists (Anakinra)
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6
Q

What are the three mechanisms thru which monoclonal Abs (mAbs) inhibit cytokine activity?

A
  1. Neutralization of soluble and transmembrane cytokines
  2. Can induce reverse signaling and cell-/complement-mediated cytotoxicity
    (1 and 2 are done by Adalimumab, Certolizumab Pegol, Infliximab, Gomilumab)
  3. Can block cytokine receptors (Tocilizumab)
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7
Q

What is the advantage of cytokine receptor-targeted therapy?

A

It can selectively silence individual receptor subtypes when multiple receptor subtypes ligate a single cytokine.

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8
Q

The cellular basis of the RA cytokine profile may center on what type of cell?

A

Th17 cells

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9
Q

What cytokines promote differentiation of naive T cells to the Th17 phenotype?

A

TGF-B, IL-1B, IL-6, IL-21, IL-23 promote differentiations.

IL’s-15 and 23 reinforce this phenotype.

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10
Q

What is the defining cytokine produced by Th17 cells, and what does this cytokine induce?

A

IL-17; it induces production of IL-1, IL-6, and TNF from macrophages/monocytes

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11
Q

What 5 biologic DMARDs block TNF-a?

A

4 mAbs and 1 soluble receptor (SR):

  1. Adalimumab
  2. Certolizumab pegol
  3. Golimumab
  4. Infliximab
  5. Etanercept (SR)
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12
Q

Route, Structure, and MoA of Abatacept?

A

Route: IV/SC
Structure: Fusion protein of human CTLA4 + IgG1 fragment
MoA: Blocks the T cell co-stimulatory signal by binding CD80/86 and preventing engagement with CD28.

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13
Q

Route, Structure, and MoA of Adalimumab?

A

Route: SC
Structure: TNF-a mAb
MoA: Binds TNF-a, blocking its interaction with p55/p75 cell-surface receptors

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14
Q

Route, Structure, and MoA of Anakinra?

A

Route: SC
Structure: Recombinant human IL-1 receptor antagonist (IL-1Ra)
MoA: Competitively inhibits IL-1alpha and IL-1beta binding to IL-1 type 1 Receptor (IL-1R1)

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15
Q

Route, Structure, and MoA of Certolizumab pegol?

A

Route: SC
Structure: Fab fragment of humanized TNF-a Ab
MoA: neutralizes both membrane associated and soluble TNF-a

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16
Q

Route, Structure, and MoA of Etanercept?

A

Route: SC
Structure: Extracellular ligand-binding portion of p75 TNF-R linked to part of human IgG Fc
MoA: binds and inactivates TNF but does not affect TNF production or serum levels

17
Q

Route, Structure, and MoA of Golimumab?

A

Route: SC
Structure: Human-derived TNF-a Ab (variable and constant regions)
MoA: binds and neutralizes both soluble and transmembrane TNF-a

18
Q

Route, Structure, and MoA of Infliximab?

A

Route: IV
Structure: Chimeric (mouse-human) IgG1k mAb against TNF-a
MoA: binds and neutralizes both soluble and transmembrane TNF-a.

19
Q

Route, Structure, and MoA of Rituximab?

A

Route: IV
Structure: Chimeric (mouse-human) IgG1k mAb against B-cell CD20 receptor
MoA: Fab domain binds CD20 & Fc domain recruits immune effector functions to mediate B-cell lysis (3 mechs: complement-dependent or Ab-dependent cellular cytotoxicity, or induction of apoptosis);
It sensitizes drug-resistant B-cell lymphoma lines to cytotoxic chemotherapy.

20
Q

Route, Structure, and MoA of Tocilizumab?

A

Route: IV
Structure: Humanized IL-6 receptor-inhibiting mAb
MoA: Binds to both soluble (serum and synovial fluid) and membrane bound IL-6 receptors and inhibits signaling.

21
Q

What is a common adverse effect of all 9 biological DMARDs? Complications/cautions that result from this effect? (5)

A

All of them produce IMMUNOSUPPRESSION:

a. ↑’d susceptibility to bacterial, TB, fungal, parasitic infections; some have BBW for this.
b. DO NOT initiate treatment in pt w/ an active infection
c. AVOID LIVE VACCINES
d. URT infections could be especially problematic or could occur more frequently in asthmatics/COPD
e. Pt’s should report s/s of an infection or a recurrent infection during therapy or within several months after discontinuation.

22
Q

Which of these drugs increases the likelihood of lymphoma/other malignancies? (5)

A

Adalimumab, Certolizumab pegol, Etanercept, Golimumab, Infliximab

23
Q

What are the ADE/complications associated with these drugs in general?

A
  1. Immunosuppression
  2. Malignancy/Lymphoma
  3. CHF or hypotension/angina/dysrhythmia
  4. Blood Dyscrasias
  5. Lupus-like syndrome
  6. SJS/Toxic Epidermal Necrosis (TEN)
  7. Hepatotoxicity
  8. Counseling proper injection techniques for self-administered SC agents
24
Q

a. Which agents have been reported to cause CHF or hypotension/angina/dysrhythmia? (4)
b. Which drug is absolutely contraindicated for pt’s with moderate-severe heart failure?

A

a. Adalimumab, Golimumab, Infliximab, Rituximab

b. Infliximab

25
Q

Which agents have been reported to cause blood dyscrasias? (4)

A

Anakinra, Certolizumab, Rituximab, Tocilizumab

Perform Routine CBCs

26
Q

Which agent has been reported to cause SJS/TEN infrequently?

A

Rituximab

27
Q

Which agents have been reported to cause Lupus-Like Syndrome (arthralgias, myalgias, fatigue, skin rashes)? (4)

A

Most likely with Adalimumab, Certolizumab, Etanercept, Infliximab

28
Q

Rx w/ which agent may complicate some blood glucose tests? Why?

A

Abatacept IV solution contains maltose, which may complicate some blood glucose tests

29
Q

Women taking ___________ must use RELIABLE CONTRACEPTION while taking the drug and avoid pregnancy for 4-6 months after?

A

Rituximab; B-cell depletion possible b/c IgG crosses placenta

30
Q

a. Liver function tests are recommended in pt’s taking which agents? (3)
b. Which agent requires serum lipid profiles?

A

a. Golimumab, Infliximab, Tocilizumab

b. Tocilizumab

31
Q

Pt’s using what route of administration should be counseled about what? What drugs are these? (6)

A

Pt’s self-administering drugs SC should be counseled about appropriate injection sites and the need for injection site rotation;
Abatacept, Adalimumab, Anakinra, Certolizumab, Etanercept, Golimumab

MSK/Rheum (7 decks)

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