Pharm - Tx for IBD Flashcards

1
Q

What are the 4 familial agents used to treat UC?

A
  • 5-ASA
  • JAK inhibitors
  • TNF-a inhibitors
  • a4 Integrin inhibitors
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2
Q

sulfasalazine
mesalamine
olsalazine
balsalazide

A

5-ASA’s

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3
Q

tofacitinib

A

JAK inhibitor

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4
Q

adalimumab
golimumab
infliximab

A

TNF-a inhibitors (for UC)

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5
Q

vedolizumab

A

a4 integrin inhibitor

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6
Q

what are the 3 familial agents used to treat Crohn disease?

A
  • IL-12/23 inhibitors
  • TNF-a inhibitors
  • a4 integrin inhibitors
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7
Q

ustekinumab

A

IL-12/23 inhibitor

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8
Q

adalimumad
certolizumab
infliximab

A

TNF-a inhibitors (for CD)

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9
Q

natalizumab

vedolizumab

A

a4 integrin inhibitors

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10
Q

what is the MOA of 5-ASA agents?

A

inhibit prostaglandin and leukotriene production via arachidonic acid pathway
- may also inhibit the activation of NF-kb, regulating transcription of pro-inflammatory proteins

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11
Q

what drug is sulfapyridine + 5-ASA?

A

sulfasalazine

  • sulfa is carrier molecule, 5-ASA provides antimicrobial property
  • watch for sulfa allergy!
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12
Q

which drug is a single 5-ASA?

A

mesalamine

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13
Q

which drug is 2 molecules of 5-ASA?

A

olsalazine

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14
Q

which drug is an inert carrier + 5-ASA? why is this drug important?

A

balsalazide

- don’t have to worry about sulfa allergy with an inert carrier!

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15
Q

which form of 5-ASA may be released in the distal/terminal ileum, colon, or throughout GI tract?

A

oral form

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16
Q

which form of 5-ASA may reach the splenic flexure and does not concentrate in the rectum?

A

rectal enemas

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17
Q

what form of 5-ASA can reach the upper rectum (15-20cm beyond the anal verge)?

A

rectal suppositories

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18
Q

what are the side effects of 5-ASA agents?

A
  • dizziness, headache, fatigue

- epigastric distress (anorexia, abd pain, NVD)

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19
Q

what drug drug is contraindicated in sulfonamide-allergic patients?

A

sulfasalazine

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20
Q

what are the indications for 5-ASA agents?

A

mild-moderate UC

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21
Q

what are the exceptions for 5-ASA indications?

A
  • olsalazine is ONLY used for maintenance of remission

- balsalazine is ONLY used for active disease (not remission)

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22
Q

this drug binds to and neutralizes membrane associated TNF-a mediated pro-inflammatory cell signaling, ultimately blocking leukocyte migration to site of inflammation

A

TNF-a inhibitor

23
Q

recombinant IgG1 monoclonal Ab

A

adalimumab

24
Q

chimeric (murine/human) IgG1 monoconal Av

A

infliximab

25
Q

recombinant humanized IgG4 monoclonal Ab

A

golimumab

26
Q

recombinant humanized Ab fragment

A

certolizumab

NOTE: does NOT contain an Fc region, thus does NOT fix complement or cause Ab-dependent cell-mediated cytotoxicity

27
Q

what two TNF-a inhibitors are approved for both UC and CD? (moderate-severe)

A

adalimumab and infliximab

think of additive and inclusive!

28
Q

what TNF-a inhibitor is approved only for moderate-severe CD?

A

certzolizumab

29
Q

what TNF-a inhibitor is approved only for moderate-severe UC?

A

golimumab

30
Q

what is the main side effect of TNF-a inhibitors?

A

infection -> MUST do Tb testing pre-therapy (to make sure they don’t have quiescent disease)

NOTE: TNF-a inhibitors are used after pt does not respond to conventional immunosuppressant therapy

31
Q

what is the black box warning of TNF-a inhibitors?

A

discontinue if pt develops serious infection or sepsis

- active Tb, invasive fungal infections, bacterial, or viral

32
Q

what are the side effects of TNF-a inhibitors?

A
  • *infections!**
  • liver toxicity
  • headache/arthralgias/fatigue
33
Q

which TNF-a inhibitor is administered subQ every 2 weeks?

A

adalimumab

34
Q

which TNF-a inhibitor is administered via IV infusion every 8 weeks?

A

infliximab

one that starts with I -> given IV

35
Q

which TNF-a inhibitors are administered subQ every 4 weeks?

A

golimumab AND certolizumab

36
Q

this drug limits integrin-associated cell adhesion and subsequent trans-endothelial migration of leukocytes to the cite of inflammation

A

a4 integrin inhibitors

NOTE: a4 integrin inhibitors are used after pt does not respond to conventional immunosuppressant OR TNF-a therapy

37
Q

this drug is a recombinant humanized IgG4 monoblonal Ab a4B1 (VCAM-1) and a4B7 (MAdCAM-1)

A

natalizumab

38
Q

this drug is a humanized IgG1 monoclonal Ab

** a4B7 (MAdCAM-1) ONLY

A

vedolizumab

39
Q

which a4 integrin inhibitor is used to treat both UC and CD? (moderate-severe)

A

vedolizumab

40
Q

which a4 integrin inhibitor is only used to treat moderate-severe CD, but can bind to both a4B1 and a4B7 receptors?

A

natalizumab

41
Q

what is the main side effect of a4 integrin inhibitors?

A
  • *infections**

- black box warning for the risk of progressive multifocal leukoencephalopathy (PML) while taking natalizumab

42
Q

what are the 3 risk factors for PML?

A
  • a4 integrin treatment >2 years
  • prior immunosuppressant treatment
  • anti-JC virus (JCV) antibodies
43
Q

which a4 integrin inhibitor is administered by IV every 4 weeks?

A

natalizumab

44
Q

which a4 integrin inhibitor is administered by IV every 8 weeks?

A

vedolizumab

45
Q

these drugs bind to P40-subunit of IL-12/23, blocking activation/differentiation of naive T cells, and activation of NK cells
- thereby inhibiting production of pro-inflammatory cytokines (Th1, TNFa, IL17, IL21)

A

interleukin (IL-12/23) inhibitors

46
Q

fully human IgG1 monoclonal Ab, administered subQ every 8 weeks, after single IV infusion for induction

A

ustekinumab

47
Q

what are the side effects of IL-12/23 inhibitors?

A
  • *infections!**
  • Tb testing recommended pre-therapy

also infusion/injection reactions, HA, arthralgia, fatigue

48
Q

which drug is used to treat moderate-severe CD, and is reserved for patients intolerant or inadequate response (resistant) to conventional, immune modulators, steroids or TNF-a therapy)

A

ustekinumab

49
Q

these drugs bind to and inhibit free-floating and bound JAK-1 and JAK-3, ultimately inhibiting gene transcription and more cytokine release

A

JAK inhibitors

50
Q

which drug is an oral JAK 1/3 inhibitor used to treat moderate-severe UC?

A

tofacitinib

- PO 2x/day

51
Q

what are the side affects of tofacitinib?

A
  • lymphopenia/lymphocytosis (know baseline values before starting tx)
  • neutropenia
  • fatigue
  • increases in LDL and HDL

NOTE: concomitant use of potent immunosuppressant therapy NOT recommended

52
Q

what drug type is the most common/powerful anti-inflammatory agent?

A

steroids!

53
Q

what are the indications for steroids?

A

acute and/or severe UC AND CD, that is uncontrolled by other conventional medications

NOTE: used for maintenance of remission unless absolutely required (don’t want to become steroid dependent)

54
Q

what is the dosing of steroid agents for UC and CD?

A

the LOWEST dose for the SHORTEST duration possible

- not good to be on steroids for extended time