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GI Final > IBS and IBD Pharm > Flashcards

IBS and IBD Pharm Flashcards

1
Q

What are the treatment agents for Ulcerative Colitis?

A

5-ASA
Corticosteroids
TNF Inhibitors
Alpha-4 integrin inhibitors

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2
Q

5-ASA

A

“sala”

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3
Q

Corticosteroids

A

“one”

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4
Q

TNF inhibitors

A

“mab”

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5
Q

What is the ONE alpha-4 integrin inhibitor?

A

Vedolizumab

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6
Q

What are the treatments for Crohn disease?

A
  • IL-12/23 inhibitors
  • Corticosteroids
  • TNF inhibitors again
  • alpha 4 integrin inhibitors
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7
Q

What is the one IL-12/23 inhibitor?

A

Ustekinumab

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8
Q

TNF?

A

mab again

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9
Q

the TWO Alpha-4 integrin inhibitors for Crohn?

A

Natalizumab

Vedolizumab

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10
Q

What is Sulfasalazine?

A

sulfapyridine and aspirin (5-ASA)

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11
Q

mesalamine?

A

just aspirin

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12
Q

Olsalazine

A

2 molecules of aspirin

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13
Q

Balsalazide

A

inert carrie and aspirin

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14
Q

How far are oral aspirin things distributed?

A

may be the entire GI tract

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15
Q

Rectal enemas… how far do they reach?

A

may reach the splenic flexure

-do not frequently concentrate int he rectum

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16
Q

Where do rectal suppositories concentrate?

A

-they reach the upper rectum

15-20 cm beyond the anal verge

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17
Q

What is 5-ASA’s Mechansim of Action?

A
  • inhibition of PG and LT production via arachidonic acid pathway
  • Reduction in PMN and macrophage chemotaxis
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18
Q

What are some side effects of 5-ASA products?

A

dizziness/headache/fatigue

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19
Q

In what patients are all 5-ASA compounds contraindicated in?

A

ASA- allergic patients

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20
Q

What patients have sulfalazine contraindications?

A

sulfonamide-allergic patients

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21
Q

What are some indications of 5ASA agent?

A

mild to moderate active UC and maintenance of Remission of UC

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22
Q

What is only used for maintenance therapy?

A

Olsalazine

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23
Q

What is only used for the treatment of active disease?

A

Balsalazide

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24
Q

What is also indicated for jevenile-arthritis

A

Sulfasalazine

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25
Q

What are the TNG-alpha inhibitors?

A

the “mab”s

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26
Q

MOA for TNF alpha inhibitors?

A
  • neutralizes membrane-associated and soluble human TNG alpha mediate pro inflammatory cell signaling
  • inhibits expression of pro-inflammatory genes
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27
Q

What are some side effects of TNG alpha inhibitors?

A

Infections

-to TB test pre-therapy

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28
Q

What are the indications for TNF alpha inhibitors?

A

treatment of active and maintenance

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29
Q

Which 2 tnf inhibitors can tread both UC and CD?

A

Adalimumab and Infliximab

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30
Q

Which TNF inhibitor only works for UC?

A

Golimumab

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31
Q

Which TNG inhibitor only works for CD?

A

the one that starts with C

-Certolizumab

32
Q

What is the dosing for each of the TNF inhibitors?

A
  • Adalimumab: SQ (subcutaneous) every other wek
  • Infliximab: IV infusion every 8 weeks
  • Golimumab: SQ every 4 weeks
  • Certolizumab: SQ every 4 weeks
33
Q

What are the alpha 4 integrin inhibitors?

A

Natalizumab: recombinant humanized IgG4 monoclonal antibody

-Vedolizumab: humanized IgG1 monoclonal antibody

34
Q

MOA of alpha 4 integrin inhibitors?

A

limits integrin’s associated cell adhesion, transendothelial migration, and immune cell activation with in inflamed tissue

35
Q

Side effects of Alpha 4 integrin inhibitors?

A

PML (this is a big deal… progressive multifocal leukoencephalopathy)

  • 3 risk factors for PML: treatment for >2 years
  • prior immunosuppressant treatment
  • anti-JC virus antibodies
36
Q

Indications for Alpha 4 integrin inhibitors

A
  • moderat to severe treatment resisntantt CD and maintenance therapy to prevent relapse (Natalizumab)
  • Moderate to severe treatment resisntant CD and UC (vedolizumab) and maintenance therapy to prevent relapse
37
Q

What is the dosing of alpha 4 integrin inhibitors?

A

Natalizumab: IV infusion every 4 weeks
Vedolizumab: IV infusion every 8 weeks

38
Q

What is the one IL-12/23 inihibitor?

A

ustekinumab

39
Q

MOA of IL-12/23 inhibitors?

A

bind to a specific subunit of IL-12/23 receptor located on surface of T cells and NK cells
-thereby inhibiting signal transduction-related activities and production of pro-inflammatory Th1 and Th17 cells

40
Q

Side effect of IL-12/23 inhibitors

A

-Infections, TB testing pre-therapy recommended

41
Q

Indications for IL-12/23 inhibitors

A

-Moderate to severe treatment resistant CD (both active disease and maintenance)

42
Q

Dosing of IL-12/23

A

Ustekinumab

  • Administered IV as a single infusion (induction)
  • SQ every 8 weeks (for maintenance)
43
Q

Glucocorticoids

A

Prednisone/methylprenisolone/dexamethasone/etc.

44
Q

Mechanism of Glucocorticoids

A

binding to specific cytoplasmic receptors induces a response by modifying transcription and, ultimately protein synthesis, to achieve the steroid’s intended action, including:

  • inhibition of leukocyte infiltration at site of inflammation
  • interference in the function of mediators of inflammatory response
  • suppression of humoral immune responses
45
Q

Adverse effects revisited

A
  • increase glucose , bp, and lipid profile
  • GI distress
  • fluid retention/edema/swelling of face and extremities
46
Q

Indications for Steroids

A

Acute and/or severe UC and CD uncontrolled by other conventional medications

47
Q

Dosing of steroids

A

use the lowest dose for shortest duration possible

48
Q

What does IBS stand for?

A

Irritable bowel syndrome

49
Q

What is IBS?

A

a complex of symptoms

  • individual symptoms w/ limited accuracy in diagnosis
  • abdominal pain
  • diarrhea or constipation
50
Q

What are antimuscarinic agents used for?

A

abdominal pain

51
Q

What are the antimuscarinic agents?

A
  • hyoscyamine
  • dicyclomine
  • clidinium
  • chlordiazepoxide
52
Q

What are the Bulk-Forming and laxative Agents?

A
  • psyllium
  • methylcellulose
  • polyethylene-glycol (PEG)
  • lactulose
  • Polycarbophil
  • Magnesium
53
Q

Anti-Diarrheals

A

Loperamide

Diphenoxylate

54
Q

Opiod agonists/antagonists

A

eluxadoline

55
Q

Serotonin (5HT3) antagonists

A

Alosetron

56
Q

Guanylate cyclase-C Agonists

A

Linaclotide

57
Q

Selective chloride (C2 channel activators)

A

Lubiprostone

58
Q

What are Antimuscarinics used for

A

for abd. pain/spasms

59
Q

MOA of antimuscarinics

A

Competitively-inhibit autonomic, post-ganglionic cholinergic receptors (multiple sites
-results in decreased GI motility and spasms

60
Q

Side effects of antimuscarinics

A

easy: just think everything anticholinergic
- dry mouth
- urinary retention
- constipation
- drowsiness
- mental confusion
- blurred vision

61
Q

What 3 classes of drugs are used for diarrhea?

A
  • Anti-Diarrheals: loperamide, diphenoxylate (bismuth)
  • Opioid Agonists/antoagonists: eluxadoline
  • Serotonin Antagonists: Alosetron
62
Q

MOA of Loperamide?

A
  • interferes with peristalsis by a direct action on circular and longitudinal muscles of the intestinal wall, slowing motility
  • also may directly inhibit fluid and electrolyte secretion and.or increase water absorption
  • chemically related to opioids without opioid actions
63
Q

Side effects of Loperamide?

A

-constipation, dizziness, drowsiness, and urinary retention (anticholinergic)

64
Q

MOA of Diphenoxylate?

A

-exerts effect locally and centrally on GI smooth muscle cells; inhibits GI motility and slows excess GI propulsion

65
Q

Side effects of Diphenoxylate?

A

-constipation, dizziness, drowsiness and urinary retention

66
Q

MOA of Alosetron?

A
  • selectively blocks GI-based 5HT3 receptors

- antagonism at 5HT3 receptors in GI tract modulate regulation of visceral pain, colonic transit and GI secretions

67
Q

Side effects of Alosetron?

A
  • GI complaints: constipation, dyspepsia, GERD and N/V

- **Ischemic Colitis*

68
Q

Indication for Alosetron?

A

Women with chronic, sever IBS-D no responsive to other conventional therapies
-so, it’s pretty intense

69
Q

MOA of Eluxadoline

A
  • agonist at opioid mu and kappa receptors in GI tract (slows peristalsis/delays digestion)
  • antagonist at delta opioid receptors in GI tract… decreases stomach, pancreas and biliary tract secretions
70
Q

Side effects of Eluxadoline

A
  • GI related
  • Hepatic.pancreatic toxicity
  • CNS-related
71
Q

What 3 drug classes are used for constipation?

A
  • Bulk-forming and laxative agents (don’t worry about them)
  • Guanylate cyclase-C agonists: Linaclotide
  • Selective Chloride (C2) channel activators: Lubiprostone
72
Q

MOA of Linaclotide

A
  • binds to Guanylate cyclase-C on luminal surface of intestinal epithelium (agonist)
  • increases cGMP
  • stimulates secretion of chloride/bicarb into intestinal lumen via activation of CFTR ion channel
  • results in increased intestinal fluid and accelerated transit
73
Q

Side effects of Linaclotide

A
  • Diarrhea

- other GI-related: abd pain/dyspepsia/N/V/Flatulence

74
Q

Indications for Linaclotide

A

IBS-C

  • Chronic Idiopathic Constipation (CIC)
  • not supported <17 years of age
75
Q

MOA of Lubiprostone

A
  • Activates apecific CIC-2 chloride channels in luminal cells of intestinal epithelium
  • produces a chloride-rich intestinal fluid secretion without altering serum electrolyte concentrations
  • a PGE-1 derivative
76
Q

Side effects of Lubiprostone

A

-Nausea, dyspepsia, dizziness

77
Q

Indications for Lubiprostone

A

IBS-C (women)… not men

-Chronic idopathic constipation (CIC) adults

GI Final (13 decks)

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