GI Flashcards

1
Q

Histamine Receptor Antagonists

A

MOA: selective, competetive blockade on basolateral side of parietal receptor cells - prevents stimulation of proton pump

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2
Q

what are some risk factors with H2RA

A

anti-adrogenic (gynecomastia, impotence), arrhytias, headache, dizziness, GI upset

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3
Q

major interactions with H2RA

A

caffeine (cimetidine)

St John’s Wart

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4
Q

PPI MOA

A

selective irreversible H/K?ATPase inhibition on luminal side of parietal cells.

  • acid-labile: broken down in stomach acid which reduces their absorption.
  • secretory activity returns 3-5 days after stopping
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5
Q

risk factors with PPIs

and interactions

A

Mg depletion, osteoporosis, c diff infections, CAP, HA, dizziness, GI
CYP - hepatic impairment
St John’s Wart and Grapefruit

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6
Q

Are PPIs or H2RAs better at immediate symptom relief and why?

A

H2RA are better for immediate relief because their onset is 30-45 minutes rather than 2-3 hours. PPIs also have a commuluative effect if they are taken multiple days in a row

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7
Q

What would you prescribe for GERD?

A

Antacids - acid buffer in lumen
H2RA - competitive antagonism of H2 receptors
PPI - Inhibit H/K/ ATPase pump

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8
Q

What site of action do PPIs and H2RAs have in common?

A

both act on the parietal cell

both inhibit proton pump (H2RA indirectly)

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9
Q

tachyphlaxis

A

rapidly diminishing response to successive doses of a drug, rendering it less effective. The effect is common with drugs acting on the nervous system

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10
Q

rx for gas

A

simethicone: siicone polymer

Alpha- galactosidase: beano

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11
Q

what can simethicone interact with?

A

thyroid medication - can decrease serum concentration

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12
Q

Simethicone

A

inert silicone polymer, de-foaming agent, reduces surface tension of gas bubbles

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13
Q

Alpha- galactosidase

A

mold-derived enzyme that cleaves oligosaccharides before reaching colonic bacteria.

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14
Q

A diabetic patient on medications wants a flatulene product, what would you recommend?

A

simethicone because

alpha-galactosidase is not recommended in diabetic patients and activated charcoal can impact absorption of medications.

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15
Q

Stimulant laxatives

A

senna (ex-lax): anthraquinone stimulates peristalsis by directly acting on mucosa nerve plexus
bisacodyl (dulcolax): irritates smooth muscle causes peristalsis

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16
Q

osmotic laxatives

A

plyethylene glycol 3350 (miralax): water retention in stool increases frequency
magnesium citrate: osmotic retention of fluid in bowel

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17
Q

stool softeners

A

docusate (colace): diocyl dosium sulfosuccinate reduces surface tension of oil water on stool and inhances incorporation of water and oil into stool

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18
Q

if a patient was taking senna, what else could you add for persistent constipation?

A

docusate stool softener

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19
Q

bulk laxatives

A

psyllium (metamucil): absorbs water in intestine and promotes peristalsis and reduces transit time

20
Q

if you are a prescribing opiates, what is important to also give?

A

laxatives

21
Q

antidiarrheal: opiate like

A

loperamide (immodium)
Diphnoxylate
Atropine

22
Q

loperamide (immodium)

A

decreases GI motility acting on circular and longitudinal muscles. Reduces GI secretions

23
Q

Diphnoxylate and Atropine

A

opiate receptro agonist inhibiting GI activity

also inhibits SLUD

24
Q

what are the actions of antidiarrheal drugs?

A

act on smooth muscle or inhance chloride channel activity to increase fluid secrtion into intestinal lumen

25
Q

lamotil and imodium have what similar mechanism of action?

A

decrease GI motility

26
Q

pharmacology for IBD

A

Corticosteroids/Glucocorticoids
Aminsalicylates - most common
Immunosuppresants
Atibiotcs

27
Q

MOA corticosteroids - Prednisone

A

modulates protein synthesis leading to reduced migration of plymophonuclear leukocytes and fibroblasts. Prevents/controls inflammation by reversing capilarry permeability

28
Q

MOA Glucocorticoid: budesonide

A

same as prednisone

interacts with grapefruit and st johns wart

29
Q

Aminosalicylates: Mesalamine MOA

A

modulates local chemical mediators of inflammatory response and supresses lukotriens, acts as free radical scavenger and inhibits tumor necrosis factor. Most *activity is topical, minimal absorption

30
Q

Aminosalicylates: sulfasalazine MOA

A

prodrug of mesalamine and bond is cleaved by colonic bacteria.

  • competetive inhibitor of folate
  • take a away from meals
  • sweat, urine, tears turns orange
31
Q

where are azo drugs released?

A

closer to colon

32
Q

Antimetabolites (immunosuppresants)

A

azathioprine:
- inhibits most rapidly proliferating cells in body.
- purine analog/antimetabolite
- inhibits purine synthesis and DNA replication, resulting in an anti-proliferative effect and induction of apoptosis of T-cells

33
Q

What is the major interaction with Azathioprine?

A

ETOH

34
Q

Monoclonal Abs: Tumor necrosis factor (TNF alpha)

A

Inhibits TNF alpha which is responsibe for induction of proinflammatory cytokines which activate neutrophils and eosinophils adn induce acute phase reactants

35
Q

what is recommended along with TNF alpha

A

premedication with antihistimines to preventand manage infusion related reactions

36
Q

Anti-TNF alpha: Infliximab

A

chimeric IgGk that binds both free and membrane bound TNF a: different ab smashed together that contain zone that will attach to ag.

37
Q

Anti-TNF a: Adalimumab (Humira)

A
human mAb (IgG1k) against TNFa
more accepted in body because comes from human, not animal.
38
Q

Explain cycle of inflammation that happens with IBD

A
  • innate cells produce increased TNF a, interleukins and chemokines
  • marked expansion of lamina propria with increased CD4 t cells (especially proinflammatory ones)
  • These secrete increased levels of cytokines and chemokines wich results in more leukocytes
  • cycle of inflammation
39
Q

Rx for Nausea/Emesis

A

serotonin antagonists

dopamine antagonists

40
Q

Serotonin Antagonists

A

Ondansetron: selectively antagonizes serotonin receptors

- hepatic metabolism

41
Q

risk factors with Ondansetron

A

QT prolongation, HA, fatigue, malaise, diarrhea

interacts with grapefruite and St johns wart

42
Q

If Serotonin antaginsts prevent nausea, what would SSRIs do

A

induce nausea

as well as decrease depression/anxiety

43
Q

Dopamine antagonists

A

promethazine

metoclopramide

44
Q

promethazine

A

blocks postsynaptic dopaminergic receptors in brain and depresses release of hormones (hypothalamic and hypophyseal)

  • anti-muscarinic and anti histimine activity
  • hepatic metabolism/CYP
45
Q

Metoclopramide

A

antagonizes dopamine receptors and blocks serotonin receptors in CNS
- prokinetic: enhanced motility and increased gastric emptying

46
Q

what receptors does metoclopramide effect?

A

D2

Seratonin

47
Q

where is the emetic center

A

medulla