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GI > PHARM_PEPTICULCER/GERD > Flashcards

PHARM_PEPTICULCER/GERD Flashcards

1
Q

what type of acetylcholine receptors are found on parietal cells which when activated promote acid secretion?

A

M3

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2
Q

both gastrin and the M3 receptor act through which type of G protein to promote acid secretion?

A

Gq

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3
Q

Histamine acts through what kind of G protein to activate adenylate cyclase and promote acid secretion?

A

Gs

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4
Q

somatostatin and prostaglandins act through what kind of G protein to inhibit adenylate cyclase and thus inhibit acid secretion?

A

Gi

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5
Q

what is the primary etiology of peptic ulcer disease?

A

H. Pylori

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6
Q

how can you diagnose an H. pylori infection?

A

blood antibody test or urea breath test

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7
Q

what are the 3 major overall goals for the treatment of peptic ulcer disease?

A
  1. eradication of H. pylori (abx-tetracycline, clarithromycin, metronidazole)
  2. relief of symptoms (antisecretory agents, antacids)
  3. healing of ulcerations (prostaglandin agonists, bismuth, sucrasulfate)
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8
Q

MOA of antacids

A

neutralize gastric acid in the stomach

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9
Q

how high do you need to get the pH if you want to prevent the transformation of pepsinogen to pepsin?

A

pH >4

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10
Q

what are the 3 main ingredients in antacids?

A

aluminum hydroxides
magnesium hydroxids
calcium carbonate

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11
Q

aluminum hydroxides can have what side effect?

A

constipation

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12
Q

magnesium hydroxides can have what adverse effect?

A

diarrhea

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13
Q

what are the therapeutic uses of antacids?

A

simple dyspepsia

adjuncts to primary therapy w/ H2 blockers or PPIs

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14
Q

when should you take antacids for them to be most effective?

A

1-3 hrs after a meal and at bedtime

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15
Q

H2 receptor antagonists MOA

A

highly selective competitive inhibitor of H2 receptor

  • inhibit basal, food-stimulated, and nocturnal gastric acid secretion
  • reduce both volume and concentration of acid secretion
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16
Q

name the most potent h2 receptor antagonist?

A

famotidine

17
Q

how often does famotidine need to be administered?

A

once daily because it has a long half life

18
Q

what if the only notable side effect of cimetidine?

A

inhibits CYP450

19
Q

PPI MOA?

A

noncompetitive irreversible inhibitor of the H+/K+ ATPase enzyme
result–>achlorhydria-all gastric acid secretion is blocked

20
Q

which 2 PPIs are effective orally b/c they have a long duration of action and are more powerful?

A

omeprazole & esomeprazole

21
Q

which PPI is metabolized to a much lower extent by the cytochrome P450 system?

A

rabeprazole

22
Q

how do the PPIs effectively reach their target tissue?

A

has enteric coating

  • in neutral pH the PPI prodrug is stable
  • lipid solubility permits absorption
  • then carried by blood and diffuse into the secretory canaliculi, where the acid pH causes protonation and trapping of the drug near the proton pump
23
Q

what are the clinical indications for PPIs?

A

short term treatment of PUD, management of ZES & in refractory gastric, esophageal and duodenal ulcers
-manage symptoms of GERD

24
Q

how does bismuth subsalicylate work?

A

enhances secretion of mucus & bicarb

  • inhibits pepsin activity
  • chelates w/ proteins at the base of the ulcer crater and forms a protective barrier against acid and pepsin
  • effective treatment of traveler’s diarrhea
25
Q

how does sucralfate work>

A

forms sticky viscous gel that adheres to gastric epithelial cells protecting them from acid and pepsin

26
Q

___________is the only agent in its calss that requires an acidic pH for its maximal activity

A

sucralfate

27
Q

when does sucralfate need to be given to promote gastric healing?

A

given 1 hr before meals and at bedtime

28
Q

which drug is used in H2-blocker or PPI-induced pneumonia in bedridden pts?

A

sucralfate

-when stomach becomes too basic this can reintroduce harmful bacteria

29
Q

how does metochloparmide work?

A

dopamine-2 receptor blockers

-w/i GI tract blocking D2 receptors increases the local release of ACh via 5HT4-R agonism

30
Q

name the 5 abx that are used to eradicate H. pylori

A
  1. clarithromycin
  2. amoxicillin
  3. tetracycline-2nd line
  4. metronidazole
  5. furazolidine-nitrofuran antibacterial & antiprotozoal
31
Q

what are 2 conditions that cause a reflux episode to occur?

A
  1. GI contents must be ready to reflux

2. the anti-reflux mech. at the LES is compromised

32
Q

name the 5 aspects of postural & dietary therapy of GERD?

A
  1. decrease gastric contents (size of meal)
  2. decrease weight
  3. bed elevation
  4. low fat diet
  5. avoid coffee, peppermint
33
Q

what are the pharmacological actions of the dopamine-2 receptor blockers?

A

stimulates GI smooth muscle
increases amplitude of esophageal contractions
accelerates gastric emptying
increases LES pressure
MAIN ANTIREFLUX= ENHANCED GASTRIC EMPTYING

34
Q

what are some of the side effects of dopamine-2 receptor blockers?

A

related to central dopaminergic antagonism like tardive dyskinesia
-prescribe for 1-2 wks only

35
Q

what are the 2 classes of antisecretory drugs used to treat GERD?

A

H2 receptor blockers

proton pump inhibitors

GI (12 decks)

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