B5-048 GI Pharmacology Flashcards

1
Q

most common secretory disorders

A

acid-peptic disease
GERD

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2
Q

most common motility disorders

A

vomiting
diarrhea
constipation

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3
Q

list the mediator, receptors, and antagonist for the neural pathway

A

mediator: Ach
receptor: muscarinic
antagonist: anti-muscarinic

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4
Q

list the mediator, receptors, and antagonist for the endocrine pathway

A

mediator: gastrin
receptor: CCKB
antagonist: H2 blocker

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5
Q

list the mediator, receptors, and antagonist for the paracrine pathway

A

mediator: histamin
receptor: H2
antagonist: H2 blocker

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6
Q

classes that inhibit gastric acid secretion

2

A

proton pump inhibitors
H2-antagonists

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7
Q

class that neutralizes gastric acid secretion

A

antacids

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8
Q

irreversibly inhibit the parietal cell proton pump

A

benzimidazole

PPI

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9
Q

proton pump inhibitors are […] that are […] at a neutral pH

A

prodrugs
inactive

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10
Q
  • activated by acid, but unstable at low pH
  • enteric coating only dissolves at alkaline pH
A

PPIs

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11
Q

how do PPIs maintain efficacy even with chronic use?

A

parietal intracellular canaliculi are upstream from the proton pump

remains acidic even when proton pump is inhibited

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12
Q

-prazole

A

proton pump inhibitor

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13
Q

most effective drug for suppressing gastric acid secretion

supresses 90-95%

A

proton pump inhibitors

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14
Q

with prolonged use, diarrhea occurs due to GIT bacterial overgrowth from removal of natural acidic barrier

A

PPIs

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15
Q

inhibition of gastric acid secretion persists after withdrawal of drug due to irreversible inhibition

A

PPIs

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16
Q

-tidine

A

H2 receptor antagonists

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17
Q

reversible block of H2 receptors leading to decreased H+ secretion by parietal cells

A

H2 antagonists

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18
Q
  • OTC preparations that block acid secretion for about 6 hrs
  • only inhibits 60-70% of acid secretion
A

H2 receptor antagonist

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19
Q

especially effective againsts nocturnal acid secretion

A

H2 receptor antagonists

largely driven by histamine

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20
Q

relative potency of H2 receptor antagonists

A

famotidine > nizatidine = ranitidine > cimetidine

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21
Q

block H2 receptors selectively to reduce gastric acid and pepsin secretion

A

H2 receptor antagonists

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22
Q

20% failure in ulcer patients who smoke and elderly

A

H2 receptor antagonists

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23
Q

should not be used in combination with PPI

A

H2 receptor antagonists

reduce efficacy

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24
Q

most common side effects of H2 receptor antagonists

A

diarrhea
headache
fatigue
myalgias
constipation
bradycardia

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25
Q

mental changes like confusion, hallucinations, and agitation may occur with IV infusion of […] in elderly or renal/hepatic dysfunction

A

H2 receptor antagonists

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26
Q
  • endocrine side effects due to androgen receptor binding
  • gynecomastia, impotence, galactorrhea
A

cimetidine

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27
Q

interferes with cytochrome P450 pathways

A

cimetidine

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28
Q

antacids

3

A
  • aluminum hydroxide
  • calcium carbonate
  • aluminum hyroxide/magnesium hydroxide
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29
Q

weak bases that neutralize gastric HCl to form salt and water

A

antacids

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30
Q

popular due to low cost and rapid action but may cause rebound acid oversecretion

A

antacids

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31
Q

rebound acid secretion

A

antacids

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32
Q

why are magnesium and aluminum typically combined in an antacid preparation?

A

mag causes diarrhea
aluminum causes constipation

offset each other

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33
Q
  • establish protective coating on peptic ulcers
  • limit exposure to acid/pepsin
A

musocal protective agents

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34
Q

binds selectively to necrotic ulcer tissue and acts as a barrier

A

sucralfate

mucosal protective agent

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35
Q

common side effect of sucralfate

A

constipation

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36
Q

requires acid pH for activation so should not be given with PPIs, H2 antagonists, or antacids

A

sucralfate

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37
Q

methyl analog of PGE1

A

misoprostol

muscoal protective agent

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38
Q

binds to PG receptors on parietal cells to inhibit acid secretion

A

misoprostol

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39
Q

used to prevent NSAID induced ulcers

A

misoprostol

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40
Q

most common adverse effects of misoprostol

A

diarrhea
abdominal pain

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41
Q

may cause abortion by stimulating uterine contractions

A

misoprostol

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42
Q
  • protective coating of ulcers
  • antibacterial against H pylori
A

bismuth subsalicylate (pepto)

mucosal protective agent

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43
Q

will darken tongue and stools as side effect

A

bismuth subsalicylate

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44
Q

gram negative bacterium causing inflammatory gastritis that contribute to peptic ulcers

A

H. pylori

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45
Q

are single antibiotic regimens effective against H pylori?

A

no

46
Q

triple therapy for Peptic Ulcer Disease/H. pylori

A
  • clarithromycin
  • amoxicillin
  • PPI

if allergic to pen, metronidazole

47
Q

mucosal protective agents

3

A
  • bismuth subsalicylate
  • misoprotrol
  • sucralfate
48
Q

single most commonly reported drug side effect

A

nausea/vomiting

49
Q

saline laxatives

2

A

magnesium citrate
sodium phosphate

50
Q

act by osmotic force to draw water into the intestinal lumen -> distension -> peristalsis

A

saline laxatives

51
Q

intensely bitter taste

A

saline laxatives

52
Q

trihydroxy alcohol that acts in rectum as lubricant and hygroscopic agent -> water retention -> perstalsis

A

glycerin

53
Q

hydrolyzed to organic acids -> acidify luminal contents -> draw water into lumen -> increase colonic propulsive motility

4

A

lactulose
sorbitol
lactitol
mannitol

54
Q

poorly absorbed and retain added water by their high osmotic pressure

A

PEG solutions

55
Q

typical colonoscopy prep
3-4 L over 3-4 hours

A

PEG solution

56
Q

mixtures of sodium sulfate, sodium bicarb, sodium chloride, and postassium chloride in isotonic solution

A

PEG solution

57
Q

osmotically active laxatives

A

saline
sugars
PEG solution

58
Q

act directly on enterocytes, neurons and muscle to induce low-grade inflammation to increase intestinal motility

A

stimulant/irritant laxatives

59
Q

diphenylmethane derivatives

2

A

bisacodyl
phelophthalein (not really used, carcinogen)

60
Q

bisacodyl should be taken at [time of day]
and [method of intake] to avoid activation in the stomach

A

bedtime
swallowed without chewing

61
Q

long term use causes melanomic pigmentation of colonic mucosa and “cathartic colon”

A

anthraquinones

62
Q

aloe
cascara sagrada
senna

are…

A

anthraquinones

63
Q
  • local irritant that increases intestinal secretion and motility
  • seldom used due to taste and toxic potential
A

castor oil

ricinoleic acid

64
Q

bulk forming laxatives

3

A

methylcellulose
lactulose
polycarbophil

65
Q

bulk forming laxatives require adequate

A

hydration

66
Q

stool softners

A

mineral oil, glycerin suppositories, docusate sodium

67
Q

ofter prescribed to prevent straining in hospitalized patients

A

docusate sodium

68
Q
  • Mu agonists relatively selective for intestinal opioid receptors
  • inhibit ACh to decrease motility

3

A

loperamide
difenoxin
diphenoxylate

low efficacy opiods

69
Q

very effective against traveler’s diarrhea
works quickly

A

loperamide

70
Q

antidiarrheals

4

A
  • mu agonists
  • kaolin/pectin
  • bismuth subsalicylate
  • somatostatin/octreotide
71
Q
  • acts by absorbing compounds and resumably bindings potential intestinal toxins
  • increases viscostiy of luminal contents
A

kaolin/pectin slurry

72
Q
  • reduces portal and splanchnic blood flow
  • inhibits secretion of intestinal hormones
  • reduces intestinal fluid and pancreatic secretion
  • reduces gallbladder contractility
A

somatostain/octreotide

73
Q

histamine H1 antagonists

4

A
  • dimenhydrinate
  • diphenhydramine
  • cyclizine
  • meclizine
74
Q

produce sedation and antimuscarinic activity to prevent motion sickness

A

Histamine H1 antagonists

75
Q

D2 antagonists

2

A

metoclopramide
trimethobenzamine

76
Q

5-HT3 antagonists

3

A

ondansetron, granisetron, dolasetron

-setron

77
Q

used for nausea and vomiting during cancer chemotherapy

A

5-HT3 antagonists

-setron

78
Q

NK-1 antagonists

3

A

aprepitant
fosaprepitant
rolapitant

-pitant

79
Q

-setron

A

5-HT3 antagonists

80
Q

-pitant

A

NK-1 antagonists

81
Q

anti-emetics classes with unclear MOA

A

D2, 5-HT3, and NK-1 antagonists

82
Q

phenothiazines and benzodiazepines used as anti-emetics

4

A

p: chlorpromazine, prochlorperazine

b: lorazepam, alprazolam

83
Q

marijauna derivatives used as anti-emetics

2

A

THC
dronabinol

84
Q

used as a prophylactic in patients receiving cancer chemotherapy

A

dronabinol

85
Q

adverse effects include increaased central sympathetic chain activity causing mood changes, laughing, paranoid reactions, and thinking abnormalities

A

THC/dronabinol

86
Q

artificial sweeteners, a-glucosidase inhibitors, osmotic laxatives cause….

A

osmotic diarrhea

87
Q

caffeine, chemotherapeutic agents, colchicine, metformin, NSAIDs, simvastin, and cholinesterate inhibitors cause…

A

secretory diarrhea

88
Q

cholinesterase inhibitors and antibiotic drugs cause…

A

motility diarrhea

89
Q

NSAIDs, oral contraceptives, PPIs, SSRIs, stimulant laxatives, chemo agents cause…

A

inflammatory diarrhea

90
Q

drugs that draw water and ions into the intestinal luman cause…

A

osmotic diarrhea

91
Q

drugs that cause and imbalance between absorption and secretion into lumen cause…

A

secretory diarrhea

92
Q

large volumes of stool, lack of red or white cells in stool, absence of other symptoms indicates

A

secretory diarrhea

93
Q

drugs that increase or decrease MMC activity cause…

A

motility diarrhea

94
Q

hypomotility results in stasis that allows for

A

bacterial overgrowth

95
Q

drugs that disrupt epithelium in GI tract cause…

A

inflammatory diarrhea

96
Q

associated with collagenous and lymphocytic collitis

A

PPIs

97
Q

SSRIs are commonly associated with […] diarrhea

A

inflammatory

paroxetine, sertraline

98
Q

drugs that commonly produce constipation

A

anticholinergic
antidepressants (TCAs)
diphenhydramine
trimethaphan
iron supplements
Opiods

there’s more but i’m lazy

99
Q

constipation from opiods is

A

does dependent and predictable

100
Q

no tolerance develops toward

A

opiod induced constipation

101
Q

coadministration of these with opiods will help prevent constipation

2

A
  • naloxone
  • methylnaltrexone
102
Q

mucosal agent that can protect GI lining from acid, but does not darken tongue or stools

A

sucralfate

103
Q

requires acidic environment for conversion to active drug form

A

PPIs

-prazole

104
Q

bisocodyl and senna are […] laxatives

A

irritant

105
Q

reduce the protection of protective prostaglandins that shield stomach wall from degradation by low pH environment

A

non selective COX inhibitors

NSAIDs

106
Q

low efficacy opiod with selectivity for the GI tract that reduces motility and symptoms of travelers diarrhea

A

diphenoxylate

107
Q

antibiotics used in the treatment of H pylori in PED

A

amoxicillin
metronidazole

108
Q

pro-drugs that require the conversion to an active drug in the acid containing canaliculi in the gastric parietal cells in order to bind and inhibit

A

PPIs

-prazoles

109
Q

antihistamine selective for H2 receptors that reduce acid production and esophageal irritation

A

-tidines

rantidine, nizatidine

110
Q

what class does trimethobenzamide belong to

A

D2 receptor antagonist

antiemetic