GI Pharmacology Flashcards

1
Q

Gastroprotectants (5)

A
  1. Antacids
  2. H2 Blockers
  3. Proton Pump Inhibitors
  4. Sucralfate
  5. Misoprostol
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2
Q

Anti-emetics (3)

A
  1. Maropitant
  2. 5-HT3 antagonists
  3. Metoclopramide
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3
Q

Prokinetics (3)

A
  1. Metoclopramide
  2. Cisapride
  3. Erythromycin
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4
Q

Appetite Stimulants (4)

A
  1. Capromorelin
  2. Mirtazapine
  3. Cyproheptadine
  4. Dronabinol
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5
Q

Antidiarrheals (4)

A
  1. Bismuth-subsalicylate
  2. Kaolin-pectin
  3. Opioids
  4. Anticholinergics
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6
Q

Three Stimuli for Gastric Acid Secretion and where they come from

A
  1. Acetylcholine (from the vagus nerve)
  2. Gastrin (from G cells)
  3. Histamine (from ECL cells)
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7
Q

Most important gastric acid mediator?

A

Gastrin

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8
Q

parietal cells

A

those which secrete gastric acid into the lumen via proton pumps

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8
Q

Diseases of Hyperacidity

A
  1. Mast Cell Tumors (release histamine)
  2. Gastrinomas (rare but release gastrin)
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8
Q

Why should we be careful when we suppress gastric acid?

A

It is important for digestion and also acts as a physical barrier in the small intestines. Acidic environments are also required for some drug administration so must be careful thinking about interactions.

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9
Q

Diseases of Damaged Mucosa

A
  1. Esophageal Diseases
  2. GI Ulcers
  3. Gastritis/Gastroenteritis
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10
Q

Antacids

A

bases combined with Al, Ca, or Mg that directly neutralize gastric acid

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11
Q

Examples of Antacids

A

TUMS, Maalox, Mylanta

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12
Q

Side Effects of Antacid Use

A

overall safe, but way overused therefore poorly effective, and also may bind other drugs causing reduced absorption

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13
Q

H2 Receptor Antagonists (Blockers)

A

blocks histamine stimulation of acid secretion; RAPID onset

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14
Q

Most Potent H2 Blocker

A

Famotidine (Pepcid)

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15
Q

Least Potent H2 Blocker

A

Cimetidine

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16
Q

Side Effect of Cimetidine

A

also a P450 inhibitor, meaning possible drug interactions

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17
Q

Side Effects of H2 Blocker Use in General

A

minimal adverse effects but tolerance can develop

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18
Q

Proton Pump Inhibitors (PPI)

A

directly inhibits acid release from parietal cells; slower onset (3-4 days)

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19
Q

Which is more effective - H2 blockers or PPIs?

A

PPIs

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20
Q

Examples of PPIs

A

the -prazoles

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21
Q

Side Effects of PPIs

A

in dogs = diarrhea
in humans = gastric hypertrophy

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22
Q

Sucralfate MOA

A

aluminum-containing polysaccharide which coaters ulcer craters, inhibits pepsin, and increases mucosal PGE

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23
Q

Indications for Sucralfate Use

A

gastric or duodenal ulceration
reflux esophagitis

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24
Q

How should sucralfate be administered?

A

SLURRY, and apart from other drugs and food!

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25
Q

Side Effects of Sucralfate

A

potential for lots of drug interactions (including ciprofloxacin and doxycyline)

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26
Q

Misoprostol MOA

A

PGE1 analog which increases mucosal blood flow, increases bicarbonate and mucus secretion, and also increases mucosal turnover

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27
Q

Indications for Misoprostol Use

A

prevents NSAID-induced ulcers, and also use in response to NSAID overdose/toxicity

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28
Q

Can misoprostol be used for steroid induced ulcers?

A

no

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29
Q

Side Effects of Misoprostol

A

cramping and diarrhea, also abortion

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30
Q

Who should absolutely not handle misoprostol?

A

pregnant women

and everyone should just wear gloves!

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31
Q

Most effective veterinary emetic?

A

Maropitant (Cerenia)

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32
Q

Maropitant MOA

A

blocks substance P binding to NK-1 receptors in the emetic center, CRTZ, and gut

33
Q

CRTZ

A

chemoreceptor trigger zone

34
Q

Indica Maropitant Use

A

acute gastroenteritis
renal/hepatic diseases
chemotherapy
motion sickness/vestibular disease

35
Q

Side Effects of Maropitant Use

A

possible pain on injection, maybe sedation; can also mask clinical signs

36
Q

Routes of Administration of Maropitant

A

PO
SQ
IV

37
Q

Maropitant Dose PO vs. IV in Dogs

A

PO dose will be 2x the IV dose

38
Q

Maropitant Dose PO vs. IV in Cats

A

PO and IV dose is the same

39
Q

Ondansetron

A

5HT3 antagonist (serotoninergic receptor) in the CRTZ and emetic centers

40
Q

What serotonin receptor is present in the emetic center?

A

HT3 (and a little HT2)

41
Q

Adverse Effects of Ondansetron in Animals?

A

none

42
Q

Can ondansetron and maropitant be used together?

A

yes

43
Q

Metoclopramide ANTIEMETIC MOA

A

5-HT3 and DA2 (dopamine) antagonists at the CRTZ

44
Q

Is metoclopramide more effective than maropitant and ondansetron?

A

no, it usually isn’t used for antiemetic purposes anyway

45
Q

Side Effects of Metoclopramide Use

A

excitation, diarrhea, cramping

46
Q

Dirty Drug

A

high rate of unintended effects

47
Q

Cisapride MOA

A

5-HT4 agonist (serotoninergic receptor) that moves the gut along (prokinetic)

48
Q

Indications for Cisapride Use in Dogs

A

prevent reflux by increasing lower esophageal sphincter tone

49
Q

Indications for Cisapride Use in Cats

A

colonic dysmotility, megacolon

50
Q

Indications for Cisapride Use in Horses

A

colic

51
Q

Why is cisapride not readily available?

A

causes severe arrythmias in humans, but has NOT been seen in animals

therefore needs to be COMPOUNDED

52
Q

Metoclopramide PROKINETIC MOA

A

5-HT4 agonist and dopamine antagonist and acts on the smooth muscle of the GI tract (mainly upper GI vs. colon)

53
Q

Indications for Metoclopromide Use

A

functional ileus (postop, enteritis, pancreatitis, foreign bodies); sometimes esophageal disease but doesn’t work as well as cisapride

54
Q

What prokinetic can be administered as a CRI?

A

metoclopramide

55
Q

Erythromycin Prokinetic MOA

A

macrolide antibiotic which can stimulate motilin receptors in the stomach and upper small intestine to enhance gastric emptying

56
Q

Which does is higher for erythromycin - prokinetic or antibiotic?

A

antibiotic (like, way higher)

57
Q

ghrelin

A

secreted in stomach during fasted states and stimulates hunger directly via hunger centers and indirectly via the vagus nerve; also stimulates growth hormone

58
Q

Capromorelin MOA

A

ghrelin agonist

59
Q

Side Effects of Ghrelin

A

weight gain, insulin resistance

60
Q

Contraindications to Capromorelin Use?

A

Diabetic and prediabetic patients!

61
Q

Brand Names for Capromorelin

A

Entyce and Elura

62
Q

Side Effects of Capromorelin in Dogs

A

diarrhea and lethargy

63
Q

Side Effects of Capromorelin in Cats

A

vomiting and hypersalivation

64
Q

Difference between Entyce and Elura?

A

concentration - that way both solutions are the same dose by weight (0.1mg/kg)

65
Q

Mirtazapine MOA

A

as an APPETITE STIMULANT inhibits 5-HT2 and 3 receptors at the CRTZ and orexigenic centers

mirtazapine also used as an antidepressant with complicated MOAs

65
Q

Routes of Mirtazapine Administration

A

oral (human approved) and transdermal (vet approved)

66
Q

Side Effects of Mirtazapine

A

mainly behavioral, including:
vocalization
agitation
vomiting
ataxia

67
Q

Cyproheptadine

A

similar to mirtazapine (serotonin antagonism at orexigenic centers) but no longer commonly used since we have a veterinary approved alternative; same side effects (excitation/aggression)

68
Q

Dronabinol

A

synthetic THC that acts via the CB1 receptor in orexigenic and emetic centers

extra-label use in animals for chronic illness and appetite stimulation, but a schedule II - III drug

69
Q

Do we use antidiarrheals a lot in vet med?

A

nah, because we really wanna find the cause (but used commonly with chemo because we know that’s the cause)

70
Q

Can bismuth-subsalicylate be used in cats?

A

absolutely not, it’s toxic! (the salicylate part)

71
Q

Indications for Bismuth-subsalicylate

A

acute diarrhea in dogs

72
Q

Side Effects of Bismuth-subsalicylate and Kaolon-Pectin

A

can interfere with drug absorption

73
Q

Kaolin-Pectin

A

GI protectant and adsorbent effective in both dogs and cats

74
Q

Examples of Opioids as Antidiarrheals

A

Imodium and Lomotil

75
Q

Opioid ANTIDIARRHEAL MOA

A

increased segmental contractions to decrease downstream movement (more time for absorption)

76
Q

Indications for Opioid Antidiarrheal Use

A

acute (<48 hours), non-infectious diarrheas, chemo-associated, or a rare primary motility disorder

77
Q

Contraindications for Opioid Antidiarrheal Use

A

infectious diarrhea
obstruction
cats
dogs with MDR1 mutation

78
Q

Side Effects of Opioids as Antidiarrheals

A

cramping and abdominal discomfort

79
Q

Anticholinergics

A

muscarinic cholinergic antagonists which block Ach receptors on gut smooth muscle

80
Q

Are anticholinergics used for diarrhea? Why or why not?

A

NO
it can mask progression of signs, mimic obstruction on AXR, and enhance endotoxin absorption