Ch.35a: Gastrointestinal Pharmacology (Hill) Flashcards

1
Q

3 strategies to prevent gastric ulceration

A

1) buffer acid
2) inhibit receptors (i.e. histamine, gastrin, ACh, PG)
3) inhibit H:K ATPase in parietal cell

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2
Q

Groups of agents that prevent gastric ulceration

A
  • antacids
  • H2 inhibitors
  • H:K ATPase (proton pump) inhibitors (PPI)
  • mucosal protectants (chelating and complexing agents)
  • prostaglandin analogs (misoprostol)
  • prokinetics (cisapride)
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3
Q

disadvantages of antacids

A
  • requires frequent administration

- divalent cations inhibit enrofloxacin absorption**

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4
Q

name 2 H2 inhibitors. Which interfere with P450 in the liver? Which is a prokinetic?

A

1) ranitidine - interferes with P450, is a prokinetic**

2) famotidine

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5
Q

Name 3 PPI

A

omeprazole
pantoprazole
lansoprazole

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6
Q

when should PPI be given?

A

before a meal, BID because they work best on open, active pumps

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7
Q

omeprazole features of note

A
  • a PPI
  • given ORALLY
  • less expensive than other PPIs
  • best for keeping gastric pH normalized
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8
Q

pantoprazole features of note

A
  • a PPI

- given IV, so can be used on anorexic patients**

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9
Q

Lansoprazole features of note

A
  • a PPI

- formulated with HCO3 as oral liquid for small dogs

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10
Q

Sucralfate features of note

A
  • a mucosal coating chelating and complexing agent**
  • a prodrug converted by acid that coats stomach lesions + an Al antacid
  • Al antacid component inhibits enrofloxacin absorption
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11
Q

which is longer acting: famotidine or ranitidine?**

A

famotidine. Also more expensive

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12
Q

Name 4 antagonists of parietal cell acid secretion**

A

1) gastrin antagonists
2) prostaglandin AGONISTS
3) H2 antagonists
4) muscarinic antagonists

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13
Q

Name a prostaglandin analog

A

misoprostol

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14
Q

Misprostol features of note

A
  • a prostaglandin analog
  • low dose: stimulates blood flow (blood flow is a key mech. of controlling ulceration in the stomach!!)
  • high dose: antacid
  • prevents ulcers from aspirin
  • does NOT prevent hemorrhage from pred.
  • can induce labor/abortion
  • used to tx NSAID overdose
  • very expensive
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15
Q

aspirin inhibits/stimulates prostaglandin production

A

inhibits

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16
Q

Name 3 classes of drugs that promote (induce) vomiting

A
dopamine agonists (apomorphine)
alpha-2 agonists (xylazine)
gastric irritants (hydrogen peroxide)
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17
Q

2 part model for vomiting composed of:

A

1) chemoreceptor trigger zone (CRTZ) in dorsal medulla

2) vomiting center in reticular formation

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18
Q

Best way to induce vomiting in DOGS***

A

apomorphine (DA agonist) applied to conjunctiva. (Cats don’t have DA receptors!)

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19
Q

Best way to induce vomiting in CATS***

A

xylazine (alpha-2 agonist)

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20
Q

apomorphine MOA

A

DA agonist; acts through CRTZ

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21
Q

Drugs/classes of drugs that reduce vomiting (7)**

A

1) M1 inhibitors (scopolamine, pirenzipine)
2) H1 inhibitors (diphenhydramine)
3) Alpha-2 antagonists/Phenothiazines (Chlorpromazine, Prochlorperazine, Acepromazine)
4) DA antagonists (Metoclopramide)
5) 5HT3 antagonists (Ondansetron)
6) Neurokinin receptor antagonists (Maropitant)
7) Antimuscarinics (Centrine)

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22
Q

Where do most antiemetics act?

A

CRTZ

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23
Q

Name 2 classes of drugs for motion sickness/reduce vomiting

A
M1 (Ach receptor) inhibitors (scopolamine, pirenzipine)
H1 inhibitors (diphenhydramine)
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24
Q

Name 3 alpha-2 antagonists/Phenothiazines and their effects

A

All 3 reduce BP, antiemetics

1) chlorpromazine
2) prochlorperazine
3) Acepromazine: also anti-motion sickness

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25
Q

Where do M1 inhibitors act?

A

vestibular apparatus and CRTZ

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26
Q

Where do H1 inhibitors act?

A

vestibular apparatus

27
Q

name a dopamine antagonist

A

metoclopramide

28
Q

features of metoclopramide

A
  • DA agonist
  • antiemetic
  • crosses BBB
  • may cause extrapyramidal effects (tremor)
  • a PROKINETIC (promotes gastric emptying)
29
Q

Name a 5HT3 (serotonin) receptor antagonist. Characteristics?

A

ondansetron:

  • antiemetic
  • may slow colonic transit
  • expensive
30
Q

Name a neurokinin (NK1) receptor antagonist. Chars.?

A

Maropitant (“Cerenia”):

  • antiemetic (acts on vomiting center and CRTZ)
  • can be used in combo with 5HT3 antagonists, but has many drug interactions
  • approved for motion sickness
31
Q

Which antiemetics used in dogs but not cats?**

A

H1 inhibitors
DA antagonists (Metoclopramide)
Maropitant (“Cerenia”) not licensed in cats, but still used

32
Q

name an antimuscarinic. Chars.?

A

Centrine:

  • weak antiemetic
  • reduces SI motility and gastric emptying (paralyzes the gut)
  • block prokinetics
  • NOT recommended to use
33
Q

Name 6 PROKINETICS (promoters of GI motility)***

A
metoclopramide**
cisapride**
5HT4 agonists**
Bethanacol**
Ranitidine**
Erythromycin
Thoracic epidural analgesia for post-op ileus
Octreotide
34
Q

Cisapride features of note

A
  • prokinetic
  • serotoninergic agent (mixed 5HT3 antagonist/5HT4 agonist)
  • promotes Ach release in SI
  • causes fatal dysrhythmia in humans
35
Q

Bethanacol features of note

A
  • prokinetic

- limited use due to SLUD

36
Q

Ranitidine MOA as a prokinetic

A

inhibits acetylcholinesterase and blocks H2

37
Q

SLUD =

A

salivation, lacrimation, urination, defecation

38
Q

2 types of motility in the stomach

A

1) FED: rapid contractions against closed pylorus to churn up food
2) UNFED: housekeeping clearing action about every 100 mins. when stomach is empty. Stimulated by Migrating Myoelectrical Complex (MMC)

39
Q

2 types of contractility in the bowel

A

propulsive and mixing

40
Q

Prokinetics general MOA

A

act on enteric nerves to increase cholinergic neurotransmission. They increase strength of propulsive contractions, improve antroduodenal coordination, and smooth m. tone.

41
Q

Octreotide features of note

A
  • an antiemetic
  • a somatostatin analog
  • must be given frequently
  • expensive, not used frequently
42
Q

Name 3 types of antidiarrheals

A

1) morphine agonists (loperamide, diphenoxalate)
2) inhibitors of SI secretion (bismuth subsalicylate)
3) absorbents (kaolin, activated charcoal)

43
Q

Name 2 morphine agonist antidiarrheals

A

Loperamide, Diphenoxalate

44
Q

Loperamide features of note***

A
  • morphine agonist (antidiarrheal)
  • slows transit and aids absorption
  • does NOT cross BBB, doesn’t cause sedation
  • is like a cork!
45
Q

Diphenoxalate features of note**

A

-morphine agonist (antidiarrheal)
-slows transit and aids absorption
slightly crosses BBB, can cause some sedation
-also inhibits secretion

46
Q

Name an inhibitor of SI secretion. MOA?

A
bismuth subsalicylate ("Pepto Bismol"):
inhibits PG and cAMP
47
Q

Name 2 absorbent antidiarrheals

A

Kaolin, Activated Charchoal

48
Q

Q: what antibiotic should you give for acute GI disease?***

A

NONE! (avoid if possible because will destabilize intestinal flora)

49
Q

What kind of bacteria are in upper intestine?**

A

G+ and -

50
Q

What kind of bacteria are in lower intestine?**

A

G- and anaerobes

51
Q

advantage of enrofloxacin. When should you use it?**

A

Doesn’t disrupt anaerobes

-use for Salmonella, acute pancreatitis, Boxer Colitis

52
Q

What abx should be used for clostridial colitis?

A

metronidazole
tylosin
vancomycin

53
Q

What tx should be used for Helicobacter?

A

combination of PPI (omeprazole) and abx

54
Q

tx for Small Intestinal Dysbiosis/SI Bacterial Overgrowth***

A

tetracycline
metronidazole
tylosin

55
Q

Name anti-inflammatory and immunosuppressive agents

A

1) Prednisone/Prednisolone
2) Dexamethason
3) Budesonide
4) Azathioprine
5) Cyclosporine
6) Leflunamide
7) Sulfasalazine (an aminosalicylate)
8) Olsalazine (an aminosalicylate)
9) Bismuth subsalicylate

56
Q

Sulfasalazine MOA

A
  • anti-inflamm/immunosuppressive
  • acts like aspirin
  • inhibits prostaglandin prod.
  • a pro-drug
57
Q

Name 2 osmotic agents that act as laxatives

A

magnesium sulfate

Colyte

58
Q

Name 6 laxatives and their MOA

A

magnesium sulfate (osmotic agent)
colyte (osmotic agent)
psyllium (bulk forming osmotic agent-soluble fiber)
lactulose (bulk forming osmotic agent-insoluble fiber)
mineral oil (lubricant)
petrolatum (lubricant)

59
Q

Name 5 agents that treat round worms

A

Benzimidazoles (i.e. Panacur)
Pyrantel (strongid)
Ivermectin
Emodepside (Profender)

60
Q

What treats tapeworm?

A

Praziquantel (Droncit)

61
Q

Which agents treat whipworms?**

A
Fenbendazole (Panacur)
Febantel (in Drontal Plus)
Moxidectin (in Advantage Multi)
Milbemycin (interceptor, Trifexis)
Emodepside (Profender)
62
Q

Probiotics

A

Population determined by food supply and environment, so must use every day or immediately eliminated. Ex:

  • Lactobacillus in yogurt
  • Bacillus cereus
  • Enterococcus faecium (in Purina)*
  • Bifidobacterium animalis (in Iams)*
  • Saccharomyces
63
Q

Prebiotics examples

A
  • oligo-saccharides: FOS, soy
  • poly-saccharides in soluble fiber: pectins, gums
  • mixed soluble and insoluble fibers: beet pulp