Gastrointestinal pharmacology Flashcards

1
Q

Which of the following is not a drug acting on the GI system?

  1. Antidiarrheals
  2. Cathartics
  3. Emetics
  4. Prokinetics
  5. Anti-ulcer medications
  6. Antiemetic
  7. All of the above
A
  1. All of the above
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2
Q

What are stimulants of appetits?

A
  • Norepinephrine (alpha-2)
  • Dopamine (D1 receptors)
  • GABA (by inhibiting the satiety center)
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3
Q

What inhibits appetite?

A

Serotonin (5-HT1)

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4
Q

Which drugs are most commonly used as appetite stimulants to “treat” anorexia/hyporexia?

A

GABA agonists

  • Benzodiazepines (Diazepam, Midazolam)
  • Propofol
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5
Q

Which drugs are serotonin (5-HT) antagonists to “treat” anorexia/hyporexia in cats and dogs?

A

Both are human label

  • Cyproheptadine in cats
  • Mirtazapine in dogs
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6
Q

Besides GABA agonists and Serotonin (5-HT) antagonists, which drugs have appetite stimulating effects to “treat” anorexia/hyporexia?

A
  • Glucocorticoids- Prednisone (good for inflammatory bowel disease)
  • B-vitamins
  • Megestrol acetate
  • Anabolic steroids- Stanozolol
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7
Q

Which GABA agonist appetite stimulant is more effective in cats than it is in dogs and is generally useful for short term only?

A

Benzodiazepines (Diazepam, Midazolam)

  • Stimulating GABA inhibits satiety center to increase appetite
  • Most common side effect is sedation
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8
Q

Which GABA agonist appetite stimulant has a very short-term (15 min) effect and should be used with caution in cats because it may cause Heinz body anemia if used for more than 5 days?

A

Propofol

  • Effect is seen at sub-hypnotic doses
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9
Q

Which appetite stimulant more commonly used in dogs than in cats, blocks both 5-HT1 and 5-HT2 receptors?

A

Mirtazapine

  • Serotonin (5-HT) antagonist
  • Also increases NE centrally
  • Cats dosed q1-3days
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10
Q

Which oral appetite stimulant is more effective in cats than it is in dogs and blocks 5-HT1 receptors?

A

Cyproheptadine

  • Serotonin (5-HT1) antagonist
  • Generally 2-3 days to see a response
  • Most common side effect is sedation
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11
Q

T or F. The emetic center and CRTZ (chemoreceptors) are both outside of the BBB.

A

False. The emetic center is inside the BBB while CRTZ is outside of the BBB

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12
Q

What is a peripherally acting emetic that is used for immediate treatment (typically at-home by client) by causing direct irritation of the oropharynx/GI lining, but should NOT be used in cats (hemorrhagic gastritis)?

A

Hydrogen peroxide 3%

  • Don’t use other peripheral antiemetics (more risk):
    • Syrup of ipecac
    • Saline solution
    • Dilute dish soap
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13
Q

Which centrally acting emetic can be given by all routes (including conjunctival sac) most effectively in dogs and stimulates dopamine (D2) receptors?

A

Apomorphine

  • Opioid
  • Cat efficacy only 10%
  • Overdose can cause respiratory depression- reverse with naloxone (note that IT WON’T REVERSE THE EMETIC EFFECT!)
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14
Q

Which centrally acting emetic is more effective in cats than it is in dogs because it is an alpha-2 agonists and cats have more alpha-2 receptors and fewer D2 receptors?

A

Xylazine or Dexmedetomidie (Dexdomitor)

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15
Q

[FYI] Which oral or injectable anti-emetic is a dopamine (D2) antagonist?

  1. Metoclopramide
  2. Maropitant (Cerenia)
  3. Ondansetron, (dolasetron)
A
  1. Metoclopramide
  • Intermittent SC or IV CRI
  • Also blocks 5-HT3 receptors at higher doses
  • Also a prokinetic
  • Antagonizes apomorphine induced emesis
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16
Q

[FYI] Which injectable anti-emetic (oral available) is more potent than metoclopramide and is a serotonin (5-HT3) antagonist?

  1. Metoclopramide
  2. Maropitant (Cerenia)
  3. Ondansetron, (dolasetron)
A
  1. Ondansetron, (dolasetron)
  • Acts on serotonin receptors centrally and peripherally
  • Initially used for chemotherapy related nausea
  • $$$
  • Usually given by injection
17
Q

[FYI] Which anti-emetic for dogs (oral or SC) and cats (SC) is a neurokinin inhibitor (NK1) receptor antagonist?

  1. Metoclopramide
  2. Maropitant (Cerenia)
  3. Ondansetron, (dolasetron)
A
  1. Maropitant citrate (Cerenia)
  • Labeled for prevention of motion sickness in dogs (oral)
  • Antagonists at NK1 receptors which blocks substance P and reduces it’s contribution to vomiting
  • Works at the level of the emetic center and the CRTZ
  • Substance P is involved in integration of pain, stress, anxiety, and vomiting
  • Injection stings!!: Reduce sting by refrigerating or diluting to administer
18
Q

[FYI] Which drug is used to antagonize apomorphine induced emesis?

A

Metoclopramide (Reglan)!

19
Q

[FYI] Which of the following is a common oral or injectable anti-ulcer drug that reduces gastric acid by blocking antihistamine H2?

  1. Misoprostol
  2. Omeprazole
  3. Famotidine
  4. Sucralfate
A
  1. Famotidine “Pepcid” (Cimetidine, Ranitidine, Nizatidine)
  • Also inhibits pepsin secretion
  • Competitive inhibition of H2 receptors
  • Cimetidine is an inhibitor of hepatic microsomal enzymes
  • Famotidine is more potent and longer lasting than cimetidine (also has far fewer drug interactions)
  • Ranitidine (Zantac) and Nizatidine have similar potency and duration to famotidine; also have some prokinetic activity (esp. in dogs)
20
Q

[FYI] Which of the following is a common oral anti-ulcer drug that reduces gastric acid by inhibiting proton pumps?

  1. Misoprostol
  2. Omeprazole
  3. Famotidine
  4. Sucralfate
A
  1. Omeprazole “Prilosec” (Pantoprazole and Lansoprazole are injectables)
  • Irreversibly inhibit H+/K+/ATPase proton pump resulting in decreased hydrochloric acid production
  • More potent than H2 blocker class
  • Raise gastric pH
  • Labeled equine product
21
Q

[FYI] Which of the following is an oral prostaglandin E1 analog that is used treat NSAID-induced gastric ulcers?

  1. Misoprostol
  2. Omeprazole
  3. Famotidine
  4. Sucralfate
A
  1. Misoprostol
  • Increases mucus and sodium bicarbonate secretion, stimulates epithelialization of the mucosa and mucosal blood flow resulting in ulcer healing (COX-1)
  • Mild direct decrease in acid production
  • Caution: abortifacient, can stimulate uterine contraction and cause diarrhea
22
Q

[FYI] What are some oral antacids used to treat/prevent ulcers by reducing gastric acid?

A

Aluminum, magnesium and calcium salts (Tums)

  • Chemically neutralize hydrochloric acid
  • Aluminum hydroxide also inactivates pepsin and binds to bile salts, may stimulate PGs
  • Bind phosphorous in the gut and can also cause constipation
23
Q

[FYI] Which of the following is a sucrose-aluminum compound given orally which acts as a gastroprotectant used to treat or prevent ulcers?

  1. Misoprostol
  2. Omeprazole
  3. Famotidine
  4. Sucralfate
A
  1. Sucralfate
  • Binds to the ulcer site and protects it against acid, pepsid and bile (requires an acidic environment to bind to mucosa)
  • May also stimulate protective PGs and antioxidants and increase mucosal blood flow
  • Poorly absorbed (acts locally) and has few side effects; constipation sometimes seen and binds to other drugs
24
Q

[FYI] The time it takes for material to get from point A to B within the GIT

A

Transit time

25
Q

Movement of the gut wall

A

Motility

26
Q

MATCHING! Which drugs increase the activity and which drugs decrease the activity of the GIT?

A. Increased activity

B. Decreased activity

  1. Norepinephrine
  2. Serotonin
  3. Peptides
  4. Endorphins
  5. Acetylcholine
  6. Dopamine
A

A. Increased activity:

    1. Serotonin (5-HT3)
    1. Peptides (motilin)
    1. Acetylcholine (parasympathetic

B. Decreased activity:

    1. Norepinephrine (sympathetic)
    1. Endorphins (opioids)
    1. Dopamine (opioids)
27
Q

[FYI] Which of the following drugs does not increase GI motility?

  1. Cholinergics such as neostigmine
  2. Atropine/Glycopyrrolate
  3. Lidocaine
  4. Metoclopramide (Reglan)
  5. Cisapride
A
  1. Atropine/Glycopyrrolate
  • Metoclopramide (Reglan) is a dopamine antagonist (Domperidone)
  • Cisapride is a serotonin (5-HT4) agonist (Mosapride)
  • Others such as Ranitidine and Erythromycin
28
Q

[FYI] Which of the following drugs does not decrease GI motility?

  1. Loperamide (Imodium)
  2. Atropine/Glycopyrrolate
  3. GI protectants/adsorbents
  4. Ranitidine
A
  1. Ranitidine
  • Atropine/Glycopyrrolate: anticholinergic side effect (Aminopentamide ‘Centrine’)
  • Loperamide (Imodium) is an opioid (Diphenoxylate and other opioids)
  • GI protectants/adsorbents such as magnesium/aluminum products, Bismuth subsalicylate (Pepto-bismol), and activated charcoal
29
Q

[FYI] What is the simplest enema? What kind of enemas should be avoided in cats?

A
  • Warm water is the simplest
  • Do not give phosphate enema to cats!
30
Q

[FYI] What type of cathartic irritates the GI mucosa to stimulate motility and secretions?

A

Irritant cathartics such as Bisacodyl (Dulcolax)

31
Q

[FYI] What type of laxatives absorb water from the lumen and swell up?

A

Simple bulk laxatives such as Psyllium (Metamucil) and prunes

32
Q

[FYI] What type of cathartic osmotically draws fluid into the GI lumen?

A

Osmotic cathartics such as sugar alcohols (sorbitol) and polyethylene glycol (GoLYTELY)

33
Q

[FYI] What type of laxative is a mechanimal lubricant like mineral oil and laxatone?

A

Emollient laxatives