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Pharmacology II > Lecture 4: Drugs for the treatment of GI disorders-2 > Flashcards

Lecture 4: Drugs for the treatment of GI disorders-2 Flashcards

1
Q

What receptors are located in the vomiting center (medulla) that can be activated

A

Alpha1, 5-HT3, NK1, H1

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2
Q

What receptors are in the vestibular nuclei that can induce vomiting

A

M1, M2, H1

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3
Q

What receptors are in the periphery (GI and pharynx) that can induce vomiting

A

5-HT3, and NK1

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4
Q

What receptors are in the chemoreceptor trigger zone that can induce vomiting

A

D2, 5-HT3, NK1

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5
Q

When is the appropriate timeline to induce vomiting

A

Within 1hr of toxin ingestion

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6
Q

When do you not want to induce vomiting

A

Ingested sharp objects, strong acids/bases or >1hr after ingestion

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7
Q

When do you want to inhibit vomiting

A

Intractable, risk of aspiration, onset of acid-base disorders, onset of electrolyte disorders

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8
Q

What are ondansetron HCl and dolasetron mesylate indicated for

A

Vomiting in cats and dogs

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9
Q

What drugs tend to cause vomiting in dogs that can be reduced with ondansetron

A

Dexmedetomidine and buprenorphine

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10
Q

What is the mechanism of action of ondansetron and dolasetron

A

5-HT3 receptor antagonists in the CRTZ, vomiting center, and periphery

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11
Q

When is PO administration ineffective with ondansetron and dolasetron

A

Acute, intractable vomiting

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12
Q

What route of administration of ondansetron and dolasetron have a greater absoprtion

A

SQ

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13
Q

What are some adverse effects of dolasetron

A

Prolongs ECG intervals- caution with arrhythmias, electrolyte imbalances, chemotherapy tx

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14
Q

What is an adverse effect/contraindication of ondansetron

A

Eliminated by P-glycoprotein so patients with MDR1 gene like collies should not be usd

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15
Q

What is maropitant citrate indicated for

A

Acute vomiting in dogs and cats, motion sickness in dogs

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16
Q

What is the mechanism of action of maropitant citrate

A

NK1 receptor antagonist in CRTZ, vomiting center and periphery

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17
Q

What are some adverse effects of maropitant citrate

A

Prolongs QT interval- caution with arrrythmuas, hypersalivation

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18
Q

What is apomorphine HCl indicated for

A

Enteric for dogs- primarily for ingested toxins

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19
Q

What is the mechanism of action of apomorphine

A

D2 receptor agonist in CRTZ

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20
Q

Since cats have fewer D2 receptors in CRTZ which drug should be used in place of apomorphine

A

Xylazine

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21
Q

What are some adverse effects of apomorphine

A

Protracted vomiting, lethargy, hypersalivation

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22
Q

If apomorphine induces protracted vomiting what can be done to treat it

A

Rinse conjunctiva

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23
Q

What are some contraindications for apomorphine

A

Seizures, obtundation, comatose, abnormal gag reflex, rabbits

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24
Q

What is chlorpromazine HCl indicated for

A

Antiemetic in dogs and cats, inhibits apomorphine induced dogs, motion sickness for cats

25
Q

What is the mechanism of action for chlorpromazine HCl

A

D2 receptor antagonist in the CRTZ

Anti-histaminic, anti-cholinergic, anti-alpha adrenergic effects

26
Q

What are some adverse effects of chlorpromazine

A

Sedation, lethargy, tremors, ataxia, diarrhea, loss of anal sphincter tone, hypotension, excitation, bradycardia, lower seizure threshold

27
Q

What are some contraindications of chlorpromazine HCl

A

Horses, dog breeds with predisposition to MDR1 mutations

28
Q

What is metoclopramide HCl indicated for

A

General antiemetic for most purposes in dogs, gastric ulceration (promotility effects)

29
Q

What is the mechanism of action of metoclopramide

A

D2 receptor antagonism in CRTZ, some 5-HT3 antagonism in CRTZ, vomiting center and periphery, sensitizes GI smooth muscle to PNS stimulation

30
Q

What are some adverse effects of metoclopramide HCl

A

Aggressive behavior in horses, changes in mentation, constipation, increased detrusor muscle tone

31
Q

What are some signs of ulcers in small animals

A

Weight loss, anorexia, sporadic/chronic vomiting with blood, abdominal pain, anemia, Melena, secondary esophagitis

32
Q

What are some causes of ulcers in small animals

A

Drug induced from NSAIDS
Helicobacter pylori

33
Q

What is equine squamous gastric ulcer syndrome associated with

A

Going off feed, because glandular stomach is constantly producing acid which is typically buffered by feed

34
Q

What is equine glandular gastric ulcer syndrome associated with

A

Breakdown in gastric mucus layer of the stomach

35
Q

What is the typical cause of equine glandular gastric ulcer syndrome resulting in breakdown of gastric mucus layer

A

NSAIDS

36
Q

What is omeprazole indicated for

A

FDA approved for gastric ulcer management in horses

ELDU- gastric ulcers in small animals, esophagitis

37
Q

What is the mechanism of action for omeprazole and pantoprazole

A

Irreversible inhibition of H+/K+ ATPase at the secretory surface of parietal cells

38
Q

What type of gastric ulcer syndrome in horses is omeprazole better at treating

A

ESGUS

39
Q

T or F: crushing omeprazole tablets is the best way to administer them

A

False, the capsules contain coated granules that protect the drug in stomach, crushing them will reduce efficacy

40
Q

What are some H2 antagonists/proton pump inhibitors

A
  1. Cimetidine
  2. Famotidine
  3. Nizatidine
  4. Ranitidine
41
Q

What are H2 antagonists/proton pump inhibitors indicated for

A

Reducing gastric acid secretion in small animals

42
Q

Which H2 antagonist can treat ESGUS and is it not better than omeprazole

A

Ranitidine, less effective than omeprazole but cheaper

43
Q

What is the mechanism of action of H2 antagonists

A

Competitive antagonists of histamine secreted from ECL cells so blocks H+/K+ ATPase through inhibition of Gs and cAMP

44
Q

Which H2 antagonists have mild inhibition of AChE and therefore increase PNS tone (prokinetic)

A

Ranitidine and nizatidine

45
Q

What does it mean to be prokinectic

A

Increase gastric motility by mild inhibition of AChE in synaptic junctions—> increase PNS activity

So ranitidine and nizatidine increase gastric motility and decrease gastric acid secretion

46
Q

What H2 antagonists inhibit P450 and what does that mean

A

Drugs: cimetidine»ranitidine
Increases time of circulation of drug/decrease metabolism. Also can affect metabolism of other drugs

47
Q

What is erythromycin indicated for

A

Primary gastroparesis, esophageal reflux, colonic motility disorders in cats and dogs

48
Q

What is the mechanism of action of erythromycin

A

Stimulates motilin receptors in cats, stimulates 5-HT3 receptors in dogs

49
Q

What are some adverse effects and contraindications for erythromycin

A

Stimulation of larger food particles into intestines causing intestinal distress

Macrolide antibiotics may cause toxic entercolitis in pocket pets

GI perforation, obstruction, hemorrhage

50
Q

What is cisapride indicated for

A

Primary gastroparesis, esophageal reflux, constipation and megacolon in cats

51
Q

What is the mechanism of action of cisapride

A

Modulates serotonin receptors

Agonist of pre synaptic 5-HT4 receptors that increase release of ACh, stimulates gastric emptying and lower esophageal motility and sphincter pressure

52
Q

What are some adverse effects of cisapride

A

Vomiting, diarrhea, abdominal pain, increase Q-T intervals, GI perforation, obstruction, hemorrhage

53
Q

What is sucralfate indicated for

A

Ulcers in any GI location (oral to duodenum) except if caused by NSAIDS

54
Q

What is the mechanism of action of sucralfate

A

Binds protein exudates and basement membranes of cells in ulcer and coats ulcer protecting it from stomach acid allowing it to heal

55
Q

What are some adverse affects of sucralfate

A

Vomiting in cats, constipation

56
Q

What is misoprostol indicated for

A

NSAID induced gastric ulceration

57
Q

What is the mechanism of action of misoprostol

A

Synthetic prostaglandin E1 analogue inhibits H+/K+ ATPase by stimulating GI and inhibiting cAMP. Promotes bicarbonate and mucus production by gastric epithelial cells. Increases gastric blood supply and turnover of gastric epithelium

58
Q

What are some adverse effects of misoprostol

A

Diarrhea, vomiting, abdominal pain, abortion (increase uterine contraction, relax and thin cervix)

Pharmacology II (36 decks)

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