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OPT 540 > GI and Antiemetic Drugs > Flashcards

GI and Antiemetic Drugs Flashcards

1
Q

What four common medical conditions involve the GI tract?

A

Peptic ulcers/GERD
Chemotherapy-induced emesis
Diarrhea
Constipation

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2
Q

What are some causes of peptic ulcer disease?

A 
Gram-negative H. Pylori infection
NSAID use
Increased HCl secretion
Inadequate mucosal defense against gastric acid
Tumors
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3
Q

What is Zollinger-Ellison syndrome?

A

A condition in which there is increased production of gastrin. Usually, a small tumor (gastrinoma) in the pancreas or small intestine produces the high levels of gastrin in the blood. Gastrin increases secretion of gastric acid.

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4
Q

What are some treatment options for peptic ulcer disease?

A

Eradicate H. Pylori infection
Reduce gastric acid secretion
Protect gastric mucosa

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5
Q

How would an H. Pylori infection be documented?

A

Biopsy
Serologic tests
Urea breath tests

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6
Q

How would an H. Pylori infection be treated?

A

Triple therapy

  • PPI
  • Metronidazole or amoxicillin
  • Clarithromycin

Quadruple therapy

  • Bismuth subsalicylate
  • Metronidazole
  • Tetracycline
  • PPI
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7
Q

What endogenous compounds stimulate gastric acid secretion?

A

ACh
Histamine
Gastrin

They activate protein kinases, which stimulate the proton pump.

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8
Q

Name some H2 receptor antagonists.

A

Cimetidine (prototype), ranitidine, famotidine, and nizatidine (the ones that end in “-tidine”)

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9
Q

What are H2 receptor antagonists used for?

A

Healing duodenal and gastric ulcers

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10
Q

True or false: recurrence of ulcers after stopping H2 receptor antagonist treatment is low.

A

False. Recurrence is 60-100%

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11
Q

When would an H2 receptor antagonist be given as an IV infusion?

A

To prevent and manage acute stress ulcers.

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12
Q

True or false: H2 antagonists can be used to treat GERD.

A

True; however, their onset is delayed (45 min)

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13
Q

True or false: antacids should be used as a long-term treatment for GERD.

A

False. Although antacids quickly and efficiently neutralize secreted acid, their action is only temporary.

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14
Q

Although cimetidine is the prototype H2 receptor antaognist, it has two notable drawbacks. What are they?

A

Acts as inhibitor of CP450, slowing metabolism of and potentiating actions of several drugs (warfarin, dizepam, phenytoin, carbamazepine, imipramine)
Acts as nonsteroidal anti-adrenergic drug

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15
Q

What advantage(s) does ranitidine have over cimetidine?

A

Longer-acting

5-10x more potent

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16
Q

What advantage(s) does famotidine have over cimetidine?

A

20-50x more potent

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17
Q

What advantage(s) does nizatidine have over the other H2 receptor antagonists?

A

It is eliminated principally by the kidneys (as opposed to the liver). Its bioavailability is nearly 100% due to little first-pass metabolism.

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18
Q

What are some adverse effects of cimetidine?

A

HA
Dizziness
Diarrhea
Muscular pain

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19
Q

Which drugs are PPIs?

A

The ones ending in “-prazole.”

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20
Q

Which PPIs are available OTC?

A

Omeprazole

Lansoprazole

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21
Q

True or false: PPIs are prodrugs with an acid-resistant enteric coating.

A

True.

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22
Q

True or false: PPIs are the preferred drugs for stress ulcer treatment.

A

True.

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23
Q

For what GI conditions are PPIs approved?

A

Stress ulcer treatment

GERD

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24
Q

True or false: PPIs increase the risk of bleeding from NSAID ulcers.

A

False. They decrease the risk.

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25
Q

Should PPIs be taken with or without food?

A

PPIs should be taken 30-60 minutes before a meal.

26
Q

What is one serious potential adverse effect of long-term PPI use?

A

Hip, wrist, and spine fractures

27
Q

Where does prostaglandin E come from and what are its effects?

A

It is secreted by the gastric mucosa, and it inhibits the secretion of HCl and stimulates secretion of mucus and bicarbonate.

28
Q

What drug is a stable analog of protaglandin E, and for what condition is it approved?

A

Misoprostol; it is approved for prevention of NSAID-caused gastric ulcers.

29
Q

In what condition would misoprostol be contraindicated?

A

Pregnancy due to uterine contractions.

30
Q

Which antacids are commonly used?

A

Aluminum hydroxide
Magnesium hydroxide
Calcium carbonate

31
Q

Which of the commonly-used antacids may also be used in the treatment of osteoporosis?

A

Calcium carbonate (as a calcium supplement)

32
Q

Which of the antacids tends to cause diarrhea, and which tends to cause constipation?

A

Aluminum hydroxide tends to cause constipation; magnesium hydroxide tends to cause diarrhea.

33
Q

What are some of the beneficial effects of mucosal protective agents?

A

Prevention of mucosal injury
Reduction of inflammation
Healing of existing ulcers

34
Q

Which drug is a complex of Al(OH)₃ and sulfated sucrose?

A

Sucralfate.

35
Q

What are the actions of sucralfate?

A

Stimulates prostaglandin, mucus and bicarbonate release

36
Q

True or false: sucralfate may be used in conjunction with antacids.

A

False. It requires an acidic pH for activation; therefore it is not compatible with PPIs, H2 antagonists, or antacids since these increase gastric pH.

37
Q

How does bismuth subsalicylate act as a mucosal protective agent?

A

Antimicrobial actions
Pepsin inhibition
Stimulation of mucus secretion

38
Q

What are some common causes of emesis?

A

Motion sickness
Pregnancy
Hepatitis

39
Q

What are some potentially serious effects of emesis?

A

Dehydration
Profound metabolic imbalances
Nutrient depletion

40
Q

What two brainstem sites are key in the vomiting reflex?

A

Chemoreceptor trigger zone, in the area postrema

Vomiting center, in the lateral reticular formation of the medulla

41
Q

How do chemotherapeutic agents trigger emesis?

A

Stimulation of D2 and 5-HT3 receptors
Color/smell
Release of serotonin from GI system, carrying signal to vomiting reflex centers

42
Q

Which drugs are useful in treatment emesis caused by motion sickness?

A

Scopolamine and H1 receptor antagonists (dimenhydrinate, meclizine, cyclizine)

43
Q

Which phenothiazine is an effective anti-emetic agent? Which emetogenic chemotherapeutic agents is it effective against?

A

Prochlorperzine; it is effective against low-to-moderate agents such as fluorouracil and doxorubicin.

44
Q

What type of drug is useful against all grades of emetogenic therapy?

A

5-HT3 receptor antagonists; drugs ending in “-setron”

45
Q

Which benzamide has antiemetic properties, and which receptor does it block?

A

Metoclopramide; D2

46
Q

Which butyrophenones have antiemetic properties, and which receptor do they block?

A

Droperidol, haloperidol; D2

47
Q

Which benzodiazepines have antiemetic properties?

A

Lorazepam, alprazolam; have mild antiemetic properties

48
Q

Which corticosteroids have antiemetic properties?

A

Dexamethasone, methylprednisolone; have mild to moderate antiemetic properties

49
Q

What might be the result of combining various antiemetic drugs?

A

Increased antiemetic activity, or decreased toxicity

50
Q

What three classes of drugs are used as antidiarrheals?

A

Antimotility agents
Adsorbents
Drugs that modify fluid and electrolyte transport

51
Q

Which antidiarrheal drugs are antimotility agents?

A

Loperamide & diphenoxylate (analogs of meperidine and have opioid-like actions on the gut)

52
Q

Which antidiarrheal drug modifies fluid and electrolyte transport?

A

Bismuth subsalicylate (used for traveler’s diarrhea, decreases fluid secretion in the bowel)

53
Q

What are two potential risks of laxative use?

A

Potential for dependency

Electrolyte imbalance

54
Q

Which laxatives fall into the category of stimulant/irritant?

A 
Senna (water and electrolyte secretion into the bowel)
Bisacodyl (potent stimulator of the colon)
Castor oil (increases peristalsis, uterine contraction)
55
Q

Which laxatives fall into the category of bulk laxatives, and when should you be cautious in prescribing them?

A

Methylcellulose, psyllium seeds, and bran; take caution with immobile patients due to intestinal obstruction

56
Q

Which laxatives fall into the category of saline and osmotic laxatives?

A

Magnesium citrate, magnesium hydroxide, and sodium phosphate (nonabsorbable salts that hold water in the intestine)

57
Q

Which laxatives fall into the category of stool softener?

A

Docusate sodium, docusate calcium, and docusate potassium

58
Q

Which laxatives fall into the category of lubricant laxatives?

A

Mineral oil and glycerin suppositories (act by facilitating the passage of hard stools)

59
Q

Which laxative falls into the category of chloride channel activator?

A

Lubiprostone (works by activating chloride channels to increase fluid secretion in the intestinal lumen)

60
Q

True or false: lubiprostone can be used for chronic constipation.

A

True; it does not appear to show tolerance or dependency.

OPT 540 (12 decks)

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