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Pharmacology by Somebody > Deja Ch 8 GI > Flashcards

Deja Ch 8 GI Flashcards

1
Q

What is the main cause of gastroesophageal reflux disease (GERD)?

A

Decreased lower esophageal sphincter pressure

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2
Q

What complications may arise from GERD?

A

Strictures; esophagitis; Barrett esophagus (squamocolumnar metaplasia)

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3
Q

What are the drug therapy goals in treating GERD?

A

To eliminate symptoms; heal esophagitis; prevent the relapse of esophagitis; prevent the development of complications

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4
Q

What types of medications may be useful in the treatment of GERD?

A

Antacids; H2-receptor antagonists; proton pump inhibitors (PPIs); prokinetic agents (cisapride, metoclopramide, bethanechol); mucosal protectants (sucralfate)

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5
Q

Give the mechanism of action for each of the following drugs or drug classes: Antacids

A

Weak bases that increase gastric pH through acid-neutralizing ability to form a salt and water

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6
Q

Give the mechanism of action for each of the following drugs or drug classes: H2–receptor antagonists

A

Competitively antagonize H2 receptors on gastric parietal cells, thereby decreasing acid production

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7
Q

Give the mechanism of action for each of the following drugs or drug classes: PPIs

A

Inhibit gastric acid secretion via inhibiting gastric parietal cell H+/K+-ATPase. Restoration of acid secretion requires resynthesis of the H+/K+-ATPase (proton pump).

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8
Q

Give the mechanism of action for each of the following drugs or drug classes: Cisapride

A

Increases lower esophageal sphincter pressure; accelerate gastric emptying time; increases amplitude of esophageal contractions; 5-HT4 agonist; 5-HT3antagonist

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9
Q

Give the mechanism of action for each of the following drugs or drug classes: Metoclopramide

A

Dopamine (D2) receptor antagonist; increases lower esophageal sphincter pressure; accelerates gastric emptying time

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10
Q

Give the mechanism of action for each of the following drugs or drug classes: Sucralfate

A

When exposed to acid, complexes with positively charged proteins to form a viscous coat, thereby protecting gastric lining from gastric acid secretions

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11
Q

What are the adverse effects caused by metoclopramide?

A

Anxiety; insomnia; extrapyramidal symptoms; increased prolactin levels

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12
Q

What are the adverse effects caused by sucralfate?

A

Constipation; nausea; abdominal discomfort

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13
Q

What are the possible adverse effects of antacids?

A

Belching (sodium bicarbonate and calcium carbonate); diarrhea (magnesium salts); constipation (calcium or aluminum salts); acid-base disturbances; bone damage via binding phosphate in the gut (aluminum salts); worsening of hypertension and congestive heart failure (CHF) (sodium salts); decreased absorption of medications via pH alteration or formation of insoluble complexes (tetracycline, fluoroquinolones, isoniazid [INH], ferrous sulfate, ketoconazole, PPIs)

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14
Q

Which antacid(s) can produce a metabolic alkalosis?

A

Sodium bicarbonate; calcium carbonate

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15
Q

What causes the milk-alkali syndrome?

A

Ingestion of excessive amounts of calcium and absorbable alkali such as sodium bicarbonate or calcium carbonate

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16
Q

What is a potential complication after discontinuing chronic antacid use?

A

Acid rebound

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17
Q

List the names of the H2-receptor antagonists:

A

Cimetidine; famotidine; ranitidine; nizatidine

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18
Q

Which H2-receptor antagonist inhibits hepatic cytochrome P-450 metabolizing enzymes?

A

Cimetidine

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19
Q

Name at least five drugs showing potential drug interactions with cimetidine:

A
  1. Warfarin 2. Diazepam 3. Phenytoin 4. Metronidazole 5. Propranolol 6. Lidocaine 7. Calcium channel blockers (CCBs) 8. Theophylline 9. Certain tricyclic antidepressants (TCAs); chlordiazepoxide
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20
Q

Which H2-receptor antagonist can cause gynecomastia?

A

Cimetidine (prolactin-stimulating activity)

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21
Q

Which H2-receptor antagonist has antiandrogenic activity?

A

Cimetidine

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22
Q

List the names of the PPIs:

A

Omeprazole; esomeprazole; lansoprazole; rabeprazole; pantoprazole

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23
Q

What are the common side effects of PPIs?

A

Headache; dizziness; nausea; diarrhea; constipation. Prolonged use can lead to bacterial overgrowth in the GI tract. Note also that a recent analysis revealed that people (age > 50) taking high doses of PPIs for more than a year were 2.6 times as likely to break a hip as were people not taking PPIs. Histamine H2-receptor inhibitors also increased fracture risk, but not to the extent as did PPIs.

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24
Q

What is the most serious side effect of cisapride?

A

Prolongation of the QT interval

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25
Q

Cisapride should be avoided in which type of patients?

A

Patients with prolonged QT intervals; patients taking medications that inhibit cytochrome P-ISO 3A4 (fluconazole, ketoconazole, itraconazole, erythromycin, clarithromycin, ritonavir)

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26
Q

What arrhythmia can be caused by prolongation of the QT interval?

A

Torsades de pointes (a polymorphic ventricular tachycardia)

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27
Q

Which drugs increase cisapride blood levels by inhibiting the cytochrome P-450 3A4 enzymes that metabolize cisapride? (Please mention at least four drugs).

A
  1. Erythromycin 2. Clarithromycin 3. Itraconazole 4. Fluconazole 5. Ketoconazole 6. Indinavir 7. Ritonavir 8. Class 1A antiarrhythmics 9. Class III antiarrhythmics 10. Certain TCAs 11. Certain antipsychotics
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28
Q

What three mediators can stimulate acid secretion from parietal cells?

A
  1. Acetylcholine 2. Histamine (via H2 receptor) 3. Gastrin
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29
Q

Name three causes of peptic ulcer disease (PUD):

A
  1. Helicobacter pylori infection (primary cause) 2. Nonsteroidal anti-inflammatory drugs (NSAIDs) 3. Extreme physiologic stress (ie, patients in the ICU setting being ventilated, burn patients)
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30
Q

What type of patients do acute peptic ulcers occur in?

A

Hospitalized patients who are critically ill (stress ulcers)

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31
Q

What is the name of the syndrome that is characterized by hypersecretion of gastric acid secondary to a gastrin-secreting tumor?

A

Zollinger-Ellison syndrome

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32
Q

Which are the drug therapy goals in treating PUD?

A

Control H. pylori infection; alleviate symptoms; promote healing; prevent recurrences; prevent complications (eg, hemorrhage)

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33
Q

What types of medications are useful for the treatment of PUD?

A

Antimicrobial agents; H2-receptor antagonists; PPIs; prostaglandins; antimuscarinic agents; antacids; mucosal protective agents; bismuth salts

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34
Q

How might H. pylori play a role in peptic ulcer development?

A

Direct mucosal damage; alterations in inflammatory response; induced hypergastrinemia

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35
Q

Meals worsen the pain associated with what type of ulcer?

A

Gastric ulcer

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36
Q

Meals relieve the pain associated with what type of ulcer?

A

Duodenal ulcer

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37
Q

What treatment options are available to eradicate H. pylori?

A

Triple therapy with a PPI added to two antimicrobial agents such as metronidazole, amoxicillin, tetracycline, or clarithromycin; four-drug regimens consisting of triple therapy plus bismuth subsalicylate; (must use triple or quadruple antibiotic therapy to eradicate H. pylori)

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38
Q

Why should you not give bismuth subsalicylate to children?

A

May be associated with Reye syndrome (contains salicylates)

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39
Q

What is Reye syndrome?

A

Acute onset encephalopathy and fatty liver formation. Symptoms begin with vomiting, lethargy, and confusion progressing to stupor, respiratory distress, coma, and seizures. Its cause is unknown, but has been found to be associated with aspirin use in young children. Therefore, aspirin administration is to be avoided in pediatric patients.

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40
Q

How do prostaglandins help treat PUD?

A

Prostaglandins such as PGE2 and PGI2inhibit gastric acid secretion and stimulate secretion of bicarbonate and mucus (cytoprotective activity); used to treat NSAID-induced peptic ulcers

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41
Q

Which prostaglandin analog is commonly used as a cytoprotective agent for the treatment of PUD?

A

Misoprostol (synthetic PGE1 analog)

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42
Q

Why should misoprostol not be given to a preterm pregnant woman?

A

Induction of premature uterine contractions (abortifacient properties)

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43
Q

What are the two forms of inflammatory bowel disease (IBD)?

A
  1. Crohn disease 2. Ulcerative colitis (UC)
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44
Q

Does treatment of IBD cure or control the disease process?

A

Control

45
Q

What types of medications are used to treat IBD?

A

Corticosteroids; aminosalicylates; immunosuppressives; monoclonal antibodies

46
Q

Sulfasalazine is cleaved by gut bacteria in the colon to produce what two compounds?

A
  1. Sulfapyridine (sulfonamide antibiotic) 2. Mesalamine (5-aminosalicylic acid, 5-ASA)
47
Q

What is the active component of sulfasalazine for IBD?

A

Mesalamine or 5-ASA; 5-ASA is the metabolite active against IBD, while sulfapyridine is the metabolite active against rheumatoid arthritis. Formulation into sulfasalazine is necessary to prevent rapid proximal gut absorption so that sufficient 5-ASA is delivered to the distal gut to effectively treat IBD.

48
Q

How does mesalamine work in the treatment of IBD?

A

Anti-inflammatory effects; immunomodulating effects

49
Q

What type of vitamin supplementation should patients receive while on sulfasalazine?

A

Folic acid since sulfasalazine may interfere with absorption of folic acid in the gut, leading to megaloblastic anemia

50
Q

What types of immunosuppressives are used to treat IBD?

A

Cyclosporine A; methotrexate; azathioprine; 6-mercaptopurine

51
Q

What is the name of the monoclonal antibody indicated for the treatment of Crohn disease?

A

Infliximab

52
Q

What is infliximab’s mechanism of action?

A

Monoclonal antibody that binds to soluble and bound forms of tumor necrosis factor-alpha (TNF-_)

53
Q

True or False? Once remission has been achieved with ulcerative colitis, corticosteroids are used as maintenance therapy.

A

False. Corticosteroids should not be used to maintain disease remission due to their high systemic toxicity. Aminosalicylates or immunosuppressive agents are used for maintenance therapy for UC.

54
Q

Name a major chemosensory area for emesis:

A

Chemoreceptor trigger zone (CTZ)

55
Q

Where is the Chemoreceptor trigger zone (CTZ) found?

A

Area postrema of the fourth ventricle of the brain

56
Q

Give examples of drug classes that are effective in the treatment of nausea and vomiting:

A

Antihistamine-anticholinergics; benzodiazepines; butyrophenones; cannabinoids; corticosteroids; phenothiazines; substituted benzamides; 5-HT3-receptor antagonists; neurokinin receptor antagonists

57
Q

Give examples of specific drugs in each of the following drug classes used in the treatment of nausea and vomiting: Antihistamine-anticholinergics

A

Diphenhydramine; hydroxyzine; meclizine; cyclizine; promethazine; pyrilamine; scopolamine; trimethobenzamide

58
Q

Give examples of specific drugs in each of the following drug classes used in the treatment of nausea and vomiting: Benzodiazepines

A

Alprazolam; diazepam; lorazepam

59
Q

Give examples of specific drugs in each of the following drug classes used in the treatment of nausea and vomiting: Butyrophenones

A

Haloperidol; droperidol; domperidone

60
Q

Give examples of specific drugs in each of the following drug classes used in the treatment of nausea and vomiting: Cannabinoids

A

Dronabinol; nabilone

61
Q

Give examples of specific drugs in each of the following drug classes used in the treatment of nausea and vomiting: Corticosteroids

A

Dexamethasone; methylprednisolone

62
Q

Give examples of specific drugs in each of the following drug classes used in the treatment of nausea and vomiting: Phenothiazines

A

Prochlorperazine; chlorpromazine; perphenazine

63
Q

Give examples of specific drugs in each of the following drug classes used in the treatment of nausea and vomiting: Substituted benzamides

A

Metoclopramide

64
Q

Give examples of specific drugs in each of the following drug classes used in the treatment of nausea and vomiting: 5-HT3–receptor antagonists

A

Ondansetron; dolasetron; granisetron

65
Q

Give examples of specific drugs in each of the following drug classes used in the treatment of nausea and vomiting: Neurokinin receptor antagonists

A

Aprepitant (oral); fosaprepitant (IV formulation converted to aprepitant)

66
Q

Do synthetic cannabinoids have psychotropic activity?

A

No

67
Q

How does metoclopramide work as an antiemetic?

A

Blocks dopamine receptors centrally in the CTZ

68
Q

What is intractable emesis leading to dehydration and hypotension during pregnancy called?

A

Hyperemesis gravidarum

69
Q

What are the drugs of choice for treating emesis during pregnancy?

A

Meclizine; cyclizine; promethazine

70
Q

What antihistamine is often used to treat motion sickness?

A

Meclizine

71
Q

What anticholinergic is often used to treat motion sickness?

A

Scopolamine

72
Q

How is scopolamine normally administered?

A

As a transdermal patch to prevent systemic anticholinergic effects

73
Q

What medication is often used in combination regimens to enhance antiemetic activity?

A

Dexamethasone

74
Q

What are the side effects of cannabinoids?

A

Anxiety; memory loss; confusion; motor incoordination; hallucinations; euphoria; relaxation; hunger; gynecomastia

75
Q

What are the side effects of the phenothiazine antiemetics?

A

Extrapyramidal symptoms; sedation; hypotension

76
Q

Why doesn’t ondansetron cause extrapyramidal side effects?

A

Blocks 5-HT3 instead of dopamine receptors in the CTZ

77
Q

What chemotherapy agent has one of the highest emetogenic potentials?

A

Cisplatin

78
Q

What over-the-counter (OTC) medication can be given in combination with metoclopramide to reduce its extrapyramidal side effects?

A

Diphenhydramine can be used for its anticholinergic properties. EPS symptoms with metoclopramide use are due to central dopamine receptor blockade, and tardive dyskinesia, if it develops, may be irreversible. Therefore, metoclopramide should only be used for short-term therapy if possible.

79
Q

What macrolide antibiotic also has prokinetic properties for the GI tract?

A

Erythromycin, though tolerance to this effect develops rapidly, limiting its usefulness

80
Q

Name three classes of drugs that are effective in the treatment of diarrhea:

A
  1. Adsorbents 2. Antimotility agents 3. Antisecretory agents
81
Q

Define adsorbent:

A

A substance offering a suitable active surface, upon which other substances may adhere to

82
Q

Give examples of specific drugs in each of the following drug classes used in the treatment of diarrhea: Adsorbents

A

Kaolin; pectin; polycarbophil; attapulgite

83
Q

Give examples of specific drugs in each of the following drug classes used in the treatment of diarrhea: Antimotility agents

A

Diphenoxylate; loperamide; morphine

84
Q

Give examples of specific drugs in each of the following drug classes used in the treatment of diarrhea: Antisecretory agents

A

Bismuth subsalicylate

85
Q

Give the antidiarrheal mechanism of action for each of the following drug classes: Adsorbents

A

Adsorbs (adheres to) drugs, nutrients, toxins, and digestive juices

86
Q

Give the antidiarrheal mechanism of action for each of the following drug classes: Antimotility agents

A

Decrease peristalsis by activating presynaptic opioid receptors in the enteric nervous system

87
Q

Give the antidiarrheal mechanism of action for each of the following drug classes: Antisecretory agents

A

Decrease fluid secretion in the bowel

88
Q

What adsorbent can absorb 60 times its weight in water and treat both diarrhea and constipation?

A

Polycarbophil

89
Q

What are the potential side effects of bismuth subsalicylate?

A

Salicylism (tinnitus, nausea, vomiting); darkening of tongue; darkening of stools; induce gout attacks in susceptible patients

90
Q

What antidiarrheal can decrease tetracycline absorption if given concomitantly?

A

Bismuth subsalicylate

91
Q

What antidiarrheal is often formulated in combination with atropine?

A

Diphenoxylate

92
Q

Which class of antidiarrheals can cause paralytic ileus?

A

Antimotility agents

93
Q

What medication is often used to treat flushing and diarrhea seen in carcinoid syndrome and vasoactive intestinal peptide secreting tumors (VIPomas)?

A

Octreotide

94
Q

What is octreotide’s mechanism of action?

A

Synthetic analog of somatostatin which blocks release of serotonin and other vasoactive peptides; direct inhibitory effects on intestinal secretion; direct stimulatory effects on intestinal absorption

95
Q

What are the non-antidiarrheal uses of octreotide?

A

Esophageal varices; acromegaly

96
Q

What medication can be used in conjunction with antibiotics to bulk stools and absorb Clostridium difficile toxins A and B in C. difficile colitis?

A

Cholestyramine, a nonabsorbable binding agent

97
Q

What types of medications cause constipation?

A

Opioid analgesics; anticholinergics; calcium-containing antacids; aluminum-containing antacids; calcium channel blockers; clonidine; iron; sodium polystyrene sulfonate

98
Q

Give examples of drug classes that are effective in the treatment of constipation:

A

Bulk forming agents; irritants and stimulants; stool softeners

99
Q

Give examples of specific drugs in each of the following drug classes used in the treatment of constipation: Bulk forming agents

A

Methylcellulose; psyllium; bran; magnesium-containing salts; polyethylene glycol

100
Q

Give examples of specific drugs in each of the following drug classes used in the treatment of constipation: Osmotic laxatives

A

Lactulose; magnesium hydroxide (milk of magnesia); sorbitol; magnesium citrate; sodium phosphate; polyethylene glycol

101
Q

Give examples of specific drugs in each of the following drug classes used in the treatment of constipation: Irritants and stimulants

A

Cascara; senna; aloe; bisacodyl

102
Q

Give examples of specific drugs in each of the following drug classes used in the treatment of constipation: Stool softeners

A

Mineral oil; docusate (oral or enema, trade name: Colace); glycerin suppository

103
Q

Give examples of specific drugs in each of the following drug classes used in the treatment of constipation: Cl_ channel activators

A

Lubiprostone (Amitiza)

104
Q

Give the mechanism of action for each of the following drug classes: Bulk-forming agents

A

Form gels in large intestine which causes water retention and intestinal distention, thereby increasing peristaltic activity

105
Q

Give the mechanism of action for each of the following drug classes: Osmotic laxatives

A

Nonabsorbable compounds which draw fluid into the colon to maintain osmotic neutrality

106
Q

Give the mechanism of action for each of the following drug classes: Irritants and stimulants

A

Irritate gut lining which subsequently increases peristalsis

107
Q

Give the mechanism of action for each of the following drug classes: Stool softeners

A

Surfactants that become emulsified with stool, thereby softening feces

108
Q

Give the mechanism of action for each of the following drug classes: Cl channel activators

A

Activate CIC-2 Cl_ channels in the apical membrane of intestinal cells increasing fluid and intestinal motility without altering serum Na+ or K+ levels. The effects are localized to the GI tract, increase fluid secretion into the intestinal lumen, and accelerate fecal transit.

109
Q

What are the potential side effects of bisacodyl?

A

Abdominal cramping; atonic colon

Pharmacology by Somebody (25 decks)

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