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Pharmacology > Gastrointestinal Pharmacology > Flashcards

Gastrointestinal Pharmacology Flashcards

1
Q

______ can occur in areas of upper GI tract that are exposed to stomach acid and pepsin

A

Peptic ulcer

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2
Q

Most common sites of peptic ulcers?

A
  • duodenum
  • stomach
  • lower esophagus
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3
Q

What condition occurs when corrosive action of gastric acid and pepsin overcome mucosal defense mechanism?

A

Peptic ulceration

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4
Q

Peptic ulceration can occur if there is an excess production of ______ or if there’s a breakdown of _____ defense mechanisms

A

acids; mucosal defense mechanisms

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5
Q

What are two common causes of ulcers?

A

1) H. pylori
2) NSAID’s

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6
Q

Proton pumps move H+ and Cl- from the ____ cell and into the lumen of the ____

A

parietal cell; stomach lumen

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7
Q

True or False: Neural and endocrine mechanism regulate acid secretion

A

True

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8
Q

Gastrin is made by the stomach and small intestines in response to ____ and intake of ____

A

gastrin; food

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9
Q

___ binds to the muscarinic receptor of the parietal cell while gastrin binds to gastrin receptor. Following this ___ binds to H2 receptor.

A

histamine

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10
Q

What is the primary defense that is used by the stomach to protect itself against harsh environments?

A

Mucosal barrier

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11
Q

Mucus is made and secreted by ___. It is made up of glycoproteins, water, electrolytes, and HCO3

A

goblet cells

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12
Q

The mucus adheres to _____ cells, protecting them from erosive actions of acid and pepsin

A

epithelial cells

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13
Q

The integrity of the mucus barrier depends on what three factors?

A

1) Blood flow to mucosa
2) Ability of mucosal cells to reproduce
3) Prostaglandins (PGEE)

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14
Q

_____ is a prostaglandin analog that is available for prevention of NSAID-induced ulcers

A

Misoprostol

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15
Q

Under normal conditions, there is a balance between ___ and ___ (defense factors).

What is one condition in which this balance is disrupted, leading to excess acid production?

A

acid/pepsin; mucus

Zollinger Ellison Syndrome

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16
Q

True or False: In stress or NSAID-induced ulcers, the ability to maintain mucus barrier becomes compromised

A

True

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17
Q

True or False: Peptic ulceration commonly occurs when corrosive action of gastric acid and pepsin overcome mucosal defense mechanisms

A

True

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18
Q

Three causes of peptic ulcer disease?

A

1) Excess acid production
2) H. pylori
3) Breakdown of mucosal defense mechanisms

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19
Q

How is H. pylori eradicated?

A

Antimicrobials eradicate H. pylori and decrease chance for recurrence

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20
Q

How does H. pylori lead to spontaneous development of ulcers?

A

Weakens mucus defense system

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21
Q

What class of drugs are considered to be the classic antacids?

A

Neutralizing agents

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22
Q

What two drug classes inhibit acid secretion?

A

1) H2 histamine antagonist
2) PPI

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23
Q

What two drugs enhance the defense factors?

A
  • Sulcralfate
  • Misoprostol
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24
Q

True or False: Anti-microbials are used to eradicate H. pylori

A

True

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25
Q

____ are inorganic bases that neutralized HCl to form salts and water

A

Neutralizing Agents

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26
Q

What are the four neutralizing agents?

A

1) Sodium Bicarbonate
2) Calcium Carbonate
3) Magnesium Hydroxide
4) Aluminum Hydroxide

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27
Q

What two neutralizing agents produce CO2 (which can lead to distension) and can cause metabolic alkalosis?

A

Calcium Carbonate and Sodium Bicarbonate

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28
Q

Which neutralizing agent has rapid onset, but short duration of action?

A

Sodium Bicarbonate

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29
Q

____ is ok for occassional symptomatic relief of heartburn and mild gastritis, but NOT for treatment of peptic ulcer disease

A

Sodium Bicarbonate

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30
Q

In patients with high calcium intake or poor renal who are taking Calcium Carbonate, ____ Syndrome can occur

A

Milk Alkali Syndrome?

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31
Q

Features of Milk Alkali Syndrome?

A

Alkalosis
Hypercalcemia
Kidney Stones
Renal Damage

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32
Q

True or False: Calcium Carbonate can lead to acid rebound (increase in acid secretion after effects wear off)

A

True

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33
Q

True or False: Calcium Carbonate is appropriate for long-term management of peptic ulcers

A

False - calcium carbonate is NOT appropriate for longer term management of peptic ulcers. However, it is OKAY for occasional or low dose usage

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34
Q

Which three neutralizing agents have the potential for drug interactions with calcium, leading to formation of insoluble complexes?

A

Calcium Carbonate Magnesium Hydroxide
Aluminum Hydroxide

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35
Q

What three drugs can lead Calcium Carbonate and MgOH to form insoluble complexes and lead to decreases effectiveness of other drugs?

A

1) Digitalis glycosides
2) Tetracyclines
3) Phenytoin

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36
Q

Which two neutralizing agents are unlikely to lead to systemic alkalosis?

A

AlOH and MgOH

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37
Q

___ is most common side effect when MgCl2 is used alone as antacids

How can this effect be minimized?

A

Diarrhea

  • Mg salts in combination with other agents that have constipating actions (AlOH)
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38
Q

In patients with poor renal function, use of _____ may lead to hypermagnesemia

A

Magnesium OH

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39
Q

True or False: Aluminum Hydroxide tend to cause constipation

A

True
- Can be minimized by using it combination with Mg2+ salts

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40
Q

The aluminum in AlOH forms an insoluble salt with ___, leading to reduced absorption of ___ within and, ultimately, _____

A

phosphate; hypophosphatemia

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41
Q

What type of adverse systemic effects can occur in patients who are taking AlOH and have impaired RENAL function?

A

Myopathies, Dementia, Seizures, and Osteodystrophy

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42
Q

Antacid mixtures are the result of ____ and ____.

Why is this combination so valuable?

A

AlOH and MgOH

  • Combination minimizes the side effects of individual agents
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43
Q

True or False: Both MgOH and AlOH are NOT well absorbed and can lead to build up of toxic levels of Mg and Al, respectively, in patients with renal insufficiency

A

True

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44
Q

Which class of drugs is currently used for SYMPTOMATIC relief of heartburn, gastritis, and peptic ulcer disease?

A

Neutralizing Agents

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45
Q

Which two agents inhibit acid secretion?

A

1) H2 antagonists
2) Omeprazole, Pantoprazole

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46
Q

____ are a class of drugs that reduce the amount of acid secreted in response to histamine, vagal stimulation, acetylcholine, and gastrin

A

H2 - histamine antagonists

47
Q

True or False: Omeprazole is used for the acute treatment and prevention of relapses in peptic ulcer disease

A

False - H2 (histamine antagonist) are used for acute treatment and prevention of relapses in peptic ulcer diseas

48
Q

Which acid secretion inhibitor is used to treat Zollinger Ellison Syndrome and reflux-esophagitis?

A

Histamine (H2) Antagonists

49
Q

Name three common Histamine Antagonists:

A

1) Cimetidine
2) Famotidine
3) Nizatidine

50
Q

Which of the H2 antagonists can lead to gynecomastia in men? Why does this occur?

A

Cimetidine
(has anti-androgen effects - only at CHRONIC and HIGH doses!)

51
Q

True or False: An active H2-R is needed for gastrin and neuronal PS stimulation of acid secretion

A

True

52
Q

Which Acid Secretion Inhibitor inhibits P450 and, therefore, has many DDI?

A

Cimedtidine

53
Q

What drug class does omeprazole belong to?

A

PPI (proton pump inhibitors)

54
Q

True or False: Esomeprazole (and other PPI’s) are very effective in reducing most types of acid secretion and may also have some activity against H. pylori

A

True

55
Q

___ are inactive prodrugs that are converted to active metabolites that covalently interact with proton pump

A

PPI’s (such as Omeprazole)

56
Q

Five uses of PPI’s?

A

1) GERD
2) Peptic Ulcer Disease
3) Zollinger Ellison Syndrome
4) Preventing stress and NSAID induced ulcers

57
Q

The main problem in ___ drugs is that the marked inhibition of acid secretion can lead to microbial over growth of upper GI with chronic use

A

PPI’s (like omeprazole)

58
Q

How are PPI’s administered? activated?

A

Administers as: inactive prodrugs

Activated by: protonation

59
Q

Where are PPI’s activated?

A

Parietal cell canaliculus

60
Q

True or False: Proton pump inhibitors reversible activate H/K ATPase

A

False - Proton Pump Inhibitors IRREVERSIBLY INACTIVATES H/K ATPase

61
Q

True or False: PPI work immediately

A

False - they take 3-7 days to reach full acid-inhibiting potential

62
Q

When should PPI’s ideally be taken?

A

1 hour before meal

63
Q

Which drug class is associated with increased risk of bone fractures in females?
A. PPI’s
B. H2 Antagonists
C. Neutralizing Agents

A

A. PPI’s

64
Q

Three primary clinical uses for PPI’s?

A

1) GERD
2) Peptic Ulcer Disease
3) Zollinger Ellison Syndrome

65
Q

What is the first line of treatment for excess acid production, as in Zollinger Ellison Syndrome?
A. PPI’s
B. Neutralizing Agents
C. Magnesium OH

A

A. PPI’s

66
Q

___ and ___ are the strongest inhibitors of CYP2C19

A

Omeprazole and Esomeprazole

67
Q

Which PPI has the least effect on CYP2C19?

A

Pantoprazole

68
Q

True or False: Clopidogreal requires activation by CYP2C19

A

True

69
Q

Inhibition of hepatic drug metabolizing enzymes and decreased gastric acidity are side effects of ___

A

PPI’s

70
Q

What three agents enhance defense factors (cytoprotective agents)?

A

Sucralfate
Misoprostol

71
Q

____ is an aluminum salt that polymerizes to form a sticky material that binds to exposed proteins in ulcer, forming a protective barrier

A

Sucralfate

72
Q

___ is a PGE1 analogue that increases mucus production and reduces acid secretion

A

Misoprostol

73
Q

True or False: Sucralfate is used to prevent NSAID induced ulceration

A

False - Misoprostol is used to prevent NSAID induced ulcerations

74
Q

Which cytoprotective agents should NOT be given to expecting mothers? Why?

A

Misoprostol, a cytoprotective agent, should NOT be given to expecting mothers because it can induce uterine contractions and abortion

75
Q

Which five microbial gents are effective against H. pylori?

A

1) Metronidazole
2) Amoxicillin
3) Tetracyclines
4) Calrithromycin
5) Colloidal Bismuth

76
Q

Triple therapy has been used to treat H.pylori and includes a ____, in conjunction with ___ and either Amoxicillin, a tetracycline, or clarithromycin

A

bismuth salt, metronidazole, tetracycline/clarithromycin

77
Q

Three major effects of chronic laxative use?

A

1) Laxative dependence
2) Alterations in bowel function
3) Electrolyte imbalances

78
Q

____: abnormally difficult passage of dry, hardened feces - results from decreased motility in relation to amount of water in fecal material

____: abnormally frequent passage of loose, watery feces. It can result from increased motility, excessive intestinal secretion, or decreased reabsorption of water

A

Constipation
Diarrhea

79
Q

4 main mechanisms by which laxatives work?

A

1) Increase motility
2) Prevent absorption of H2O
3) Enhance secretion
4) Dissolve or lubricate fecal mass

80
Q

What are the four bulk forming laxatives?

A

1) Dietary Fiber
2) Methylcellulose
3) Psyllium
4) Polycarbophil

81
Q

___ is an insoluble, hydrophilic polyacrylic resin

A

Polycarbophil

82
Q

Which forms stool faster: Bulk Forming Laxatives or Contact/Stimulant Laxatives?

A

Contact/Stimulant Laxatives (2-8 hrs)

83
Q

Which laxatives mimic the effect of a well-balanced diet and is SAFEST for chronic use?

A

Bulk Forming Laxatives

84
Q

___ laxatives absorb water and swell to form soft mass that induces peristaltic reflexes

A

Bulk forming laxatives

85
Q

True or False: Dietary fibers is a classic bulk forming agent

A

True

86
Q

Which class of laxatives act on intestinal mucosa to enhance secretion, INHIBIT water absorption, or induce peristalsis?

A

Contact/Stimulant Laxatives

87
Q

Which class of laxatives is associated with laxative dependence?

A

Contact/Stimulant Laxatives

88
Q

What are the three contact/stimulant laxatives?

A

1) Bisacondyl
2) Senna/sennosides
3) Phenolphthalein

89
Q

___ is a contact/stimulant laxative that acts on the bowel to INHIBIT absorption of water and may stimulate peristaltic movements

A

Phenolphthalein

90
Q

Castor Oil is hydrolyzed in the small intestines to release ____, the active agent that acts on the mucosa of the ____ to inhibit absorption of ___ and stimulates ____

A

ricinoleic acid; small intestine; fluid; peristaltic movements

91
Q

True or False: Castor oil is associated with watery evacuation, pain, and cramping

A

True

92
Q

True or False: Both Bulk Forming Laxatives and Osmotic Laxatives are poorly absorbed

A

True

93
Q

How do osmotic laxatives work? How long does it take for them to have an effect?

A

Exert osmotic effect to hold water in intestinal tract
1-6 hours

94
Q

What are the three osmotic laxatives and cathartics?

A

1) MgOH
2) Lactulose
3) Polyethylene Glycol

Note: MgOH is both an osmotic laxative AND a neutralizing agent

95
Q

____ is a widely used osmotic laxative/cathartic, particularly to prepare bowel for diagnostic/surgical procedure

A

Polyethylene Glycol

96
Q

___ is a poorly absorbed lubricating agent that coats and lubricates fecal mass

A

Mineral Oil

97
Q

Risks of Mineral Oil?

A

Lipid Pneumonitis (aspiration)

98
Q

Surface Active Agents are also known as ____

A

Fecal Softeners

99
Q

___ is a fecal softener/surface active agent that exerts a detergent effect to break and soften fecal mass + may stimulate secretion of fluid

A

Docusate Sodium

100
Q

True or False: Detergent effect of Docusate Sodium may increase solubility and absorption of other drugs

A

True

101
Q

___ activates chloride channels on the intestinal brush border and, thereby, increases fluid secretion.

Used to treat chronic idiopathic constipation and IBS!!!!

A

Lubiprostone

102
Q

Best drug for chronic idiopathic constipation and IBS in females?

A

Luboprostone

103
Q

Prokinetic Agents increase __ motility

A

GI

104
Q

____ is a cholinomimetic agonist that stimulates M3 receptors on muscle cells and myenteric plexus synapses

A

Bethanechol

105
Q

____ is a prokinetic agent that can be used to treat Ogilvie’s syndrom

A

Neostigmine
(achetylcholinesterase Inhibitor)

106
Q

Why is neostigmine better than bethanechol?

A

The latter just acts at a receptor, whereas neostigmine inhibits Ach breakdown

(have some neural control over when Ach is present)

107
Q

____ is a prokinetic agent that constricts lower GI sphincter, promotes gastric emptying, and can be used to treat GERD or esophagitis.

It is an anti-emetic!!!!!

A

Metoclopramide

108
Q

What condition can metoclopramide prevent?

A

Gastroparesis and GERD

109
Q

___ can be used as an anti-mimetics and is a prokinetic agent. How is it achieved?

A

metoclopramide
- blocks dopamine receptors in CNS

110
Q

___ is an anti-microbial agent that directly stimulates motilin receptors on GI smooth muscle and can treat DIABETIC GASTROPARESIS

A

Erythromycin

111
Q

True or False: Methylnaltrexone and Alvimopan are selective opioid antagonists of the u-opioid receptor and cross the BBB

A

False - DO NOT cross BBB

112
Q

Methylnaltrexone use?

A

-Opioid induced constipation
-Gastreparesis

113
Q

Alvimopan use?

A

Post-op Ileus

Pharmacology (53 decks)

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