PUD+ GERD Dr. J Flashcards

1
Q

True or false: PPIs are prodrugs

A

True

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2
Q

What type of environment do PPIs need to be in to be activated?

A

Acidic

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3
Q

What 3 components make up a PPI?

A
  1. Benzimidazole
  2. Methylsulfinyl
  3. Pyridine
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4
Q

When Omeprazole is activated by a proton catalyzed process, what does it generate?

A

A sulphenamide

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5
Q

The sulphenamide interacts _____ with the sulphydryl groups of cysteine residues

A

Covalently

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6
Q

To prevent premature degradation of proton pump inhibitors by acid in the gastric lumen, oral dosage forms are supplied in what kind of formulations?

A

Enteric coated

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7
Q

How are PPIs absorbed and how does it reach its site of action?

A

Systemically; through the blood

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8
Q

What CYP enzymes extensively metabolize PPIs?

A
  1. 2C19
  2. 3A4
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9
Q

Protonix is is freely ____ in water

A

Soluble

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10
Q

The stability of protonix in aqueous solution is dependent on what?

A

pH

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11
Q

The delayed release and enteric coated tablets dissolve only at what pH for PPIs?

A

Alkaline

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12
Q

What inhibits acid production by reversible competing with histamine for binding to H2 receptors on the basolateral membrane of parietal cells?

A

H2RAs

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13
Q

True or false: H2RAs are less potent than PPIs

A

True

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14
Q

The H2RAs predominantly inhibit what?

A

Basal acid secretion

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15
Q

Because of what H2RAs inhibit, what are they efficacious for?

A

Suppressing nocturnal secretion

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16
Q

True or false: H2RAs need to have enteric coating

A

False

17
Q

Why isn’t ranitidine on the market?

A

NDMA levels increase in ranitidine even under normal storage conditions

18
Q

H2RAs are rapidly absorbed after oral administration with peak serum concentrations within how many hours?

A

1-3

19
Q

Absorption of H2RAs may be enhanced by ____ or decreased by ______

A

Food; antacids

20
Q

What type of cells are the most prevalent in the acid secreting regions of the stomach?

A

Enterochromaffin like cells (ECL)

21
Q

What cytoprotective effects does PGE2 have? 3

A
  1. Stimulation of mucin
  2. Stimulation of bicarbonate secretion
  3. Increase mucosal blood flow
22
Q

Misoprostol is an agonist at what receptor?

A

EP3

23
Q

True or false: mistoprostol is a prodrug

A

True

24
Q

What does misoprostol decrease?

A

Acid secretion

25
Q

What does sucralfate undergo in an acidic environment?

A

Extensive cross-linking

26
Q

What does sucralfate produce?

A

Viscous, sticky polymer that adheres to epithelial cells and ulcer craters

27
Q

What are the 4 mechanisms of sucralfate cytoprotection?

A
  1. Protective effects in mucus
  2. Antipeptic effect
  3. Barrier effect
  4. Enhanced tissue growth
28
Q

Antacids can prolong neutralizing effects on the pH in the presence of _____.

A

Food

29
Q

H. Pylori releases cytokines, toxins, and chemokines that result in

A

A massive inflammatory response

30
Q

Neutrophils are released from the capillaries to kill H. Pylori, but what else does it destroy?

A

Mucus secreting mucous membranes of the stomach