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Flashcards in Upper GI Drugs Deck (50)
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1

Peptic Ulcer Disease (PUD) is ____ erosions d/t corroding factors overwhelming protective factors

Peptic Ulcer Disease (PUD) is mucosal erosions d/t corroding factors overwhelming protective factors

2

Gastric ulcers from NSAID use and epigastric pain is _____ by eating

whereas

Duodenal ulcers from H. pylori infection, epigastric pain ____ by eating

 

Gastric ulcers from NSAID use and epigastric pain is worsened by eating

whereas

Duodenal ulcers from H. pylori infection, epigastric pain relieved by eating

3

Describe the image 

2 physiological states of gastric acid production: Basal & Meal stimulated 

4

Antacids are weak ____ obtained without prescription → causes ____ of low gastric pH → protects esophageal mucosa from ____

 

 

Antacids are weak bases obtained without prescription → causes neutralization of low gastric pH → protects esophageal mucosa from reflux corrosion

Antacid + HCl → salt + H2O

Time of onset: 5 minutes
Duration of action: 30 mins – 1 hour

5

Antacids can affect other drugs by ____ gastric and urinary pH or by _____ gastric emptying.

All can cause ____.

Antacids can affect other drugs by increasing gastric and urinary pH or by delaying gastric emptying.

All can cause hypokalemia.

6

(Antacids)

Aluminum Hydroxide causes ____  

 Magnesium Hydroxide causes ____

therefore, combined to produce _____

(Antacids)

Aluminum Hydroxide causes constipation  
"Aluminimum amount of feces"

 Magnesium Hydroxide causes osmotic diarrhea
"Must go 2 the washroom (Mg2+)"

Al and Mg combined to produce no change in bowel movements

7

Calcium Carbonate is an ____, CO2 causes _____, can lead to metabolic _____, aka ____ syndrome.

Calcium Carbonate is an antacid, CO2 causes belching, can lead to metabolic alkalosis, aka milk alkali syndrome.

8

describe antacid drug interactions 

  • Binding/chelation of many drugs
  • Increased gastric pH alters dissolution of weakly charged drugs
  • Decreased absorption of co-administered:
    • TetracyclinesFluoroquinolonesItraconazole, Iron

9

H2 receptor antagonists suppress ___-induced gastric acid secretion, and reduce signal transduction for ____ and ____-induced gastric acid production

H2 receptor antagonists suppress histamine-induced gastric acid secretion, and reduce signal transduction for ACh and Gastrin-induced gastric acid production

10

H2 receptor antagonists are selective _____ inhibitors at the ____ cell H2 Gs protein coupled receptor

Time of onset: 2.5 hours
Duration of action: 4- 10 hours
_____ develops in 2- 6 weeks

H2 receptor antagonists are selective competitive inhibitors at the parietal cell H2 Gs protein coupled receptor

Time of onset: 2.5 hours
Duration of action: 4- 10 hours
Tachyphylaxis develops in 2- 6 weeks

11

list the H2 Receptor Antagonists

  • Cimetidine – prototype with many adverse effects

  • Ranitidine, Famotidine, Nizatidine – 2nd generation with no anti-androgenic or CNS adverse effects

12

describe the effect of H2RAs on Gastric Acid Secretion

H2RAs strongly suppress basal gastric acid secretion

13

list the H2 receptor antagonist indications 

  • GERD
  • PUD
  • Nonulcer dyspepsia
  • Prophylaxis against stress-related gastritis

14

what is the only H2 receptor antagonist with adverse effects 

CIMETIDINE

15

AEs of Cimitidine

  • acts as nonsteroidal anti-androgen and prolactin stimulant → gynecomastia, galactorrhea, and male impotence
  • Crosses BBB → confusion, dizziness and headaches
  • Increases gastric pH → B12 deficiency and myelosuppression (long term use)
  • Potent CYP450 inhibitor increasing serum [ ] of:
    • Warfarin, DiazepamPhenytoin

16

______  are the most potent inhibitors of gastric acid secretion → inhibit 90–98% of 24-hour acid secretion

Proton pump inhibitors are the most potent inhibitors of gastric acid secretion → inhibit 90–98% of 24-hour acid secretion

17

PPIs ____ bind and inhibit the ____ ATPase pump of gastric ____ cells

suppressing the final ____ pathway of gastric acid secretion

PPIs irreversibily bind and inhibit the H+-K+ ATPase pump of gastric parietal cells

suppressing the final common pathway of gastric acid secretion

18

describe the image

PPIs strongly suppress basal & meal stimulated gastric acid production

19

list PPIs

  • Omeprazole
  • Esomeprazole
  • Lansoprazole
  • Rabeprazole
  • Pantoprazole

20

list the indications for PPIs

  • Patients who fail twice-daily H2RA therapy
  • Severe symptoms of GERD that impair quality of life
  • PUD
    • H. pylori eradication
    • NSAID associated ulcers
    • Prevention of peptic ulcer rebleeding
  • Gastrinoma
  • Nonulcer dyspepsia
  • Prophylaxis against stress-related gastritis

21

PPI adverse effects

  • Vitamin B12 deficiency – d/t reduced pepsin function
  • Increased risk of CAP and C. difficile colitis
  • Hypomagnesemia
  • Osteopenia – possibly via reduced Ca2+ absorption or osteoclast inhibition
    • FDA-mandated warning of possible increased risk of fractures
  • Diarrhea, abdominal pain and headache reported in less than 5% of patients

22

____ and ____ inhibit CYP450 decreasing metabolism of which drugs? 

Omeprazole and Cimitidine inhibit CYP450 decreasing metabolism of Warfarin, Diazepam, Phenytoin

23

Clopidogrel (prodrug) requires activation by hepatic P450 _____ isoenzyme

drugs that affect this isoenzyme are (3) - what is their effect on clopidogrel?

Clopidogrel (prodrug) requires activation by hepatic P450 CYP2C19 isoenzyme

(LEO) Lansoprazole, Esomeprazole, Omeprazole inhibit CYP2C19 reducing Clopidogrel activation

24

____ or ____ are preferred in persons taking clopidogrel

pantoprazole or rabeprazole are preferred in persons taking clopidogrel

25

H. Pylori is gram ____, contains ____ and H +/-?

causes inflammatory response, with increased risk of: 

H. Pylori is gram negative, contains urease and H+

causes inflammatory response, with increased risk of: 

  • Peptic ulcer disease (esp. duodenal)
  • Gastritis
  • Gastric MALToma
  • Gastric adenocarcinoma

26

H. Pylori eradication triple therapy combines two ____ with a ____, resulting in <15% recurrence

H. Pylori eradication triple therapy combines two antibiotics with a PPI, resulting in <15% recurrence

 

27

describe how PPIs promote eradication of H. pylori

  1. Direct antimicrobial properties
  2. Increased gastric pH → lowers minimal inhibitory concentrations of antibiotics needed to clear the organism

28

Triple therapy for ____ days - which drugs? 

Triple therapy for 10-14 days - which drugs? 

Clarithromycin + Amoxicillin + PPI

Clarithromycin + Metronidazole + PPI

29

Quadruple therapy for ___ days - which drugs? 

Quadruple therapy for 14 days

Bismuth Subsalicylate + Tetracycline + Metronidazole + PPI

30

list the mucosal protective agents 

  • Misoprostol

  • Sucralfate

  • Bismuth Subsalicylate