Gastrointestinal Drugs I Flashcards

1
Q

Basic pathophysiology leading to ulcers?

A
  1. Increased acid
  2. Decreased mucosal resistance
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2
Q

Three receptors on the parietal cell? Overall effect?

A
  1. Histamine
  2. Gastrin
  3. ACh

Stimulate K+/H+ ATPase activity

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3
Q

By what mechanism does Histamine work to increase stomach acidity?

A

Histamine hits receptor that causes an increase in cAMP and K+/H+ action

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4
Q

Describe the mechanism of action of gastrin to increase acidity of stomach. ACh?

A

Both hit their respective receptors and cause an influx of Ca2+ activating K+/H+ ATPase

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5
Q

Where do Gastrin and ACh come from, respectively?

A
  • Gastrin - antrum
  • ACh - Vagal inputs
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6
Q

What are the goals of pharmacologic intervention for ulcer Tx?

A
  1. Relieft of Syx, especially pain
  2. Promotion of healing
  3. Prevention of complications such as perforation, hemorrhage, or scar formation
  4. Prevention of recurrence
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7
Q

Tx plan for ulcer?

A
  1. Neutralize acid
  2. Decrease acid production
  3. Increase mucosal resistance
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8
Q

Antacid neutralizing efficacy based on:

A
  1. The neutralizing power of the antacid
  2. The degree or rate of acid secretion
  3. Rate of stomach emptying
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9
Q

What are the active ingredients of antacid preparations?

A
  • CaCO3
  • NaHCO3
  • Mg(OH)2 and MgCO3
  • Al(OH)2
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10
Q

Mjr SE of CaCO3

A

Milk-alkali syndrome, nephrocalcinosis, rebound acidity, digitalis antagonism

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11
Q

SE of NaHCO3

A

Systemic alkalosis and therefore rarely used

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12
Q

SE of Mg(OH)2?

A

Diarrhea, Hypokalemia, Hypermagnesemia, complexing of enteric iron and therefore iron deficiency

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13
Q

Why is Al(OH)2 less likely to cause electrolyte imbalances?

A

Al precipitates with enteric phosphate and is not absorbed in the gut

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14
Q

Adverse effects of Al(OH)2?

A

Constipation, Phosphate depletion and sequelae

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15
Q

What would an equivalent procedure be to using an Anticholinergic agent?

A

Vagotomy

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16
Q

What are the SE of anticholinergic agents?

A
  • Dryness of mouth
  • Blurred vision
  • Atony of the bladder
  • Constipation
  • Drowsiness
  • Mental Confusion
17
Q

What are the anticholinergic drugs?

A

Atropine, Prpantheline, Metantheline bromide

18
Q

What are the two big guns of the H2 blocker family? The lesser kids?

A
  • Cimetidine and ranitidine
  • Famotidine
  • Nizatidine
19
Q

What is an important consideration when prescribing an H2 blocker?

A

Cimetidine and ranitidine bind to CP450 interfering with the metabolism of drugs such as theophylline, warfarin, dilantin, or lidocaine

20
Q

What are the H+/K+ ATPase inhibitors?

A
  • Omeprazole
  • Lansoprazole
  • Rabeprazole
  • Esomeprazole
  • Pantoprazole
  • Dexlansoprazole
21
Q

Which H+/K+ ATPase inhibitor has the best bioavailability?

A

Lansoprazole

22
Q

Which H+/K+ ATPase inhbitor has the greatest P450 inhbition? Moderate? Least?

A
  • Most - Omeprazole
  • Moderate - Rabeprazole
  • Least - Pantoprazole
23
Q

Which H+/K+ ATPase inhibitor has the greatest bioavailability and least P450 inhibition?

A

Pantoprazole

24
Q

What are the advantages of H+K+ ATPase inhibitors over the H2 inhibitors?

A
  • Better pain relief
  • Faster healing of ulcer
  • Heal H2 antagonist refractory ulcers
25
Q

SE of HKAIs?

A
  • Gynecomastia
  • P450 inhibition and delayed metabolism of diazepam, warfarin, dilantin
  • Gastric hyperplasia in humans

Not recommended for long term Tx

26
Q

What are two exogenous agents that can cause ulcers?

A
  • NSAIDS
  • H. Pylori
27
Q

MOA of Bismuth Salts?

A

In acidic environment, salts precipitate and coat ulcer

28
Q

MOA of sucralfate?

A

Al(OH)2 complex of sucrose activated in acidic environment and binds to ulcer

29
Q

Which ulcer-coating agent is most efficacious?

A

Bismuth salts

30
Q

In a patient taking chronic NSAIDs, what would be a good medication to prescribe to prevent ulcers?

A

Presribe misoprostol to compensate for prostaglandin defciency due to NSAIDs.

31
Q

What is the adverse effects of misoprostol?

A

Transient diarrhea, can’t be used in pregnancy

32
Q

Tx for H. pylori infection?

A

Bismuth salts, Metrinidazole+ tetracycline/amoxicillin

33
Q

Preferred Tx for H. pylori infection?

A
  • Twice a day PPI (proton pump inhibitor)
  • OR
  • Ranitidine bismuth citrate twice a day
  • PLUS
  • Two of these guys: Amoxicillin, clarithromycin, metronidazole
34
Q

In what scenario is an advantage in ranitidine bismuth triple Tx observed for H. pylori infection over PPI?

A

When resistant H. pylori present

35
Q

What is quadruple Tx for H pylori?

A
  • PPI
  • Tetracycline
  • Bismuth subsalicylate or subcitrate
  • Metronidazole