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GI II Exam 2 > Lecture 7: Antacids and Anti-Ulcer Agents > Flashcards

Lecture 7: Antacids and Anti-Ulcer Agents Flashcards

1
Q

Antacids are used only for what?

A

Short-term, temporary relief of mild pain and sx’s of PUD/GERD

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2
Q

What are the 3 low-systemic agents used as antacids?

A
  1. Aluminum-based
  2. Calcium-based
  3. Magnesium-based
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3
Q

What is the high-systemic agent used as an antacid?

A

Sodium salts

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4
Q

What is the MOA of antacids?

Do they inhibit secreton or production of acid?

A
  • Combine chemically w/ H+ ions and make byproducts (i.e., H2O, CO2..)
  • They DON’T reduce acid secretion or production
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5
Q

With chronic use of antacids what may be seen with acid production?

A

Rebound acid production

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6
Q

Which 2 antacids have rapid onset, a long duration of action, and good/very good acid neutralizing capacity?

A

1) Calcium = very good ANC
2) Magnesium = good ANC

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7
Q

What is the onset, duration of action, and acid neutralizing capacity of sodium-based antacids?

A
  • Onset = rapid
  • DOA = short
  • ANC = fair/good
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8
Q

What is a supplemental compound that is often co-administered with antacids?

MOA and use?

A
  • Simethicone
  • A surfactant - decreases surface tension
  • Aids in the expulsion of gas
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9
Q

What are two dose-related adverse effects associated with aluminum-based antacids?

A
  • Constipation
  • Hypophosphatemia –> acute tx for hyperphosphatemia
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10
Q

What are two dose-related adverse effects associated with magnesium-based antacids?

A
  • Diarrhea (stool-softening/laxative-like activity)
  • Hypermagnesemia
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11
Q

What are four dose-related adverse effects associated with calcium-based antacids?

May produce what syndrome?

A
  • Constipation (‘C’ for Calcium)
  • Hypercalcemia –> ‘Milk-Alkali Syndrome’ = nephropathy and metabolic alkalosis
  • Hypophosphatemia
  • Calcium-based kidney stones
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12
Q

What are three dose-related adverse effects associated with sodium-based antacids?

A
  • Gas/flatulence (‘bicarb. burp’)
  • Hypernatremia
  • Metabolic alkalosis
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13
Q

Are there drug interactions that need to be considered when taking antacids?

What is the recommendation for dosage timing in a patient taking other meds + antacids?

A
  • TONS!
  • Take all antacids 1-2 hours BEFORE other meds OR

- 2-4 hours AFTER other meds

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14
Q

What is the suffix for the H2 Receptor Antagonists used as Anti-Ulcer drugs?

List the 4 most common

A

-tidine

  • Cimetidine
  • Famotidine
  • Nizatidine
  • Ranitidine
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15
Q

What is the suffix for the PPI’s used as Anti-Ulcer drugs?

List the 6 most common

A

-prazole

  • Lansoprazole
  • Dexlansoprazole
  • Omeprazole
  • Esomeprazole
  • Pantoprazole
  • Rabeprazole
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16
Q

What is the surface acting agent used as an anti-ulcer drug?

A

Sucralfate

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17
Q

What is the PGE1 analog used as an anti-ulcer drug?

A

Misoprostol

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18
Q

Some of the H2 receptor antagonists used as anti-ulcer drugs are formulated with what?

A

Antacids –> calcium + magnesium

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19
Q

What is the MOA of the H2-receptor antagonists used as anti-ulcer drugs?

A

Reversibly inhibit H2-receptors on baso-lateral membrane of parietal cells

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20
Q

The adverse effects associated with H2-receptors antagonists are primarily of what 2 type?

A
  1. GI-related –> Nausea/Diarrhea/Constipation
  2. CNS-related –> Headache
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21
Q

The H2-receptor antagonist, Cimetidine, has been associated with what rare side-effects with long-term high doses?

A
  • Decreases testosterone binding to androgen receptors
  • Gynecomastia in men
  • Galactorrhea in women
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22
Q

Which H2-receptor antagonist used as an anti-ulcer drug is a prototypical inhibitor of several CYP450 isoenzymes?

Why is this bad?

A
  • Cimetidine
  • LOTS of drug-drug interactions
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23
Q

H2-receptor antagonists as anti-ulcer drugs are relatively contraindicated during pregnancy, but which drugs in this class can be used if absolutely necessary?

A
  • Ranitidine (most data) or

- Famotidine

24
Q

What is the MOA of the PPI’s (-prazoles) used as anti-ulcer drugs?

A
  • Covalently bind sulfhydryl groups of H+/K+-ATPase at parietal cells secretory sites
  • Inhibit gastric acid secretion by irreversibly inhibiting “-ase” pumps
25
Q

With QD dosing how long do the effects of PPI’s last?

What % of acid is inhibited?

A
  • Effects last ~24 hours w/ QD dosing
  • Inhibit 50-90+% of acid
26
Q

Which anti-ulcer drug class is associated with Clostridium Difficile Associated Diarrhea (CDAD)?

A

PPI’s (-prazoles)

27
Q

Which PPI is a prototypical CYP450 inhibitor?

How does this effect drug-drug interactions?

A
  • Omeprazole
  • Many drug-drug interactions
28
Q

PPI’s are relatively contraindicated in pregnancy, but if necessary which drugs from this class can be used?

A
  • Lansoprazole (common)
  • Pantoprazole

*Try to avoid omeprazole

29
Q

What is the MOA of the surfacing acting agent, Sucralfate, used as an anti-ulcer drug?

A
  • Undergoes cross-linking from interaction w/ stomach acid
  • Creates viscous, sticky polymer which adheres to epithelial cells around ulcer’s crater = prevents H+ access to ulcer sites
30
Q

The anti-ulcer drug, Sucralfate, may also stimulate production of which cytoprotectant agents?

A
  • Local prostaglandin and mucous production
  • Epidermal GF
31
Q

Although indicated for Duodenal Ulcers, Sucralfate may also be used off-label for what other disorders?

A
  • Aphthous ulcers
  • Mucositis/Stomatitis
  • Radiation proctitis/ulcers (enema)
  • Bile reflux gastropathy
32
Q

What is an adverse effect associated with the anti-ulcer drug, Sucralfate?

A

Constipation since contains Al(OH)3

33
Q

The anti-ulcer drug, Sucralfate, is relatively contraindicated in which patients?

A

Severe Renal Failure -> aluminum-containing antacids should be avoided

34
Q

Are there drug-drug interactions when taking the anti-ulcer drug, Sucralfate?

How many doses taken/day and recommendations when taking other meds?

A
  • Possible
  • Dosed QID
  • Take 2-hours AFTER other meds
35
Q

What is the MOA of the anti-ulcer drug Misoprostol?

How does it provide cytoprotection?

A
  • Acts as PGE1 analog
  • Provides protective prostaglanding to gastric mucosa and reduces gastric acid release from parietal cells
  • Cytoprotection by increasingHCO3-, mucous, andblood flow
36
Q

What is the indicated use for the anti-ulcer drug, Misoprostol?

A

Prevention of NSAID-induced gastric ulceration in patients at high risk of ulcerations and complications

37
Q

What are 3 common off-label uses of Misoprostol?

A
  • With/Without mifepristone (pregnancy termination)
  • Alone for cervical ripening (preparing for delivery)
  • Treating post-partumhemorrhaging (high dose)
38
Q

What are the 2 common systems where adverse effects of Misoprostol take place and what are they?

A

1) Primarily GI-related –> Diarrhea (with/without N/V and cramping)
2) CNS-related –> headache/dizziness

39
Q

What are the contraindications for the use of Misoprostol?

A
  • Pregnancy unless specifically used for common, off-label issues
  • IBD (avoid if possible)
40
Q

Bismuth compounds were originally developed as what type of agents?

They are most well known for which of their actions?

A
  • Anti-diarrheal agents
  • Most well known for their antimicrobial actions
41
Q

How does the use of Bismuth Compounds differ when taken as OTC’s vs. Prescribed?

A
  • OTC’s = use alone for reflux (heartburn), indigestion, and diarrhea
  • Rx = used in combo w/ antibiotics and acid suppressant for H. pylori
42
Q

What are 2 adverse effects associated with Bismuth Compounds?

A
  1. Constipation (anti-diarrheal actions)
  2. Black/dark (REGULARLY-formed) stools

*Important to realize they are regularly-formed dark stools, because dark stools are a red flag if they are anything but regularly formed!

43
Q

Are there drug interactions associated with Bismuth Compounds?

What is the recommendation for using these compounds while on other meds?

A
  • LOTS!
  • Take 2 hours AFTER other meds
44
Q

What are the 2 relative contraindications for Bismuth Compounds?

A
  • Pts on AntiplateletsandAnticoagulants (Bismuth subsalicylate)
  • Severe renal failure
45
Q

What are the 2 absolute contraindications for Bismuth Compounds?

A
  • GI bleeding
  • Salicylate hypersensitivity
46
Q

What is required drug wise for treating H. pylori?

A
  • Combo therapy is a must!
  • At least 2 antibiotics + an acid reducer (PPI or H2 blocker)
47
Q

What is the recommended amount of days for a drug-regimen in treating H. pylori?

A

10-14 days

48
Q

What is the “classic” triple therapy for H. pylori?

Dosing frequency and for how many days?

A
  • 14 days all at B.I.D
    1) A PPI
    2) Clarithromycin
    3) Amoxicillin or Metronidazole
49
Q

What is the quadruple therapy for H. pylori?

Dosing frequency and for how many days?

A
  • 10-14 days w/ PPI given B.I.D and ALL others Q.I.D
    1) PPI
    2) Metronidazole
    3) Tetracycline
    4) Bismuth subsalicylate
50
Q

After a 10-14 day treatment regimen for H. pylori what treatment should be considered for complete healing of ulcers?

A

PPI therapy for 4-8 weeks

51
Q

For H. pylori treatment in someone with a penicillin allergy, what should you use?

A

Substitue metronidazole (consider Bismuth quad.)

52
Q

For H. pylori treatment in community with metronidazole resistance, what should you use?

A
  • Substitute tetracycline
  • Consider quad therapy (w/ clarithromycin and amoxicillin)
53
Q

For H. pylori treatment in a community with clarithromycin resistance, what should you use?

A
  • Substitute amoxicillin or tetracycline
  • Consider Bismuth quad. therapy
54
Q

If a pregnant patient has PUD without H. pylori how should you treat this?

Moderate symptoms?

Severe symptoms?

A
  • Consider short course of antacids or sucralfate
  • Moderate symptoms, consider ranitidine (H2 antagonist)
  • Severe symptoms, consider lansoprazole (PPI)
55
Q

If patient is NSAID-at risk for PUD and the NSAID is not required what should be recommended?

A

Consider acetaminophen and D/C NSAID

56
Q

If patient is NSAID-at risk for PUD and the NSAID is required what should be recommended?

A
  • Consider COX-2 NSAID and/or
  • Consider PPI or Misoprostol

GI II Exam 2 (15 decks)

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