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GI II Exam 1 > Antacids and Anti-Ulcer Agents > Flashcards

Antacids and Anti-Ulcer Agents Flashcards

1
Q
A
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2
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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3
Q

What is the goal of antacids?

A

Put the patient on the SHORTEST dose, for the SHORTEST amount of time for symptomatic relief.

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4
Q

What are the 2 main types of antacids and what is the supplimental class?

A
  1. Low-systemic agents
  2. High-systemic agents
  3. Simethicone (supplimental agent)
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5
Q

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

A
  1. Aluminum salts
  2. Calcium salts
  3. Magnesium salts
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6
Q

What is the high-systemic agents used as antacids?

A

Sodium salts

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7
Q

Clinically, which antacid will we never use or prescribe and why?

A

Sodium-based agent, because will increase Na+ too high.

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8
Q

What is the MOA of antacids?

Do they reduce acid secretion or production?

A
  • Bind to extracellular H+ ions secreted by PP & make byproducts (i.e., H2O, CO2..)
  • They DON’T reduce acid secretion or production
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9
Q

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

A

Rebound acid production

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10
Q

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

A

Calcium (very good acid neutralizing capacity) and Magnesium (good acid neutralizing capacity)

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11
Q

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

A
  • Slow
  • Short
  • Fair/weak
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12
Q

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

A
  • Rapid
  • Short
  • Fair
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13
Q

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

MOA and use?

A
  • Simethocone
  • A surfactant (decreases surface tension)
  • Helps to relieve gas (fart)
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14
Q

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

A
  1. Constipation
  2. Hypophosphatemia
    1. Can be used as an acute treatment for hyperphosphatemia
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15
Q

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

A
  1. Diarrhea
    1. Can be used as a laxative/stool softner (“milk of magnesia)
  2. Hypermagnesemia
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16
Q

What are 4 dose-related adverse effects associated with calcium-based antacids?

May produce what syndrome?

A
  1. Constipation (‘C’ is for calcium)
  2. Hypercalcemia
    • Milk-alkali syndrome => nephropathy and metabolic alkalosis
  3. Ca2+-kidney stones
  4. Hypophosphatemia
    • Used as tx for hyperphosphatemia
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17
Q

What are 3 dose-related adverse effects associated with Na+-based antacids?

A
  1. Gas/bloating
  2. Hypernatremia
  3. Metabolix alkalosis
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18
Q

Antacids

  • Drug interactions?
  • Dosage timing when taking with other medications?
A
    • TONS
    • Do not takes meds at the same time
      • 1-2 hours BEFORE meds or 2-4 hours AFTER other mids
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19
Q

If patient has chronic diarrhea, what anatacid will we NOT give them?

A

Mg2+- based antacid

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20
Q

What are the 5 types of Anti-Ulcer drugs?

A
  1. H2 receptor ANT
  2. PPI
  3. Surface Acting Agents
  4. PGE1 Analogs
  5. Bismuth Compounds
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21
Q

H2 Receptor ANT

  • Suffix
  • Drugs?
A
  • -tidine
  1. ​Cimetidine (po/iv)
  2. Famotidine (po/iv)
  3. Nizatidine (po)
  4. Ranitidine (po/iv)
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22
Q

PPIs

  • Suffix
  • Drugs?
A
  • -prazole
  1. ​Lansoprazole
  2. *Dexlansoprazole (isomer)
  3. Omeprazole
  4. ​*Esomeprazole (isomer)
  5. Pantoprazole
  6. Rabeprazole
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23
Q

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

A

Sucralfate

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24
Q

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

A

Misoprostol

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25
Q

What is the bismuth compound used as an anti-ulcer drug?

A

Bismuth subsalicylate

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26
Q

All H2 receptor ANT can be taken by po/IV, except ______

A

Nizatidine (po only)

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27
Q

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

A

Antacids (Ca2+ and Mg2+)

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28
Q

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

A
  • Reversibly inhibit H2-R on BL membrane of parietal cells => ↓ acid (H+) production, but doesnt completely shut off.
    • Gastrin binds to CCK on ECL cell => release HA => HA binds to H2R on the parietal cell => produces acid.
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29
Q

How do H2 ANT decrease GERD symptoms?

Ulcers?

A
  • Prompt onset and relief (longer than antacids, but shorter than PPIs)
  • Ulcers heal in 4-8 weeks.
30
Q

H2-receptors antagonists

Adverse effects

A

Mild, transient and infrequent

  • Mainly GI related (N/D/Constip)
  • Some CNS related (HA)
31
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 interactions

32
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
  1. Ranitidine (most data) or
  2. Famotidine
33
Q

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

A
  • Covalently bind sulfhydryl groups of H+/K+-ATPase on parietal cells secretory sites, inhibit secretion of gastric acid by irreversibly inhibiting “-ase” pumps
34
Q

Can we give enough PPIs to stop ALL acid production?

A

Yes; becaues it is the final pathway.

35
Q

Which works the fastest?

Antacid, H2 ANT, PPI?

A

Antacids > H2 ANT > PPI

36
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
37
Q

How do PPIs compare with H2 ANT in when the full sx effects are seen and how long ulcers heal?

A
  • Full sx effects seen in few-several days (longer than H2)
  • 4-8 weeks
38
Q

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

A

PPI’s (-prazoles)

39
Q

AE of PPIs

A
  1. GI
    1. N/D/dyspepsia
    2. CDAD
  2. CNS
    1. HA/dizziness
  3. Rare
    1. Myalgias, fatigue, myopathies
40
Q

Which PPI is a prototypical CYP450 inhibitor?

How does this effect drug-drug interactions?

A
  • Omeprazole
  • Many drug-drug interactions
41
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

42
Q

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

A
  • Cross-linking d/t interaction with stomach acid, creating viscous, sticky polymer (band-aid) that sticks to epithelial cells around ulcer’s crater = prevents H+ access to ulcer sites
43
Q

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

A
  1. Prostaglandin
  2. Mucous
  3. Epidermal GF
44
Q

Sulcralfate _______ pH.

A

Does not affect

45
Q

What are uses for Sulcalfate?

A
  • Indicated for duodenal ulcers.
  • Off label use for:
    1. Apthous ulcers
    2. Mucositis/stomatitis
    3. Radiation proctitis/ulvers (enema)
    4. Bild reflux gastropathy.
46
Q

AE Sucralfate

A

Constipation because it contains aluminum

47
Q

Sulcalfrate relative CI

A

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

48
Q

Sulcralfate

  • Interactions
  • Dosage when taking other meds
A
  • Possible
  • QID; take 2 hours after other meds
49
Q

MOA anti- ulcer drug Misoprosto (PGE1 analog)?

How does it provide cytoprotection?

A
  • PGE1 analog that protects gastric mucosa and reduces gastric acid release from parietal cells
  • Cytoprotection by increasing:
  • HCO3-
  • mucous
  • blood flow
50
Q

Indications for Misoprostol

A

Prevents of NSAID-induced gastric ulcers in patients at high risk of ulcerations and complications

51
Q

3 common off-label uses of Misoprostol?

A
    • With/Without mifepristone (pregnancy termination)
    • Alone for cervical ripening (preparing for delivery)
    • Treating post-partum hemorrhaging (high dose)
52
Q

Misoprostol AE

A
  1. Mainly GI
    1. Diarrhea (w/wo N/V and cramping)
  2. CNS
    1. HA/dizziness
53
Q

MIsoprostol CI

A
  1. Pregnancy unless specifically used for common, off-label issues
  2. IBD (avoid if possible)
54
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
55
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 = use w/ ABX and acid suppressant for H. pylori
56
Q

Bismuth compounds AE

A
    1. Constipation (anti-diarrhea)
    1. Black/dark NL poop
      *
57
Q

What is the vital question to ask if a patient taking bismuth compounds has very dark poop?

A

What is the shape?

  • If NL = bismuth
  • If like tar => GI bleed (melena)
58
Q

Bismuth compounds

  • Drug interactions
  • Dosage when using other meds
A
  • LOTS
  • 2 hours AFTER other meds
59
Q

Bismuth compounds relative CI and absolute CI

A
  • Relative CI
      1. Antiplatelet/anticoagulants (bismuth subsalicylate)
      1. Severe renal failure
  • Absolute
      1. GI bleed
      1. Salicyclate hypersensitivity
60
Q

What is required drug wise for treating H. pylori?

A
  • Combo therapy is a must!
  • At least 2 ABX + an acid reducer (PPI or H2 blocker)
61
Q

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

A

10-14 days

62
Q

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

Dosing frequency and for how many days?

A

14 days BID

  1. PPI
  2. Clarithromycin
  3. Amoxicillin or metronidazole (unless in a highly resistant area)
63
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 (BID)
  • 2) Metronidazole (QID)
  • 3) Tetracycline (QID)
  • 4) Bismuth subsalicylate (QID)
64
Q

When performing tests to detect H.Pylori, what should the patient do?

A

Stop taking agents (bismuth, antimicrobials and PPIs) that supress H. pylori 4 weeks before because could lead to a false (-).

65
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

66
Q

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

A

Substitue metronidazole (consider Bismuth quad.)

67
Q

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

A
    • Take tetracycline
    • Consider quad therapy (w/ clarithromycin and amoxicillin)
68
Q

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

A
  1. Substitute amoxicillin or tetracycline
  2. Consider Bismuth quad. therapy
69
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)
70
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

71
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 1 (19 decks)

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