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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
With QD dosing how long do the effects of PPI's last? What % of acid is inhibited?
- Effects last **~24 hours** w/ **QD dosing** - Inhibit **50-90+%** of acid
26
Which anti-ulcer drug class is associated with Clostridium Difficile Associated Diarrhea (CDAD)?
PPI's (-prazoles)
27
Which PPI is a prototypical CYP450 inhibitor? How does this effect drug-drug interactions?
- Omeprazole - **Many** drug-drug interactions
28
PPI's are relatively contraindicated in pregnancy, but if necessary which drugs from this class can be used?
- **Lansoprazole** (common) - **Pantoprazole** \*Try to **avoid** omeprazole
29
What is the MOA of the surfacing acting agent, Sucralfate, used as an anti-ulcer drug?
- 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
The anti-ulcer drug, Sucralfate, may also stimulate production of which cytoprotectant agents?
- Local **prostaglandin** and **mucous** production - **Epidermal GF**
31
Although indicated for Duodenal Ulcers, Sucralfate may also be used off-label for what other disorders?
- Aphthous ulcers - Mucositis/Stomatitis - Radiation proctitis/ulcers (enema) - Bile reflux gastropathy
32
What is an adverse effect associated with the anti-ulcer drug, Sucralfate?
**Constipation** since contains **Al**(OH)3
33
The anti-ulcer drug, Sucralfate, is relatively contraindicated in which patients?
**Severe Renal Failure** -\> aluminum-containing antacids should be avoided
34
Are there drug-drug interactions when taking the anti-ulcer drug, Sucralfate? How many doses taken/day and recommendations when taking other meds?
- Possible - Dosed **QID** - Take **2-hours AFTER** other meds
35
What is the MOA of the anti-ulcer drug Misoprostol? How does it provide cytoprotection?
- Acts as **PGE1 analog** - Provides **protective** prostaglanding to gastric mucosa and **reduces** gastric acid release from parietal cells - **C****yto**protection by increasing**HCO3-, mucous**, and**blood flow**
36
What is the indicated use for the anti-ulcer drug, Misoprostol?
**Prevention** of **NSAID-induced** gastric ulceration in patients at high risk of ulcerations and complications
37
What are 3 common off-label uses of Misoprostol?
- With/Without mifepristone (**pregnancy termination**) - Alone for **cervical ripening** (preparing for delivery) - Treating **p****ost-partum****hemorrhaging** (high dose)
38
What are the 2 common systems where adverse effects of Misoprostol take place and what are they?
1) **Primarily** **GI-related** --\> Diarrhea (with/without N/V and cramping) 2) CNS-related --\> headache/dizziness
39
What are the contraindications for the use of Misoprostol?
- **Pregnancy** unless specifically used for common, off-label issues - **IBD** (avoid if possible)
40
Bismuth compounds were originally developed as what type of agents? They are most well known for which of their actions?
- Anti-diarrheal agents - **Most well known** for their **antimicrobial actions**
41
How does the use of Bismuth Compounds differ when taken as OTC's vs. Prescribed?
- **OTC's** = use alone for reflux (heartburn), indigestion, and diarrhea - **Rx** = used in combo w/ antibiotics and acid suppressant for *H. pylori*
42
What are 2 adverse effects associated with Bismuth Compounds?
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
Are there drug interactions associated with Bismuth Compounds? What is the recommendation for using these compounds while on other meds?
- **LOTS!** - Take **2 hours AFTER** other meds
44
What are the 2 relative contraindications for Bismuth Compounds?
- Pts on **A****ntiplatelets**and**A****nticoagulants** (Bismuth sub**salicylate**) - **Severe renal failure**
45
What are the 2 absolute contraindications for Bismuth Compounds?
- GI bleeding - Salicylate hypersensitivity
46
What is required drug wise for treating *H. pylori?*
- **Combo** therapy is a must! - At least **2 antibiotics** + an acid reducer (**PPI** or H2 blocker)
47
What is the recommended amount of days for a drug-regimen in treating *H. pylori?*
**10-14 days**
48
What is the "classic" triple therapy for *H. pylori?* Dosing frequency and for how many days?
- **14 days** all at **B.I.D** 1) A **PPI** 2) **Clarithromycin** 3) **Amoxicillin** or **Metronidazole**
49
What is the quadruple therapy for H. pylori? Dosing frequency and for how many days?
- **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
After a 10-14 day treatment regimen for *H. pylori* what treatment should be considered for complete healing of ulcers?
**PPI** therapy for **4-8 weeks**
51
For *H. pylori* treatment in someone with a **penicillin allergy**, what should you use?
Substitue **metronidazole** (consider Bismuth quad.)
52
For *H. pylori* treatment in community with **metronidazole resistance**, what should you use?
- Substitute **tetracycline** - Consider **quad therapy** (w/ **clarithromycin** and **amoxicillin**)
53
For *H. pylori* treatment in a community with **clarithromycin resistance**, what should you use?
- Substitute **amoxicillin** or **tetracycline** - Consider **Bismuth quad. therapy**
54
If a pregnant patient has PUD without *H. pylori* how should you treat this? Moderate symptoms? Severe symptoms?
- Consider **short course** of **antacids** or **sucralfate** - **Moderate** symptoms, consider **ranitidine** (H2 antagonist) - **Severe** symptoms, consider **lansoprazole** (PPI)
55
If patient is NSAID-at risk for PUD and the NSAID is not required what should be recommended?
Consider **acetaminophen** and D/C NSAID
56
If patient is NSAID-at risk for PUD and the NSAID **is required** what should be recommended?
- Consider **COX-2 NSAID** and/or - Consider **PPI** or **Misoprostol**

GI II Exam 2 (15 decks)

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