Antacids and Anti-Ulcer Agents Flashcards
(72 cards)
1
Q
A
2
Q
Antacids are used only for what?
A
Short-term, temporary relief of mild pain and sx’s of PUD/GERD
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.
4
Q
What are the 2 main types of antacids and what is the supplimental class?
A
- Low-systemic agents
- High-systemic agents
- Simethicone (supplimental agent)
5
Q
What are the 3 low-systemic agents used as antacids?
A
- Aluminum salts
- Calcium salts
- Magnesium salts
6
Q
What is the high-systemic agents used as antacids?
A
Sodium salts
7
Q
Clinically, which antacid will we never use or prescribe and why?
A
Sodium-based agent, because will increase Na+ too high.
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
9
Q
With chronic use of antacids what may be seen with acid production?
A
Rebound acid production
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)
11
Q
What is the onset, duration of action, and acid neutralizing capacity of aluminum-based antacids?
A
- Slow
- Short
- Fair/weak
12
Q
What is the onset, duration of action, and acid neutralizing capacity of Na+-based antacids?
A
- Rapid
- Short
- Fair
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)
14
Q
What are two dose-related adverse effects associated with aluminum-based antacids?
A
- Constipation
-
Hypophosphatemia
- Can be used as an acute treatment for hyperphosphatemia
15
Q
What are two dose-related adverse effects associated with magnesium-based antacids?
A
-
Diarrhea
- Can be used as a laxative/stool softner (“milk of magnesia)
- Hypermagnesemia
16
Q
What are 4 dose-related adverse effects associated with calcium-based antacids?
May produce what syndrome?
A
- Constipation (‘C’ is for calcium)
-
Hypercalcemia
- Milk-alkali syndrome => nephropathy and metabolic alkalosis
- Ca2+-kidney stones
-
Hypophosphatemia
- Used as tx for hyperphosphatemia
17
Q
What are 3 dose-related adverse effects associated with Na+-based antacids?
A
- Gas/bloating
- Hypernatremia
- Metabolix alkalosis
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
- Do not takes meds at the same time
19
Q
If patient has chronic diarrhea, what anatacid will we NOT give them?
A
Mg2+- based antacid
20
Q
What are the 5 types of Anti-Ulcer drugs?
A
- H2 receptor ANT
- PPI
- Surface Acting Agents
- PGE1 Analogs
- Bismuth Compounds
21
Q
H2 Receptor ANT
- Suffix
- Drugs?
A
- -tidine
- Cimetidine (po/iv)
- Famotidine (po/iv)
- Nizatidine (po)
- Ranitidine (po/iv)
22
Q
PPIs
- Suffix
- Drugs?
A
- -prazole
- Lansoprazole
- *Dexlansoprazole (isomer)
- Omeprazole
- *Esomeprazole (isomer)
- Pantoprazole
- Rabeprazole
23
Q
What is the surface acting agent used as an anti-ulcer drug?
A
Sucralfate
24
Q
What is the PGE1 analog (mimic PGE1) used as an anti-ulcer drug?
A
Misoprostol
25
What is the **bismuth compound** used as an **anti-ulcer drug**?
**Bismuth subsalicylate**
26
All **H2 receptor ANT** can be taken by **po/IV**, except \_\_\_\_\_\_
**Nizatidine (po only)**
27
Some of the **H2 receptor antagonists** used as anti-ulcer drugs are combined with what?
**Antacids** (Ca2+ and Mg2+)
28
What is the **MOA** of the **H2-receptor antagonists** used as anti-ulcer drugs?
* **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.
29
How do **H2 ANT** decrease GERD symptoms?
Ulcers?
* **Prompt** **onset** and **relief** (longer than antacids, but shorter than PPIs)
* Ulcers heal in **4-8 weeks.**
30
**_H2-receptors antagonists_**
## Footnote
**Adverse effects**
**_Mild, transient_** **and** **_infrequent_**
* **Mainly GI related** (N/D/Constip)
* Some **CNS related** (HA)
31
Which H2-receptor antagonist used as an anti-ulcer drug is a prototypical **inhibitor** of several **CYP450 isoenzymes**?
Why is this bad?
**Cimetidine**
LOTS of drug interactions
32
**H2-receptor antagonists** as anti-ulcer drugs are **relatively contraindicated during pregnancy,** but which drugs in this class can be used if absolutely necessary?
1. **Ranitidine** (most data) or
2. Famotidine
33
What is the **MOA** of the **PPI's** (-prazoles) used as anti-ulcer drugs?
- Covalently bind sulfhydryl groups of **H+/K+-ATPase** on parietal cells secretory sites, inhibit secretion of gastric acid by **irreversibly** inhibiting "-ase" pumps
34
Can we give enough **PPIs** to stop ALL acid production?
**Yes**; becaues it is the final pathway.
35
**_Which works the fastest?_**
Antacid, H2 ANT, PPI?
**_Antacids_ \> _H2 ANT_ \> _PPI_**
36
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
37
How do **PPIs** compare with H2 ANT in when the full sx effects are seen and how long ulcers heal?
* Full sx effects seen in **few-several days (longer than H2)**
* **4-8 weeks**
38
Which anti-ulcer drug class is associated with **Clostridium Difficile Associated Diarrhea** (CDAD)?
**PPI's (-prazoles)**
39
AE of **PPIs**
1. **GI**
1. N/D/dyspepsia
2. CDAD
2. **CNS**
1. HA/dizziness
3. **Rare**
1. Myalgias, fatigue, myopathies
40
Which **PPI** is a prototypical CYP450 inhibitor?
How does this effect drug-drug interactions?
- Omeprazole
- **Many** drug-drug interactions
41
**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
42
What is the **MOA** of the surfacing acting agent, **Sucralfate**, used as an anti-ulcer drug?
- 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
The anti-ulcer drug, **Sucralfate**, may also stimulate production of which cytoprotectant agents?
1. Prostaglandin
2. Mucous
3. Epidermal GF
44
**Sulcralfate** _______ pH.
**Does not affect**
45
What are uses for **Sulcalfate**?
* Indicated for **duodenal ulcers.**
* Off label use for:
1. Apthous ulcers
2. Mucositis/stomatitis
3. Radiation proctitis/ulvers (enema)
4. Bild reflux gastropathy.
46
AE **Sucralfate**
**Constipation** because it contains aluminum
47
**Sulcalfrate** relative CI
**Severe Renal Failure** -\> aluminum-containing antacids should be avoided
48
**_Sulcralfate_**
* Interactions
* Dosage when taking other meds
* **Possible**
* **QID**; take **2 hours after** other meds
49
MOA anti- ulcer drug **Misoprosto (PGE1 analog)**?
How does it provide cytoprotection?
- PGE1 analog that protects gastric mucosa and reduces gastric acid release from parietal cells
- Cytoprotection by increasing:
* HCO3-
* mucous
* blood flow
50
Indications for **Misoprostol**
Prevents of **NSAID-induced gastric ulcers** in patients at high risk of ulcerations and complications
51
3 common off-label uses of **Misoprostol**?
1. - With/Without mifepristone (**pregnancy termination**)
2. - Alone for cervical ripening (**preparing for delivery**)
3. - Treating **post-partum hemorrhaging (**high dose)
52
**Misoprostol AE**
1. Mainly GI
1. **Diarrhea** (w/wo N/V and cramping)
2. CNS
1. **HA/dizziness**
53
**MIsoprostol CI**
1. **Pregnancy** unless specifically used for common, off-label issues
2. **IBD** (avoid if possible)
54
**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**
55
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** = use w/ ABX and acid suppressant for H. pylori
56
**Bismuth compounds** AE
* 1. **Constipation** (anti-diarrhea)
* 2. **Black/dark NL poop**
*
57
What is the vital question to ask if a patient taking **bismuth compounds** has very dark poop?
What is the shape?
* If **NL** = bismuth
* If like **tar** =\> GI bleed (melena)
58
**_Bismuth compounds_**
* Drug interactions
* Dosage when using other meds
* **LOTS**
* **2 hours AFTER** other meds
59
**Bismuth compounds** relative CI and absolute CI
* **Relative CI**
* 1. Antiplatelet/anticoagulants (bismuth subsalicylate)
* 2. Severe renal failure
* **Absolute**
* 1. GI bleed
* 2. Salicyclate hypersensitivity
60
What is required drug wise for treating H. pylori?
- Combo therapy is a must!
- **At least 2 ABX** + an **acid reducer** (PPI or H2 blocker)
61
What is the recommended amount of days for a drug-regimen in treating H. pylori?
**10-14 days**
62
What is the "**classic" triple therapy** for H. pylori?
Dosing frequency and for how many days?
**_14 days BID_**
1. PPI
2. Clarithromycin
3. Amoxicillin or metronidazole (unless in a highly resistant area)
63
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 (BID)
* 2) Metronidazole (QID)
* 3) Tetracycline (QID)
* 4) Bismuth subsalicylate (QID)
64
When performing tests to detect H.Pylori, what should the patient do?
Stop taking agents (bismuth, antimicrobials and PPIs) that supress H. pylori 4 weeks before because could lead to a false (-).
65
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
66
For H. pylori treatment in someone with a **penicillin allergy**, what should you use?
Substitue **metronidazole** (consider Bismuth quad.)
67
For H. pylori treatment in community with **metronidazole resistance**, what should you use?
1. - Take **tetracycline**
2. - Consider **quad therapy** (w/ clarithromycin and amoxicillin)
68
For H. pylori treatment in a community with **clarithromycin resistance**, what should you use?
1. Substitute amoxicillin or tetracycline
2. Consider Bismuth quad. therapy
69
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)**
70
If patient is **NSAID-at risk for PUD** and the NSAID is **not required** what should be recommended?
Consider **acetaminophen** and D/C NSAID
71
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**
72
