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GI II - Week 1 > Anti-Ulcer Drugs (Segars) > Flashcards

Anti-Ulcer Drugs (Segars) Flashcards

1
Q

What are the categories of drug families for anti-ulcer treatment?

A
    • H2 receptor antagonists
    • Proton pump inhibitors
    • Surface acting agents
    • PGE1 analogs
    • Bismuth compounds
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2
Q

What is the common suffix for the drugs in the H2 receptor antagonist family?

A

-tidine

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3
Q

What drugs are in the H2 receptor antagonist family?

A
    • Cimetidine
    • Ranitidine
    • Famotidine
    • Nizatidine

***Taken by mouth or IV!

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4
Q

Most H2 receptor antagonists are OTC. Some products are also made with ________ included (calcium/magnesium).

A

Antacids

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5
Q

Can H2 receptor antagonists totally block all acid production?

A

No, there are other pathways still there

***Inhibits 20-50% of acid production depending on dose and duration!

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6
Q

Explain the mechanism of action of H2 receptor antagonists.

A

They reversibly inhibit H2 receptors on the basolateral membrane of parietal cells. It stops the receptors from stimulating the cAMP-dependent pathway that powers the H+, K+ ATPase (thus releasing acid).

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7
Q

H2 receptor antagonists have a relatively prompt onset of action and relief of GERD symptoms. Onset is _______ hours (longer than antacids, but shorter than PPIs).

A

0.5 - 2

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8
Q

How long does ulcer healing take for H2 receptor antagonists?

A

4-8+ weeks

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9
Q

T/F. H2 receptor antagonists can have severe CNS adverse effects, so must be monitored closely.

A

False. H2 receptor antagonists are very tolerable and rarely have adverse effects.

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10
Q

This is a rare side effect of ________, a H2 receptor antagonist. It can decrease testosterone binding to androgen receptors (weak anti-androgen effects).

A

Cimetidine

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11
Q

What are the resultant effects of Cimetidine when it decreases testosterone binding to androgen receptors?

A

Gynecomastia in men (breast development)

Galactorrhea in women (liquid secretion from breasts)

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12
Q

What is another rare side effect of H2 receptor antagonists?

A

Blood dyscrasias – Neutropenia and Thrombocytopenia

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13
Q

The rare side effects that occur with H2 receptors antagonists are more likely with long-term use and (HIGH/LOW) dosing.

A

High

***Very high doses, these kinds of doses are not used at all anymore!

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14
Q

This H2 receptor antagonist is a prototypical inhibitor of several CYP450 isoenzymes.

A

Cimetidine

***Remember, CYP450 enzymes are what metabolize drugs faster. So their inhibition will make drugs metabolize more slowly. Have to watch for causing drug toxicity!

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15
Q

This H2 receptor antagonist has about 10% of the CYP450 inhibition compared to Cimetidine.

A

Ranitidine

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16
Q

What are relative contraindications for H2 receptor antagonists?

A

Pregnancy

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17
Q

If necessary, what H2 receptor antagonists can be given to pregnant women?

A

Ranitidine, but others can be used too such as Famotidine

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18
Q

This drug family is the most common and most effective in ulcer treatment.

A

PPIs (Proton Pump Inhibitors)

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19
Q

What is the common suffix for the PPIs?

A

-prazole

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20
Q

What drugs are considered PPIs?

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

For their mechanism of action, PPIs covalently bind to ________ groups of H+/K+ ATPase at parietal cell secretory sites, thereby inhibiting gastric acid secretion by irreversibly inhibiting functioning ‘-ase’ pumps.

A

Sulfhydryl

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22
Q

______ will inhibit pump-induced egress of gastric acid, and it will take several days to create a new steady-state of pump activity.

A

PPIs

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23
Q

Can PPIs completely stop acid production?

A

Yes they can get very close (50-90%) depending on dose, frequency, and duration.

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24
Q

Full symptom effects of PPIs are seen in a few to several days (longer than H2 receptor antagonists), and ulcerations usually heal in 4-8+ weeks. What should we consider if the ulcers do not heal after this amount of time?

A

Need to consider H. pylori and also give antibiotics!

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25
Q

PPIs adverse effects are relatively mild and infrequent. They can be GI or CNS related. What is the major GI related risk we have to watch out for?

A

Clostridium Difficile-Associated Diarrhea (CDAD)

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26
Q

This drug is a prototypical PPI for CYP450 inhibition.

A

Omeprazole

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27
Q

What is a relative contraindication for PPIs?

A

Pregnancy

28
Q

Only if necessary, what PPI is used for women that are pregnant?

A

Iansoprazole (commonly used) but other can used too, such as Pantoprazole

29
Q

This surface acting agent is a sulfated polysaccharide. Only one in its group.

A

Sucralfate

30
Q

Sucralfate is an octasulfate of sucrose with _______ added.

A

Al(OH)3

31
Q

Explain the mechanism of action for Sucralfate.

A

Undergoes cross-linking from interaction with stomach acid, creating a viscous, sticky polymer which adheres to epithelial cells around ulcer’s crater. Prevents acid access to ulcer sites.

***Called the Band-Aid Drug!

32
Q

Sucralfate may also stimulate local ________ and mucous production and ________. This is called ________. Does not affect pH.

A

Prostaglandin
EGF (epidermal growth factor)
Cytoprotection

33
Q

Sucralfate works on the superficial epithelial cells rather than the ________ cells like the previous medications.

A

Parietal

34
Q

Sucralfate is indicated for DU, but is also used off-label for what?

A
    • Aphthous ulcers
    • Mucositis/Stomatitis
    • Radiation proctitis/ulcers (enema)
    • Bile reflux gastropathy
    • Others…
35
Q

What are the adverse effects of Sucralfate?

A

Constipation (due to the Al(OH)3)

36
Q

This is a relative contraindication for the use of Sucralfate, but is only relative considering it’s just a short-term therapy.

A

Severe renal failure (due to the aluminum)

***Aluminum-containing antacids should be avoided!

37
Q

Why is it important to take Sucralfate 2-hours after other medications?

A

So other meds can’t get stuck in it!

38
Q

Sucralfate is dosed ______ for active ulcers, so plan dosing other meds accordingly if possible.

A

QID

39
Q

This drug is the only PGE1 analog.

A

Misoprostol

40
Q

Explain the mechanism of action of Misoprostol.

A

It provides protective prostaglandin to gastric mucosa and reduces gastric acid release from parietal cells. These are vital when a patient chronically uses NSAIDs, because NSAIDs will block prostaglandin production thus resulting in ulcers. PGE1 analogs will produce these and stop acid production.

41
Q

Misoprostol provides _________ by increasing mucosal defenses. It stimulates bicarbonate and mucous production and increases mucosal blood flow.

A

Cytoprotection

42
Q

T/F. Standard doses of Misoprostol reduce basal and nocturnal acid output (less than H2 antagonists and PPIs).

A

True

43
Q

Misprostol is used for prevention (primary prophylaxis) of _______-induced gastric ulceration in patients at high risk of ulcerations and complications.

A

NSAID

44
Q

NSAIDs block bad prostaglandins, but they also block the good ones and can result in ulcers. Misoprostol is for patients who can NOT stop taking NSAIDs. Otherwise, what would be the primary treatment for these patients?

A

Stop taking the NSAIDs – no more ulcers

45
Q

What are the contraindications for Misoprostol?

A

– Pregnancy (only for common off-label issues)

– IBD (if patient has IBD, avoid use if possible because Misoprostol has diarrheal affects)

46
Q

Bismuth compounds include pesto-bismol, kaeopectate, etc. They are also in combination packs for H. pylori. What is the drug in this category?

A

Bismuth Subsalicylate

47
Q

Bismuth compounds were originally developed as anti-diarrheal agents, but they are well known for their __________ actions.

A

Antimicrobial

48
Q

Bismuth compounds antibacterial actions are believed to prevent microbial attachment to mucosa, possible inactivation of _________, and disruption of bacterial cells wall.

A

Enterotoxins

49
Q

What are Bismuth compounds used for OTC and Rx?

A

OTC = Used alone for reflux (heartburn), indigestion, and diarrhea

Rx = Used in combination with antibiotic and acid suppressant for H. pylori

50
Q

What are the adverse effects of Bismuth compounds, which are dosage related?

A

– Constipation (due to anti-diarrheal actions)

– Black/Dark (regularly-formed) stools –> If the stools appear tarry then it’s something else!

51
Q

There are a lot of drug interactions with Bismuth compounds, so they should be taken _______ after other medications.

A

2 hours

52
Q

What are relative contraindications for Bismuth compounds?

A

– Antiplatelets and anticoagulants (because Bismuth Subsalicylate can slightly increase bleeding)

– Severe renal failure

53
Q

What are absolute contraindications for Bismuth compounds?

A
    • GI bleeding

- - Salicylate hypersensitivity

54
Q

For treatment of H. pylori, combination therapy is a must! What is the combination used?

A

At least 2 antibiotics and an acid reducer (PPI or H2 blocker)

55
Q

For the treatment of H. pylori, the American College of Gastroenterology (ACG) recommends ______ days of a triple-drug regimen containing: a PPI, _________, and either ________ or _______ (for 1st line of therapy; unless high-resistance area).

A

10-14
Clarithromycin
Amoxicillin
Metronidazole

56
Q

Bismuth preparations, some antimicrobials, and some PPIs suppress H. pylori. Ingestion of these substances within 4 weeks prior to performing gastric urease or urea breath-tests for H. pylori detection may lead to…

A

False negative tests

***Patient must avoid using these agents for at least 4 weeks prior to tests!

57
Q

What is used for the H. pylori triple therapy, lasting for 14 days?

A

All at BID dosing

    • PPI
    • Clarithromycin
    • Amoxicillin or Metronidazole
58
Q

What is used for the H. pylori quadruple therapy, lasting for 10-14 days?

A

PPI taken BID, all other meds taken at QID dosing

    • PPI
    • Metronidazole
    • Tetracycline
    • Bismuth subsalicylate
59
Q

What is available to make treatment for H. pylori much easier?

A

Medication packs that have the triple and quadruple therapies all in one place.

60
Q

To ensure the complete healing of ulcers, consider ______ therapy for a few/several weeks after 10-14 day H. pylori combination therapy.

A

PPI

61
Q

What should be done if there is failure of eradication with a metronidazole-containing triple-therapy?

A

Should follow with a non-metronidazole containing quadruple therapy

62
Q

What do we do if the patient needs to be treated for H. pylori and has an allergy to penicillins?

A

Do not give them amoxicillin in the triple therapy, instead give them Metronidazole or consider using the Bismuth quadruple therapy.

63
Q

What do we do if the patient needs to be treated for H. pylori and has Metronidazole resistance?

A

Substitute Tetracycline for it, or consider the quadruple therapy (with clarithromycin and amoxicillin)

64
Q

What do we do if the patient needs to be treated for H. pylori and has Clarithromycin resistance?

A

Substitute it for Amoxicillin or Tetracycline, or consider the Bismuth quadruple therapy

65
Q

If there is a pregnant patient with PUD that is not caused by H. pylori, we should consider the use of a short course of antacids or ________. For moderate symptoms, consider ________, but for severe symptoms, consider ________.

A

Sucralfate (topical)
Ranitidine
Iansoprazole

66
Q

For PUD due to NSAID use, if the NSAIDs are not required then consider using _________ and D/C NSAID.

A

Acetaminophen

67
Q

For PUD due to NSAID use, if the NSAIDs can’t be discontinued, consider a _______ NSAID and/or a _______ or _______.

A

COX-2
PPI
Misoprostol

GI II - Week 1 (4 decks)

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