Anti-Ulcer Pharm Flashcards

1
Q

What are the main classes of anti-ulcer agents?

A
  • H2 receptor antagonists
  • PPIs
  • surface acting agents (sucralfate)
  • PGE1 analogs (misoprostol)
  • bismuth compounds
  • antacids
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2
Q

What is a good example of why it is important to ask about OTC medications that is exemplified by anti-ulcer medications?

A

some OTC medications have CYP450 inhibition

  • cimetidine
  • omeprazole

*both are prototypical examples of CYP inhibitors used in questions

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3
Q

What anti-ulcer classes are used in an acute settings to decrease acid?

What is their relative order of effective onset of action/symptom relief?

A

antacids > H2 antagonists > PPIs

rapid/instant > 0.5-2 hours > 1-2 days

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4
Q

What anti-ulcer medications are used primarily in prophylactic settings?

A

-PGE1 analogs (misoprostol)

*prophylactic for NSAID related ulcers

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5
Q

What anti-ulcer class does not affect amount of acid produced/present?

A

-surface acting agents (sucralfate)

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6
Q

What is the common suffix of H2 receptor antagonists?

What are the main drugs in the class?

A

-tidine

  • cimetidine
  • famaotidine
  • nizatidine
  • ranitidine (zantac)
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7
Q

Where do H2 receptor antagonists act and what is their mechanism of action?

How does this relate to its effectiveness in reducing acid production?

A

indirect inhibition of acid production

  • reverisbly inhibits H2 receptor on basolateral membrane of parietal cells
  • decreases cAMP -> decreased acid production

Because there are multiple pathways of stimulating acid production and this is only indirectly blocks acid production via one pathway, other pathways can still stimulate acid production (20-50% reduction in acid)

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8
Q

What are the general adverse effects of H2 receptor antagonists?

A

relatively uncommon and mild -> most are OTC for this reason

Adverse effects:

-GI s/x (diarrhea/constipation)

-CNS s/x (HA/dizziness)

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9
Q

What adverse effects are associated with cimetidine specifically?

A

Rare (assoc. w/ long-term use and high does)

  • weak anti-androgen effect (most prominent in cimetidine) -> gynecomastia in men/galactorrhea in women
  • even more rare, impotency in men
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10
Q

What drug interactions occur with H2 receptor antagonists?

A
  • cimetidine is a CYP450 inhibitor -> many interactions
  • ranitidine also but 10%
  • no interacitons in others
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11
Q

What are contraindications for H2 receptor antagonist use?

A

-pregnancy (relative contraindication) - if necessary, use ranitidine

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12
Q

What is the common suffix of PPIs?

What are the main drugs in the class?

A

-prazole

  • omeprazole**
  • esomeprazole
  • lansoprazole/dexlansoprazole
  • pantoprazole
  • rabeprazole
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13
Q

Where do PPIs act and what is their mechanism of action?

How does this relate to its effectiveness in reducing acid production?

A

direct inhibition of acid production:

  • irreverisbly inhibit H+/K+ ATPase on apical surface of parietal cells
  • covalently binds sulfhydryl group preventing function

Directly inhibits acid secretion 50-90+% reduction in acid depending on dose/frequency

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14
Q

What are the adverse effects of PPIs?

A

relatively uncommon and mild -> some are OTC for this reason

Adverse effects:

  • risk of CDAD (C. difficile-associated diarrhea)
  • GI s/x (diarrhea/constipation)
  • CNS s/x (HA/dizziness)
  • decreased Mg2+/Mg2+
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15
Q

What drug interactions occur with PPI use?

A

-omeprazole is a CYP450 inhibitor -> many interactions

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16
Q

What are contraindications for PPIs use?

A

development of profuse, watery diarrhea -> likely developed CDAD

-pregnancy (relative contraindication) - if necessary, use lansoprazole

17
Q

What is the main surface acting agent used for ulcer treatment?

A

-sucralfate (carafate)

octasulfate of sucrose with aluminum hydroxide added

18
Q

What is the mechanism of action of sucralfate?

A

Acts as a bandaid:

-cross-links in stomach acid creating a viscous substance that covers ulcers and protects from further acid damage

-no effect on pH -> does not fix underlying problem, just provides symptomatic relief

19
Q

What are the adverse effects of sucralfate?

A

-constipation (from aluminum)

20
Q

What drug interactions occur with sucralfate use?

A

-viscous polymer formed can trap other medications taken with it -> take 2 hours after other medicatoins

21
Q

How does sucralfate complicate medication schedules?

A
  • must be given at least 2 hours after other medicaitons due to its ability to trap them (all oral meds, not just anti-ulcer)
  • sucralfate is administered QID while most other anti-ulcer medications are less frequently leading to complicated scheduling (especially since must be taken 2 hours after)
22
Q

What are contraindications for sucralfate use?

A

-severe renal failure (aluminum exacerbates)

23
Q

What is the main PGE2 analog used for ulcer-prevention?

A

misoprostol

24
Q

What is the mechanism of action for misoprostol and what is it used for because of this?

A

analog to PGE2 which stimulates bicarbonate and mucous release (cytoprotective) and inhibits acid production

-PGE2 production is blocked by aspirin/NSAIDs so misoprostol is for prophylaxis of NSAID-induced gastritis

25
Q

What are the adverse effects of misprostol?

A

relatively uncommon and mild

Adverse effects:

-GI s/x (diarrhea/constipation)

-CNS s/x (HA/dizziness)

26
Q

What are contraindications for misoprostol use?

A
  • desired pregnancy (teminates pregnancy; this is also an off-label use)
  • IBD
27
Q

What is the main bismuth compound?

A

-bismuth subsalicylate**

28
Q

What is the action of bismuth subsalicylate?

A
  • anti-microbial actions (H. pylori)
  • anti-diarrheal
29
Q

What are the adverse effects of bismuth subsalicylate?

A

Dose related adverse effects:

  • constipation (due to anti-diarrheal effect)
  • black/dark, regularly formed stools from formation of bismuth sulfide, a black pigment (as opposed to dark/tarry in GI bleed)
30
Q

What are contraindications for bismuth subsalicylate use?

A

mostly related to salicylate component

Relative:

  • taking antiplatelet/anticoagulants
  • severe renal failure

Absolute:

  • GI bleeding
  • salicylate hypersensitivity
31
Q

After what time frame should H2 receptor antagonists and PPIs show full symptomatic relief?

What should be considered if symptoms persist?

A

symptoms should resolve without medications after 4-8 weeks as the ulcer should be fully healed by that time

-if symptoms persist, H. pylori should be investigated as these ulcers will not heal w/o antibiotics

32
Q

How does anti-ulcer treatment affect H. pylori testing?

A

bismuth and PPIs inhibit ​H. pylori but don’t eliminate it and can give false negatives on gastric urease or urea breath tests

-should be off these meds for 4 weeks prior to test

33
Q

What is the first line treatment for H. pylori?

(schedule/duration)

A

triple-drug regimen of two abx and a PPI:

  • clarithromycin
  • amoxicillin -or- metronidazole
  • PPI

taken BID for 14 days

34
Q

What drug is sometimes added to H. pylori treatment making it a quadruple therapy?

What are the benefits/complicaitons of this?

A

-bismuth subsalicylate

Benefits:

-more effective, often used after failure of triple therapy w/ consideration of replacing abx

Complications:

  • abx and bismuth given QID while PPI given BID, complicating scheduleing
  • bismuth increases risk of constipation
35
Q

What changes should be made if a patient doesn’t respond to standard triple therapy for H. pylori containing metronidazole​?

A

Replace metronidazole and consider quadruple therapy:

  • metronidazole -> tetracycline -or- amoxicillin
  • keep clarithromycin
  • addition of bismuth subsalicylate -> abx and bismuth given QID w/ PPI gien BID
36
Q

What changes should be made in treating clarithromycin resistant H. pylori?

A

Replace clarithromycin and consider quadruple therapy:

  • clarithromycin -> tetracycline -or- metronidazole/amoxicillin (whichever isn’t already in regimen)
  • keep other abx
  • addition of bismuth subsalicylate -> abx and bismuth given QID w/ PPI gien BID
37
Q

What changes should be made in treating H. pylori in a pt with a penicillin allergy?

A

Triple therapy (w/o amoxicillin as option):

  • clarithromycin
  • metronidazole (instead of metronidazole or amoxicillin)
  • PPI
38
Q

How should PUD be treated in a pregnant woman (no H. pylori)

A

H2 receptor antagonists and PPIs relatively contraindicated

  • first consider antacids or sucralfate
  • if insufficient -> ranitidine (H2 antagonist)
  • if still insufficient -> lansoprazole (PPI)

Misoprostol absolutely contraindicated -> termination of pregnancy

39
Q

What considerations should be taken with NSAIDs and PUD?

A

If not required:

-d/c NSAID and consider acetaminophen

If required:

  • consider COX-2 NSAID instead of COX-1
  • additionally consider adding PPI or misoprostol (PGE2 analog) to either COX-1/2 NSAID