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GI II Final > Antacid and Anti-Ulcer Pharmacology > Flashcards

Antacid and Anti-Ulcer Pharmacology Flashcards

1
Q

What types of meds are used only for short-term, temporary relief of mild pain and symptoms associated with PUD/GERD

A

Antacids

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2
Q

Classes of antacids

A

Low-systemic agents: aluminum salts, calcium salts, magnesium salts

High-systemic agents: sodium salts

Supplemental agents: simethicone

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3
Q

MOA of antacids

A

Combine chemically with H+ ions —> generation of byproducts like water, CO2, and Cl-

Note that they DO NOT reduce acid secretion or production, and rebound acid production is possible!

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4
Q

Antacids are shown to increase ____ at higher doses

A

LES tone

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5
Q

Onset, DOA, and Acid Neutralizing Capacity (ANC) of calcium carbonate antacids

A

Onset: rapid

DOA: long

ANC: very good

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6
Q

Onset, DOA, and Acid Neutralizing Capacity (ANC) of aluminum hydroxide antacids

A

Onset: slow

DOA: short

ANC: fair/weak

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7
Q

Onset, DOA, and Acid Neutralizing Capacity (ANC) of magnesium hydroxide/carbonate/trisilicate antacids

A

Onset: rapid

DOA: long

ANC: good

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8
Q

Onset, DOA, and Acid Neutralizing Capacity (ANC) of sodium bicarbonate antacids

A

Onset: rapid

DOA: short

ANC: fair/good

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9
Q

MOA of simethicone antacids

A

Acts as a surfactant, decreasing surface tension and aiding in expulsion of gas

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10
Q

Adverse effects of aluminum hydroxide antacids

A

Constipation
Hypophosphatemia [thus can be used as acute tx for hyperphosphatemia]

[also renal osteodystrophy and encephalopathy]

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11
Q

Adverse effects of magnesium antacids

A

Diarrhea (stool-softening/laxative-like activity)

Hypermagnesemia

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12
Q

Calcium antacid adverse effects

A

Constipation

Hypercalcemia (Milk-alkali syndrome —> nephropathy and metabolic alkalosis)

Hypophosphatemia

Calcium-based kidney stones

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13
Q

Adverse effects of sodium antacids

A

Gas/flatulence

Hypernatremia

Metabolic alkalosis

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14
Q

What antacids are typically paired together to reduce GI side effects?

A

Magnesium + Calcium antacids

[Mg causes diarrhea, Ca causes constipation — together cancels out]

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15
Q

There are many drug interactions with antacids — what is the rule of thumb for how to best avoid these?

A

Take all antacids 1-2 hours before other medications OR 2-4 hours after other medications

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16
Q

Classes of Anti-Ulcer agents

A

H2 Receptor Antagonists

Proton Pump Inhibitors

Surface Acting Agents

PGE1 Analogs

Bismuth Compounds

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17
Q

H2 blockers used as anti-ulcer meds

A

Cimetidine
Ranitidine
Famotidine
Nizatidine

[some also made with antacids included]

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18
Q

MOA of H2 blockers

A

Reversibly inhibit H2 receptors on basolateral membrane of parietal cell

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19
Q

T/F - H2 blockers can cause total achlorhydria

A

False — they do not completely stop H+ production

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20
Q

H2 blockers have relatively prompt onset of 0.5-2 hours and have QD to BID dosing. How much do they reduce acid production, and how long does it take for ulcer healing?

A

Inhibit 20-50% of acid production [depending on dose/duration]

Ulcer healing occurs in 4-8+ weeks UNLESS CAUSED BY H.PYLORI

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21
Q

Adverse effects of H2 blockers

A

Primarily GI related: nausea, diarrhea, constipation

Some CNS related: Headache

[note that these are relatively mild, transient, and infrequent; with long-term high dosing can see blood dyscrasias like neutropenia and thrombocytopenia]

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22
Q

______ is an H2 blocker that, with long-term high dosing, can decrease testosterone binding to its androgen receptor —> gynecomastia in men and galactorrhea in women

A

Cimetidine

23
Q

Which H2 blocker is a prototypical inhibitor of several CYP450 enzymes, thus leading to many drug-drug interactions?

A

Cimetidine

[Ranitidine has ~10% of the CYP450 inhibition compared to cimetidine]

24
Q

A relative contraindication to H2 blockers is pregnancy. What H2 blocker can be used if absolutely necessary?

A

Ranitidine (or famotidine)

25
Q

Proton pump inhibitors used as anti-ulcer meds

A 
Omeprazole
Esomeprazole
Lansoprazole
Dexlansoprazole
Pantoprazole
Rabeprazole
26
Q

MOA of PPIs

A

PPIs covalently bind to sulfhydryl groups of H/K-ATPase at parietal cell secretory sites, thereby inhibiting gastric acid secretion by irreversibly inhibiting functioning ‘-ase’ pumps

[possible to generate achlorhydria!]

27
Q

Describe PPIs in terms of duration of action, degree of acid inhibition and time for ulcers to heal

A

Effects of PPIs last 24 hours (usually QD dosing),

Inhibit 50-90% of acid [depending on dose/frequence/duration]

Full symptom effects seen in several days (longer than H2 blockers)

Ulcerations healed in 4-8+ weeks — unless caused by H.pylori!!

28
Q

Adverse effects of PPIs

A

GI: diarrhea, dyspepsia, nausea, CDAD — Clostridium Difficile-associated Diarrhea

CNS: headache, dizziness

Rare AEs: generalized myalgias, fatigue, myopathies

29
Q

PPIs are associated with increased risk for what 3 conditions?

A

Kidney disease (AKI)

Bone fractures

Cardiovascular disease (MI)

30
Q

Drug interactions with PPIs

A

Omeprazole is a prototypical PPI for CYP450 inhibition —> many drug interactions

31
Q

Pregnancy is a relative contraindication to PPI use. Which drug can be used if absolutely necessary?

A

Lansoprazole (or pantoprazole)

—try to avoid omeprazole!!

32
Q

MOA of sucralfate

A

Undergoes cross-linking from interaction with stomach acid —> viscous, sticky polymer which adheres to epithelial cells around ulcer’s crater — preventing acid access to ulcer sites

May also stimulate local prostaglandin and mucous production and epidermal growth factor (cytoprotective)

Does not affect pH!

33
Q

Sucralfate is indicated for short-term tx of duodenal ulcers, but is also used off-label for what conditions?

A

Aphthous ulcers
Mucositis/stomatitis
Radiation proctitis/ulcers (enema)
Bile reflux gastropathy

34
Q

Adverse effect associated with sucralfate

A

Constipation

[formula includes Al(OH)3 — aluminum component associated with constipation]

35
Q

Relative contraindications to sucralfate

A

Severe renal failure (d/t aluminum component)

36
Q

Drug interactions are possible with sucralfate, so what is the recommendation?

A

If possible, take 2-hours after other meds

[note that sucralfate is dosed QID for active ulcers, so timing can be difficult]

37
Q

Which anti-ulcer med is recommended for people who also require NSAID therapy?

A

Misoprostol — because it has NSAID diclofenac

38
Q

MOA of misoprostol

A

Prostaglandin E1 analog — provides protective prostaglandin to gastric mucosa and reduces gastric acid release from parietal cell

[thus provides cytoprotection by increasing mucosal defenses; standard doses reduce basal and nocturnal acid output]

39
Q

Primary indication for misoprostol is prevention of NSAID-induced gastric ulceration in pts at high risk of ulcerations and complications. What are some off-label uses for misoprostol?

A

When given with mifepristone —> pregnancy termination

Alone for cervical ripening

Post-partum hemorrhaging

40
Q

Adverse effects of misoprostol

A

Primarily GI: diarrhea (possibly with N/V + cramping)

CNS: headache, dizziness

41
Q

Contraindications to misoprostol

A

Pregnancy (unless specifically for off-label use)

IBD

42
Q

MOA of bismuth compounds

A

Originally developed as anti-diarrheal agent - most well known for its antimicrobial actions (used in combo pack for H.pylori)

Exact mechanism for PUD is not known, but as a salicylate derivative can function similar to ASA and inhibit prostaglandin synthesis

43
Q

OTC vs. Rx use of bismuth compounds

A

OTC: used alone for reflux, indigestion, and diarrhea

Rx: used in combo with abx and acid-suppressant for H.pylori [believed to prevent microbial attachment to mucosa, possible inactivation of enterotoxins, and disruption of bacterial cell wall]

44
Q

Adverse effects of Bismuth compounds

A

Constipation

Black/dark regularly-formed stools [know it is not GI bleed bc it is regularly formed!]

45
Q

T/F: bismuth compounds are not associated with drug interactions

A

False, there are many drug interactions - so these should be taken 2 hours after other meds

46
Q

Relative and absolute contraindications to bismuth compounds

A

Relative: antiplatelets and anticoagulants, severe renal failure

Absolute: GI bleeding, salicylate hypersensitivity

47
Q

Combination therapy for tx of H.pylori is a MUST — what must this combination include?

A

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

The American College of Gastroenterology recommends 10-14 days of a triple-drug regimen containing: a PPI, clarithromycin, and either amoxicillin or metronidazole [all BID dosing]

48
Q

What is included in the more powerful quadruple therapy for H.pylori?

A

PPI (BID)
Metronidazole (QID)
Tetracycline (QID)
Bismuth subsalicylate (QID)

49
Q

The Helidac (QID) used for H.pylori treatment includes bismuth subsalicylate 525 mg, Metronidazole 250 mg, and Tetracycline 500 mg. What must you remember to add to this regimen?

A

PPI or H2 antagonist

50
Q

What would you give a pt with H.pylori who is allergic to penicillin?

A

PPI
Clarithromycin
Metronidazole

[consider quad therapy with bismuth]

51
Q

What would you give a pt with H.pylori that is metronidazole-resistant?

A

PPI
Clarithromycin
Tetracycline

[consider quad therapy with clarithromycin and amoxicillin]

52
Q

What would you give a pt with H.pylori that is resistant to Clarithromycin?

A

PPI
Amoxicillin or tetracycline
Metronidazole

[consider bismuth quad therapy]

53
Q

How would you treat a pregnant patient with PUD without evidence of H.pylori?

A

Consider short course of antacids or sucralfate

[if moderate symptoms, consider ranitidine; if severe symptoms, consider lansoprazole]

54
Q

How would you tx a pt w/ PUD that is considered NSAID-at risk?

A

If NSAIDnot required, consider acetaminophen and discontinue NSAID

If NSAID required, consider COX-2 NSAID and/or consider PPI or Misoprostol

GI II Final (8 decks)

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