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

Antacid and Anti-Ulcer Pharmacology Flashcards

(54 cards)

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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

23
Q

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

Study These Flashcards
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?

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A

Ranitidine (or famotidine)

25
Proton pump inhibitors used as anti-ulcer meds
``` Omeprazole Esomeprazole Lansoprazole Dexlansoprazole Pantoprazole Rabeprazole ```
26
MOA of PPIs
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
Describe PPIs in terms of duration of action, degree of acid inhibition and time for ulcers to heal
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
Adverse effects of PPIs
GI: diarrhea, dyspepsia, nausea, CDAD — Clostridium Difficile-associated Diarrhea CNS: headache, dizziness Rare AEs: generalized myalgias, fatigue, myopathies
29
PPIs are associated with increased risk for what 3 conditions?
Kidney disease (AKI) Bone fractures Cardiovascular disease (MI)
30
Drug interactions with PPIs
Omeprazole is a prototypical PPI for CYP450 inhibition —> many drug interactions
31
Pregnancy is a relative contraindication to PPI use. Which drug can be used if absolutely necessary?
Lansoprazole (or pantoprazole) —try to avoid omeprazole!!
32
MOA of sucralfate
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
Sucralfate is indicated for short-term tx of duodenal ulcers, but is also used off-label for what conditions?
Aphthous ulcers Mucositis/stomatitis Radiation proctitis/ulcers (enema) Bile reflux gastropathy
34
Adverse effect associated with sucralfate
Constipation [formula includes Al(OH)3 — aluminum component associated with constipation]
35
Relative contraindications to sucralfate
Severe renal failure (d/t aluminum component)
36
Drug interactions are possible with sucralfate, so what is the recommendation?
If possible, take 2-hours after other meds [note that sucralfate is dosed QID for active ulcers, so timing can be difficult]
37
Which anti-ulcer med is recommended for people who also require NSAID therapy?
Misoprostol — because it has NSAID diclofenac
38
MOA of misoprostol
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
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?
When given with mifepristone —> pregnancy termination Alone for cervical ripening Post-partum hemorrhaging
40
Adverse effects of misoprostol
Primarily GI: diarrhea (possibly with N/V + cramping) CNS: headache, dizziness
41
Contraindications to misoprostol
Pregnancy (unless specifically for off-label use) IBD
42
MOA of bismuth compounds
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
OTC vs. Rx use of bismuth compounds
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
Adverse effects of Bismuth compounds
Constipation Black/dark regularly-formed stools [know it is not GI bleed bc it is regularly formed!]
45
T/F: bismuth compounds are not associated with drug interactions
False, there are many drug interactions - so these should be taken 2 hours after other meds
46
Relative and absolute contraindications to bismuth compounds
Relative: antiplatelets and anticoagulants, severe renal failure Absolute: GI bleeding, salicylate hypersensitivity
47
Combination therapy for tx of H.pylori is a MUST — what must this combination include?
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
What is included in the more powerful quadruple therapy for H.pylori?
PPI (BID) Metronidazole (QID) Tetracycline (QID) Bismuth subsalicylate (QID)
49
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?
PPI or H2 antagonist
50
What would you give a pt with H.pylori who is allergic to penicillin?
PPI Clarithromycin Metronidazole [consider quad therapy with bismuth]
51
What would you give a pt with H.pylori that is metronidazole-resistant?
PPI Clarithromycin Tetracycline [consider quad therapy with clarithromycin and amoxicillin]
52
What would you give a pt with H.pylori that is resistant to Clarithromycin?
PPI Amoxicillin or tetracycline Metronidazole [consider bismuth quad therapy]
53
How would you treat a pregnant patient with PUD without evidence of H.pylori?
Consider short course of antacids or sucralfate [if moderate symptoms, consider ranitidine; if severe symptoms, consider lansoprazole]
54
How would you tx a pt w/ PUD that is considered NSAID-at risk?
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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