Antacids and Anti-ulcer Drugs Flashcards by Zach Visinoni

Which salts are considered to be low-systemic agents? (3)

Aluminum salts
Calcium salts
Magnesium salts

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Which salt is considered to be a high-systemic agent?

Sodium salts

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What is Simethicone?

A supplemental agent

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What is the MOA of antacids?

What byproducts are produced as a result? (3)

They combine with H+ ions.

Water, CO2, Cl-

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What are antacids capable of doing at higher doses?

Increase LES tone

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Antacids do NOT…

What might be possible as a result?

Do NOT reduce acid secretion or production.

Rebound acid production is possible.

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Calcium

Onset:
DOA:
ANC:

Onset: rapid
DOA: long
ANC: very good

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Aluminum

Onset:
DOA:
ANC:

Onset: slow
DOA: short
ANC: fair/weak

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Magnesium

Onset:
DOA:
ANC:

Onset: rapid
DOA: long
ANC: good

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Sodium

Onset:
DOA:
ANC:

Onset: rapid
DOA:short
ANC: fair/good

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Simethicone is a…

What does it aid in?

A surfactant - reduces surface tension.

Aids in expulsion of gas.

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Adverse effects of Aluminum (4)

Constipation

Hypophosphatemia (can be used acutely for hyperphosphatemia)

Renal osteodystrophy (ESRD)

Encephalopathy

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Adverse effects of Magnesium (2)

Diarrhea

Hypermagnesemia

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Adverse effects of Calcium (4)

Constipation

Hypercalcemia

Hypophosphatemia (can be used for hyperphosphatemia)

Calcium-based kidney stones

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What causes “Milk-Alkali Syndrome”?

Occurs due to hypercalcemia and results in nephropathy and metabolic alkalosis.

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Adverse effects of Sodium (3)

Gas

Hypernatremia

Metabolic alkalosis

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What are “common, important patient factors” in determining an antacid for a patient? (4)

Dosage form/paliability

Presence of renal or CVD

Electrolyte status

Diseases associated with diarrhea and constipation

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Antacids should never be taken…

With another med at the same time.

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When should antacids be taken?

1-2 hrs. prior to other meds or 2-4 hrs. after.

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MOA of -tidines

H2 receptor antagonists

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MOA of -prazoles

Proton pump inhibitors

MOA of Sucralfate

Surface acting agents

MOA of Misoprostol

PGE1 analogs

5 anti-ulcer agent classes

H2 receptor antagonists

PPIs

Surface acting agents

PGE1 analog

Bismuth compounds

All H2 receptor antagonists can be given IV/PO, except _______, which is given only PO.

Nizatidine

MOA of Histamine type-2 blockers

Reversibly inhibit H2-Rs on basolateral membrane of parietal cells

What is the onset of H2-R blockers? What is the dosing? When does ulcer healing occur? What are the adverse effects?

0.5-2 hrs. (longer than antacids, quicker than PPIs) QD to BID dosing 4-8+ wks. GI-related (N/D/C) and some CNS related (HA)

What unique adverse effect can occur from Cimetidine?

Decreased testosterone binding to androgen (weak anti-androgen effects)

What is the major drug interaction of Cimetidine? What is the major drug interaction of Ranitidine?

Prototypical inhibitor of several CYP450 enzymes. Same, but occurs at approx. 10% of the rate.

What is relative contraindication of H2-R blockers and PPIs?

Pregnancy (if a must, give Ranitidine (H2R antagonist), Lansoprazole (PPI))

All of the PPIs are given PO, except __________, which can be given PO or IV.

Esomeprazole

MOA of PPIs

Covalently bind to SH- groups of H+/K+ ATPase at parietal cell secretory sites, thereby inhibiting gastric acid secretion. After a few days, a new steady-state of pump activity is created.

What is the dosing for PPIs? How long does it take to achieve full symptom effects? How long until it heals ulcerations?

QD, effects last approx. 24 hrs. A few to several days (longer than H2-R antagonists). 4-8+ wks.

What is the major adverse effect of PPIs? | What is the "additional risk"?

GI-related: diarrhea, dyspepsia, nausea. | -C. diff-associated diarrhea

Which PPI is the prototypical PPI for CYP450 inhibition?

Omeprazole

MOA of Sucralfate What is the major indication for it? What is the major adverse effect?\ What is the relative contraindication? How long should they be taken after other meds?

Cross-links via interaction with stomach acid and creates a viscous, sticky polymer that adheres to epithelial cells around the ulcer's crater. -Prevents acid access to the ulcer site. Duodenal ulcers Constipation (Al(OH)3) Severe RF 2 hrs. after other meds

Aside from the the typical MOA of Sucralfate, what might also be stimulated?

Local PG and mucous production and EGF (cytoprotection).

MOA of Misoprostol The standard doses reduces...

It is a PGE1 analog and provides protection to the gastric mucosa and reduces gastric acid release from parietal cells. - Cytoprotection (stimulates bicarb and mucous production) - Increases mucosal blood flow Basal and nocturnal acid output.

What is the indication for Misoprostol? What is the major adverse effect? Contraindications? (2)

Prevention of NSAID-induced gastric ulceration in patients with high risk. GI-related (diarrhea) Pregnancy, IBD

What is the major action of bismuth compounds? What was it originally developed as?

Antimicrobial action - believed to prevent microbial attachment, inactivation of enterotoxins and disruption of cell walls Anti-diarrheal agent

What is the OTC vs. Rx use of bismuth compounds?

OTC - reflux, indigestion and diarrhea Rx - used in combo with abx and acid suppressant for H. pylori

What are the 2 major adverse effects of bismuth compounds? What are the Rx interactions?

Constipation Black (regularly formed) stools Lots, take 2 hrs. post other meds.

What are the 2 relative contraindications and 2 absolute contraindications for bismuth compounds?

Relative - antiplatelets and anticoagulants (bismuth subsalicylate) - severe RF Absolute - GI bleeding - salicylate hypersensitivity

What is the treatment for H. pylori?

Combination therapy is a must: *at least* 2 abx and an acid reducer (PPI or H2-R blocker)

What is the triple therapy for H. pylori? What is the dosing and for how long?

PPI Clarithromycin Amoxicillin or Metronidazole BID for 14 days

What is quadruple therapy for H. pylori? What is the dosing and for how long?

PPI Metronidazole Tetracycline Bismuth subcitrate potassium PPI at BID, all others at QID for 10-14 days

What is in the Prevpac (BID) for PUD?

Amoxicillin Clarithromycin Lansoprazole

What is in the Omeclamox-Pak (BID) for PUD?

Amoxicillin Clarithromycin Omeprazole

What is in the Helidac (QID) for PUD?

Bismuth subsalicylate Metronidazole Tetracycline + PPI

What is in the Pylera (3 capsules QID) for PUD?

Bismuth subcitrate potassium Metronidazole Tetracycline + PPI (omeprazole)

H. pylori with a PCN allergy, give: H. pylori with Metronidazole resistance, give: H. pylori with Clarithromycin resistance, give:

Substitute Metronidazole for Amoxicillin Substitute Tetracycline Substitute either Amoxicillin or Tetracycline

Pregnant patients with PUD, but without H. pylori, give: If moderate? If severe?

Short courses of antacids or sucralfate - if moderate, consider ranitidine - if severe, consider lansoprazole