Treatments for Acid-Peptic Diseases Flashcards by Kayla Schenheit

What drugs do you need to know for Eradication of H. pylori?

Amoxicillin
Bismuth subsalicylate
Clarithromycin
Metronidazole/Tinidazole
Tetracycline
Rifabutin

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What drugs do you need to know for the promotion of mucosal defense?

Bismuth subsalicylate
Misoprostol
Simethicone
Sucralfate

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What drugs do you need to know for reduction in intragastric acidity?

Antacids
Antimuscarinics
H2 blockers
Proton Pump Inhibitors

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What are the antacids?

Aluminum hydroxide
Calcium carbonate
Magnesium hydroxide
Sodium bicarbonate

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What are the antimuscarinics?

Atropine

- Pirenzipine

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What are the H2 blockers?

Cimetidine
Famotidine
Nizatidine
Ranitidine
Roxatidine

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What are the Proton Pump Inhibitors?

Lansoprazole
Omeprazole
Esomeprazole
Pantoprazole
Rabeprazole

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What are the most effective drugs for preventing and treating peptic ulcer disease? Why?

Antimicrobials (Amoxicillin, Clarithromycin, Metronidazole, Rifabutin and Tetracycline). Because they eradicate H. pylori.

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What is the penicillin of choice for H. pylori treatment?

Amoxicillin

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Why is Amoxicillin the penicillin of choice?

It is more acid stable and more than twice the blood levels are achieved with the same oral dose.

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What is the macrolide antibiotic of choice for H. pylori treatment?

Clarithromycin

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Why is Clarithromycin the macrolide of choice?

It has the lowest MIC50 and is more acid stable.

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What antibiotic CAN be used to treat H. pylori infections?

Tetracycline

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What happens if Tetracycline is co-administered with antacids?

Antacids significantly decrease antibiotic efficacy due to chelation

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What drugs effectively decrease all forms of gastric acid secretion (esp. nocturnal)?

H2 receptor blockers:

Cimetidine
Famotidine
Nizatidine
Ranitidine

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What drugs have few side effects, leading to their OTC status?

H2 receptor blockers (except Cimetidine)

What drugs are the most effective agents for reducing intragastric acidity?

Proton Pump Inhibitors:

Omeprazole
Esomeprazole
Rabeprazole
Lansoprazole
Pantoprazole

What is the mechanism of proton pump inhibitors?

Irreversibly block the final common pathway in acid secretion - H+/K+ ATPase

What are the weak bases?

Antacids:

Aluminum hydroxide
Calcium carbonate
Magnesium hydroxide
Sodium bicarbonate

What are the weak bases used for?

To buffer stomach acid

What do antacids differ greatly in?

Efficacy and side effects

How can the differences in antacids be predicted?

Based on the degree of systemic absorption, rate of dissolution and reactivity, as well as the effects of cations and/or reaction products.

Antacids:

Rapid onset but short duration of action; no prevention of ulcer recurrence –> useful for intermittent dyspepsia

H2 blockers:

Relatively rapid onset, intermediate duration, some prevention –> many uses

PPIs:

Slow onset of action, very long duration of action, excellent prevention --> drugs of choice for Zollinger-Ellison syndrome and GERD, as well as ulcer treatment

What two drugs protect the ulcer surface by different mechanisms?

Sucralfate and Bismuth Subsalicylate

What is the drug of choice based on MOA for ulcers induced by NSAIDS?

Misoprostol (PGE1), although side effects and the need for frequent dosing limit its use. It is an abortifacient.

What are two of the many drug-drug interactions that have been documented for anti-ulcer medications?

1. Among the drugs within the anti-ulcer regimens (Tetracycline + antacids, for example) 2. Alterations in the pharmacokinetics of other drugs a patient is taking (especially in cases where luminal pH is critical for absorption, as both increases and decreases in bioavailability have been documented). The fact that many of these drugs are available OTC must be considered also.

What are the main uses for anti-ulcer drugs?

1. Treatment of Peptic Ulcer disease - H. pylori, 65 percent - NSAIDs, 25 percent - Others, 10 percent 2. GERD and NERD (non-errosive reflux disease) - Eliminating H. pylori may make these worse 3. Hypersecretory states - Dyspepsia (self limiting) - Stress ulcers (ICU) - Gastronoma (Zollinger-Ellison Syndrome) - Systemic mastocytosis (hyper secretion of stomach acid)

What are the goals of anti-ulcer drug treatment?

1. Heal lesion 2. Relieve pain 3. Remove possibility of recurrence 4. Avoid complications 5. Eliminate Maintenances 6. Prevent development of resistance (antibiotics)

What are treatment strategies with anti-ulcer drugs?

1. Eliminate H. pylori 2. Decrease Pain - Decrease stimulation of acid production (H+) - Decrease acid production (H+) - Buffer acid - Protect surface 3. Replace PGEs (NSAID induced ulcers)

What factors influence the choice of specific antimicrobial agents for treatment of H. pylori infection?

1. Susceptibility of H. pylori to drug (MIC 50/90 - lower value is better) 2. Distribution of drug (pharmacokinetics) 3. Resistance (metronidazole is being phased out)

From what directions can drugs attack H. pylori?

From the stomach, through the mucus gel layer and from the blood stream through the mucus cells.

What make Amoxicillin the penicillin of choice?

1. Effective against gram - 2. Orally available 3. Acid stable

What is Amoxicillin's MOA and toxicity?

- Bactericidal - Cell Wall Inhibitor - Major toxicity = Hypersensitivity Reactions