*GI drugs Flashcards
Antacids
Antacids work through chemical neutralization of
gastrointestinal acids but do not treat the production of gastric
acid, therefore tend to be used to relieve symptoms only
Examples of Proton Pump Inhibitors (PPI)
- Omeprazole
- Lansoprazole
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Indications of Omeprazole
- GERD
- Gastric ulcer
- Gastric ulcer prophylaxis (NSAID associated)
- Hypersecretory Disorders
- H pylori infection:
Mechanism of action of omeprazole (PPI)
- Irreversibly inhibits gastric parietal cell H+-K+-ATPase,
thereby inhibiting gastric acid secretion
Adverse effects of Omeprazole (PPI)
- Headache,
- constipation or diarrhea,
- xerostomia (dry mouth)
- flatulence
H2 RECEPTOR BLOCKERS
- Ranitidine [Zantac®]
- Famotidine [Pepcid®]
- Cimetidine [Tagamet®]
- Nizatidine
Ranitidine was introduced in 1981 and became the world’s top-selling drug in 1988; it’s
considered safer and more potent
• Ranitidine was pulled off the marked in April 2020 after finding carcinogenic contaminants
• Cimetidine first came to market in 1976 and became a world-renowned top-selling drug
Indications of Famotidine (H2 blocker)
- GERD
- Duodenal/gastric ulcer:
Mechanism of action of Famitidine
- Block histamine release from enterchromaffin cells in response to gastrin or vagal stimulation by selective competitive antagonism of parietal cell H2 receptors
- Acid secretion in response to direct stimulation of the parietal cell by gastrin or vagal stimulation is reduced in presence of H2 receptor blockade
• Like H1 antihistamines, the H2 antihistamines are actually considered to act more like inverse agonists rather than pure antagonists
Adverse reactions of Famotidine (H2 blocker)
Common:
- Headache,
- dizziness
Serious:
- Food and drug allergies,
- psychosis,
- depression,
- reversible impotence,
- gynecomastia