Pharmacology of Proton-Pump Inhibitors
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Pharmacology of Proton-Pump Inhibitors

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Questions and Answers

What is the mechanism of action of salt-containing osmotic agents?

  • They retain water in the lumen by osmosis (correct)
  • They decrease the absorption of water from the intestine
  • They inhibit the release of digestive enzymes
  • They increase the contraction of intestinal muscles
  • Which of the following laxatives is used rectally?

  • Polyethylene glycol
  • Methylcellulose
  • Psyllium
  • Glycerin (correct)
  • What is the onset of action of salt-containing osmotic agents after oral administration?

  • 12-24 hours
  • 1-2 hours
  • 3-6 hours (correct)
  • 6-12 hours
  • Which of the following is a limitation of mineral oil as a laxative?

    <p>It decreases the absorption of fat-soluble vitamins</p> Signup and view all the answers

    What is the main use of salt-containing osmotic agents?

    <p>Short-term evacuation of the bowel before surgery or diagnostic procedures</p> Signup and view all the answers

    Which of the following is a bulk-forming laxative?

    <p>Psyllium</p> Signup and view all the answers

    What is the effect of lubricant laxatives on the absorption of water?

    <p>They decrease the absorption of water from the intestine</p> Signup and view all the answers

    What is the route of administration of sodium phosphates?

    <p>Oral or rectal</p> Signup and view all the answers

    What is the mechanism of action of osmotic agents, salt-free?

    <p>They retain water in the lumen by osmosis</p> Signup and view all the answers

    What is the effect of adequate hydration on the action of osmotic agents?

    <p>It increases the action of osmotic agents</p> Signup and view all the answers

    Study Notes

    • Act as prophylaxis for recurrent ulcers in patients at risk
    • Can be treated with proton-pump inhibitors (PPIs) such as omeprazole, which reduces both meal-stimulated and basal acid secretion

    Proton-pump Inhibitors (PPIs)

    • Irreversible inhibitors of the H+/K+-ATPase proton pump in parietal cells
    • Block the transport of acid from the cell into the lumen
    • Indications: gastroesophageal reflux disease (GERD), peptic ulcer disease, nonulcer dyspepsia, stress-induced gastritis, and gastrin-secreting tumors (Zollinger-Ellison syndrome)
    • Adverse effects: headaches, gastrointestinal disturbances, and reduction in acid production may permit bacterial overgrowth
    • Major drug interactions: inhibit the metabolism of other drugs like warfarin, can result in drug toxicity

    Prostaglandins

    • Misoprostol (Cytotec) is a methyl analog of PGE1 that acts on parietal cells to inhibit acid secretion and stimulate bicarbonate and mucus production
    • Increases uterine contractions
    • Clinical uses: prevention of NSAIDs-induced ulcer, termination of pregnancy, and induction of labor (off-label)
    • Side effects: diarrhea, abortion, premature birth, birth defects, and uterine rupture (life-threatening)

    Protective Agents

    • Sucralfate (Carafate) is a polysaccharide complexed with aluminum hydroxide that protects ulcerated areas from further damage and promotes healing
    • Effects: stimulates mucosal production of prostaglandins, inhibits pepsin, and has side effects of constipation and nausea
    • Used in critical care settings for stress-related gastritis

    Antacids

    • Weak bases taken orally to partially neutralize gastric acid and reduce pepsin activity
    • Reduce the pain associated with ulcers and may promote healing
    • Prototype agents: sodium bicarbonate, calcium carbonate (TUMS, Os-Cal)

    Other Agents

    • Histamine1 (H1)-receptor antagonists: doxylamine + Vit B6, meclizine, and promethazine, used to treat motion sickness and morning sickness
    • Dopamine antagonists: metoclopramide, used to treat nausea and vomiting, with side effects of sedation, diarrhea, and motor dysfunction
    • 5-HT3 antagonists: ondansetron, used to treat nausea and vomiting, with side effects of mild constipation
    • Benzodiazepines: lorazepam, diazepam, used as anxiolytic agents to reduce anticipatory emesis

    Agents Used to Treat Diarrhea

    • Opiates and opioid-containing preparations: act directly on opiate µ-receptors to decrease GI motility and increase transit time
    • Diphenoxylate: a synthetic morphine analogue used to treat diarrhea
    • Loperamide: an opioid agonist with no CNS activity, used to treat diarrhea, with a potential for severe constipation
    • Bulk-forming laxatives: psyllium and methylcellulose, used to treat constipation
    • Osmotic agents: magnesium citrate, magnesium sulfate, magnesium hydroxide, and sodium phosphates, used to treat constipation
    • Lubricant laxatives: mineral oil and glycerin, used to treat constipation, with limitations of decreasing absorption of fat-soluble vitamins

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    Description

    Learn about the mechanisms of proton-pump inhibitors, such as omeprazole, in preventing stress-related gastritis and recurrent ulcers. Understand how they work to block acid transport in parietal cells.

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