Pharmacology of Prokinetic Agents
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Questions and Answers

What is the mechanism of action of 5-HT 3 receptor antagonists in reducing visceral afferent sensation?

  • Inhibition of afferent gastrointestinal 5-HT 3 receptors (correct)
  • Activation of central 5-HT 3 receptors
  • Blockade of extrinsic sensory neurons
  • Stimulation of the type 2 chloride channel
  • Which medication is approved for the treatment of patients with severe IBS with diarrhea?

  • Tegaserod
  • Alosetron (correct)
  • Hyoscyamine
  • Dicyclomine
  • What is the indication for tegaserod?

  • Short-term treatment of women with IBS who had predominant constipation (correct)
  • Severe IBS with constipation
  • Chronic constipation
  • Severe IBS with diarrhea
  • Why was tegaserod voluntarily removed from the market?

    <p>Increased number of cardiovascular deaths</p> Signup and view all the answers

    Which medication is used in the treatment of chronic constipation?

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

    What is the mechanism of action of lubiprostone?

    <p>Stimulation of the type 2 chloride channel</p> Signup and view all the answers

    Which type of receptor is antagonized by alosetron?

    <p>5-HT 3 receptor</p> Signup and view all the answers

    What is the indication for lubiprostone in IBS treatment?

    <p>Women with IBS with predominant constipation</p> Signup and view all the answers

    Which medication is used in the treatment of women with severe IBS with diarrhea?

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

    What is the effect of blockade of central 5-HT 3 receptors?

    <p>Reduced central response to visceral afferent stimulation</p> Signup and view all the answers

    What is the effect of metoclopramide on 5-HT4-receptors?

    <p>Enhances ACh release</p> Signup and view all the answers

    Which type of antibiotic directly stimulates motilin receptors on gastrointestinal smooth muscle?

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

    What is the characteristic of irritable bowel syndrome (IBS)?

    <p>Idiopathic chronic disorder</p> Signup and view all the answers

    What is the mechanism of action of itopride?

    <p>Antidopaminergic and anti-acetylcholinesterase</p> Signup and view all the answers

    What is the goal of pharmacologic therapies for IBS?

    <p>To relieve abdominal pain and improve bowel function</p> Signup and view all the answers

    What is the effect of macrolides in patients with gastroparesis?

    <p>Rapidly develops tolerance</p> Signup and view all the answers

    What is the primary function of Lactobacillus acidophilus in the gut?

    <p>To balance potentially harmful bacteria and maintain a healthy gut microbiome</p> Signup and view all the answers

    What is the major cause of diarrhea and colitis in patients exposed to antibiotics?

    <p>Clostridium difficile infection</p> Signup and view all the answers

    What is the benefit of probiotic supplements like Lactobacillus acidophilus?

    <p>Balancing the gut microbiome and reducing harmful bacteria</p> Signup and view all the answers

    What is the concern with using antidiarrheal agents in patients with fever?

    <p>They may mask the underlying cause of the fever</p> Signup and view all the answers

    What is the benefit of using Super ORS compared to traditional ORS?

    <p>It reduces the frequency of diarrhea along with rehydration</p> Signup and view all the answers

    What is the mechanism of action of adsorbents like kaolin and pectin?

    <p>They coat the GI tract wall and adsorb toxins and bacteria</p> Signup and view all the answers

    What is the effect of 5-HT 3 receptor antagonists on visceral afferent sensation?

    <p>Reduce unpleasant visceral afferent sensation</p> Signup and view all the answers

    What is the indication for alosetron?

    <p>Severe IBS with diarrhea</p> Signup and view all the answers

    What is the mechanism of action of lubiprostone?

    <p>Stimulates the type 2 chloride channel</p> Signup and view all the answers

    What is the current status of tegaserod?

    <p>It was voluntarily removed from the market</p> Signup and view all the answers

    Which medication is used in the treatment of women with IBS with predominant constipation?

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

    What is the effect of 5-HT 3 receptor antagonists on the central nervous system?

    <p>Reduce the central response to visceral afferent stimulation</p> Signup and view all the answers

    Study Notes

    5-HT3 Receptor Antagonists

    • Blockade of 5-HT3 receptors in the gut reduces visceral afferent sensation, thereby decreasing the perception of pain and discomfort.

    Medications for IBS

    • Alosetron is approved for the treatment of severe IBS with diarrhea in women.

    • Tegaserod was once indicated for IBS with constipation, but was voluntarily removed from the market due to concerns about cardiovascular safety.

    • Lubiprostone is indicated for chronic constipation and IBS with constipation.

    • Metoclopramide is used for IBS with constipation.

    Mechanism of Action

    • Lubiprostone acts as a chloride channel activator, increasing intestinal fluid secretion, promoting bowel movements.

    • Alosetron is a selective 5-HT3 receptor antagonist, primarily targeting the gut.

    • Metoclopramide is a dopamine antagonist and a 5-HT4 receptor agonist, accelerating gastric emptying.

    • Itopride is a phosphodiesterase type 10 (PDE10) inhibitor, contributing to the stimulation of intestinal motility.

    Other Medications

    • Macrolides (e.g., erythromycin) are antibiotics that directly stimulate motilin receptors on gastrointestinal smooth muscle, promoting gastric emptying.

    Probiotics

    • Lactobacillus acidophilus is a common probiotic found in yogurt and supplements. It helps in maintaining gut health and reducing diarrhea.

    Antidiarrheal Agents

    • Antidiarrheal agents should be used cautiously in patients with fever, as they can mask serious infections.
    • Super Oral Rehydration Solution (ORS) contains higher electrolyte concentrations and is more effective than traditional ORS in combating dehydration.
    • Adsorbents like kaolin and pectin work by binding to toxins and bacteria in the gut, reducing diarrhea.

    Central Nervous System

    • Blockade of central 5-HT3 receptors can lead to sedation and antiemetic effects.

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    Description

    Test your knowledge of prokinetic agents, their mechanisms of action, and their effects on the gastrointestinal system. Learn about the role of metoclopramide and macrolide antibiotics in stimulating the small intestine and their potential benefits in treating postoperative ileus and chronic intestinal pseudo-obstruction.

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