Pharmacology of Peptic Ulcer Treatment

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Questions and Answers

What is the primary mechanism of action for sucralfate in treating peptic ulcer disease?

  • Enhances mucosal barrier through prostaglandin synthesis (correct)
  • Inhibits gastric acid secretion
  • Stimulates gastric emptying
  • Directly neutralizes stomach acid

Which side effect is commonly associated with sucralfate?

  • Constipation (correct)
  • Hypercalcemia
  • Flatulence
  • Diarrhea

Bismuth subsalicylate has several roles in treatment. Which of the following is NOT one of them?

  • Binding intestinal toxins
  • Inhibiting intestinal motility
  • Being part of quadruple therapy for H. pylori
  • Stimulating gastric mucosal barrier (correct)

Why should sucralfate not be taken with antacids, H2 blockers, or proton pump inhibitors?

<p>It requires an acidic environment for activation (A)</p> Signup and view all the answers

In patients taking sucralfate, when should other medications be administered to avoid interference?

<p>At least 2 hours after sucralfate (D)</p> Signup and view all the answers

What is the likely reason for the patient's elevated PT levels?

<p>Use of cimetidine (B)</p> Signup and view all the answers

Which of the following medications can lead to gynecomastia?

<p>Cimetidine (C)</p> Signup and view all the answers

What is the mechanism of action of H2 receptor blockers?

<p>They block the action of histamine on parietal cells. (D)</p> Signup and view all the answers

Which clinical condition is NOT typically treated with H2 receptor blockers?

<p>Asthma (C)</p> Signup and view all the answers

What symptom did the 59-year-old man present with that is suggestive of a gastric ulcer?

<p>Upper abdominal pain after meals (A)</p> Signup and view all the answers

Which of the following side effects is specifically associated with cimetidine?

<p>Gynecomastia (D)</p> Signup and view all the answers

What lifestyle factors are relevant in assessing the 59-year-old man's condition?

<p>Heavy alcohol and tobacco use (B)</p> Signup and view all the answers

What is one of the primary effects of prochlorperazine when used as an anti-emetic agent?

<p>Blocking the D2 dopamine receptor (B)</p> Signup and view all the answers

Which of the following is a common side effect associated with prochlorperazine and metoclopramide?

<p>Extrapyramidal symptoms including tardive dyskinesia (D)</p> Signup and view all the answers

What is the mechanism of action for bulking laxatives?

<p>Drawing water into the intestine via osmosis (A)</p> Signup and view all the answers

Lactulose is indicated for which of the following clinical uses?

<p>Treatment of hepatic encephalopathy (D)</p> Signup and view all the answers

Which of these medications is considered a stimulant laxative?

<p>Senna (D)</p> Signup and view all the answers

What is a common side effect of laxatives?

<p>Abdominal cramps (D)</p> Signup and view all the answers

Which clinical scenario best describes the use of stool softeners?

<p>Softening hard stool (C)</p> Signup and view all the answers

What activity does prochlorperazine inhibit that leads to its anti-emetic effect?

<p>Activation of the vomiting reflex pathway (B)</p> Signup and view all the answers

What is one reason an 82-year-old woman may experience constipation?

<p>Use of OxyContin (D)</p> Signup and view all the answers

What is the primary mechanism by which lactulose improves encephalopathy associated with hyperammonemia?

<p>It promotes the production of nitrogen excretion compounds. (D)</p> Signup and view all the answers

What side effect is commonly associated with the use of lactulose?

<p>Abdominal cramps (C)</p> Signup and view all the answers

What is the action of rifaximin in treating hepatic encephalopathy?

<p>It decreases the production of ammonia by inhibiting gut bacteria. (C)</p> Signup and view all the answers

Which of the following is NOT a clinical use of lactulose?

<p>Management of systemic hypertension (A)</p> Signup and view all the answers

What condition is a 54-year-old man with a history of alcoholic cirrhosis AT RISK for, as suggested by his symptoms?

<p>Hyperammonemia (D)</p> Signup and view all the answers

Which of the following drugs is effective for treating simple traveler's diarrhea?

<p>Rifaximin (C)</p> Signup and view all the answers

What are the common side effects of rifaximin?

<p>Peripheral edema, fatigue, and nausea (A)</p> Signup and view all the answers

What indicates a significant change in a patient when using lactulose?

<p>Improvement in mental status due to reduced ammonia levels (C)</p> Signup and view all the answers

Which physical exam finding is indicative of hepatic encephalopathy?

<p>Asterixis (B)</p> Signup and view all the answers

Flashcards

What are gastric mucosal protective agents?

Gastric mucosal protective agents are drugs that help protect the stomach lining from damage, often by promoting prostaglandin synthesis.

How does sucralfate work and what to avoid when taking it?

Sucralfate acts as a barrier against stomach acid, but requires an acidic environment to work. It can be taken with PPIs, but should not be taken with antacids or H2 blockers.

What are the actions of bismuth subsalicylate?

Bismuth subsalicylate has multiple actions, including reducing intestinal motility, binding intestinal toxins, and stimulating fluid absorption. It can also be used as an anti-diarrheal medication and in quadruple therapy for H. pylori infections.

What are the common side effects of bismuth subsalicylate?

Common side effects of bismuth subsalicylate can include dark-colored tongue and stool, as well as hindering the absorption of tetracycline.

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What are the clinical uses of gastric mucosal protective agents?

Gastric mucosal protective agents are used in the treatment of peptic ulcer disease and promote healing of ulcers. Bismuth subsalicylate is also used as an anti-diarrheal agent and in quadruple therapy for H. pylori infections.

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What is the mechanism of action for H2 receptor blockers?

Drugs that block the H2 receptors on parietal cells, decreasing cyclic AMP levels and inhibiting the H+/K+ proton pump, ultimately reducing gastric acid secretion.

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List four examples of H2 receptor blockers.

Ranitidine, cimetidine, famotidine, and nizatidine.

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What are the clinical uses of H2 receptor blockers?

Gastroesophageal reflux disease, peptic ulcer disease, and other diseases associated with gastric ulcers.

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What are some side effects of H2 receptor blockers?

Cimetidine, in particular, can cause gynecomastia (breast enlargement in men) due to its anti-androgenic effects. It can also inhibit CYP450 enzymes, leading to potential interactions with drugs like warfarin.

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How can H2 receptor blockers affect drug interactions?

H2 receptor blockers may interfere with the metabolism of other drugs, potentially leading to increased drug levels in the body.

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What is peptic ulcer disease?

A condition where the lining of the stomach or duodenum is inflamed or irritated.

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Describe a patient with potential peptic ulcer disease.

A 59-year-old man presents with upper abdominal pain after meals, weight loss, and dark stools. This suggests potential peptic ulcer disease.

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What is the mechanism of action of prochlorperazine and what are its other actions?

Prochlorperazine is an anti-emetic that blocks dopamine receptors in the chemoreceptor trigger zone, preventing activation of the vomiting reflex. It also has some anti-cholinergic and alpha-1 adrenergic blocking activity.

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What are the common side effects of prochlorperazine?

Prochlorperazine can cause sedation, hypotension, diarrhea, extrapyramidal symptoms (including tardive dyskinesia), peripheral edema, depression, and neuroleptic malignant syndrome.

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What are laxatives and how do they work?

Laxatives are medications used to treat constipation by increasing bowel movements. They work by different mechanisms, such as stimulating gut motility, drawing water into the intestine, or softening the stool.

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How do irritant or stimulant laxatives work?

Irritants or stimulants like castor oil, senna, and bisacodyl increase intestinal peristalsis by irritating the gut lining, leading to faster movement of stool.

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How do bulking laxatives work?

Bulking laxatives, such as lactulose, sorbitol, polyethylene glycol, and magnesium salts, attract water into the intestine via osmosis, distending the bowel and promoting bowel movements.

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How do stool softeners work?

Stool softeners, such as docusate and mineral oil, soften the stool by emulsifying with it, making it easier to pass.

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What are the clinical uses of laxatives?

Laxatives are used to treat constipation and prepare the bowel for colonoscopic procedures.

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What are the common side effects of laxatives?

Common side effects of laxatives include abdominal cramps and diarrhea.

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What is another clinical use of lactulose?

Lactulose is also used in the treatment of hepatic encephalopathy, a condition characterized by brain dysfunction due to liver failure.

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Hepatic Encephalopathy

A condition characterized by impaired brain function due to high levels of ammonia in the blood, often seen in patients with liver disease.

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Lactulose

A synthetic sugar that is not absorbed by the body but broken down by gut bacteria into acids that lower pH and promote ammonia excretion.

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How does Lactulose work?

Lactulose helps by acidifying the gut and promoting nitrogen excretion, which reduces ammonia levels in the blood.

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Rifaximin

A non-absorbable antibiotic that inhibits bacterial RNA polymerase, reducing ammonia-producing bacteria in the gut.

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How does Rifaximin work?

Rifaximin targets ammonia-producing bacteria, lowering ammonia levels in the blood and improving hepatic encephalopathy.

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Cirrhosis

A condition where the liver is unable to function properly, leading to a buildup of toxins in the blood.

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Asterixis

Rapid, involuntary flapping movements of the hands when the arms are extended and the wrists are dorsiflexed, often a sign of hepatic encephalopathy.

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Jaundice

A yellowing of the skin and whites of the eyes, indicating a buildup of bilirubin in the blood, often associated with liver dysfunction.

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Hyperammonemia

An increased level of ammonia in the blood, often found in patients with liver disease.

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Study Notes

Gastrointestinal Agents

  • Agents used to treat peptic ulcer disease include antacids, mucosal protective agents, H₂ receptor blockers, and proton pump inhibitors
  • Anti-emetics include ondansetron and metoclopramide
  • Other gastrointestinal agents include laxatives, anti-diarrheal agents, and others

Mechanism of Gastric Acid Secretion

  • Gastric parietal cells contain carbonic anhydrase, which converts CO2 and H2O into H⁺ and HCO3⁻
  • Bicarbonate (HCO3⁻) is exchanged for chloride (Cl⁻) into the bloodstream
  • Hydrogen (H⁺) is pumped out of the parietal cell by H⁺/K⁺ ATPase, and chloride follows
  • H⁺ and Cl⁻ form hydrochloric acid (HCl) in the stomach lumen

Regulation of Gastric Acid Secretion

  • Gastrin stimulates H⁺ secretion by interacting with an uncharacterized receptor
  • Histamine stimulates acid secretion by activating H₂ receptors, leading to increased cyclic AMP
  • The vagus nerve stimulates acid secretion via M3 receptors on parietal cells and G cells
  • Chyme and low pH inhibit gastrin secretion and acid secretion

Antacids

  • Antacids are weak bases that react with gastric hydrochloric acid to increase pH and reduce acidity
  • Antacids inactivate pepsin, decreasing protein breakdown
  • Some antacids may stimulate prostaglandin synthesis, increasing the mucosal barrier

Mucosal Protective Agents

  • Sucralfate is believed to enhance the mucosal barrier by either stimulating prostaglandin synthesis or acting as a physical barrier
  • Bismuth subsalicylate inhibits intestinal motility, binds toxins, and stimulates fluid absorption

H₂ Receptor Blockers

  • H₂ receptor blockers (ranitidine, cimetidine, famotidine, nizatidine) reversibly block histamine binding to H₂ receptors on parietal cells
  • This inhibits cyclic AMP and decreases the activity of the H⁺/K⁺ proton pump, reducing gastric acid secretion

Proton Pump Inhibitors

  • Proton pump inhibitors (omeprazole, lansoprazole, pantoprazole, esomeprazole, rabeprazole, dexlansoprazole) irreversibly inhibit the H⁺/K⁺ ATPase pump
  • This suppresses gastric acid secretion

Ondansetron

  • Ondansetron blocks 5-HT3 receptors in the chemoreceptor trigger zone and GI tract, inhibiting activation of the vomiting reflex pathway
  • Treatment for nausea and vomiting

Metoclopramide

  • Metoclopramide is a dopamine receptor antagonist, stimulating gastric and small intestinal motility
  • It treats diabetic gastroparesis and is an anti-emetic

Laxatives

  • Bulking laxatives (lactulose, sorbitol, polyethylene glycol, magnesium salts) increase intestinal motility by drawing water into the intestine
  • Irritants or stimulants (Castor oil, senna, bisacodyl) increase intestinal peristalsis through mucosal irritation or stimulation

Lactulose

  • Lactulose is degraded by bacteria into lactic acid and acetic acid, which increase gut pH and promote nitrogen excretion, improving hepatic encephalopathy
  • Treatment for hepatic encephalopathy

Anti-diarrheal Agents

  • Diphenoxylate and loperamide bind to opioid receptors in the intestine, inhibiting acetylcholine release and decreasing gut peristalsis
  • Treatment of diarrhea

Sulfasalazine

  • Bacteria in the colon metabolize sulfasalazine into sulfapyridine and 5-ASA
  • 5-ASA is an anti-inflammatory, inhibiting prostaglandin and leukotriene production, preventing further mucosal damage

Ursodiol

  • Ursodiol decreases cholesterol gallstones by inhibiting cholesterol synthesis, decreasing intestinal reabsorption of cholesterol, and inhibiting cholesterol secretion into bile
  • Treatment for primary biliary cirrhosis and cholesterol gallstones

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