Drugs for Treatment of Ulcers

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Questions and Answers

What is the mechanism of action of proton pump inhibitors?

  • They inhibit the final step of acid secretion by binding to the proton pump. (correct)
  • They increase gastrin production to enhance acidity.
  • They block histamine receptors on parietal cells.
  • They neutralize gastric acid by increasing bicarbonate secretion.

Which statement best describes the limitation of cimetidine?

  • It inhibits P450 enzymes, limiting its clinical use. (correct)
  • It has no significant interactions with other drugs.
  • It is a more effective acid secretion inhibitor than proton pump inhibitors.
  • It enhances the biotransformation of other drugs.

How do H2 antagonists, like cimetidine, compare to proton pump inhibitors in their effects on ulcer treatments?

  • Proton pump inhibitors reduce acid secretion significantly more than H2 antagonists. (correct)
  • H2 antagonists are more effective than proton pump inhibitors.
  • Both have the same efficacy in reducing acid secretion.
  • H2 antagonists only work at night while proton pump inhibitors work all day.

What are some common side effects associated with cimetidine and other H2 antagonists?

<p>Cognitive impairment and gastrointestinal upset. (D)</p> Signup and view all the answers

What role does histamine play in acid secretion?

<p>Histamine enhances acid secretion by acting on parietal cells. (B)</p> Signup and view all the answers

What is the primary mechanism of action for proton pump inhibitors?

<p>Decreasing gastric acid production (A)</p> Signup and view all the answers

Which condition is NOT commonly treated with proton pump inhibitors?

<p>Hyperthyroidism (A)</p> Signup and view all the answers

Which of the following is a potential consequence of long-term use of proton pump inhibitors?

<p>Increased risk of gastrointestinal infections (C)</p> Signup and view all the answers

Which adverse effect is least likely associated with proton pump inhibitors?

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

In what way does histamine influence acid secretion?

<p>It stimulates parietal cells to secrete more gastric acid. (C)</p> Signup and view all the answers

What percentage of patients may experience adverse effects from proton pump inhibitors?

<p>2-5% (A)</p> Signup and view all the answers

What is a significant risk associated with chronic use of proton pump inhibitors?

<p>Increased risk for anemia (B)</p> Signup and view all the answers

Which drug interaction can occur due to decreased gastric acid levels from proton pump inhibitors?

<p>Decreased absorption of digoxin (B)</p> Signup and view all the answers

How do H2 antagonists primarily differ from proton pump inhibitors?

<p>H2 antagonists reduce acid secretion without directly affecting proton pumps. (B)</p> Signup and view all the answers

Which medication would MOST likely be used for an NSAID-induced ulcer?

<p>Proton pump inhibitors (B)</p> Signup and view all the answers

What is the primary mechanism of action of H2 receptor antagonists in treating ulcers?

<p>They block histamine stimulation of acid secretion. (D)</p> Signup and view all the answers

How do proton pump inhibitors function in ulcer treatment?

<p>They block the acid secretory process. (C)</p> Signup and view all the answers

Which of the following statements is true regarding the comparison of ulcer medications?

<p>H2 antagonists are less effective than proton pump inhibitors. (C)</p> Signup and view all the answers

What side effect is commonly associated with the use of aluminum hydroxide as an antacid?

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

What role does histamine play in the secretion of gastric acid?

<p>It acts on H2 receptors to enhance acid secretion. (D)</p> Signup and view all the answers

Which type of antacid is absorbed into the body?

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

Which medication class directly inhibits acid secretion by blocking the proton pump?

<p>Proton pump inhibitors (B)</p> Signup and view all the answers

What adverse effect may result from the excessive use of sodium bicarbonate as an antacid?

<p>Increased blood pressure (A)</p> Signup and view all the answers

What is the function of mucous neck cells in the stomach?

<p>They form a protective mucous layer. (D)</p> Signup and view all the answers

Which of the following medications is primarily used to treat excessive gastric acid secretion?

<p>Proton pump inhibitors (D)</p> Signup and view all the answers

Which statement about histamine's role in acid secretion is accurate?

<p>Histamine promotes acid secretion at night. (C)</p> Signup and view all the answers

What effect do non-steroidal anti-inflammatory drugs (NSAIDs) have on the stomach lining?

<p>They inhibit prostaglandin synthesis. (C)</p> Signup and view all the answers

Which of the following statements is true regarding muscarinic receptor antagonists?

<p>They block acid secretion induced by the nervous system. (A)</p> Signup and view all the answers

Which medication class is fast acting but offers short-term relief from gastric irritation?

<p>Antacids (A)</p> Signup and view all the answers

Flashcards

Cimetidine's limitation

Cimetidine's clinical use is limited due to its inhibition of P450 enzymes, impacting the biotransformation of other drugs.

Proton Pump Inhibitors (PPIs)

PPIs effectively reduce stomach acid by permanently binding to the proton pump, significantly decreasing acid secretion.

PPI mechanism of action

PPIs permanently bind to the proton pump, halting its activity until a new protein is synthesized.

PPI effectiveness

PPIs can reduce acid secretion by 90% or more.

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PPI naming convention

All PPIs in this class end with "-prazole" (e.g., omeprazole).

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Omeprazole's function

Omeprazole is a proton pump inhibitor that reduces stomach acid secretion.

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Proton pump inhibitors

Drugs that block the action of proton pumps, decreasing stomach acid production.

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Clinical uses of PPI

Treat ulcers, GERD (acid reflux), and conditions where reducing stomach acid is necessary.

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Adverse effects of PPIs

Potential side effects include headache, abdominal pain, diarrhea, and rare skin rashes, occurring in a small percentage of patients.

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Consequences of reduced stomach acid

Chronic reduction of stomach acid can lead to issues like anemia (due to vitamin B12 absorption problems) and increase the risk of infections (Salmonella and Shigella).

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Vitamin B12 absorption

Stomach acid is needed to release vitamin B12 from food for absorption.

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Drug absorption with reduced acid

Some drugs, like cardiac glycosides, may experience reduced absorption with lowered stomach acid levels.

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Stress-related ulcers

Ulcers that develop due to stress.

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NSAID-induced ulcers

Ulcers caused by non-steroidal anti-inflammatory drugs (NSAIDs).

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Gastric acid suppression

Act of inhibiting the production of gastric acid.

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Gastrin role in acid secretion

Gastrin, a hormone released by stomach cells, stimulates acid production by acting directly on parietal cells and stimulating histamine secretion from enterochromaffin-like cells.

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Parietal cells role in acid secretion

Parietal cells contain proton pumps that transport hydrogen ions (protons) into the stomach, crucial for acid production.

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Role of Histamine in acid secretion

Histamine acts upon H2 receptors on parietal cells, further stimulating acid secretion.

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Acid's role in protein digestion

Acid converts pepsinogen into pepsin, an enzyme crucial for protein digestion in the stomach.

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Lower Esophageal Sphincter (LES)

The LES prevents stomach acid from refluxing back into the esophagus.

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Mucous Neck Cells

Mucous neck cells secrete mucus, forming a protective layer on the stomach lining, and bicarbonate to neutralize acid.

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Role of Prostaglandins in ulcers

Prostaglandins protect the stomach lining by inhibiting acid secretion and promoting mucus production.

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Antacids Mechanism

Antacids neutralize stomach acid by reacting with it chemically.

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H2 Receptor Antagonists

H2 receptor antagonists reduce acid secretion by blocking histamine's action.

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Muscarinic Receptor Antagonists

Muscarinic receptor antagonists inhibit nerve-stimulated acid secretion.

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Antacids (systemic)

Systemic antacids are absorbed into the bloodstream, altering the body's chemistry.

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Antacids (non-systemic)

Non-systemic antacids do not significantly impact the bloodstream, working directly in the stomach.

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Histamine H2 Receptor Antagonists' effect on acid secretion

These drugs can reduce acid secretion by as much as 70% and also suppress nighttime acid secretion.

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Study Notes

Drugs for Treatment of Ulcers

  • Acid Secretion in Stomach: Stomach acid is produced in response to food, distension, and CNS stimuli. Antral cells release gastrin, which stimulates enterochromaffin-like cells to secrete histamine. Histamine then stimulates parietal cells to release acid. Parietal cells also directly respond to gastrin.

Controlling Acid Secretion

  • Active Process: Protons (H+) are transferred into the stomach, exchanging for potassium (K+). This happens through a proton pump (H+/K+ ATPase).
  • Acid Function: Acid converts pepsinogen to pepsin, an enzyme critical for protein digestion. However, too much acid can damage the stomach lining.

Natural Defenses to Acid

  • Lower Esophageal Sphincter (LES): Prevents acid reflux back into the esophagus.
  • Mucous Neck Cells: Secrete mucous, forming a protective layer on the stomach lining. They also secrete bicarbonate, which neutralizes acid.
  • Prostaglandins: Protect against ulcers by promoting mucus and bicarbonate secretion. NSAIDs block prostaglandin production, increasing ulcer risk.

Drugs That Control Acid

Antacids

  • Mechanism: Neutralize stomach acid.
  • Types: Alkaline substances like calcium, magnesium, and aluminum salts.
  • Fast Acting: Neutralization occurs within minutes.
  • Limited Duration: Relief generally lasts less than 2 hours.
  • Uses: Excess acid, overeating, drinking, and acute heartburn.
  • Systemic: Can be absorbed into the body (e.g., sodium bicarbonate).
  • Non-Systemic: Not absorbed (e.g., magnesium hydroxide or aluminum hydroxide); safer with systemic absorption as they are less likely to increase sodium levels.

Histamine-2 (H2) Receptor Antagonists

  • Mechanism: Block histamine receptors on parietal cells, reducing stomach acid secretion.
  • Effectiveness: Suppress acid secretion by ~70%, generally more effective than other types, particularly at night.
  • Duration: Relief lasts for 1-2 hours but can last up to 12 hours.
  • Uses: Excess acid, peptic ulcer disease.

Muscarinic Receptor Antagonists

  • Mechanism: Block muscarinic receptors on parietal cells, reducing vagal nerve influence on acid secretion.
  • Efficacy: Effectiveness limited to 40%.
  • Use: Limited. Histamine and gastrin play significant roles in acid production.

Proton Pump Inhibitors

  • Mechanism: Permanently bind to and block the proton pump (H+/K+ ATPase), preventing acid secretion.
  • Effectiveness: Very effective
  • Uses: Gastric ulcer disease, stress-related ulcers, and NSAID-induced ulcers.

Clinical Use of Proton Pump Inhibitors

  • Treatment: Gastric ulcer disease, stress-related ulcers, NSAID-induced ulcers.

  • Adverse Effects: Diarrhea, headache, abdominal pain, muscle soreness. (Low frequency).

Consequences of Decreasing Acid

  • Nutrients: Difficulty in absorbing certain nutrients (e.g., vitamin B12).
  • Bacterial Infections: Increased risk of certain bacterial infections (e.g., Salmonella, Shigella).
  • Drug Interactions: Reduced absorption of certain medications, such as cardiac glycosides.

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