Pharmacology: H2 Antagonists and PPIs
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Questions and Answers

What is the primary action of H2 antagonists in treating ulcer disease?

  • Blocking H2 receptors on parietal cells (correct)
  • Stimulating the release of gastrin
  • Inhibiting the release of prostaglandins
  • Increasing hydrochloric acid production

Which of the following drugs is specifically eliminated by the kidneys?

  • Nizatidine (correct)
  • Ranitidine
  • Famotidine
  • Cimetidine

What adverse effect is specifically associated with long-term use of cimetidine?

  • Gynecomastia (correct)
  • Hypotension
  • Dizziness
  • Diarrhea

Which H2 antagonist is considered the prototype?

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

What is a common gastrointestinal side effect of H2 antagonists?

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

Which of the following H2 antagonists is approved for use in children ages 1 to 16?

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

Which side effects can occur with high levels of H2 antagonists?

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

What caution should be considered when prescribing H2 antagonists?

<p>Risk of liver dysfunction (C)</p> Signup and view all the answers

What is the main action of the drugs that block acid production in the stomach?

<p>Block the H+, K+-ATPase pump (C)</p> Signup and view all the answers

Which condition is NOT treated with proton pump inhibitors?

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

How quickly do proton pump inhibitors reach peak levels in the body?

<p>3 to 5 hours (B)</p> Signup and view all the answers

What is a common central nervous system side effect of proton pump inhibitors?

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

What adverse effect is associated with long-term use of proton pump inhibitors?

<p>Increased incidence of Clostridium difficile diarrhea (A)</p> Signup and view all the answers

Which proton pump inhibitor is preferred for children under 18 years?

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

What common adverse effect may occur in the gastrointestinal system due to proton pump inhibitors?

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

Why are laxative drugs commonly abused?

<p>To stimulate gastrointestinal movement (A)</p> Signup and view all the answers

Which of the following is a common adverse effect of frequent laxative use?

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

What can excessive laxative use potentially lead to?

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

Which laxative works by pulling fluid into the lumen of the small intestine?

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

What is NOT a central nervous system effect commonly associated with laxative use?

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

Which laxative type increases motility by enhancing bulk and stimulating local receptors?

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

In which condition are bulk laxatives contraindicated?

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

What is the effect of polyethylene glycol-electrolyte solution on patients with a history of seizures?

<p>Causes electrolyte absorption issues (B)</p> Signup and view all the answers

What type of agent is magnesium citrate considered?

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

What are the most common gastrointestinal adverse effects associated with bulk laxatives?

<p>Diarrhea, abdominal cramping, and nausea (D)</p> Signup and view all the answers

What is the primary function of docusate as a laxative?

<p>Coat the intestinal bolus to retain moisture (B)</p> Signup and view all the answers

Which adverse effect is less likely to occur with lubricant laxatives compared to stimulants?

<p>CNS effects like dizziness (C)</p> Signup and view all the answers

What form is glycerin used in for its laxative effects?

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

What contraindications are associated with the use of lubricant laxatives?

<p>Heart block, CAD, and acute abdominal conditions (D)</p> Signup and view all the answers

What common CNS effects may accompany laxative use?

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

What type of laxative stimulates the nerve plexus in the intestinal wall?

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

How does mineral oil function as a laxative?

<p>By forming a barrier that prevents water absorption (D)</p> Signup and view all the answers

Which laxative is commonly used when a thorough evacuation of the intestine is desirable?

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

What is a potential issue associated with the use of mineral oil?

<p>Leakage and staining due to stool consistency (C)</p> Signup and view all the answers

Which laxative is considered milder than castor oil and is typically used for overnight effects?

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

Why are laxatives contraindicated in patients with acute abdominal disorders?

<p>They may exacerbate inflammation or lead to rupture. (D)</p> Signup and view all the answers

What is one of the adverse effects associated with laxative use?

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

Which laxative should be avoided during pregnancy due to its potential to induce premature labor?

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

Which of the following laxatives is least likely to be absorbed into the system?

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

In which condition should laxatives be used with caution due to the risk of electrolyte changes?

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

Flashcards

H2 Antagonists

A type of medication that selectively blocks H2 receptors on parietal cells in the stomach, preventing the release of gastrin and histamine, ultimately reducing hydrochloric acid production.

Gastrin

A hormone that stimulates the release of histamine and hydrochloric acid production in the stomach.

Histamine

A chemical messenger that triggers the release of hydrochloric acid in the stomach.

Hydrogen-Potassium Adenosine Triphosphatase (H+, K+-ATPase)

An enzyme system found on the surface of gastric parietal cells that is responsible for the final step in hydrochloric acid production.

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Gastric Acid Pump Inhibitors (Proton Pump Inhibitors)

A class of drugs that specifically inhibit the H+, K+-ATPase enzyme system, effectively blocking the final step in hydrochloric acid production.

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H2 Receptor Antagonists

A drug class that includes cimetidine, ranitidine, famotidine, and nizatidine, which decrease the production of gastric acid by blocking H2 receptors.

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Gynecomastia

A side effect of H2 antagonists that can occur with long-term use, particularly with cimetidine, and is characterized by the development of breast tissue in men.

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Galactorrhea

A side effect associated with some H2 antagonists, especially cimetidine, that involves the production of breast milk in men.

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Cathartic dependence

A condition where the GI tract becomes dependent on laxatives, leading to constipation and stool impaction when laxatives are stopped.

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Bulk stimulants

A drug class that increases the motility of the GI tract by increasing the fluid in the intestinal contents, which enlarges the bulk, stimulates local stretch receptors, and activates local activity.

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Lactulose

A type of osmotic laxative that pulls fluid out of the venous system and into the lumen of the small intestine.

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Contraindications for Bulk Laxatives

Laxatives that are contraindicated in acute abdominal disorders like appendicitis, diverticulitis, and ulcerative colitis.

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Polyethylene glycol-electrolyte solution

A hypertonic fluid containing many electrolytes that pulls fluid out of the intestinal wall to increase the bulk of the intestinal contents.

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Side Effects of Laxatives

Adverse effects of laxatives can include dizziness, headache, sweating, palpitations, flushing, and even fainting.

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Cautions for Laxative Use

Laxatives should be used with caution in individuals with heart block, CAD, debilitation, and during pregnancy and lactation.

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Magnesium citrate and hydroxide

A milder and slower-acting laxative that works by a saline pull, bringing fluids into the lumen of the GI tract.

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Proton Pump Inhibitors

Drugs that block the final step of acid production in the stomach, reducing acid levels.

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Uses for Proton Pump Inhibitors

Short-term treatment for duodenal ulcers, GERD, erosive esophagitis, and gastric ulcers, long-term management of hypersecretory conditions, and maintenance therapy for healing erosive esophagitis and ulcers. Also used for H. pylori infection.

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Pharmacokinetics of Proton Pump Inhibitors

These drugs are rapidly absorbed in the gut, reaching peak levels in 3 to 5 hours, and undergo extensive metabolism in the liver, being excreted in urine. Omeprazole is faster acting and more readily excreted.

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Contraindications and Cautions for Proton Pump Inhibitors

Caution is advised for pregnant and lactating women due to potential effects on the fetus or baby. Safety and effectiveness in children under 18 years are not established, except for lansoprazole, which is the preferred choice for children when a proton pump inhibitor is needed.

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Adverse Effects of Proton Pump Inhibitors

Side effects arise from their action on the H+, K+-ATPase pump in parietal and other cells.

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CNS Side Effects of Proton Pump Inhibitors

Common CNS effects include dizziness and headache. Other possible CNS effects include asthenia (weakness), vertigo, insomnia, apathy, and abnormal dreams.

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GI Side Effects of Proton Pump Inhibitors

Common GI effects include diarrhea, abdominal pain, nausea, vomiting, dry mouth, and tongue atrophy.

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Respiratory Side Effects of Proton Pump Inhibitors

Possible upper respiratory tract symptoms include cough, stuffy nose, hoarseness, and nosebleeds.

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Chemical Stimulants

These laxatives work by irritating the lining of the gastrointestinal (GI) tract, stimulating nerve reflexes that increase movement and promote bowel emptying.

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Lubricants

These laxatives lubricate the intestinal lining, making it easier for stool to pass. They act as a lubricant, allowing stool to move smoothly through the GI tract.

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Castor Oil

These laxatives cause a strong, thorough evacuation of the intestines and are used when a complete bowel emptying is desired.

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Cascara

A laxative that is milder than castor oil and is often used when overnight bowel evacuation is needed.

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Senna

A laxative available in various forms (tablets, syrup, suppositories) that stimulates bowel activity.

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Contraindications for Laxative Use

Laxatives should NOT be used in these conditions as they can worsen the situation.

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What are the common side effects of bulk laxatives?

Bulk laxatives often lead to digestive side effects like diarrhea, stomach cramps, and nausea.

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How do bulk laxatives affect the nervous system?

Bulk laxatives can cause problems with the central nervous system like dizziness, headache, and weakness. This often happens due to fluid and electrolyte imbalances caused by the laxative.

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What is the purpose of lubricant laxatives?

Lubricants help make bowel movements easier without stimulating the digestive tract.

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How does Docusate work as a laxative?

Docusate softens stools by acting like a detergent, mixing fats and water for easier passage.

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Explain the mechanism of Glycerin as a laxative.

Glycerin acts as a hyperosmolar laxative, drawing water into the rectum to soften stools.

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How does Mineral Oil function as a laxative?

Mineral oil coats the stool, preventing water absorption and keeping it soft.

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When are lubricant laxatives contraindicated?

Lubricants are not advised for people with acute abdominal issues like appendicitis, diverticulitis, or ulcerative colitis.

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What are the potential side effects of lubricant laxatives?

Lubricants may cause diarrhea, stomach cramps, nausea, leakage, and staining, especially with mineral oil.

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Study Notes

Chapter 9: Gastrointestinal System

  • This chapter covers drugs used to treat ulcer disease, constipation, and related topics.

Drugs Used to Treat Ulcer Disease

  • Histamine-2 Antagonists: These drugs selectively block H2 receptors on parietal cells.

    • This prevents gastrin release, which reduces histamine release.
    • It ultimately blocks hydrochloric acid production and decreases pepsin production.
    • H2 receptor sites are also in the heart, and high drug levels can cause cardiac arrhythmias.
    • Examples include cimetidine (Tagamet, Tagamet HB), famotidine (Pepcid, Pepcid AC), nizatidine (Axid), and ranitidine (Zantac).
    • Specific uses and special considerations for each drug are provided.

  • Pharmacokinetics:

    • Cimetidine, ranitidine, and famotidine are available in oral and parenteral forms.
    • Nizatidine is available only in oral form.
    • Cimetidine (prototype) is associated with antiandrogenic effects like gynecomastia and galactorrhea.
    • It is metabolized in the liver and can slow the metabolism of other drugs. It's excreted in urine.
    • Ranitidine and famotidine are more potent, longer-acting, and don't have the same antiandrogenic effects or marked slowing of metabolism as cimetidine. They are also metabolized in the liver and excreted in urine.
    • Famotidine is approved for use in children aged 1 to 16 years.
    • Nizatidine is similar to ranitidine in its effects but is eliminated by the kidneys, with no first-pass liver metabolism. It's the drug of choice for patients with liver dysfunction.

  • Contraindications and Cautions:

    • Use caution during pregnancy or lactation due to potential fetal/newborn effects.
    • Exercise caution with hepatic or renal dysfunction as it may affect drug metabolism and excretion.
    • Note adverse effects like diarrhea, constipation, CNS effects, cardiac arrhythmias, and hypotension. Also, long-term cimetidine use can cause gynecomastia and impotence.

  • Proton Pump Inhibitors (PPIs):

    • Specifically inhibit the H+, K+-ATPase enzyme system.
    • This lowers gastric acid levels in the stomach.
    • Recommended for short-term treatment of active duodenal ulcers, GERD, erosive esophagitis and benign, active gastric ulcers. Also for long-term treatment of certain pathological conditions.
    • Used as maintenance therapy for healing, and in combination with amoxicillin and clarithromycin for H. pylori infection treatment.
    • Several examples like dexlansoprazole, esomeprazole, lansoprazole, omeprazole, pantoprazole, and rabeprazole are listed, with their indications for use.
    • Pharmacokinetics and safety considerations for these drugs are also discussed.
    • Note adverse effects like GI effects, CNS effects, upper respiratory symptoms, and possible effects like bone loss, low calcium/magnesium levels, and C. difficile diarrhea/pneumonia in long-term use..

Drugs Used in the Treatment of Constipation

  • Laxatives:

    • Used for short-term relief of constipation.
    • Available as OTC preparations.
    • Overuse can lead to chronic intestinal disorders.
    • Types include chemical stimulants (irritate GI lining), bulk stimulants (bulk up stool), and lubricants (facilitate movement).

  • Chemical Stimulants:

    • Directly stimulate nerve plexus in intestinal wall.
    • Examples include castor oil, bisacodyl, cascara, and senna. Important to note their specific effects and situations where they are recommended.

  • Bulk Stimulants:

    • Increase intestinal motility by increasing fluid and bulk in intestinal contents.
    • Examples include lactulose, magnesium citrate/hydroxide, polyethylene glycol-electrolyte solution, and psyllium. Note different types and how they work.

  • Lubricants:

    • Ease defecation without stimulating GI tract movement.
    • Examples include mineral oil, docusate, and glycerin. Note these are used for lubrication.

  • Pharmacokinetics and Contraindications:

    • The methods of absorption, and excretion are described for each drug class.
    • Notes are included about contraindications, such as cautions with acute abdominal disorders, pregnancy, and lactation.
    • Potential for adverse effects such as diarrhea and abdominal cramping are also discussed.

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Chapter 9 Gastrointestinal System PDF

Description

This quiz tests your knowledge on H2 antagonists and proton pump inhibitors (PPIs) in treating ulcer disease. Questions include drug actions, side effects, and specific usage in children. Assess your understanding of these critical medications in gastroenterology.

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