Chapter 5

Drugs acting on gastrointestinal tract

By kedirD
 OBJECTIVES
At the end of this chapter, you will be able to:

List the symptoms and risk factors of GERD and PUD

List and categorize medications used to treat GERD and PUD
Describe the mechanism of action and common side effects of
antiemetics, laxatives and antidiarrheal drugs
 6.1 Introduction to GIT

The gastrointestinal (GI) tract encompasses the organs responsible for

digesting food, absorbing nutrients, and excreting waste.
These organs include
 the stomach

 gallbladder

 liver, pancreas,

small intestine, and

large intestine (colon).

6.1 Introduction to GIT ….
[Link] Process
Several organs contribute to food digestion by secreting enzymes into
the small intestine.
Bile is transported from the liver (via the hepatic duct) and the
gallbladder (via the cystic duct) to the duodenum.
The pancreas, located behind the stomach, also provides enzymes
crucial for digestion
 6.1 Introduction to GIT….
[Link] Stomach
• The stomach is the most distensible part of the GI tract, situated in the
upper left abdominal quadrant, just beneath the diaphragm.

• Its wall consists of four layers:

Mucosa

Submucosa

Muscularis propria

Serosa
 6.1 Introduction to GIT….
[Link] Structure
• The mucosa has two compartments:
1. Superficial foveolar compartment
2. Deeper glandular compartment
Glandular Compartment
Cardia Glands: Contain mucus-secreting cells only.
• Oxyntic (Fundic) Glands: Composed of:
 Parietal Cells:
• Produce and secrete gastric acid (HCl).
• Primary site of action for many acid-controller drugs.
 Chief Cells:
• Secrete pepsinogen (a proenzyme).
• Activated by acid to become pepsin, which breaks down proteins (proteolytic).
 Mucoid Cells:
• Mucus-secreting surface epithelial cells.
• Provide a protective mucous coat, shielding against self-digestion by HCl.
 6.1 Introduction to GIT

[Link] Acid Secretion

• Gastric acid secretion is a complex, continuous process influenced by various central
and peripheral factors, ultimately leading to the secretion of H ⁺ by parietal cells.
• Key regulators of acid secretion include:

• Acetylcholine (ACh)

• Histamine

• Gastrin
6.2. Common Gastro-intestinal tract diseases
 6.2. Common Gastro-intestinal tract diseases…

[Link]: Inflammation of the stomach mucosa.

Causes: Linked to stress, medications, infections (e.g., Helicobacter
pylori), autoimmune diseases, alcohol consumption, bile reflux, and NSAID
use.
Symptoms:
Belching,
Nausea,
Vomiting,
Bloating,
Burning sensation
 6.2. Common Gastro-intestinal tract diseases…

[Link]: Inflammation of the intestinal lining.

Causes: viruses, bacteria, or parasites.
Symptoms:
Diarrhea
Abdominal pain
Vomiting
Headache
Fever
Chills
Loss of appetite
 6.2. Common Gastro-intestinal tract diseases…

[Link] Reflux Disease (GERD): Condition where acid and pepsin

from the stomach flow back into the esophagus.
Symptoms:
• Radiating burning or chest pain
• Acid taste in the mouth
Commonly Known As: Heartburn
[Link] Ulcer Disease (PUD): Disorders of the upper gastrointestinal tract
caused by excessive acid secretion.
Types of Ulcers:
• Gastric Ulcers: Localized lesions in the gastric mucosa.
• Duodenal Ulcers: Occur in the duodenum, often due to hypersecretion of acid.
• Stress Ulcers: Result from loss of mucosal resistance due to severe physiological stress.
 6.2. Common Gastro-intestinal tract diseases…

Causes: Imbalance between mucosal defensive factors (mucus,

bicarbonate, prostaglandins) and aggressive factors (H. pylori, NSAIDs,

gastric acid, pepsin).

 Four major classes of drugs used to treat acid-peptic diseases:

1. Antacids
 Mechanism: Neutralize gastric acid through a chemical reaction.

 Common Ingredients: Aluminum hydroxide, magnesium hydroxide, calcium carbonate,

sodium bicarbonate.
 Use: Provide quick relief from heartburn and indigestion by increasing gastric pH.

2. Proton Pump Inhibitors (PPIs)

 Mechanism: Inhibit the proton pump (H+/K+ ATPase) in the stomach lining, reducing
gastric acid secretion.
 Examples: Omeprazole, esomeprazole, lansoprazole, pantoprazole.

 Use: Effective for long-term management of conditions like GERD and peptic ulcers.
 Four major classes of drugs used to treat acid-peptic diseases:

3. Histamine H2-Receptor Antagonists

 Mechanism: Block H2 receptors on gastric parietal cells, decreasing acid production.

 Examples: Ranitidine, famotidine, cimetidine.

 Use: Provide relief from heartburn and are used in the treatment of ulcers and GERD.
4. Gastric Protectants
 Mechanism: Protect the gastric mucosa and promote healing.

 Examples:

 Misoprostol: A prostaglandin analog that increases mucus and bicarbonate secretion.

 Sucralfate: Forms a protective barrier over ulcers and enhances mucosal defense.

 Use: Often used in conjunction with NSAIDs to prevent ulcers and promote healing.
 6.7 Eradication of H. pylori
: H. pylori is linked to gastritis and peptic ulcers;
 eradication reduces ulcer recurrence.

Treatment Regimen:
Omeprazole 20 mg BID + Clarithromycin 500 mg BID + Amoxicillin 1 g BID for 14
days.
Metronidazole can replace amoxicillin in penicillin-allergic patients.
 6.8 Emetics and Anti-emetics
Anti-emetics: Prevent or treat nausea and vomiting.
Common Causes: Motion sickness, pregnancy, drug-induced (e.g., opioids,
anticancer drugs).
Drug Classes
Antihistamines: Promethazine, dimenhydrinate, diphenhydramine
 Effective for motion sickness and postoperative nausea; sedation is a common side effect.
Anticholinergics: Scopolamine (hyoscine)
 Used as a transdermal patch for motion sickness; may cause sedation and confusion.
Dopamine D2 Antagonists: Metoclopramide, chlorpromazine
 Effective for nausea from various stimuli but not for motion sickness.
5-HT3 Receptor Antagonists: Ondansetron, Granisetron Widely used for chemotherapy-
induced nausea; common side effects include headache and constipation.
Emetics : Induce vomiting, especially in cases of toxic substance ingestion.
• Common Emetic: Syrup of ipecac, which irritates the gastric mucosa and acts on
the chemoreceptor trigger zone.
 6.9 Drugs Used for Constipation (Laxatives)

: Constipation is characterized by decreased stool frequency and difficulty in

passage.
Causes
• Lack of dietary fiber, medications, hormonal disturbances, neurogenic disorders.

Common Laxatives

Magnesium Sulfate, Bisacodyl, Cascara sagrada, Glycerin, Liquid paraffin,

Docusate sodium, Lactulose, Senna.
 6.10 Antidiarrheal Agents
Diarrhea involves increased gastrointestinal motility and secretion, leading to
fluid and electrolyte loss.
Treatment Approaches
[Link] and Electrolyte Balance: Oral rehydration is the first priority (e.g., Oral
Rehydration Salts).

[Link] Anti-infective Agents: For certain types of enteritis (e.g., typhoid, cholera).

[Link]-Antimicrobial Antidiarrheal Agents:

1. Antimotility Agents: Diphenoxylate, loperamide.

2. Adsorbents: Kaolin, pectin.

3. Fluid and Electrolyte Modifiers: Bismuth subsalicylate, Zinc sulfate for zinc-losing conditions.
 6.11 Anti-Flatulent Agents

Example: Simethicone

Indications:
• Flatulence

• Gastric bloating

• Postoperative gas pains

Mechanism of Action (MOA)

Reduce surface tension, resulting in gas bubbles being released more easily
Adverse Reactions

• Diarrhea

• Nausea
 Class work
[Link] of the following medications is classified as a proton pump inhibitor (PPI)?
A) Ranitidine B) Omeprazole C) Simethicone D) Bisacodyl
[Link] is the primary mechanism of action for H2-receptor antagonists?
A) Inhibit gastric acid secretion B) Neutralize stomach acid
C) Coat the stomach lining D) Increase gastrointestinal motility
[Link] combination of drugs is typically used in the triple therapy for H. pylori
eradication?
A) PPI, Amoxicillin, Metronidazole B) PPI, Ranitidine, Simethicone
C) Bismuth, Tetracycline, Clarithromycin
D) PPI, Amoxicillin, Clarithromycin
 ide?
[Link] of the following is a common side effect of metoclopram
ea
A) Constipation B) Drowsiness C) Hypertension D) Diarrh
[Link] is the dosage range for loperamide in adults?
A) 2 mg after each loose stool, max 8 mg/day
B) 4 mg after each loose stool, max 16 mg/day
C) 1 mg after each loose stool, max 12 mg/day
for OTC
D) 4 mg initially, then 2 mg after each loose stool, max 8 mg/day
x carbohydrates to
[Link] anti-flatulent agent works by breaking down comple
reduce gas?
A) Simethicone B) Activated Charcoal C) Beano (Alpha-galactosidase)
[Link] is the primary purpose of bismuth subsalicylate in treating gastrointestinal
conditions?
A) Increase intestinal motility B) Antimicrobial activity against H. pylori
C) Coating the stomach lining D) Reducing diarrhea and treating upset stomach
[Link] of the following medications is NOT typically used to treat gastroesophageal
reflux disease (GERD)?

A) Omeprazole B) Ranitidine C) Diphenoxylate D) Simethicone

[Link] is the maximum recommended daily dose of bisacodyl for treating constipation?

A) 5 mg B) 15 mg C) 30 mg D) 10 mg

[Link] of the following is a common side effect of using laxatives?

A) Abdominal cramping B) Increased appetite C) Nausea D) Weight gain

Summary
[Link] Symptoms and Risk Factors
Gastroesophageal Reflux Disease (GERD):
• Symptoms: Heartburn, regurgitation, chest pain, difficulty swallowing, chronic
cough, and sore throat.
• Risk Factors: Obesity, smoking, pregnancy, certain medications, and dietary choices
(e.g., spicy foods, caffeine).
Peptic Ulcer Disease (PUD):
• Symptoms: Abdominal pain, bloating, nausea, vomiting, and loss of appetite.
• Risk Factors: Helicobacter pylori infection, NSAID use, excessive alcohol
consumption, and smoking.
Gastritis:
• Symptoms: Abdominal pain, nausea, vomiting, loss of appetite, and indigestion.
• Risk Factors: Chronic alcohol use, stress, bacterial infections (e.g., H. pylori),
autoimmune conditions, and certain medications (e.g., NSAIDs).
[Link] Symptoms and Risk Factors……

Gastroenteritis:

• Symptoms: Diarrhea, vomiting, abdominal cramps, and fever.

• Risk Factors: Viral or bacterial infections (e.g., norovirus, rotavirus), contaminated

food or water, and close contact with infected individuals.

2. Medications for GERD, PUD, Gastritis, and Gastroenteritis
Antacids: Neutralize stomach acid (e.g., magnesium hydroxide, aluminum
hydroxide).
H2-Receptor Antagonists: Reduce acid production (e.g., ranitidine,
famotidine).
Proton Pump Inhibitors (PPIs): Block acid production more effectively
(e.g., omeprazole, esomeprazole).
Antibiotics: For H. pylori eradication (e.g., amoxicillin, clarithromycin,
metronidazole).
Protective Agents: Coat the stomach lining (e.g., sucralfate).
Antiemetics: For nausea and vomiting (e.g., ondansetron).
Rehydration Solutions: For gastroenteritis to prevent dehydration.
 3. Eradication of H. pylori

Triple Therapy:
•Dosage:
Proton Pump Inhibitor (PPI): e.g., Omeprazole 20 mg twice daily.
Amoxicillin: 1000 mg twice daily.
Clarithromycin: 500 mg twice daily.
•Duration: Typically 10 to 14 days.
•Goal: Achieve a high eradication rate of H. pylori.
3. Eradication of H. pylori…

 Quadruple Therapy:

 Dosage:

 Proton Pump Inhibitor (PPI): e.g., Omeprazole 20 mg twice daily.

 Bismuth Subsalicylate: 525 mg four times daily.

 Metronidazole: 500 mg three times daily.

 Tetracycline: 500 mg four times daily.

•Duration: Usually 10 to 14 days.

•Goal: Effective for patients who have failed triple therapy or have penicillin allergies.
 4. Mechanisms and Side Effects of Key Drug
Classes

Antiemetics: Prevent nausea and vomiting.

• Mechanism: Block neurotransmitter receptors (e.g., serotonin, dopamine).

• Common Side Effects: Drowsiness, dizziness, dry mouth, and constipation.

Antiemetics dosage
Ondansetron:

• Dosage: 4 mg to 8 mg orally or IV every 8 hours as needed.

Metoclopramide:

• Dosage: 10 mg to 15 mg orally or IV 30 minutes before meals and at

bedtime.
Promethazine:

• Dosage: 12.5 mg to 25 mg orally or IM every 4 to 6 hours as needed .

 4. Mechanisms and Side Effects of Key Drug
Classes…
Laxatives(Constipation Drugs ): Facilitate bowel movements.

•Categories:

•Bulk-forming: Increase stool bulk (e.g., psyllium).

•Stimulant: Increase intestinal motility (e.g., bisacodyl).

•Osmotic: Draw water into the bowel (e.g., polyethylene glycol).

•Common Side Effects: Abdominal cramping, bloating, and diarrhea.

 Laxatives (Constipation Drugs)….

Psyllium (Bulk-forming):
Dosage: 1 tablespoon in 8 ounces of water once to three times daily.

Bisacodyl (Stimulant):
• Dosage: 5 mg to 15 mg orally once daily or 10 mg rectally as needed.

Polyethylene Glycol (Osmotic):

• Dosage: 17 g (one capful) dissolved in 8 ounces of water once daily.
4. Mechanisms and Side Effects of Key Drug Classes…

Antidiarrheal Drugs: Reduce diarrhea frequency.

 Mechanism: Decrease intestinal motility or absorb excess fluid (e.g., loperamide).

 Loperamide: Dosage: 4 mg initially, followed by 2 mg after each loose stool (max 8 mg/day

for OTC; 16 mg/day for Rx).

 Bismuth Subsalicylate: Dosage: 524 mg every 30 to 60 minutes as needed (max 4200 mg/day).

 Diphenoxylate/Atropine (Lomotil):Dosage: 2.5 mg of diphenoxylate

 and 0.025 mg of atropine, 1 to 2 tablets up to four times daily.

 Common Side Effects: Constipation and abdominal discomfort.

Anti-Flatulent Agents:

 Simethicone:
• Dosage: 40 mg to 125 mg taken after meals and at bedtime as
needed (max 500 mg/day).

Activated Charcoal:
• Dosage: 520 mg to 1040 mg taken after meals as needed (not
to exceed 4 grams/day).
Protective Agents: Promote healing of the stomach lining
Sucralfate:
•Dosage: 1 gram taken orally four times a day on an empty stomach.
•Mechanism: Forms a protective barrier over ulcers and the stomach lining,
promoting healing.
Misoprostol
•Dosage: 200 mcg taken orally four times a day, with food, to prevent NSAID-induced
gastric ulcers.
•Mechanism: Stimulates the secretion of mucus and bicarbonate, and enhances
mucosal blood flow, providing a protective effect on the gastric lining.
THANK YOU