Kee: Pharmacology, 8th Edition

Chapter 48: Antiulcer Drugs

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Peptic ulcer is a broad term for an ulcer occurring in the esophagus, stomach, or
duodenum within the upper gastrointestinal (GI) tract.
Peptic ulcers occur when there is a hypersecretion of hydrochloric acid and pepsin, which
erode the GI mucosal lining. Hydrochloric acid (HCl) is released from the parietal cells
of the stomach and is influenced by histamine, gastrin, and acetylcholine.
The gastric secretions in the stomach strive to maintain a pH of 2 to 5. Pepsin, a digestive
enzyme, is activated at a pH of 2, and the acid-pepsin complex of gastric secretions can
cause mucosal damage. If the pH of gastric secretions increases to pH 5, the activity of
pepsin declines.

PREDISPOSING FACTORS IN PEPTIC ULCER DISEASE

The nurse needs to assist the patient in identifying possible causes of the ulcer and to
teach ways to alleviate them. Predisposing factors include mechanical disturbances,
genetic influences, bacterial organisms, environmental factors, and certain drugs.
Helicobacter pylori, a gram-negative bacillus, is linked with the development of peptic
ulcer and known to cause gastritis, gastric ulcer, and duodenal ulcer.
There are various protocols for treating H. pylori infection. The combination of drugs
differs for each patient according to the patients drug tolerance. A common treatment
protocol is the triple therapy of metronidazole, omeprazole, and clarithromycin. The drug
regimen eradicates more than 90% of peptic ulcer caused by H. pylori.
Gastroesophageal reflux disease (GERD) is an inflammation of the esophageal mucosa
caused by reflux of gastric acid content into the esophagus. Medical treatment is similar
to the treatment for peptic ulcers. Treatment includes H2 blockers and PPIs.
GERD is a chronic disorder that requires continuous care.

NONPHARMACOLOGIC MEASURES FOR MANAGING PEPTIC ULCER AND

GASTROESOPHAGEAL REFLUX DISEASE

With a GI disorder, nonpharmacologic measures, along with drug therapy, are an

important part of treatment.
Once the GI problem is resolved, the patient should continue to follow nonpharmacologic
measures to avoid recurrence of the condition.
Certain drugs like NSAIDs, which include aspirin, should be taken with food or in a
decreased dosage.

Copyright 2015, 2012, 2009, 2006, 2003, 2000, 1997, 1993 by Saunders, an imprint of Elsevier Inc.

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48-2

ANTIULCER DRUGS

There are seven groups of antiulcer agents: (1) tranquilizers, which decrease vagal
activity; (2) anticholinergics, which decrease acetylcholine by blocking the cholinergic
receptors; (3) antacids, which neutralize gastric acid; (4) H2 blockers, which block the H2
receptor; (5) PPIs, which inhibit gastric acid secretion, regardless of acetylcholine or
histamine release; (6) the pepsin inhibitor sucralfate, and (7) the prostaglandin E1
analogue misoprostol, which inhibits gastric acid secretion and protects the mucosa.

Tranquilizers
Tranquilizers have minimal effect in preventing and treating ulcers; however, they reduce
vagal stimulation and decrease anxiety.
Anticholinergics
Anticholinergics and antacids relieve pain by decreasing GI motility and secretion. They
act by inhibiting acetylcholine and blocking histamine and hydrochloric acid.
Anticholinergics should be taken before meals to decrease the acid secretion that occurs
with eating. Antacids can slow the absorption of anticholinergics and therefore should be
taken 2 hours after anticholinergic administration.
Anticholinergics have many side effects, including dry mouth, decreased secretions,
headache, blurred vision, drowsiness, dizziness, lethargy, palpitations, bradycardia,
tachycardia, urinary retention, and constipation.
Antacids
Antacids promote ulcer healing by neutralizing hydrochloric acid and reducing pepsin
activity; they do not coat the ulcer.
Sodium bicarbonate has many side effects, including sodium excess, water retention,
metabolic alkalosis, and acid rebound; therefore, it is seldom used for peptic ulcers.
Calcium carbonate is most effective in neutralizing acid; however, one-third to one-half
of the drug can be systemically absorbed and can cause acid rebound. Hypercalcemia and
Burnetts syndrome can result from excessive use of calcium carbonate.
Nonsystemic antacids are composed of alkaline salts such as aluminum and magnesium;
there is a small degree of systemic absorption with these drugs, mainly of aluminum. The
combination of magnesium and aluminum salts neutralizes gastric acid without causing
severe diarrhea or constipation.
Antacids containing magnesium salts are contraindicated in patients with impaired renal
function because of the risk of hypermagnesemia.
Histamine2 Blockers
The histamine2 (H2) blockers are used to treat gastric and duodenal ulcers and prevent
acid reflux in the esophagus. These drugs block the H2 receptors of the parietal cells in
the stomach, thus reducing gastric acid secretion and concentration.
Side effects and adverse reactions of H2 blockers include headaches, dizziness,
constipation, pruritus, skin rash, gynecomastia, decreased libido, and impotence.

Copyright 2015, 2012, 2009, 2006, 2003, 2000, 1997, 1993 by Saunders, an imprint of Elsevier Inc.

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48-3

Cimetidine, the first H2 blocker, interacts with many drugs by inhibiting hepatic drug
metabolism; it enhances the effects of oral anticoagulants, theophylline, and phenytoin
among others. Cimetidine can cause an increase in BUN, serum creatinine, and serum
alkaline phosphatase.

Proton Pump Inhibitors

The PPIs suppress gastric acid secretion by inhibiting the hydrogen/potassium adenosine
triphosphatase (ATPase) enzyme system located in the gastric parietal cells. They tend to
inhibit gastric acid secretion up to 90% greater than the H2 blockers.
PPIs can enhance the action of digoxin, oral anticoagulants, certain benzodiazepines, and
phenytoin, because they interfere with liver metabolism of these drugs.
Pepsin Inhibitor
Sucralfate, a complex of sulfated sucrose and aluminum hydroxide, is classified as a
pepsin inhibitor. It is nonabsorbable and combines with protein to form a viscous
substance that covers the ulcer and protects it from acid and pepsin. This drug does not
neutralize acid or decrease acid secretions.
Because sucralfate is not systemically absorbed, side effects are few; however, it can
cause constipation.
Prostaglandin Analogue Antiulcer Drug
Misoprostol, a synthetic prostaglandin analogue, is a drug used to prevent and treat peptic
ulcer. It appears to suppress gastric acid secretion and increase cytoprotective mucus in
the GI tract. It causes a moderate decrease in pepsin secretion.
Misoprostol is contraindicated during pregnancy and for women of childbearing age.
NURSING PROCESS
Antiulcer: Antacids
Evaluate patients pain, including type, duration, severity, and frequency.
Check patients renal function.
Assess for fluid and electrolyte imbalances, especially serum phosphate and calcium
levels.
Avoid administering antacids with other oral drugs, because antacids can delay their
absorption. An antacid should definitely not be given with tetracycline, digoxin, or
quinidine, because it binds with and inactivates most of the drug. Antacids are given 1 to
2 hours after other medications.
Shake suspension well before administering; follow with water.
Monitor electrolytes and urinary pH, calcium, and phosphate levels.
Teach patient to report pain, coughing, or vomiting of blood.
Encourage patient to drink 2 oz of water after antacid to ensure that drug reaches the
stomach.

Copyright 2015, 2012, 2009, 2006, 2003, 2000, 1997, 1993 by Saunders, an imprint of Elsevier Inc.

Downloadable Key Points

48-4

Direct patient to take antacid 1 to 3 hours after meals and at bedtime. Do not take
antacids at mealtime; they slow gastric emptying time, causing increased GI activity and
gastric secretions.
Advise patient to notify health care provider if constipation or diarrhea occurs; the
antacid may have to be changed. Self-treatment should be avoided.
Warn that taking an unlimited amount of the antacid is contraindicated.
Warn patient to avoid taking antacids with milk or foods high in vitamin D.
Guide patient to check antacid labels for sodium content if on a sodium-restricted diet.
Alert patient to consult with health care provider before taking self-prescribed antacids
for longer than 2 weeks.
Teach patient how to take antacids correctly. Chewable tablets should be thoroughly
chewed and followed with water. With liquid antacid, 2 to 4 ounces of water should
follow the antacid. Increased amount of water with antacids increases gastric emptying
time.
Direct patient to avoid food and beverages that can cause gastric irritation (high-fat or
spicy meals; caffeine-containing coffee and soda; alcohol).
Explain to patient that stools may become speckled or white.
Determine the effectiveness of the antiulcer treatment and the presence of side effects.
Patient should be free of pain, and healing should progress.

Antiulcer: Histamine2 Blocker

Determine patients pain, including type, duration, severity, frequency, and location.
Evaluate GI complaints.
Check mental status.
Assess fluid and electrolyte imbalances, including intake and output.
Monitor gastric pH (>5 is desired), blood urea nitrogen (BUN), and creatinine.
Determine drug history; report probable drug-drug interactions.
Administer drug just before meals to decrease food-induced acid secretion or at bedtime.
Be alert that reduced doses of drug are needed by older adults, who have less gastric acid.
Metabolic acidosis must be prevented.
Administer IV drug in 20 to 100 mL of solution.
Teach patient to report pain, coughing, or vomiting of blood.
Advise patient to avoid smoking, because it can hamper effectiveness of drug.
Direct patient to separate ranitidine and antacid dosage by at least 1 hour.
Warn patient not to drive a motor vehicle or engage in dangerous activities until
stabilized on the drug.
Tell patient that drug-induced impotence and gynecomastia are reversible.
Teach patient to eat foods rich in vitamin B12 to avoid deficiency as a result of drug
therapy.
Antiulcer: Pepsin Inhibitor
Evaluate patients pain, including type, duration, severity, and frequency. Ulcer pain
usually occurs after meals and during the night.

Copyright 2015, 2012, 2009, 2006, 2003, 2000, 1997, 1993 by Saunders, an imprint of Elsevier Inc.

Downloadable Key Points

48-5

Determine patients renal function. Report urine output of <600 mL/d or <30 mL/h.
Assess for fluid and electrolyte imbalances.
Measure gastric pH (>5 is desired).
Patient will have relief of abdominal pain after 1 to 2 weeks of antiulcer drug
management.
Administer drug on empty stomach.
Administer antacid 30 minutes before or 30 minutes after sucralfate. Allow 1 to 2 hours
to elapse between sucralfate and other prescribed drugs; sucralfate binds with certain
drugs (e.g., tetracycline, phenytoin), reducing their effect.
Advise patient to take drug exactly as ordered. Therapy usually requires 4 to 8 weeks for
optimal ulcer healing. Advise patient to continue to take drug even if feeling better.
Increase fluids, dietary bulk, and exercise to relieve constipation.
Monitor for severe, persistent constipation.
Emphasize cessation of smoking as indicated.
Direct patient to report pain, coughing, or vomiting of blood.

Copyright 2015, 2012, 2009, 2006, 2003, 2000, 1997, 1993 by Saunders, an imprint of Elsevier Inc.