Dr. Rockafellow is assistant professor of pharmacy and Dr. Berardi is professor of pharmacy at the University of Michigan College of Pharmacy, Ann Arbor.
Heartburn, the most common symptom of acid reflux, indigestion, and gastroesophageal reflux disease (GERD), also may occur with other diseases such as peptic ulcer disease. Heartburn is described as a substernal burning sensation that radiates upward toward the neck or throat.1 For many individuals, heartburn is mild, infrequent, and predictable. For others, heartburn is frequent (occurs 2 or more days a week), persistent, and more severe.
GERD develops when reflux of gastric contents into the esophagus causes troublesome symptoms (eg, heartburn 2 or more days a week, sleep disturbances) or complications (eg, esophagitis, esophageal stricture), which adversely affect the patient’s well-being.2,3 Postprandial heartburn, sometimes accompanied by a sour taste in the mouth (regurgitation), usually occurs within several hours of ingesting a meal and is often precipitated by lying down or bending over. Heartburn may limit food and beverage choices and disrupt sleep or work.1,3 Frequent, nighttime (nocturnal) heartburn is associated with more severe esophageal injury. Extraesophageal manifestations of GERD include asthma, chronic cough, laryngitis, and noncardiac chest pain.1-3 Pharmacists play an important role in determining whether self-treatment of heartburn is appropriate, or whether the patient should be referred for further medical evaluation.1
Exclusions to the Self-Treatment of Heartburn
• Troublesome heartburn that has persisted for >3 months
• Painful or difficult swallowing
• Chronic coughing or hoarseness
• Heartburn or chest pain accompanied by sweating, nausea, shortness of breath, or radiation of pain to the arm, neck, back, or jaw
• Vomiting blood or black, tarry stools
• Unexplained weight loss
• Heartburn that persists or recurs after 2 weeks of treatment with an OTC histamine2-receptor antagonist (H2RA) or proton pump inhibitor (PPI)
The self-treatment of heartburn is aimed at nonpharmacologic measures and the use of OTC medications. Individuals should keep a diary to aid in identifying troublesome dietary, lifestyle, and medication triggers so that strategies are tailored to the individual. Evidence-based measures that support improved clinical outcomes include elevating the head of the bed, weight loss, and avoiding late-night eating.2-4 Whereas there is insufficient data to support dietary and lifestyle measures for all patients,certain factors may precipitate heartburn in subsets of patients. Adoption of the following specific behavioral changes are recommended for these individuals based on their history.1,3
• Nocturnal symptoms: Elevate the head of the bed by using 6-inch blocks or a foam wedge; using stacked pillows may worsen symptoms. Avoid eating within 3 hours of bedtime.
• Postprandial symptoms: Avoid exercise, bending over, or lying down after meals. Eat smaller and more frequent meals.
• Dietary avoidance: Avoid citrus fruits, tomatoes, spicy foods, carbonated beverages, high-fat and fried foods, chocolate, mint, and beverages with caffeine.
• Lifestyle modifications: Weight reduction for overweight individuals, avoid wearing tight clothes around the abdomen, and reduce or discontinue smoking and/or alcohol.
• Medications: Certain medications may trigger or worsen heartburn by decreasing lower esophageal sphincter pressure, delaying gastric emptying, or by damaging the esophageal mucosa.
Antacids, H2RAs, PPIs, and bismuth subsalicylate (BSS) are all effective OTC medications when used for the selftreatment of heartburn.1-3,5,6 The selection of a specific agent is based on the frequency and severity of the heartburn and the onset and duration of symptom relief provided by the drug.1
Antacids provide quick (within minutes) relief of mild infrequent heartburn, but relief is only temporary (about 30 minutes on an empty stomach).1,5 Liquid formulations usually act faster than chewable tablets, but quick-dissolving tablets provide the most rapid symptom relief. Antacids are available as a single salt or a combination of salts and many have been reformulated to contain calcium. Antacids also may contain alginic acid, which forms a “foam” barrier to protect the esophagus from noxious acid refluxate, and simethicone, which may decrease discomfort associated with intestinal gas.
Magnesium-containing antacids and combination aluminum/magnesium products are associated with dose-dependent diarrhea. Aluminum-containing antacids cause constipation at higher daily dosages. Calcium carbonate— and sodium bicarbonate–containing antacids may be associated with belching and flatulence due to the release of carbon dioxide. Magnesium-containing antacids should be avoided in patients with impaired renal function. Drug interactions can usually be avoided by separating the antacid from other medications by 2 hours. Patients should not exceed the maximum daily antacid dose. If antacids are needed for >2 days a week, the patient may require an OTC H2RA or PPI.
OTC H2RAs (cimetidine, famotidine, nizatidine, ranitidine) are effective for the treatment of mild-to-moderate infrequent heartburn.1 The lower OTC dosages should be used for mild symptoms, whereas the higher dosages are used for patients with moderate symptoms. The onset of symptom relief is 30 to 45 minutes, and the duration lasts up to 10 hours.1 A twice-daily regimen provides improved symptom control for patients with daytime and nighttime heartburn. H2RAs should be taken preferably on a “when-needed” basis, as tachyphylaxis (tolerance) may develop to the antisecretory effect when taken every day.1,3,5 Taking an antacid with an H2RA provides immediate relief (antacid) of heartburn as well as a longer duration of symptom relief (H2RA). An H2RA may be taken 30 to 60 minutes prior to eating or exercise to prevent anticipated symptoms.
H2RAs are well-tolerated and have a low incidence of side effects, which include headache, diarrhea, constipation, dizziness, and drowsiness. Cimetidine, and to a lesser extent ranitidine, interact with numerous drugs that are metabolized by the liver, including phenytoin, warfarin, diazepam, and tricyclic antidepressants. Famotidine and nizatidine are spared the hepatic drug interaction.1 Patients who remain symptomatic after 2 weeks of treatment may require an OTC PPI or referral for medical evaluation.
OTC PPIs are indicated for patients with frequent heartburn who have symptoms ≥2 days per week.1,7 Although omeprazole is the only currently available OTC PPI, other PPIs such as lansoprazole may soon be approved by the FDA for OTC use. The onset of symptom relief is 2 to 3 hours, and the duration may last for up to 24 hours.1 PPIs should be taken 30 to 60 minutes before eating every morning for 14 days. This regimen can be repeated after 4 months if symptoms recur.7 Tachyphylaxis does not develop to the antisecretory effect when taken daily.1,3
PPIs are well-tolerated and have a low incidence of side effects, similar to H2RAs. Omeprazole may interact with diazepam, phenytoin, and warfarin. If heartburn recurs while taking omeprazole, persists for >14 days, or recurs in <4 months, the patient should be counseled to seek further medical evaluation.
BSS is not an antacid, but it is included in some products with common antacid brand names. Bismuth salts may cause the stool and tongue to turn black. BSS should be used with caution in patients at risk of developing salicylate toxicity. Avoid BSS in children at risk of developing Reye’s syndrome.
Individuals with heartburn or acid indigestion often consult their pharmacists for advice. If self-treatment is indicated, counseling on diet, lifestyle, and medications should be individualized and based on symptom assessment.
References1. Zweber A, Berardi RR. Heartburn and Dyspepsia. In: Berardi RR, Ferreri S, Hume A , et al, eds. Handbook of Nonprescription Drugs: An Interactive Approach to Self-Care. Washington, DC: American Pharmacists Association; 2009 (in press).
2. Kahrilas PJ, Shaheen NJ, Vaezi MF, Hiltz SW, Black E, Modlin IM. American Gastroenterological Association Medical Position Statement on the Management of Gastroesophageal Reflux Disease. Gastroenterology. 2008;135:1383-1391.
3. Kahrilas PJ. Clinical Practice: Gastroesophageal reflux disease. N Engl J Med 2008;359(16):1700-1707.
4. Kaltenbach K, Crockett S, Gerson LB. Are lifestyle measures effective in patients with gastroesophageal reflux disease? Arch Intern Med 2006;166(9):965-971.
5. Fugit RV, Berardi RR. Upper Gastrointestinal Disorders. In: Koda-Kimble MA, Guglielmo BJ, Young LY, Kradian WA, Alldredge, BK, eds. Applied Therapeutics: The Clinical Use of Drugs. Baltimore, MD: Lippincourt Williams & Wilkins; 2009.
6. Boparai V, Rajagopalan J, Triadafilopoulos G. Guide to the use of proton pump inhibitors in adult patients. Drugs 2008;68(7):925-947.
7. Prilosec OTC Product Monograph. Prilosec Web site. www.prilosecotc.com/en_US/hcp/media/downloads/Monograph.pdf. Accessed December 7, 2008.