Cooling the Fire of Heartburn

After assessing the frequency and severity of their patients' symptoms, pharmacists can recommend the right OTC products for individuals with heartburn.

Heartburn, also known as pyrosis, is characterized as a burning sensation that usually arises from the substernal area and moves up toward the neck or throat.¹ In the United States, heartburn affects an estimated 45% of the population, with an equal occurrence among men and women.¹ An estimated 45% of those who experience heartburn report having 2 or more days of heartburn per week, and an estimated 7% to 10% report experiencing daily heartburn.¹ If heartburn occurs within 2 hours after eating, especially when bending over or lying down, it is classified as postprandial heartburn. Nocturnal heartburn refers to the type of heartburn that occurs during sleep and is often responsible for waking an individual.¹

Patients with heartburn may present with 1 or more of the following symptoms^1,2:

• Painful burning sensation in the chest, just behind the breastbone, typically 1 to 4 hours after eating

• Sour or bitter taste in the mouth

• Excessive burping

• Hoarse, sore throat

• Coughing or choking while lying down

• Problems sleeping after eating

Heartburn that is frequent and persistent (lasting 3 months or more) is the most common symptom of gastroeosphageal reflux disease, which, if left untreated, can cause long-term complications, such as esophagitis, gastrointestinal bleeding, Barrett’s esophagus, and esophageal cancer. ¹ Patients with frequent episodes of heartburn or severe heartburn symptoms should always be referred for further medical evaluation.

Certain factors can contribute to or exacerbate episodes of heartburn, including an individual’s diet, lifestyle, use of certain pharmacologic agents, and certain medical conditions.^1,3

Pharmacologic Therapy

In selecting the most effective OTC agent for the self-treatment of heartburn, various factors may be considered, including severity, frequency, and duration of symptoms, dosing intervals, dosage form, potential drug interactions and contraindications, and cost.1

OTC products include antacids, histamine₂ (H₂)-receptor antagonists, and proton pump inhibitors (PPIs), as well as combination products containing H2-receptor antagonists and an antacid for the treatment of mild-to-moderate episodes of heartburn. In addition to these agents, bismuth subsalicylate, marketed as Pepto-Bismol (Procter & Gamble), is also indicated for the treatment of heartburn.¹

Antacids

Antacids are indicated for the treatment of mild, infrequent heartburn and indigestion. These agents relieve heartburn and dyspepsia by neutralizing gastric acid.¹ OTC antacid products contain various salts, including magnesium salts (hydroxide, carbonate, and trisilicate), aluminum salts (phosphate and hydroxide), calcium carbonate, and sodium bicarbonate.¹ Onset of symptom relief may be experienced within 5 minutes of taking antacids.¹ Patients taking agents such as tetracyclines, digoxin, iron supplements, fluoroquinolones, and ketoconazole should not use antacids within 2 hours of ingesting these medications. ¹ Patients with impaired renal function should not use antacids containing aluminum and magnesium.¹ Individuals using antacids should be counseled to take these products as directed.

H₂-Receptor Antagonists

OTC H₂-receptor antagonists (cimetidine, ranitidine, famotidine, and nizatidine) are indicated for the treatment of mild-tomoderate, infrequent, episodic heartburn and for the prevention of heartburn associated with acid indigestion and dyspepsia.¹ These agents exert their mechanism of action by inhibiting the effect of histamine on the H₂-receptor of the parietal cell and by decreasing the volume of secreted acid.¹ These agents should be taken at the onset of symptoms or at least 1 hour before symptoms are expected. Combination products that contain both an H₂-receptor antagonist and an antacid appear to provide faster relief of heartburn.¹ Onset of symptom relief can be expected within 30 to 45 minutes.¹

Self-treatment dosing of these agents should be limited to no more than twice daily.¹ The most common adverse effects include headache, dizziness, diarrhea, drowsiness, and constipation.¹ Pharmacists should screen for potential drug interactions and contraindications prior to recommending H₂-receptor antagonists. For example, potential drug interactions for cimetidine include theophylline, antidepressants, phenytoin, and warfarin.¹

Proton Pump Inhibitors

Currently, 2 PPIs, omeprazole and lansoprazole, are available as OTC heartburn treatments. PPIs are indicated for individuals 18 years and older for the treatment of frequent heartburn (2 or more days per week).^1,4,5

In May 2009, the FDA approved the PPI lansoprazole, marketed as Prevacid 24HR (Novartis Consumer Health), for the treatment of frequent heartburn. In December 2009, the FDA approved Zegerid OTC (Schering-Plough Healthcare Products Inc) for the management of heartburn. Zegerid OTC—a dual-ingredient formula that contains omeprazole and sodium bicarbonate—is available as a once-daily capsule.

PPIs are not intended for the immediate relief of occasional or acute heartburn episodes.^1,4,5 Patients should take these agents only once per day with a glass of water every morning at least 30 minutes before breakfast for 14 days and should be advised to complete the full 14-day course of therapy. The onset of symptom relief may occur 2 to 3 hours after taking a dose, but complete relief may be realized 1 to 4 days after starting therapy.^1,4,5 The tablet/ capsule should be swallowed whole and not be chewed or crushed. If symptoms still occur after completion of therapy or recur within 4 months, patients should be encouraged to seek medical evaluation.^1,7,8 Most common adverse effects associated with omeprazole are comparable with the H₂-receptor antagonists. Examples of potential drug interactions associated with PPIs include warfarin, ketoconazole, diazepam, digoxin, atazanavir, and tacrolimus. ^1,4,5

Conclusion

Prior to recommending any OTC products for heartburn, pharmacists should always ascertain the appropriateness of self-treatment and screen for possible drug interactions or contraindications. Individuals with preexisting medical conditions and pregnant or lactating women should be encouraged to seek advice from their primary health care provider prior to using any of these products. Patients younger than 12 years of age should always be referred to their primary health care provider before taking an OTC product for heartburn relief.

Patients with recurring episodes of heartburn or those exhibiting atypical or severe symptoms should always be referred for further medical evaluation to avoid further complications. Patients using these OTC products should be informed to seek immediate medical care if their symptoms worsen or show no signs of improvement after 14 days of selftreatment. It also is important to remind patients that these products should not be used for more than 2 weeks unless directed by a physician. In addition to providing patients with key information about the proper use and adverse effects associated with the use of these products, pharmacists can also suggest possible nonpharmacologic measures that may be beneficial in reducing the incidence of heartburn, such as avoiding eating late at night and eating large meals, stopping smoking, losing weight if needed, not exercising immediately after eating, avoiding foods and drinks that may aggravate or contribute to heartburn, and avoiding lying down within 30 minutes of eating.^1,2,4

Table 1Risk Factors and Potential Triggers for Heartburn

Dietary Habits

• Eating less than 2 hours before bedtime
• Eating large meals
• Eating foods such as citrus fruits, chocolate, peppermint, tomatoes, raw onions, garlic, black pepper, and fatty or spicy foods
• Drinking alcoholic beverages, particularly before bedtime
• Drinking beverages such as coffee, tea, citrus juices, and caffeinated or carbonated beverages

Lifestyle Habits

• Being overweight
• Completing certain types of exercises (weight lifting, cycling, sit-ups)
• Lying down within 2 hours after eating
• Wearing restrictive or tight clothing
• Smoking
• Having stress

Pharmacologic Agents

• Anticholinergic agents
• Aspirin
• Benzodiazepines
• Beta-blockers
• Bisphosphonates
• Calcium channel blockers
• Chemotherapy
• Dopamine
• Estrogens
• Iron salts
• Narcotic analgesics
• Nitrates
• Nonsteroidal anti-inflammatory drugs
• Potassium
• Progesterone
• Tetracyclines
• Theophylline
• Tricylic antidepressants
• Zidovudine

Medical Conditions

• Gastroesophageal reflux disease
• Hiatal hernia
• Motility disorders (eg, gastroparesis)
• Pregnancy
• Peptic ulcer disease
• Scleroderma
• Zollinger-Ellison syndrome

Adapted from references 1, 3-6.

Table 2

Patients Should Be Encouraged to Seek Medical Care if They Experience:

• Chest pain, dizziness, light-headedness
• Continuous nausea and vomiting
• Difficulty or pain in swallowing
• Heartburn that awakens them at night
• Unexplained weight loss

Adapted from reference 1.

Table 3Examples of OTC Heartburn Products

Drug Class

Brand Name (Active Ingredients)

Antacids

• Children’s Mylanta Chewable Tablets (calcium carbonate 400 mg, tablets)
• Gaviscon Extra Strength Liquid (aluminum hydroxide 254 mg, magnesium carbonate 237.5 mg per 5 mL, liquid)
• Maalox Regular Strength (calcium carbonate 600 mg, tablets)
• Mylanta Supreme Liquid (calcium carbonate 400 mg, magnesium hydroxide 135 mg per 5 mL, liquid)
• Mylanta Ultimate Strength Liquid (aluminum hydroxide 500 mg, magnesium hydroxide 500 mg per 5 mL)
• Tums Regular Strength (calcium carbonate USP 750 mg, tablets)
• Tums Ultra 1000 (calcium carbonate USP 1000 mg, tablets)

H₂-Receptor Antagonists

• Axid AR (nizatidine 75 mg, tablets)
• Maximum Strength Zantac 150 (ranitidine 150 mg, tablets)
• Pepcid AC Original Strength (famotidine 10 mg, tablets)
• Pepcid AC Maximum Strength (famotidine 20 mg, tablets)
• Tagamet HB 200 (cimetidine 200 mg, tablets)
• Zantac 75 (ranitidine 75 mg, tablets)

H₂-Receptor Antagonists with Antacid

• Pepcid Complete (famotidine 10 mg, calcium carbonate 800 mg, magnesium hydroxide 165 mg, tablets)
• Tums Dual Action (famotidine 10 mg, calcium carbonate 800 mg, magnesium hydroxide 165 mg, tablets)

Proton Pump Inhibitors

• Prevacid 24HR (lansoprazole 15 mg, capsules)
• Prilosec OTC (omeprazole magnesium 20.6 mg, tablets)
• Zegerid OTC (omeprazole 20 mg, sodium bicarbonate 1100 mg, tablets)

Combination Products

• Alka Seltzer Gold (sodium bicarbonate 1050 mg, anhydrous citric acid 1000 mg, potassium bicarbonate 344 mg, tablets)
• Maalox Advanced Regular Strength (aluminum hydroxide 200 mg, magnesium hydroxide 200 mg, simethicone 20 mg per 5 mL, liquid)
• Maalox Advanced Maximum Strength (calcium carbonate 1000 mg, simethicone 60 mg, tablets)
• Mylanta Regular Strength (aluminum hydroxide 200 mg, magnesium hydroxide 200 mg, simethicone 20 mg per 5 mL, liquid)
• Rolaids Multi-Symptom (calcium carbonate 675 mg, magnesium hydroxide 135 mg, simethicone 60 mg, tablets)

Adapted from references 1 and 3.

Ms. Terrie is a clinical pharmacy writer based in Haymarket, Virginia.

References

• Zweber Ann, Beradi Rosemary. Heartburn and Dyspepsia. In: Berardi R, Newton G, McDermott JH, et al, eds. Handbook of Nonprescription Drugs. 16th ed. Washington, DC: American Pharmacists Association; 2006 :231-246.
• What is Heartburn? ZantacOTC. Boehringer Ingelheim. website. http://www.zantacotc.com/heartburn/index.jsp Accessed May 2, 2010.
• Causes of Heartburn. Mylanta Products. Johnson and Johnson website. http://www.mylanta.com/causes-heartburn. Accessed May 2, 2010.
• Prevacid 24HR Capsules Product Information. Novartis Consumer Health, Inc. website. http://www.prevacid24hr.com/24-hour-relief.jsp. Accessed May 2, 2010.
• Zegerid OTC Product Information. Schering Plough Healthcare Products website. http://www.zegeridotc.com/download/zegeridotc_product_labeling.pdf. Accessed May 2, 2010.
• Heartburn or GERD. The American College of Gastroenterology website. http://www.acg.gi.org/patients/women/whatisgerd.asp. Accessed May 2, 2010.
• Heartburn Triggers. Zegerid OTC. Schering Plough Healthcare Products website. http://www.zegeridotc.com/zegeridotc/heartburn/heartburn-triggers.jspa. Accessed May 5, 2010.
• What is heartburn? TagametHB.GlaxoSmithKline website. http://www.essentialsforlivingwell.com/Products/TagametHB/AboutHeartburn.aspx. Accessed May 5, 2010.