US Pharm. 2014;39(12):8-11.
In a typical workday, the average pharmacist fields several questions from patients about stomach discomfort and heartburn. With a good knowledge of the various options for heartburn, pharmacists can make rapid and accurate decisions to ensure that patients obtain the optimal treatment.
The Problem of Heartburn
Heartburn is the lay term for a burning sensation in the general area of the heart, often due to gastroesophageal reflux disease (GERD).1 Normally, swallowed food passes down the esophagus, reaching a muscular band known as the lower esophageal sphincter (LES). When the person swallows, the LES relaxes so that ingestants can enter the stomach. The LES is usually closed, and food remains in the stomach. However, in certain situations, stomach contents push upward (reflux) into the esophagus. Stomach contents are acidic and contain damaging materials (e.g., pepsin, enzymes) that induce esophageal damage and cause the characteristic midchest pain and associated symptoms of GERD.
In discussions of GERD and its treatment, the National Institutes of Health (NIH) lists general alarm symptoms that necessitate a physician appointment.1-3 They include worsening symptoms, symptoms that do not improve with lifestyle changes or medications, and daily or nocturnal symptoms. The list also includes choking, coughing, shortness of breath, feeling filled up quickly when eating, nausea and vomiting, frequent vomiting, blood in the vomitus or stools, black and/or tarry stools, bloating or cramping, severe and/or unremitting diarrhea, dysphagia, and odynophagia. Other alarm symptoms include sweating; bleeding from any other area not previously mentioned; hoarseness; fever in conjunction with abdominal pain; anorexia; abdominal pain in a nonepigastric area; unexplained weight loss; chest pain; pain in the lower belly, on the side, or in the back; and pain that radiates to the jaw, neck, or arm. These alarming referral symptoms could also be indicative of myocardial infarction, gastric cancer, appendicitis, peptic ulcer, gallstones, bowel problems, or other morbid conditions.1-3
Nonprescription antacids carry FDA-approved labeling for heartburn.3,4 Each product label includes a minimum age below which the product should not be used without physician supervision. For patient safety, the pharmacist should urge the patient to closely observe these instructions. Antacid labels also warn patients not to use the product for longer than 2 weeks. The pharmacist should question the patient about the onset of symptoms and refer the patient if they have been present for >2 weeks.3,4
Magnesium hydroxide (e.g., Milk of Magnesia) is a common antacid, but it can cause diarrhea and kidney stones, and patients with renal problems can experience hypermagnesemia.3 Calcium carbonate (e.g., Tums) is a potent antacid with a rapid onset of action. The product is usually safe when used as directed, but it can cause constipation.3,4 Regardless of the individual differences among them, antacids share one advantage over the other nonprescription heartburn medications—they act rapidly. However, they also share one major drawback—they cannot reduce the amount of acid produced.
Histamine-2 (H2) Blockers
H2 blockers, otherwise known as H2 receptor antagonists (H2RAs), have an inherent superiority over antacids in their ability to reduce the amount of acid produced, although they do not provide immediate relief. These nonprescription products include cimetidine (Tagamet HB 200), famotidine (Pepcid AC, Maximum Strength Pepcid AC), and ranitidine (Zantac 75, Zantac 150).5-9 They should not be used without physician supervision in patients who are pregnant or breastfeeding, or in any patient <12 years of age.
Patients are cautioned against self-use if they are allergic to the ingredient or to other acid reducers, have trouble or pain when swallowing, or are using other acid reducers. All five product labels also advise against unsupervised self-use if the patient has vomiting with blood or has bloody or black stools, as those may be signs of a serious condition for which the patient should see a physician. The label of Maximum Strength Pepcid AC also carries an FDA-mandated warning against self-use if the patient has kidney disease, unless directed by a physician.7
Labels of all five products warn patients to speak to a physician before use if they have any of the following: 1) heartburn for more than 3 months; 2) lightheadedness, sweating, or dizziness with their heartburn; 3) chest pain or shoulder pain with shortness of breath, sweating, pain spreading to arms, neck, or shoulders, or lightheadedness; 4) frequent chest pain; 5) frequent wheezing, particularly with heartburn; 6) unexplained weight loss; 7) nausea or vomiting; and 8) stomach pain.5-9
Patients are cautioned on all H2-blocker labels to stop using the product and speak to a physician if their heartburn continues or worsens and if they need to take the product for more than 14 days. The label of Tagamet HB 200 also adds, “If stomach pain continues.”5
Tagamet HB 200 is the only nonprescription H2 blocker that inhibits the CYP450 system. For this reason, it carries the following drug interaction warning: “Ask a doctor or pharmacist before use if you are taking theophylline (oral asthma medicine), warfarin (blood thinning medicine), or phenytoin (seizure medicine).”5
Patients are directed on all product labels to take one tablet with a glass of water to relieve symptoms.5-9 They should not take more than two tablets in any consecutive 24-hour period. If they wish to prevent symptoms, they should take one tablet with a glass of water before eating or drinking anything that causes heartburn.
The products vary in the timing of dosing for prevention. Tagamet HB 200 may be taken just before or any time up to 30 minutes before the ingestion, while Pepcid AC may be taken from 15 to 60 minutes before the food/drink, and Pepcid AC Maximum Strength may be taken 10 to 60 minutes before eating or drinking.5-7 Both Zantac products may be taken 30 to 60 minutes before the troublesome food or drink.8,9
Proton Pump Inhibitors (PPIs)
PPIs lessen stomach acid production more effectively than the H2 blockers. Single-entity nonprescription products include omeprazole 20-mg tablets (Prilosec OTC), lansoprazole 15-mg capsules (Prevacid 24HR), and the newest Rx-to-OTC switch product, esomeprazole 20-mg capsules (Nexium 24HR).10-12 Zegerid OTC is a combination product containing 20 mg of omeprazole and 1,100 mg of sodium bicarbonate per capsule.13
The indications for PPIs differ from those for antacids and H2 blockers. PPIs are approved only to treat frequent heartburn (occurring on two or more days a week). In other words, patients who have heartburn only one day a week (or less frequently) should use other products. Labels also advise patients of the following in regard to onset of action: “Not intended for immediate relief of heartburn; this drug may take 1 to 4 days for full effect.” Patients are warned not to use the product if they are allergic to the ingredients and are advised to speak to a healthcare professional before use if they are pregnant or breastfeeding.10-13
Patients should not use PPIs if they have trouble or pain swallowing food, vomiting with blood, or bloody/black stools, as these may be signs of a serious medical condition that requires physician care. PPI labels warn patients to speak to a physician before use if they experience any of the following: 1) heartburn for >3 months; 2) lightheadedness, sweating, or dizziness with their heartburn; 3) chest pain or shoulder pain with shortness of breath, sweating, or pain spreading to arms, neck, or shoulders; 4) frequent chest pain; 5) frequent wheezing, particularly with heartburn; 6) unexplained weight loss; 7) nausea or vomiting; and 8) stomach pain.10-13 The label of Zegerid OTC also provides a caution for patients who are on a sodium-restricted diet, and the label of Prevacid 24HR adds a warning for patients with liver disease.11,13
All PPI labels include the warning to speak to a physician or pharmacist before use if the patient is taking warfarin, prescription antifungal medications, digoxin, or tacrolimus.10-13 The labels of Prilosec OTC, Nexium 24HR, and Zegerid OTC warn against concomitant use with clopidogrel, cilostazol, and diazepam.10,12,13 The label of Prevacid 24HR advises against use with theophylline.11 The labels of Prilosec OTC, Nexium 24HR, and Zegerid OTC also carry a warning against use with prescription antiretrovirals for HIV,10,12,13 while the label of Prevacid 24HR specifically warns against use with atazanavir (Reyataz) for HIV.11 Finally, the label of Zegerid OTC carries a global warning against unsupervised use with any other prescription medication due to the possibility that sodium bicarbonate might cause an interaction.13
The PPI labels caution patients to stop use and speak to a physician in the following cases: 1) heartburn continues or worsens; 2) the patient needs to take the product for more than 14 days; or 3) the patient needs to take more than one course of treatment every 4 months.10-13 Labels of Prilosec OTC, Nexium 24HR, and Zegerid OTC also warn patients to stop use and speak to a physician if they develop diarrhea.10,12,13
The directions for all four PPIs are almost identical.10-13 If the prospective patient is <18 years of age, the parent is advised to speak to a physician, since heartburn in children may be caused by a serious condition. Patients are instructed to take the PPI only once daily, every 24 hours for 14 days, and they are advised that it may take 1 to 4 days for full effect, although some people experience complete symptom relief within 24 hours. Patients should swallow one capsule/tablet with a glass of water before eating in the morning, every day for 14 days. They are not to use it for more than 14 days unless directed by their physician. They should swallow it whole, without chewing or crushing, and the label of Zegerid OTC also advises patients not to open the capsule to sprinkle it on food.13
A final set of instructions on all four PPI product labels is critical for preventing overuse in case the patient has a serious condition such as an ulcer. Patients are advised that, if needed, they may repeat the 14-day course of treatment every 4 months (i.e., three times yearly), but they are warned not to take the drug for more than 14 days or more often than every 4 months, unless directed to do so by a physician.10-13
What Is Heartburn?
Heartburn is a common condition in which the food or drink you eat cannot stay in your stomach for digestion. Instead, it moves backward up into your esophagus (a process known as reflux), where the acids and enzymes cause burning and produce the troubling discomfort in your chest.
What Causes Heartburn?
The main problem lies in a small muscle between your esophagus and stomach that is supposed to shut down tightly after you eat or drink, so that your food and drink will remain in your stomach. When this muscle does not work properly, the damaging materials move upward into your esophagus.
How Can You Prevent Heartburn?
You can reduce the possibility of heartburn by making some lifestyle changes. Wear clothing that is loose around the waist to reduce pressure on the stomach. Eat smaller meals, and eat more slowly. Since reflux is common at night, make your last meal small and be sure to finish eating as long as 5 to 6 hours before bedtime. Heartburn also occurs more frequently in those who are overweight or pregnant.
Fatty foods worsen reflux, so you should avoid them as much as possible. The long list of high-fat foods includes chocolate, bacon, potato chips, margarine, butter, and fried foods. You may find that other foods cause problems, such as orange juice, pizza, or tomato-based sauces. When you have identified such an irritant, avoid it in the future. Nicotine and alcohol both worsen reflux, so you should avoid cigarettes, cigars, chewing tobacco, and all forms of alcohol.
How Can You Treat Heartburn?
When you first recognize possible reflux, your pharmacy is a good place to go for advice on when to see a physician. Your pharmacist will need to know your age, your status regarding pregnancy or breastfeeding, and a list of all of your symptoms. There are many dangerous symptoms that will require a physician visit to ensure that you do not have a serious condition such as an ulcer or stomach cancer.
If the pharmacist believes your problem to be nothing more than reflux, he or she may recommend nonprescription products. Whichever you choose, be sure to read every set of warnings, precautions, and instructions on the label. Failure to understand and follow all of these guidelines can have drastic consequences.
Some heartburn products are simple antacids, such as Tums and Alka-Seltzer. They are usually inexpensive and act rapidly, although they do not reduce the amount of acid produced. Other OTC products are effective at reducing the amount of stomach acid produced, although they may not give relief as quickly and tend to cost more. These stronger products fall into two groups. One is histamine-2 (H2) blockers, including Tagamet HB 200, Pepcid AC, Maximum Strength Pepcid AC, Zantac 75, and Zantac 150. They can be used by those age 12 years or older. The second group is proton pump inhibitors (PPIs), which include Prilosec OTC, Prevacid 24HR, Nexium 24HR, and Zegerid OTC. They can only be used by those age 18 years or older.
Remember, if you have questions, Consult Your Pharmacist.
1. Gastroesophageal reflux disease. MedlinePlus. www.nlm.nih.gov/medlineplus/ency/article/000265.htm. Accessed October 18, 2014.
2. Gastroesophageal reflux—discharge. MedlinePlus. www.nlm.nih.gov/medlineplus/ency/patient-instructions/000197.htm. Accessed October 18, 2014.
3. Taking antacids. MedlinePlus. www.nlm.nih.gov/medlineplus/ency/patientinstructions/000198.htm. Accessed October 18, 2014.
4. Tums Ultra 1000 product details. GlaxoSmithKline. www.tums.com/products/ultra-1000.html. Accessed October 18, 2014.
5. Tagamet HB 200. www.drugstore.com/tagamet-hb-200-reduces-stomach-acid-for-heartburn-control/qxp473528?catid=184249. Accessed October 18, 2014.
6. Original Strength Pepcid AC. McNeil Consumer Pharmaceuticals. www.pepcid.com/products/original-strength-pepcid-ac. Accessed October 18, 2014.
7. Maximum Strength Pepcid AC. McNeil Consumer Pharmaceuticals. www.pepcid.com/products/maximum-strength-pepcid-ac. Accessed October 18, 2014.
8. Zantac 75. Boehringer Ingelheim Pharmaceuticals. www.zantacotc.com/zantac-regular-strength.html#learn-more. Accessed October 18, 2014.
9. Maximum Strength Zantac 150. Boehringer Ingelheim Pharmaceuticals. www.zantacotc.com/zantac-maximum-strength.html. Accessed October 18, 2014.
10. Prilosec OTC clear labeling. Procter & Gamble. www.prilosecotc.com/hcp/ClearLabeling. Accessed October 18, 2014.
11. Prevacid 24HR drug facts and patient package insert. Novartis Consumer Health. www.prevacid24hr.com/hcp/patient-package-insert.jsp. Accessed October 18, 2014.
12. About Nexium 24HR. Pfizer. www.nexium24hr.com/us/about. Accessed October 18, 2014.
13. Zegerid OTC product labeling. MSD Consumer Care. www.zegeridotc.com/download/zegeridotc_product_labeling.pdf. Accessed October 18, 2014.