Ms. Wick is a senior clinical research pharmacist at the National Cancer Institute, National Institutes of Health, Bethesda, Maryland. The views expressed are those of the author and not those of any government agency.
Pharmacists are likely to see many heartburn patients. In Western populations, and the United States in particular, up to 40% of individuals experience heartburn's mid-chest discomfort, moving up to the throat and neck, or substernal burning,1 with approximately 5% experiencing frequent symptoms.2 Heartburn can be relatively benign or become a frequent problem (occurring .2 days per week) that can have great impact on the patient's quality of life. Myths and presuppositions about heartburn relief are abundant and persistent because, in the past, research validating what to recommend as the most appropriate and durable relief in OTC settings has been nonexistent.3
Most patients know what causes their heartburn. Citrus juices, bread, coffee, cucumber, and rich and spicy meals are common triggers. Overindulgence in food and alcohol (especially right before bed), smoking, excess weight, and stress are other common causes. When garden-variety heartburn is the problem, the goal is to relieve symptoms and restore quality of life; reduce risk of more serious disease states; and introduce short- and long-term acid suppression using an OTC acid-suppressing agent.4,5 Creating a gastric pH >4 using 1 of 3 classes of OTC drugs—antacids and alginates, histamine H2-receptor antagonists (H2RAs), or proton pump inhibitors (PPIs)—can be an effective strategy.6,7
Antacids and Alginates
Many patients with heartburn self-medicate with OTC antacids and alginates, scheduling a visit with a physician only if symptoms escalate or persist. Initially, they may appreciate antacids' rapid but relatively short-term symptom relief. Viscous alginates, generally provided in combination with an antacid, create a protective barrier on top of gastric contents, preventing acid contact with the esophagus.
Although OTC antacids and alginates may be useful in mild heartburn,8 one small study showed that only around 25% of patients report OTC antacids provide acceptable symptom relief.9 The few controlled studies available to date indicate that OTC antacids' and alginates' strong point is prevention and treatment of postprandial symptomatic relief. This defines their niche as appropriate for occasional meal-induced episodes or for breakthrough symptoms in patients using longer-acting treatments like H2RAs or PPIs.
Histamine H2-Receptor Antagonists
H2RAs competitively and reversibly block parietal cell H2-receptors, thus inhibiting acid secretion.10 They can be used to self-medicate during a heartburn episode, or for prophylaxis before consumption of food or drink known to trigger reflux symptoms. Although H2RAs have a slower onset of action than the antacids, they generally suppress gastric acid for up to 12 hours.3 Usually given twice daily, H2RAs suppress approximately 70% of acid over 24 hours.11 Pharmacologic tolerance can develop with as few as 3 days of daily use,6 and with chronic use, the antisecretory effect may diminish, leading to less than satisfactory control.12-16
Proton Pump Inhibitors
PPIs directly and irreversibly block the final common pathway for acid secretion in the stomach, the gastric acid pump (H+,K+-ATPase), making them the drugs of choice for gastric acid suppression.7 PPIs' once-daily dosing improves patients' ability to adhere to treatment, especially when compared with frequent antacid dosing.17 A recent study (Miner et al) has quantified the acid suppression of omeprazole, a PPI, versus famotidine, an H2RA, in an OTC setting.6 The results establish that, contrary to popular belief, omeprazole's ability to suppress acid on day 1 of a 14-day course of treatment is comparable to famotidine's, and better in days following. Although this study did not measure the onset of action or symptom relief, PPIs' and H2RAs' clinical effectiveness is directly related to gastric acid suppression above a pH of 4.
Most patients who experience heartburn want day 1, if not immediate, relief. In fact, even patients who have more serious reflux disease look for and often prefer on-demand relief.18 Although alginates or antacids will provide prompt relief, patients often want a more enduring relief and look to an OTC H2RA or PPI. Using an OTC H2RA or PPI can bring a period of heartburn under control; this may decrease the toal amount of medication taken and the cost.18 Researchers have believed that H2RAs surpass PPIs in terms of acid suppression in the first 24 hours, based on findings using prescription-strength drugs. An OTC PPI can suppress acid significantly on day 1, however, compared with baseline and comparably to a regular (10 mg) and maximum strength (20 mg) OTC H2RA. Acid suppression in study participants taking the lower-dose H2RA decreased significantly beginning day 3 (Figure).6
Until recently, clinicians generally recommended H2RAs rather than PPIs for ondemand therapy because they surmised that they would produce faster acid suppression on day 1 of treatment.19 Existing guidelines for the treatment of heartburn in primary care consider cost-effectiveness of therapy and can guide pharmacists toward providing the best care.
The American College of Gastroenterology's evidence-based guidelines recommend patient-directed lifestyle changes and OTC antacids or acid suppressants for patients presenting mild heartburn symptoms.20 The general approach— one that is sometimes mandated by insurers—is to start with an antacid for occasional or brief heartburn episodes, using H2RA for more frequent or persistent symptoms, and reserving the PPI (due to its perceived slower onset of anti-secretory activity) for patients with more frequent heartburn or patients who have failed other OTC therapy, in a step-up approach.4,19,20
A study of 593 people reporting heartburn compared step-up therapy and step-down therapy (use of a PPI followed by an H2RA) with lansoprazole alone from the start. Researchers concluded that treatment with a PPI provides more consistent heartburn relief than an H2RA, or step-up or step-down therapy.21 A recent survey of approximately 1000 primary care physicians (PCPs) found that the step-up approach has been largely abandoned; instead, PCPs tend to use a step-in approach. In the step-in approach, PCPs start therapy with a PPI.22
The Reflux Mnemonic ALARMS:
Further study is needed to verify whether reserving the PPI until H2RA failure is necessary; OTC PPIs appear to suppress acid comparably to OTC H2RAs in the first 24 hours, providing a more consistent sustained effect without developing tolerance. Experts indicate that the recent decrease in cost, established safety, and wide availability of PPIs make them preferable for monotherapy for the empiric treatment of typical heartburn symptoms.4
Pharmacists should ask open-ended questions about concurrent medications and supplements, such as NSAIDs, aspirin, glucosamine, and others, that may list heartburn among their side effects. Sometimes pointed questions about lifestyle can help patients select appropriate lifestyle modifications. Pharmacists should remember that for gastrointestinal reflux, certain symptoms should raise an alarm (Box). If patients report any symptom indicative of one of these, referral to a physician is warranted.
Refer patients to their doctor if they:
In the last several years, OTC treatment options for heartburn have expanded. These options vary in cost, dosing convenience, and ability to suppress acid. Pharmacists can recommend OTC products for heartburn with confidence that patients can be satisfied with the relief that follows. Patients with periodic heartburn may find antacids and alginates convenient, inexpensive, and effective. H2RAs will continue to have a role for patients who need a brief intervention that lasts longer than that offered by antacids. Consumers with frequent heartburn (≥2 days per week) may develop tolerance to an H2RA rapidly with daily use; an OTC PPI may provide more durable protection.