Antireflux Medications to Manage Heartburn/Gastroesophageal reflux disease (GERD)
For many people with mild symptoms, lifestyle modifications are an effective therapy that either reduces or completely eliminates GERD. However, for a successful relief of more severe symptoms, behavior adjustments need to be combined with antireflux medications that reduce stomach (gastric) acidity. The most commonly used medications fall into three categories: proton pump inhibitors (PPIs), histamine-2 receptor antagonists (H2RAs) and antacids. PPIs and H2RAs inhibit the production of stomach acid, while antacids neutralize it.
Although all of these medications are available over the counter, it is best not to start the therapy on your own. Research has shown that optimal symptom relief is achieved when patients take medications under their doctors’ guidance.
Proton pump inhibitors (PPIs)
PPIs are the most effective therapy for GERD. With correct dosing, PPIs heal irritation of the esophagus in ~85 % of patients.
The following PPIs are available over the counter:
omeprazole (Prilosec OTC)
ompeprazole with sodium bicarbonate (Zegerid)
esomeprazole magnesium (Nexium 24)
For more severe GERD symptoms, these and other PPIs are available as prescription drugs. Comparative studies found that all PPIs are similarly effective in relieving GERD.
How to use. All PPIs are prodrugs – in order to exert the desired effect, they first have to be converted to an active form. PPIs are activated in the body by the stomach acid that gets secreted in response to food ingestion.
Because of their mechanism of action, PPIs are best administered 30 minutes before the first meal of the day.
Expected onset and duration of action. PPIs have a delayed onset of action (1-2 hours) but are effective for 48 hours after they have been administered. Maximum effect is typically seen after several days of daily PPI use.
Precautions. Stomach acid plays a vital role in protecting us from pathogenic bacteria that can be ingested with food or water. It also helps with digestion and absorption of micronutrients. Due to such important functions of the stomach acid, concerns have been raised about possible negative effects of a prolonged use of PPIs on infection susceptibility and micronutrient malabsorption.
Studies have shown that long-term use of PPIs increases the risk of infection by Clostridium difficile, a bacterium that can cause mild to life-threatening health problems. If you experience persistent diarrhea while taking PPIs, talk to your doctor about tests that diagnose C. difficile infection.
Long-term use of PPIs has been associated with decreased absorption of iron, vitamin B12, magnesium, and calcium. If you require long-term PPI therapy, make sure you check the levels of these micronutrients periodically. If deficiency is detected, discuss supplementation with your doctor.
Histamine2 antagonist receptor (H2RAs)
Less effective than PPIs, H2ARs are used for treating mild GERD and infrequent heartburn.
The following H2RAs are available over the counter:
famotidine (Pepcid AC)
In September 2019 popular drug ranitidine (Zantac) has been recalled due to the presence of a low amount of a known carcinogen, N-nitrosodimethylamine (NDMA).
H2RA medications are available by prescription as well.
How to use. H2RAs are fast-acting and most commonly used as the on-demand therapy - to control occasional heartburn or prevent symptoms associated with the consumption of heartburn trigger foods. H2RAs are not suitable as a long-term therapy because they rapidly (within 2 weeks of use) become less effective in reducing the production of stomach acid.
H2RAs can be combined with antacids for faster heartburn relief. However, they should not be combined with PPIs, as they lower their efficacy.
Expected onset and duration of action. H2RAs have a faster onset of action than PPIs (less than 1 hour) and their effect can last for about 10 hours.
Precautions. People with cardiac, kidney and liver dysfunction should consult their doctor prior to starting H2RA therapy.
Antacids are weak bases that directly neutralize stomach acid. Because of their mechanism of action, antacids provide rapid but temporary heartburn relief.
Numerous antacids are available over the counter:
These agents contain the salts and/or hydroxides of the following metals: sodium, calcium, aluminum and magnesium. Some antacids (Gaviscon) contain a foaming agent, alginic acid, that provides a physical barrier between the esophagus lining and stomach acid.
Your choice of antacids should depend on your overall health, the frequency of use and duration of therapy.
How to use. Antacids are used as on-demand therapy, to control symptoms of heartburn episodes that are already in progress. Antacids are sometimes combined with H2RAs and PPIs (Zegerid contains both omeprazole (PPI) and sodium bicarbonate (antacid)), to provide quick relief until the slower but more effective antireflux drug begins to act.
Expected onset and duration of action. Antacids are fast-acting, providing symptom relief approximately 5 minutes after administration. However, their effect lasts only 30-60 minutes.
Precautions. Magnesium-based antacids can cause diarrhea, while the calcium- and aluminum-based ones may result in constipation. People on a low sodium/salt diet should avoid sodium-based antacids.
Long-term, frequent use of calcium and magnesium antacids may lead to abnormally high levels of calcium and magnesium in the blood ( hypercalcemia and hypermagnesemia). Prolonged use of antacids that contain aluminum may lead to kidney problems and reduction in phosphate levels (phosphate has important cellular functions).
Generic vs. brand-name medications
PPIs and H2RAs are available both as generic and brand name products.
To be approved by the U.S. Food and Drug Administration (FDA) generic drugs must have the same quality, strength, purity, and stability as brand-name medications. Generic drugs, thus, must have the same effectiveness as brand-name medications but are substantially less expensive (manufacturers of generic drugs have no research and development or marketing costs). Choosing generic antireflux drugs can bring you more than 30% cost savings. However, some concerns have been raised about the ability of the FDA to provide strong oversight of the generic drugs largely manufactured oversees.
Last updated: October 4, 2019