GERD and Heartburn Medications

• Gastroesophageal reflux disease (GERD) is a condition that causes the esophagus to become irritated and inflamed because acid (gastric juices) from the stomach and also duodenal juices (for example, bile, pancreatic secretions) leak back or reflux into the esophagus.
• Heartburn is an uncomfortable but common feeling of burning or warmth in the chest. Although the burning associated with heartburn is felt in the chest, it has nothing to do with the heart. Instead, heartburn is a typical symptom due to GERD.

The food a person swallows travels from the mouth to the stomach through a hollow tube called the esophagus (the food pipe). Before entering the stomach, food must pass through a tight muscle at the lower part of the esophagus called the lower esophageal sphincter (LES). The LES is a defense mechanism that prevents food from traveling backward into the esophagus.

In the stomach, stomach acid assists in continuing the digestion of food. This acid is very strong and can damage most parts of the body. The stomach is protected from its own acid by a special mucous layer. The esophagus, however, does not have any such special protection. If the LES does not close properly, the lower part of the esophagus can be damaged by stomach acid and GERD can occur. When this happens, a person may experience heartburn.

Conditions such as hiatal hernia, pregnancy, obesity, or diabetes may predispose individuals to reflux disease. Also certain medications (beta agonists, calcium channel blockers, nitrates, anticholinergics) and foods (fatty meals, alcohol, coffee etc.) can cause transient relaxation of the LES muscle, which renders the LES inadequate to prevent reflux into the esophagus. As a result GERD develops.

Infants, particularly premature infants, commonly experience reflux disease, and adults over the age of 40 have a higher prevalence of GERD.

Heartburn is the most common symptom of gastroesophageal reflux disease (GERD). Voice changes may occur, particularly upon wakening. Hoarseness is typical and results from stomach acid refluxing all the way up in the esophagus to the throat where it irritates the vocal cords.

The following GERD-associated complications are serious and require immediate medical attention:

• Esophageal stricture: This is a narrowing of the esophagus that makes it hard to swallow foods or liquids.
• Erosive esophagitis: This results in ulcer formation in your esophagus.
• Vomiting blood or blood in the stools: When there is blood in the stools, the stool may look dark or tarry.
• Barrett's esophagus and ulcers: These are caused by prolonged exposure of the esophagus to stomach acid. Barrett's esophagus sometimes precedes cancer of the esophagus, so the doctor will want to assess the state of the patient's Barrett's esophagus from time to time.
• Esophageal cancer (adenocarcinoma): This has become more common in the past 20 years and is linked with GERD and Barrett's esophagus.

The medical treatment options are used to prevent complications and reduce morbidity associated with GERD, and they include antacids, H2 receptor antagonists, proton pump inhibitors, coating, and promotility agents. In addition to medications, the following lifestyle modifications below are recommended:

• Instead of eating large meals, eat small meals more frequently.
• Avoid caffeine-containing foods and beverages (for example, coffee, tea, soft drinks, chocolate).
• Avoid foods that decrease lower esophageal sphincter (LES) pressure (for example, peppermint, fatty or fried foods, alcohol).
• Avoid acidic foods that may irritate the esophagus (for example, spicy foods, citrus fruits and juices, tomatoes, tomato sauce).
• If overweight, lose weight. People with excess weight have an increased incidence of reflux disease.
• Quit smoking. Smoking weakens the LES and increases reflux.
• Do not eat immediately before bedtime.
• Avoid lying down immediately following a meal (ideally, a person should wait at least three hours). Elevate the head end of the bed by four to six inches if nighttime heartburn is experienced.

Antacids are efficacious in controlling mild symptoms of GERD. Antacids should be taken after each meal and at bedtime. Antacids are readily available over-the counter (without a prescription) and also come in various generic forms. Antacids typically contain aluminum in various forms (for example, aluminum hydroxide, aluminum phosphate, aluminum carbonate), calcium carbonate, magnesium hydroxide, sodium bicarbonate, or a combination of these ingredients. Several familiar examples include Gaviscon, Maalox, Mylanta, Tums, Rolaids, AlternaGEL, Amphojel, Philips Milk of Mangesia etc. Some may contain a foaming agent to help block the stomach acid from backing up into the esophagus (Gaviscon).

• How antacids work: Antacids neutralize stomach acid, thereby decreasing the acid's ability to cause irritation and inflammation of the esophagus.
• Who should not use these medications: Individuals who have experienced an allergic reaction to any component of an antacid should avoid use of antacids containing the offending component.
• Use: Antacids are available as liquids or chewable tablets. Dosages vary, so follow package directions. If symptoms are not relieved after regular use over several weeks, contact a doctor.
• Drug interactions: The absorption of many drugs (including vitamins and iron) may be affected by antacids, which change the acidity of stomach contents. If a person is taking other medications, ask a doctor or pharmacist for information on interactions with antacids.
• Food interactions: High-protein meals may decrease the effect of aluminum-containing antacids. Prolonged antacid use and excessive consumption of calcium may cause high calcium levels (hypercalcemia) and result in serious metabolic disease.
• Side effects: After regular use for several weeks, antacids may cause diarrhea (magnesium-containing antacids) or constipation (aluminum-containing antacids). They may impair calcium metabolism and may cause magnesium to accumulate, which may damage the kidneys.

Histamine-2 (H2) receptor antagonists/blockers are considered the first-line agents for patients who have mild to moderate symptoms of GERD. Cimetidine (Tagamet), famotidine (Pepcid), nizatidine (Axid), and ranitidine (Zantac) are examples of H2 blockers. Several of these drugs are available over-the counter and can be purchased without a prescription in low doses to treat mild, occasional heartburn. Higher doses require a doctor's prescription.

• How H2 blockers work: These drugs decrease the amount of acid produced by the stomach.
• Who should not use these medications: Individuals who have experienced an allergic reaction to H2 blockers should not take them.
• Use: Various dosage regimens are used. If using an over-the-counter nonprescription product, carefully follow the directions for use on the package. For prescription-strength products, the doctor will instruct the patient on how to take the medication. H2 blockers are available in tablet, capsule, and oral liquid forms.
• Drug or food interactions: Many drugs interact with H2 blockers (particularly with cimetidine). If taking other medications, ask a doctor or pharmacist for information on interactions with H2 blockers. These drugs decrease the body's ability to excrete caffeine. Individuals who consume large quantities of caffeine may experience tremors, insomnia, or heart palpitations. Cimetidine may increase the likelihood of alcohol intoxication.
• Side effects: Confusion, depression, and hallucinations have been reported, particularly in elderly individuals or those who are unable to adequately excrete the drugs (for example, people with kidney disease). High doses taken over a long period of time have caused breast enlargement and sexual dysfunction in men. Rarely, H2 blockers cause liver toxicity or decreased platelet counts. (Platelets are blood cells that form clots and decrease bleeding.) If you take these drugs regularly, a doctor will monitor the patient's blood for adverse effects.

Proton Pump Inhibitors (PPIS) are considered to be the most potent medical options available to treat GERD. These classes of drugs have relatively fewer side effects and have been used for longer periods of time. However, recent studies have shown the potential for the development of cardiac issues and osteoporosis.

Esomeprazole (Nexium), lansoprazole (Prevacid), omeprazole (Prilosec), pantoprazole (Protonix), and rabeprazole (Aciphex) are examples of proton pump inhibitors. Esomeprazole is a newer, improved form of omeprazole and has been found to provide sustained relief of heartburn pain more quickly than omeprazole (in five days with esomeprazole taken at 40 mg/day versus seven to nine days with omeprazole at 20 mg/day).

• How proton pump inhibitors work: These drugs are more potent than H2 blockers in blocking acid secretion from the stomach.
• Who should not use these medications: Individuals who have experienced an allergic reaction to these drugs should not take them.
• Use: Proton pump inhibitors are taken orally as a once-daily dose. Pharmacists may make liquid forms of omeprazole and lansoprazole for children. Contents of esomeprazole capsules may be sprinkled on a tablespoon of applesauce immediately before administration for people who cannot swallow capsules.
• Drug or food interactions: These drugs may increase blood levels of diazepam (Valium), warfarin (Coumadin), phenytoin (Dilantin), and digoxin (Lanoxin), and may interfere with the absorption of iron products like ketoconazole (Nizoral) and itraconazole (Sporanox), thereby decreasing their effectiveness. However, data have shown that PPIs can interfere with calcium homeostasis and may aggravate cardiac issues. They are also linked to hip fracture in postmenopausal women. Specifically with omeprazole, high doses and long-term use (one year or longer) may increase the risk of osteoporosis-related fractures of the hip, wrist, or spine. Therefore, it is important to use the lowest doses and shortest duration of treatment necessary for the condition being treated.
• Side effects: Common adverse effects include headache, diarrhea, gas, and stomach pain.

Sucralfate (Carafate) may be used initially to protect an irritated or inflamed esophagus.

• How coating drugs work: This drug binds to proteins from secretions in the stomach and esophagus, which forms a substance that protects the lining of the stomach and esophagus.
• Who should not use these medications: Individuals who have experienced an allergic reaction to this drug should not take it.
• Use: Sucralfate must be taken four times a day on an empty stomach, and at least one hour before meals.
• Drug or food interactions: Sucralfate may decrease effects of ketoconazole (Nizoral), ciprofloxacin (Cipro), levofloxacin (Levaquin), tetracycline (Sumycin), phenytoin (Dilantin), warfarin (Coumadin), quinidine (Quinaglute, Cardioquin, Quinidex), and theophylline (SLO-BID, Theo-24, Theo-Dur, Uniphyl).
• Side effects: Sucralfate should be used with caution in people with kidney failure because it contains aluminum, which may accumulate in the body. The drug often causes constipation.

Metoclopramide (Clopra, Maxolon, Reglan) may be used if reflux is a result of a condition that delays stomach emptying (for example, diabetes). Promotility drugs are mostly reserved only for patients with mild symptoms. Long-term use of promotility drugs may have serious, even potentially fatal, complications and should be discouraged.

• How promotility drugs work: Promotility drugs treat reflux by increasing lower esophageal sphincter (LES) tone and enhancing emptying of food from the stomach.
• Who should not use these medications: People with the following conditions should not use promotility drugs:
  • Allergy to metoclopramide
  • Gastrointestinal bleeding or obstruction
  • Pheochromocytoma or seizure disorders
• Use: Take these drugs 30 minutes before meals and at bedtime.
• Drug or food interactions: Promotility drugs should not be used with drugs that cause extrapyramidal symptoms, such as muscle stiffness, tremor, twitching, and uncontrolled movements of the face, tongue, eyes, neck or head. Examples of drugs that may cause extrapyramidal symptoms include bupropion (Wellbutrin, Zyban) and phenothiazines (chlorpromazine [Thorazine], fluphenazine [Prolixin], haloperidol [Haldol], olanzapine [Zyprexa], thioridazine [Mellaril]). Do not use promotility drugs within 14 days of taking monoamine oxidase inhibitors (MAOIs) (Marplan, Nardil, Parnate), tricyclic antidepressants (amitriptyline [Elavil, Endep]), or stimulants such as diet pills or decongestants (Sudafed).
• Side effects: Common effects include drowsiness, and constipation. Promotility drugs may cause irregular heartbeat. Contact a doctor immediately if a person experiences any of the previously described extrapyramidal symptoms.