Last week at http://www.canmedglobal.com/blog/?p=38, we discussed Gastro-esophageal Reflux Disease (GERD), commonly called reflux. We looked at the anatomy and physiology of the disease, the symptoms and diagnosis and we provided you with some tips for getting rid of heartburn symptoms. Briefly we described the medication used to treat Gastro-esophageal Reflux Disease (GERD). This week we will review all the available treatments for reflux. We hope this will help you in your decision process to choose the medication appropriate for you.
We have separated the medications by class of drugs and explained the pro and con of each.
Antacids (Tums, Rolaids, Gaviscon, Maalox, Pepto-Bismol)
If you suffer infrequently and your reflux symptoms are mild, antacids are an alternative for you. Antacids neutralize the acid in the stomach so the reflux content will be less acidic. The problem with antacids is that their action lasts about an hour, which allows time for acid to re-accumulate. Your CanMedGlobal pharmacist suggests taking antacids approximately one hour after each meal or just before the symptoms of acid reflux begin. Since the food from meals slows the emptying from the stomach, an antacid taken after a meal stays in the stomach longer and is effective longer. You can benefit from a second dose, two hours after a meal.
Antacids may be aluminum, magnesium, or calcium-based.
The calcium-containing antacids, such as Tums and Rolaids, stimulate the release of gastrin from the stomach and duodenum. Gastrin is the hormone that is primarily responsible for the stimulation of acid secretion by the stomach. Therefore, theoretically, the release of gastrin can result in an overproduction of acid and produce what is called the rebound effect. Acid rebound, however, has not been shown to be clinically important and is only theoretically harmful. We know Tums and Rolaids are effective for mild to moderate heartburn and are really cheap.
Aluminum-containing antacids like Gaviscon or Maalox have a tendency to cause constipation, while magnesium-containing antacids (Milk of Magnesia) tend to cause diarrhea. If diarrhea or constipation becomes a problem, it may be necessary to switch antacids or alternately use antacids containing aluminum and magnesium. Another option is Pepto-Bismol.
You can buy these without a prescription in grocery stores and drugstores. Antacids probably won’t help people with bad symptoms.
Histamine antagonists (Zantac, Axid, Tagamet, Pepcid)
If your symptoms are more severe or persistent during the day you need a more potent acid reflux neutralizer. You should start thinking about Histamine antagonists like Zantac (Ranitidine), Axid (Nizatidine), Tagamet (Cimetidine) or Pepcid (Famotidine).
The first medication developed for more effective and convenient treatment of GERD (gastro-esophageal reflux disease) was a histamine antagonist, specifically Tagamet (Cimetidine). Histamine is a critical component implicated in the cascade of acid production in the stomach. Histamine attaches to receptors (binders) on the stomach’s acid-producing cells and stimulates the cells to produce acid. Histamine antagonists work by blocking the receptor for histamine and thereby preventing histamine from stimulating the acid-producing cells.
Your CanMedGlobal pharmacist always recommends using H2 antagonists 30 minutes before meals. The reason is simple: H2 antagonists will perform at their maximum efficacy after the meal, when the stomach is actively producing acid. Also, some people who suffer from heartburn have symptoms during the night. If you are one of them you should think about taking a last H2 antagonist capsule just before bedtime to suppress night-time acid production.
People who suffer from heartburn may experience only mild symptoms but if these symptoms are not treated the acid will produce what we call oesophagus erosion.
At first, it will only cause inflammation, but if the acid continues to attack the oesophagus, the inflammation may lead to swelling of the tissues lining in the esophageal tube. This swelling can cause narrowing of the passageway, making it difficult to swallow food and even saliva. The erosion of the esophagus can occur at any point along the tube.
At the last stage, people can suffer from ulcers and bleeding in the esophageal tube.
H2 antagonists are very good for relieving the symptoms of GERD, particularly heartburn. However, they are not very good for healing the inflammation (esophagitis) that may accompany GERD. In fact, they are used primarily for the treatment of heartburn in GERD that is not associated with inflammation or complications, such as oesophagus erosions or ulcers, strictures, or Barrett’s esophagus.
Four different H2 antagonists are available including Cimetidine (Tagamet), Ranitidine (Zantac), Nizatidine (Axid), and Famotidine, (Pepcid). All four are also available over-the-counter (OTC), without the need for a prescription. However, the OTC dosages are lower than those available by prescription.
Proton pump inhibitors (PPIs)(Prilosec, Nexium, Aciphex, Prevacid, Protonix)
Proton pump inhibitors (PPIs) decrease the amount of acid produced in the stomach by blocking acid production. PPIs block the proton pumps in the stomach, which are responsible for acid secretion. This has the effect of reducing the concentration of hydrochloric acid in the stomach, resulting in the healing of the eroded portions of the esophagus or the ulcers in the intestines or the stomach. Proton pump inhibitors are the most potent drugs in the treatment of all types of disease related to Gastro-esophageal Reflux Disease (GERD).
Following is a quick explanation, so you understand why PPIs are so effective compared to the Histamine antagonist drugs. If you look at the picture below you will see that the cells in your stomach have three receptors; one for acetylcholine, one for gastrin and one for histamine. When these receptors are activated they will propel acid into the stomach. When using Histamine antagonists you are just blocking one of the three possible sources of acid production. In comparison, Proton pump inhibitors block the final step of acid production by blocking the pump itself.
Based on this explanation, Proton pump inhibitors (PPIs) are potent, long-acting medication. They are so powerful that most people don’t need more than one pill a day. The best time to take your medication is 30 minutes before breakfast.
Your physician will usually recommend one of 5 different medications, depending on the exact nature of your disease : Prilosec (Omeprazole), Prevacid (Lansoprazole), Nexium (Esomeprazole), Aciphex(Rabeprazole), Protonix (Pantoprazole)
Pro-motility drugs
Pro-motility drugs work by stimulating the muscles of the gastrointestinal tract. Metoclopramide (Reglan),a pro-motility drug, is approved for GERD. By increasing the pressure in the lower esophageal sphincter and strengthen the contractions (peristalsis) of the esophagus the reflux is reduced. However, these effects on the sphincter and esophagus are small. Therefore, it is believed that the primary effect of metoclopramide may be to speed up emptying of the stomach, which would also be expected to reduce reflux.
Pro-motility drugs are most effective when taken 30 minutes before meals and again at bedtime. They are not very effective for treating either the symptoms or complications of GERD. Therefore, the pro-motility agents are reserved either for patients who do not respond to other treatments or are added to enhance other treatments for GERD. These are essentially the last resort.
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