Medication Summary
A variety of pharmacologic agents are available for suppressing gastric acid secretion. These include H2RAs such as famotidine, nizatidine, and cimetidine; proton pump inhibitors (PPIs) such as omeprazole; prokinetic agents such as cisapride and tegaserod; and mucosal cytoprotectants such as sucralfate. Evidence that supports the efficacy of the H2RAs is questionable. PPIs are significantly more potent and reliably achieve a greater magnitude of gastric acid inhibition. In addition, compared with esophageal symptoms, significantly greater acid inhibition is required to relieve supraesophageal symptoms and, especially, to achieve mucosal healing. Hence, the choice of PPIs over H2RAs is clear as a first-line pharmacologic intervention.
Omeprazole has been studied most extensively and is the only agent used in the clinical trials evaluating efficacy of PPIs in supraesophageal disorders. However, experience with lansoprazole is increasing, and newer agents (rabeprazole, pantoprazole [24] ) promising sustained and more potent gastric acid suppression with once daily dosing have recently arrived.
Prokinetic agents accelerate esophageal clearance and increase lower esophageal sphincter (LES) tone. The prokinetic agent cisapride has been discontinued because of serious adverse effects or ventricular arrhythmia. Tegaserod decreases reflux and LES relaxation events and is useful for treating laryngopharyngeal reflux (LPR) associated with esophageal dyskinesia.
Tegaserod was temporarily withdrawn from the US market in March 2007. The marketing of tegaserod was suspended because of a meta-analysis of safety data pooled from 29 clinical trials that involved more than 18,000 patients. The results showed an excess number of serious cardiovascular adverse events, including angina, myocardial infarction, and stroke, in those taking tegaserod compared with placebo.
However, since July 27, 2007, restricted use of tegaserod has been permitted via a treatment investigational new drug (IND) protocol. The protocol allows the use of tegaserod therapy for irritable bowel syndrome with constipation (IBS-C) or chronic idiopathic constipation (CIC), in women younger than 55 years who meet specific guidelines. Its use is further restricted to those in critical need who have no known or preexisting heart disease.
Sucralfate is a polysulfated salt of sucrose that may be helpful as an adjunct in protecting injured mucosa from the harmful effects of acid and pepsin.
Proton pump inhibitors
Class Summary
Inhibit gastric acid secretion by inhibition of the H+/K+ -ATPase enzyme system in the gastric parietal cells.
Omeprazole (Prilosec)
Specifically suppress gastric acid secretion by potent inhibition of the H+/K+ -ATPase enzyme system at secretory surface of gastric parietal cell. This blocks the final step in gastric acid production. Effect is dose related and inhibits both basal and meal-stimulated acid secretion. Omeprazole has been studied most extensively and is the only agent used in the clinical trials evaluating efficacy in supraesophageal disorders.
Lansoprazole (Prevacid)
Suppresses gastric acid secretion by specific inhibition of the H+/K+ -ATPase enzyme system (ie, proton pump) at the secretory surface of the gastric parietal cell. It blocks the final step of acid production. The effect is dose related and inhibits both basal and stimulated gastric acid secretion, thus increasing gastric pH levels.
Pantoprazole (Pantoloc, Protonix)
Suppresses gastric acid secretion by specifically inhibiting H+/K+ -ATPase enzyme system at the secretory surface of gastric parietal cells. Use of the IV preparation has only been studied for short-term use (ie, 7-10 d).
Histamine H2 Antagonists
Class Summary
H2 receptor antagonists are reversible competitive blockers of histamine (H2) receptors, particularly those in the gastric parietal cells, where they inhibit acid secretion.
Ranitidine (Zantac, Zantac 150 Maximum Strength, Zantac 75)
Ranitidine hydrochloride competitively inhibits histamine at the H2 receptor of gastric parietal cells, resulting in reduced gastric acid secretion, gastric volume, and hydrogen ion concentrations. On April 1, 2020, the US Food and Drug Administration (FDA) requested that all ranitidine prescription and over-the-counter products be withdrawn from the market owing to concerns over the contaminant N-Nitrosodimethylamine (NDMA). According to the FDA, in some ranitidine products, the level of the impurity rises over time and when stored at above room temperature, potentially reaching unacceptably high concentrations.
Cimetidine (Tagamet HB)
Cimetidine inhibits histamine at H2 receptors of gastric parietal cells, decreasing gastric acid secretion, gastric volume, and hydrogen ion concentrations.
Famotidine (Pepcid, Pepcid AC)
Famotidine competitively inhibits histamine at H2 receptors of gastric parietal cells, resulting in reduced gastric acid secretion, gastric volume, and hydrogen concentrations.
Prokinetic agents
Class Summary
These agents may stimulate peristaltic reflex.
Tegaserod hydrogen maleate (Zelnorm)
Available in US by restricted treatment IND for irritable bowel syndrome with constipation (IBS-C) or chronic idiopathic constipation (CIC) in women younger than 55 years who meet specific guidelines. Used for the short-term treatment of women with irritable bowel syndrome in whom constipation is the predominant symptom. Serotonin type 4 receptor partial agonist with no affinity for 5-HT3 receptors. May trigger peristaltic reflex via 5-HT4 activation, which enhances basal motor activity and normalizes impaired GI motility. Research studies have shown inhibitory activity of the drug on visceral activity in the GI tract.
Gastrointestinal agents
Class Summary
These agents may protect the GI lining against peptic acids.
Sucralfate (Carafate)
Binds to positively charged proteins in exudates and forms a viscous, adhesive substance that protects GI lining against pepsin, peptic acid, and bile salts. Used for short-term ulcer management.
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The RSI documents the presence and degree of nine laryngopharyngeal reflux (LPR) symptoms both before and after treatment; maximum score: 45.
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The reflux finding score (RFS) documents the presence and degree of eight laryngopharyngeal reflux (LPR) findings during fiberoptic laryngoscopy; maximum score: 26.
Tables
Author |
n |
Pharmacologic Intervention |
Treatment Duration wk |
Symptom Improvement |
Laryngoscopic Improvement |
Follow-up wk |
Repeat Treatment |
|
Laryngeal |
Esophageal |
|||||||
Koufman |
33 |
Ranitidine 300-600 mg/d or Famotidine 80 mg/d |
24 |
85% |
… |
85% |
44 |
50% |
Kamel |
16 |
Omeprazole 40 mg/d |
6-24 |
79% |
96% |
56% |
6 |
Majority |
Hanson |
182 |
Step-wise treatment Famotidine 20 mg/d, Omeprazole 20-40 mg/d |
6-12 |
96% |
… |
96% |
>6-12 |
79% |
Shaw |
68 |
Omeprazole 20 mg bid |
12 |
Significantly improved |
40% |
Significantly improved |
None |
… |
Wo |
21 |
Omeprazole 40 mg/d |
8 |
40% |
48% |
50% |
8 |
38% |
Metz |
10 |
Omeprazole 20 mg bid |
4 |
60% |
100% |
… |
… |
… |
Hanson |
16 |
Omeprazole 20 mg/d |
6-9 |
Significantly improved acoustic parameters |
… |
… |
… |
… |
