Gastro-esophageal Reflux Disease (GERD)
Also known as: Gastroesophageal Reflux Disease / Gastro-esophageal Reflux Disease / GERD / GERD Gastroesophageal Reflux Disease / Gastro-Oesophageal Reflux Disease / Gastrooesophageal reflux disease / GERD (Gastroesophageal Reflux Disease) / Esophageal Reflux / GERD - Gastro-Esophageal Reflux Disease / Gastroesophageal Reflux Disease (GERD) / Gastro-esophageal Reflux Diseases / Oesophageal reflux / Esophagitis / Gastrooesophageal reflux / Gastroesophageal reflux / Esophageal reflux NOS
| Drug | Drug Name | Drug Description |
|---|---|---|
| DB00501 | Cimetidine | A histamine congener, it competitively inhibits histamine binding to histamine H2 receptors. Cimetidine has a range of pharmacological actions. It inhibits gastric acid secretion, as well as pepsin and gastrins output. It also blocks the activity of cytochrome P-450 which might explain proposals for use in neoadjuvant therapy. |
| DB00736 | Esomeprazole | Esomeprazole, sold under the brand name Nexium, is a proton pump inhibitor (PPI) medication used for the management of gastroesophageal reflux disease (GERD), for gastric protection to prevent recurrence of stomach ulcers or gastric damage from chronic use of NSAIDs, and for the treatment of pathological hypersecretory conditions including Zollinger-Ellison (ZE) Syndrome. It can also be found in quadruple regimens for the treatment of _H. pylori_ infections along with other antibiotics including [DB01060], [DB01211], and [DB00916], for example [A177271, F4498]. Its efficacy is considered similar to other medications within the PPI class including [DB00338], [DB00213], [DB00448], [DB05351], and [DB01129]. Esomeprazole is the s-isomer of [DB00338], which is a racemate of the S- and R-enantiomer. Esomeprazole has been shown to inhibit acid secretion to a similar extent as [DB00338], without any significant differences between the two compounds _in vitro_. Esomeprazole exerts its stomach acid-suppressing effects by preventing the final step in gastric acid production by covalently binding to sulfhydryl groups of cysteines found on the (H+, K+)-ATPase enzyme at the secretory surface of gastric parietal cell. This effect leads to inhibition of both basal and stimulated gastric acid secretion, irrespective of the stimulus. As the binding of esomeprazole to the (H+, K+)-ATPase enzyme is irreversible and new enzyme needs to be expressed in order to resume acid secretion, esomeprazole's duration of antisecretory effect persists longer than 24 hours [FDA Label]. PPIs such as esomeprazole have also been shown to inhibit the activity of dimethylarginine dimethylaminohydrolase (DDAH), an enzyme necessary for cardiovascular health. DDAH inhibition causes a consequent accumulation of the nitric oxide synthase inhibitor asymmetric dimethylarginie (ADMA), which is thought to cause the association of PPIs with increased risk of cardiovascular events in patients with unstable coronary syndromes [A177577, A177580]. Due to their good safety profile and as several PPIs are available over the counter without a prescription, their current use in North America is widespread. Long term use of PPIs such as esomeprazole have been associated with possible adverse effects, however, including increased susceptibility to bacterial infections (including gastrointestinal _C. difficile_), reduced absorption of micronutrients including iron and B12, and an increased risk of developing hypomagnesemia and hypocalcemia which may contribute to osteoporosis and bone fractures later in life [A177571]. Rapid discontinuation of PPIs such as esomeprazole may cause a rebound effect and a short term increase in hypersecretion [A177574]. Esomeprazole doses should be slowly lowered, or tapered, before discontinuing to prevent this rebound effect. |
| DB00927 | Famotidine | A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion. |
| DB00448 | Lansoprazole | Lansoprazole marketed under the brand Prevacid, is a proton pump inhibitor (PPI) and is structurally classified as a substituted benzimidazole.[A177065] It reduces gastric acid secretion by targeting gastric H,K-ATPase pumps and is thus effective at promoting healing in ulcerative diseases, and treating gastroesophageal reflux disease (GERD) along with other pathologies caused by excessive acid secretion.[A177053] |
| DB00585 | Nizatidine | A histamine H2 receptor antagonist with low toxicity that inhibits gastric acid secretion. The drug is used for the treatment of duodenal ulcers. |
| DB00338 | Omeprazole | Originally approved by the FDA in 1989, omeprazole is a _proton-pump inhibitor_, used to treat gastric acid-related disorders. These disorders may include gastroesophageal reflux disease (GERD), peptic ulcer disease, and other diseases characterized by the oversecretion of gastric acid. This drug was the first clinical useful drug in its class, and its approval was followed by the formulation of many other proton pump inhibitor drugs [A174232]. Omeprazole is generally effective and well-tolerated, promoting its popular use in children and adults [FDA label]. |
| DB00213 | Pantoprazole | Pantoprazole is a first-generation proton pump inhibitor (PPI) used for the management of gastroesophageal reflux disease (GERD), for gastric protection to prevent recurrence of stomach ulcers or gastric damage from chronic use of NSAIDs, and for the treatment of pathological hypersecretory conditions including Zollinger-Ellison (ZE) Syndrome. It can also be found in quadruple regimens for the treatment of _H. pylori_ infections along with other antibiotics including [DB01060], [DB01211], and [DB00916], for example [A177271][F4498]. Its efficacy is considered similar to other medications within the PPI class including [DB00338], [DB00736], [DB00448], [DB05351], and [DB01129]. Pantoprazole exerts its stomach acid-suppressing effects by preventing the final step in gastric acid production by covalently binding to sulfhydryl groups of cysteines found on the (H+, K+)-ATPase enzyme at the secretory surface of gastric parietal cell. This effect leads to inhibition of both basal and stimulated gastric acid secretion, irrespective of the stimulus. As the binding of pantoprazole to the (H+, K+)-ATPase enzyme is irreversible and new enzyme needs to be expressed in order to resume acid secretion, pantoprazole's duration of antisecretory effect persists longer than 24 hours [FDA Label]. Due to their good safety profile and as several PPIs are available over the counter without a prescription, their current use in North America is widespread. Long term use of PPIs such as pantoprazole have been associated with possible adverse effects, however, including increased susceptibility to bacterial infections (including gastrointestinal _C. difficile_), reduced absorption of micronutrients including iron and B12, and an increased risk of developing hypomagnesemia and hypocalcemia which may contribute to osteoporosis and bone fractures later in life [A177571]. PPIs such as pantoprazole have also been shown to inhibit the activity of dimethylarginine dimethylaminohydrolase (DDAH), an enzyme necessary for cardiovascular health. DDAH inhibition causes a consequent accumulation of the nitric oxide synthase inhibitor asymmetric dimethylarginie (ADMA), which is thought to cause the association of PPIs with increased risk of cardiovascular events in patients with unstable coronary syndromes [A177577, A177580]. Pantoprazole doses should be slowly lowered, or tapered, before discontinuing as rapid discontinuation of PPIs such as pantoprazole may cause a rebound effect and a short term increase in hypersecretion [A177574]. |
| DB01129 | Rabeprazole | Rabeprazole is an antiulcer drug in the class of proton pump inhibitors. It is a prodrug - in the acid environment of the parietal cells it turns into active sulphenamide form. Rabeprazole inhibits the H+, K+ATPase of the coating gastric cells and dose-dependent oppresses basal and stimulated gastric acid secretion. |
| DB00863 | Ranitidine | Ranitidine is a commonly used drug, classified as a _histamine H2-receptor antagonist_. This drug helps to prevent and treat gastric-acid related conditions, including ulcers, because of its ability to decrease gastric acid secretion [A176759], [FDA label]. It is often referred to as _Zantac_, and is available in various forms, including a regular tablet, injection, and effervescent tablet [FDA label], [F4253]. One common use of this drug is to relieve the symptoms of gastric esophageal reflux disease (GERD) [FDA label], which often leads to heartburn symptoms and acid regurgitation. The prevalence of GERD is thought to be 10-20% in western countries [A176843]. Ranitidine has proven to be an effective agent in relieving the above symptoms and is therefore widely used in GERD and other gastric-acid related conditions [A176849], [FDA label]. |
| DB00364 | Sucralfate | Sucralfate is a medication that is widely used to prevent and treat a number of diseases in the gastrointestinal tract such as duodenal ulcers [FDA label], gastro-esophageal reflux disease (GERD), gastritis, peptic ulcer disease, stress ulcer, in addition to dyspepsia [A177655]. It is considered a _cytoprotective agent_, protecting cells in the gastrointestinal tract from damage caused by agents such as gastric acid, bile salts, alcohol, and acetylsalicylic acid (aspirin), among other substances [A177655, F4519]. Sucralfate has been shown to be a well-tolerated and safe drug. It is sold under many brands and is available in both tablet and suspension forms. It was approved by the FDA 1982 in tablet form, and in 1994 for the suspension form [L6073, L6076]. |