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

DrugDrug NameDrug Description
DB00501CimetidineA 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.
DB00736EsomeprazoleEsomeprazole, 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.
DB00927FamotidineA competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
DB00448LansoprazoleLansoprazole 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]
DB00585NizatidineA histamine H2 receptor antagonist with low toxicity that inhibits gastric acid secretion. The drug is used for the treatment of duodenal ulcers.
DB00338OmeprazoleOriginally 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].
DB00213PantoprazolePantoprazole 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].
DB01129RabeprazoleRabeprazole 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.
DB00863RanitidineRanitidine 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].
DB00364SucralfateSucralfate 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].
DrugDrug NameTargetType
DB00501CimetidineHistamine H2 receptortarget
DB00501CimetidineCytochrome P450 1A2enzyme
DB00501CimetidineCytochrome P450 2D6enzyme
DB00501CimetidineCytochrome P450 2C19enzyme
DB00501CimetidineCytochrome P450 3A4enzyme
DB00501CimetidineCytochrome P450 3A5enzyme
DB00501CimetidineCytochrome P450 3A7enzyme
DB00501CimetidineMultidrug resistance protein 1transporter
DB00501CimetidineSolute carrier family 22 member 2transporter
DB00501CimetidineSolute carrier family 22 member 1transporter
DB00501CimetidineSolute carrier family 22 member 3transporter
DB00501CimetidineSolute carrier family 22 member 5transporter
DB00501CimetidineSolute carrier family 22 member 6transporter
DB00501CimetidineSolute carrier family 22 member 8transporter
DB00501CimetidineMultidrug and toxin extrusion protein 1transporter
DB00501CimetidineSolute carrier family 22 member 4transporter
DB00501CimetidineSolute carrier family 22 member 11transporter
DB00501CimetidineSolute carrier family 22 member 7transporter
DB00501CimetidineCytochrome P450 11B1, mitochondrialenzyme
DB00501CimetidineCytochrome P450 2C8enzyme
DB00501CimetidineCytochrome P450 2C9enzyme
DB00501CimetidineCytochrome P450 2E1enzyme
DB00501CimetidineDimethylaniline monooxygenase [N-oxide-forming] 3enzyme
DB00501CimetidineDimethylaniline monooxygenase [N-oxide-forming] 1enzyme
DB00501CimetidineBile salt export pumptransporter
DB00501CimetidineMultidrug and toxin extrusion protein 2transporter
DB00736EsomeprazolePotassium-transporting ATPase alpha chain 1target
DB00736EsomeprazoleCytochrome P450 2C19enzyme
DB00736EsomeprazoleCytochrome P450 3A4enzyme
DB00736EsomeprazoleN(G),N(G)-dimethylarginine dimethylaminohydrolase 1target
DB00736EsomeprazoleMultidrug resistance protein 1transporter
DB00736EsomeprazoleSolute carrier family 22 member 8transporter
DB00927FamotidineHistamine H2 receptortarget
DB00927FamotidineCytochrome P450 2C19enzyme
DB00927FamotidineSolute carrier family 22 member 2transporter
DB00927FamotidineSolute carrier family 22 member 8transporter
DB00448LansoprazolePotassium-transporting ATPase alpha chain 1target
DB00448LansoprazoleCytochrome P450 2C19enzyme
DB00448LansoprazoleCytochrome P450 2C9enzyme
DB00448LansoprazoleCytochrome P450 3A4enzyme
DB00448LansoprazoleMultidrug resistance protein 1transporter
DB00448LansoprazoleATP-binding cassette sub-family G member 2transporter
DB00448LansoprazoleCytochrome P450 1A1enzyme
DB00448LansoprazoleCytochrome P450 1B1enzyme
DB00448LansoprazoleCytochrome P450 2C18enzyme
DB00448LansoprazoleCytochrome P450 2C8enzyme
DB00448LansoprazoleCytochrome P450 2D6enzyme
DB00448LansoprazoleMicrotubule-associated protein tautarget
DB00448LansoprazoleSolute carrier family 22 member 8transporter
DB00448LansoprazoleSolute carrier family 22 member 1transporter
DB00448LansoprazoleSolute carrier family 22 member 2transporter
DB00448LansoprazoleSolute carrier family 22 member 3transporter
DB00585NizatidineHistamine H2 receptortarget
DB00585NizatidineMultidrug resistance protein 1transporter
DB00585NizatidineCholinesteraseenzyme
DB00338OmeprazolePotassium-transporting ATPase alpha chain 1target
DB00338OmeprazoleCytochrome P450 2C19enzyme
DB00338OmeprazoleCytochrome P450 3A4enzyme
DB00338OmeprazoleCytochrome P450 2C9enzyme
DB00338OmeprazoleCytochrome P450 1A2enzyme
DB00338OmeprazoleCanalicular multispecific organic anion transporter 2transporter
DB00338OmeprazoleMultidrug resistance protein 1transporter
DB00338OmeprazoleATP-binding cassette sub-family G member 2transporter
DB00338OmeprazoleCytochrome P450 1A1enzyme
DB00338OmeprazoleCytochrome P450 1B1enzyme
DB00338OmeprazoleCytochrome P450 2C18enzyme
DB00338OmeprazoleCytochrome P450 2C8enzyme
DB00338OmeprazoleCytochrome P450 2D6enzyme
DB00338OmeprazoleAryl hydrocarbon receptortarget
DB00213PantoprazolePotassium-transporting ATPase alpha chain 1target
DB00213PantoprazoleCytochrome P450 2C19enzyme
DB00213PantoprazoleCytochrome P450 3A4enzyme
DB00213PantoprazoleMultidrug resistance protein 1transporter
DB00213PantoprazoleATP-binding cassette sub-family G member 2transporter
DB00213PantoprazoleSolute carrier family 22 member 8transporter
DB00213PantoprazoleN(G),N(G)-dimethylarginine dimethylaminohydrolase 1target
DB01129RabeprazolePotassium-transporting ATPase alpha chain 1target
DB01129RabeprazoleCytochrome P450 3A4enzyme
DB01129RabeprazoleCytochrome P450 2C19enzyme
DB01129RabeprazoleATP-binding cassette sub-family G member 2transporter
DB01129RabeprazoleCytochrome P450 1A1enzyme
DB01129RabeprazoleCytochrome P450 1A2enzyme
DB01129RabeprazoleCytochrome P450 2C9enzyme
DB01129RabeprazoleCytochrome P450 2D6enzyme
DB01129RabeprazoleCytochrome P450 2C8enzyme
DB00863RanitidineHistamine H2 receptortarget
DB00863RanitidineCytochrome P450 1A2enzyme
DB00863RanitidineCytochrome P450 2D6enzyme
DB00863RanitidineSolute carrier family 22 member 1transporter
DB00863RanitidineMultidrug resistance protein 1transporter
DB00863RanitidineSolute carrier family 22 member 8transporter
DB00863RanitidineCytochrome P450 3A4enzyme
DB00863RanitidineAcetylcholinesterasetarget
DB00863RanitidineSolute carrier family 22 member 2transporter
DB00863RanitidineCholinesterasetarget
DB00364SucralfateFibrinogentarget
DB00364SucralfatePepsintarget
DB00364SucralfatePro-epidermal growth factortarget
DB00364SucralfateFibroblast growth factor 2target
DrugDrug NamePhaseStatusCount
DB00693Fluorescein0Terminated1
DB01123Proflavine0Terminated1
DB06723Aluminum hydroxide1Completed1
DB06723Aluminum hydroxide1Recruiting1
DB00594Amiloride1Completed1
DB05351Dexlansoprazole1Completed2
DB00736Esomeprazole1Completed4
DB00448Lansoprazole1Completed2
DB12884Lavoltidine1Completed1
DB11920Lesogaberan1Completed2
DB09481Magnesium carbonate1Completed1
DB09481Magnesium carbonate1Recruiting1
DB15325ONO-85391Completed1
DB00213Pantoprazole1Completed1
DB00213Pantoprazole1Unknown Status1
DB04216Quercetin1Completed1
DB01129Rabeprazole1Completed3
DB05351Dexlansoprazole1 / 2Withdrawn1
DB00736Esomeprazole1 / 2Unknown Status1
DB01065Melatonin1 / 2Unknown Status1
DB05269Activated charcoal2Terminated1
DB09278Activated charcoal2Terminated1
DB06723Aluminum hydroxide2Completed1
DB12031Ammonio methacrylate copolymer type A2Completed1
DB05031Arbaclofen Placarbil2Completed1
DB08892Arbaclofen Placarbil2Completed1
DB05351Dexlansoprazole2Completed2
DB11074Dimethicone2Completed1
DB00736Esomeprazole2Completed3
DB00736Esomeprazole2Not Yet Recruiting1
DB00736Esomeprazole2Terminated1
DB00736Esomeprazole2Unknown Status1
DB11964Ilaprazole2Unknown Status1
DB12884Lavoltidine2Completed1
DB11920Lesogaberan2Active Not Recruiting1
DB11920Lesogaberan2Completed4
DB09104Magnesium hydroxide2Completed1
DB00338Omeprazole2Completed1
DB12402Pumosetrag2Completed1
DB01129Rabeprazole2Completed3
DB00863Ranitidine2Completed1
DB11132Silicon dioxide2Completed1
DB01222Budesonide2 / 3Completed1
DB00736Esomeprazole2 / 3Completed1
DB00736Esomeprazole2 / 3Unknown Status1
DB00540Nortriptyline2 / 3Completed1
DB00213Pantoprazole2 / 3Completed1
DB01129Rabeprazole2 / 3Completed1
DB13518Alginic acid3Completed1
DB13518Alginic acid3Recruiting1
DB00181Baclofen3Completed1
DB01151Desipramine3Completed1
DB05351Dexlansoprazole3Completed5
DB01184Domperidone3Recruiting2
DB01184Domperidone3Withdrawn1
DB00668Epinephrine3Completed1
DB00736Esomeprazole3Completed9
DB00736Esomeprazole3Unknown Status1
DB00736Esomeprazole3Withdrawn1
DB11964Ilaprazole3Completed2
DB00458Imipramine3Completed1
DB00448Lansoprazole3Completed1
DB00448Lansoprazole3Unknown Status1
DB00281Lidocaine3Completed1
DB01065Melatonin3Withdrawn1
DB00585Nizatidine3Completed1
DB00540Nortriptyline3Completed1
DB00338Omeprazole3Completed2
DB00338Omeprazole3Recruiting1
DB00338Omeprazole3Unknown Status1
DB00213Pantoprazole3Completed4
DB00213Pantoprazole3Unknown Status2
DB00213Pantoprazole3Withdrawn1
DB01129Rabeprazole3Completed8
DB01129Rabeprazole3Unknown Status1
DB01129Rabeprazole3Withdrawn1
DB00980Ramelteon3Unknown Status1
DB00863Ranitidine3Completed2
DB09372Tannic acid3Completed1
DB01079Tegaserod3Completed2
DB13518Alginic acid4Unknown Status1
DB01060Amoxicillin4Not Yet Recruiting1
DB00181Baclofen4Withdrawn1
DB00215Citalopram4Recruiting1
DB01211Clarithromycin4Not Yet Recruiting1
DB05351Dexlansoprazole4Completed2
DB05351Dexlansoprazole4Enrolling by Invitation1
DB01184Domperidone4Completed2
DB01184Domperidone4Not Yet Recruiting1
DB00736Esomeprazole4Completed21
DB00736Esomeprazole4Unknown Status1
DB00448Lansoprazole4Completed3
DB00448Lansoprazole4Enrolling by Invitation1
DB00448Lansoprazole4Not Yet Recruiting1
DB00448Lansoprazole4Unknown Status1
DB00338Omeprazole4Completed4
DB00338Omeprazole4Recruiting1
DB00338Omeprazole4Unknown Status1
DB00213Pantoprazole4Completed4
DB00213Pantoprazole4Recruiting1
DB00213Pantoprazole4Terminated1
DB11097Plantago seed4Active Not Recruiting1
DB06480Prucalopride4Recruiting1
DB01129Rabeprazole4Completed4
DB01129Rabeprazole4Not Yet Recruiting1
DB00181BaclofenNot AvailableCompleted1
DB00501CimetidineNot AvailableCompleted1
DB00215CitalopramNot AvailableNot Yet Recruiting1
DB05351DexlansoprazoleNot AvailableWithdrawn1
DB01184DomperidoneNot AvailableAvailable1
DB01184DomperidoneNot AvailableNot Yet Recruiting1
DB01184DomperidoneNot AvailableTerminated1
DB05265EcabetNot AvailableCompleted1
DB00668EpinephrineNot AvailableRecruiting1
DB00736EsomeprazoleNot AvailableCompleted5
DB00736EsomeprazoleNot AvailableNot Yet Recruiting2
DB00927FamotidineNot AvailableCompleted1
DB00875FlupentixolNot AvailableNot Yet Recruiting1
DB12770LafutidineNot AvailableCompleted1
DB00448LansoprazoleNot AvailableCompleted2
DB00448LansoprazoleNot AvailableNot Yet Recruiting1
DB00448LansoprazoleNot AvailableWithdrawn1
DB00281LidocaineNot AvailableRecruiting1
DB13384MelitracenNot AvailableNot Yet Recruiting1
DB11675MosaprideNot AvailableNot Yet Recruiting2
DB13760NiperotidineNot AvailableCompleted1
DB00585NizatidineNot AvailableCompleted1
DB00338OmeprazoleNot AvailableCompleted5
DB00338OmeprazoleNot AvailableNot Yet Recruiting1
DB00338OmeprazoleNot AvailableWithdrawn1
DB00213PantoprazoleNot AvailableCompleted5
DB00213PantoprazoleNot AvailableNot Yet Recruiting1
DB01129RabeprazoleNot AvailableActive Not Recruiting1
DB01129RabeprazoleNot AvailableCompleted2
DB01129RabeprazoleNot AvailableNot Yet Recruiting1
DB01129RabeprazoleNot AvailableUnknown Status1
DB00863RanitidineNot AvailableCompleted1
DB08806Roxatidine acetateNot AvailableCompleted1
DB09153Sodium chlorideNot AvailableRecruiting1
DB00364SucralfateNot AvailableWithdrawn1
DB01586Ursodeoxycholic acidNot AvailableCompleted1