Heartburn

Also known as: [D]Heartburn / Pyrosis / Indigestion / Dyspepsia

DrugDrug NameDrug Description
DB13595AlmasilateAlmasilate is a buffering antacid that has been used in peptic ulcers and dyspepsia. It is a crystalline polyhydrate of aluminium/magnesium silicate and mediates its buffering activity by binding hydrogen ions within the polymer. However its therapeutic efficacy is not comparable to other approved antacids, as it is no more effective in neutralizing acid and binding bile salts than other conventional antacids [A27138]. Given that there are generally more widely available conventional antacids that are just as - if not more - effective than almasilate, almasilate products are only available in certain parts of Europe and/or Asia.
DB06723Aluminum hydroxideAluminum hydroxide is an inorganic salt used as an antacid. It is a basic compound that acts by neutralizing hydrochloric acid in gastric secretions. Subsequent increases in pH may inhibit the action of pepsin. An increase in bicarbonate ions and prostaglandins may also confer cytoprotective effects.
DB01294Bismuth subsalicylateBismuth subsalicylate is the active ingredient in the popular medication Pepto-Bismol that is used to treat nausea, heartburn, indigestion, upset stomach, diarrhea, and other temporary discomforts of the stomach and gastrointestinal tract. It is also the main ingredient of Kaopectate. It displays anti-inflammatory action (due to salicylic acid) and also acts as an antacid and mild antibiotic.
DB06724Calcium carbonateCalcium carbonate is an inorganic salt used as an antacid. It is a basic compound that acts by neutralizing hydrochloric acid in gastric secretions. Subsequent increases in pH may inhibit the action of pepsin. An increase in bicarbonate ions and prostaglandins may also confer cytoprotective effects. Calcium carbonate may also be used as a nutritional supplement or to treat hypocalcemia.
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.
DB04272Citric acidA key intermediate in metabolism. It is an acid compound found in citrus fruits. The salts of citric acid (citrates) can be used as anticoagulants due to their calcium chelating ability.
DB05351DexlansoprazoleDexlansoprazole is a new generation proton pump inhibitor (PPI) used for the management of symptoms associated with gastroesophageal reflux disease (GERD) and erosive esophagitis. Dexlansoprazole is the R-enantiomer of [DB00448], which is composed of a racemic mixture of the R- and S-enantiomers. Compared to the older generation of PPIs (which includes [DB00213], [DB00338], and [DB00448]) [A178084], dexlansoprazole MR has a unique pharmacokinetic profile due to its delayed-release and dual-delivery release system. The active ingredient is released in two phases at different pH values and at different time points, resulting in two peak concentrations in the blood; 25% of the dose is released at pH 5.5 in the proximal duodenum, while the remaining 75% is released at pH 6.75 in the distal small intestine [A19567]. As a result, dexlansoprazole has a peak concentration within 1-2 hours after dosing and another within 4-5 hours [FDA Label]. Dexlansoprazole's unique pharmacokinetics addresses limitations of the older generation PPIs including short plasma half-life, break-through symptoms, and need for meal-associated dosing [A19568]. These characteristics make dexlansoprazole a good option for people who struggle with adherence and strict dosage timing before meals[A178087, A19566]. Dexlansoprazole exerts its stomach acid-suppressing effects in the same way as other drugs in the PPI family by inhibiting the final step in gastric acid production. Dexlansoprazole targets the (H+, K+)-ATPase enzyme, which is involved in the secretion of hydrochloric acid through the exchange of H+ ions from the cytoplasm for K+ ions. Normally functioning (H+, K+)-ATPase stimulates hydrochloric acid secretion into the gastric lumen thereby increasing stomach acidity and lowering pH. Once absorbed into circulation, dexlansoprazole covalently binds to the sulfhydryl groups of cysteines found on the (H+, K+)-ATPase enzyme at the secretory surface of gastric parietal cells, which leads to inhibition of both basal and stimulated gastric acid secretion. Despite dexlansoprazole's unique pharmacokinetic profile, efficacy in management of GERD symptoms is considered similar to other medications within the PPI class including [DB00338], [DB00736], [DB00448], [DB00213], and [DB01129]. 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 dexlansoprazole 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 dexlansoprazole 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 dimethylarginine (ADMA), which is thought to cause the association of PPIs with increased risk of cardiovascular events in patients with unstable coronary syndromes [A177577, A177580]. Dexlansoprazole doses should be slowly lowered, or tapered, before discontinuing as rapid discontinuation of PPIs such as dexlansoprazole may cause a rebound effect and a short term increase in hypersecretion [A177574].
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 cells. 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 has been associated with possible adverse effects, however, including increased susceptibility to bacterial infections (including gastrointestinal _C. difficile_), reduced absorption of micronutrients such as 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.
DB09459L-tartaric acidTartaric acid is a white crystalline organic acid that occurs naturally in many plants, most notably in grapes.Tartaric is an alpha-hydroxy-carboxylic acid, is diprotic and aldaric in acid characteristics, and is a dihydroxyl derivative of succinic acid.
DB08938MagaldrateMagaldrate is an antacid drug used for the treatment of esophagitis, duodenal and gastric ulcers, and gastroesophageal reflux. Magaldrate has been discontinued in the US market.
DB09481Magnesium carbonateMagnesium carbonate, also known as magnesite, is a common over the counter remedy for heartburn and upset stomach caused by overproduction of acid in the stomach [FDA Label].
DB09104Magnesium hydroxideMagnesium hydroxide is an inorganic compound. It is naturally found as the mineral brucite. Magnesium hydroxide can be used as an antacid or a laxative in either an oral liquid suspension or chewable tablet form. Additionally, magnesium hydroxide has smoke suppressing and flame retardant properties and is thus used commercially as a fire retardant. It can also be used topically as a deodorant or for the relief of canker sores (aphthous ulcers).
DB01377Magnesium oxideMagnesium oxide is an inorganic compound that occurs in nature as the mineral periclase. In aqueous media combines quickly with water to form magnesium hydroxide. It is used as an antacid and mild laxative and has many nonmedicinal uses.
DB09281Magnesium trisilicateMagnesium trisilicate is an inorganic compound that is used as an antacid in the treatment of peptic 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].
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].
DB14116SilodrateNot Available
DB01390Sodium bicarbonateSodium bicarbonate is a white, crystalline powder that is commonly used as a pH buffering agent, an electrolyte replenisher, systemic alkalizer and in topical cleansing solutions.
DB09154Sodium citrateSodium citrate is the sodium salt of citric acid. It is white, crystalline powder or white, granular crystals, slightly deliquescent in moist air, freely soluble in water, practically insoluble in alcohol. Like citric acid, it has a sour taste. From the medical point of view, it is used as alkalinizing agent. It works by neutralizing excess acid in the blood and urine. It has been indicated for the treatment of metabolic acidosis.
DrugDrug NameTargetType
DB01294Bismuth subsalicylateSerum albumincarrier
DB01294Bismuth subsalicylateSerotransferrincarrier
DB00501CimetidineHistamine H2 receptortarget
DB00501CimetidineCytochrome P450 1A2enzyme
DB00501CimetidineCytochrome P450 2D6enzyme
DB00501CimetidineCytochrome P450 2C19enzyme
DB00501CimetidineCytochrome P450 3A4enzyme
DB00501CimetidineCytochrome P450 3A5enzyme
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
DB04272Citric acidCell division protein FtsZtarget
DB04272Citric acidAngiogenintarget
DB04272Citric acidBeta-lactamase 2target
DB04272Citric acidUridine-cytidine kinase 2target
DB04272Citric acidTumor necrosis factor ligand superfamily member 13Btarget
DB04272Citric acidBetaine--homocysteine S-methyltransferase 1target
DB04272Citric acidTryptophan--tRNA ligasetarget
DB04272Citric acidAldose reductasetarget
DB04272Citric acidCitrate synthase, mitochondrialtarget
DB04272Citric acidHeparan sulfate glucosamine 3-O-sulfotransferase 3A1target
DB04272Citric acidcGMP-specific 3',5'-cyclic phosphodiesterasetarget
DB04272Citric acidProto-oncogene tyrosine-protein kinase Srctarget
DB04272Citric acidRibonuclease pancreatictarget
DB04272Citric acidIsocitrate dehydrogenase [NADP]target
DB04272Citric acidGlycine N-methyltransferasetarget
DB04272Citric acidEosinophil cationic proteintarget
DB04272Citric acidBeta-lactamasetarget
DB04272Citric acidMolybdenum cofactor guanylyltransferasetarget
DB04272Citric acidFumarate hydratase class IItarget
DB04272Citric acid6-phosphogluconolactonasetarget
DB04272Citric acidOxygen-insensitive NAD(P)H nitroreductasetarget
DB04272Citric acidGag-Pro-Pol polyproteintarget
DB04272Citric acidL-amino-acid oxidasetarget
DB04272Citric acidMacrophage migration inhibitory factortarget
DB04272Citric acidCarboxy-terminal domain RNA polymerase II polypeptide A small phosphatase 1target
DB04272Citric acid1-deoxy-D-xylulose 5-phosphate reductoisomerasetarget
DB04272Citric acidTryptophan synthase alpha chaintarget
DB04272Citric acidSialidasetarget
DB04272Citric acidKHG/KDPG aldolasetarget
DB04272Citric acidCytochrome c peroxidasetarget
DB04272Citric acidHepatocyte growth factor-regulated tyrosine kinase substratetarget
DB04272Citric acidInvasintarget
DB04272Citric acidIntron-associated endonuclease 1target
DB04272Citric acidShort tail fiber proteintarget
DB04272Citric acidMalate dehydrogenase, mitochondrialtarget
DB04272Citric acidN5-carboxyaminoimidazole ribonucleotide mutasetarget
DB04272Citric acid50S ribosomal protein L4target
DB04272Citric acidCarboxypeptidase Btarget
DB04272Citric acidHexon proteintarget
DB04272Citric acidRiboflavin biosynthesis protein RibFtarget
DB04272Citric acidBeta-fructosidasetarget
DB04272Citric acidPutative stringent starvation protein Atarget
DB04272Citric acidCitrate synthasetarget
DB04272Citric acidRNA 3'-terminal phosphate cyclasetarget
DB04272Citric acidU6 snRNA-associated Sm-like protein LSm6target
DB04272Citric acidPleckstrin homology domain-containing family A member 1target
DB04272Citric acidFe(3+)-binding periplasmic proteintarget
DB04272Citric acidSignal recognition particle receptor FtsYtarget
DB04272Citric acidNicotinate-nucleotide adenylyltransferasetarget
DB04272Citric acidN utilization substance protein B homologtarget
DB04272Citric acidComplement component C8 gamma chaintarget
DB04272Citric acidRibonucleoside-diphosphate reductase subunit betatarget
DB04272Citric acidGlutamine synthetase 1target
DB04272Citric acidCitrate synthasetarget
DB04272Citric acidProstaglandin F synthasetarget
DB04272Citric acidAdenine phosphoribosyltransferasetarget
DB04272Citric acidGlucose-1-phosphate thymidylyltransferasetarget
DB04272Citric acidGlyoxalase family proteintarget
DB04272Citric acidLaccase domain protein YfiHtarget
DB04272Citric acidRibose-5-phosphate isomerase Atarget
DB04272Citric acidGMP synthase [glutamine-hydrolyzing]target
DB04272Citric acidInosine triphosphate pyrophosphatasetarget
DB04272Citric acidLysozymetarget
DB04272Citric acidGlycerol uptake operon antiterminator regulatory proteintarget
DB04272Citric acid3-carboxy-cis,cis-muconate cycloisomerasetarget
DB04272Citric acidPyruvate decarboxylasetarget
DB04272Citric acidSolute carrier organic anion transporter family member 2B1transporter
DB05351DexlansoprazolePotassium-transporting ATPase alpha chain 1target
DB05351DexlansoprazoleCytochrome P450 2C19enzyme
DB05351DexlansoprazoleCytochrome P450 3A4enzyme
DB05351DexlansoprazolePotassium-transporting ATPase subunit betatarget
DB05351DexlansoprazoleN(G),N(G)-dimethylarginine dimethylaminohydrolase 1target
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
DB00927FamotidineSolute carrier family 22 member 2transporter
DB00927FamotidineSolute carrier family 22 member 8transporter
DB09459L-tartaric acidGalactosylgalactosylxylosylprotein 3-beta-glucuronosyltransferase 1enzyme
DB09459L-tartaric acidHypoxia-inducible factor 1-alpha inhibitorenzyme
DB09481Magnesium carbonateTransient receptor potential cation channel subfamily M member 6transporter
DB09481Magnesium carbonateSolute carrier family 41 member 3transporter
DB09481Magnesium carbonateMetal transporter CNNM2transporter
DB09481Magnesium carbonateTransient receptor potential cation channel subfamily M member 7transporter
DB09481Magnesium carbonateGlutamate (NMDA) receptortarget
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
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
DB01390Sodium bicarbonateElectrogenic sodium bicarbonate cotransporter 1transporter
DB01390Sodium bicarbonateSodium bicarbonate cotransporter 3transporter
DB01390Sodium bicarbonateElectroneutral sodium bicarbonate exchanger 1transporter
DB01390Sodium bicarbonateElectrogenic sodium bicarbonate cotransporter 4transporter
DB01390Sodium bicarbonateHydrogen ionstarget
DB01390Sodium bicarbonateSodium-driven chloride bicarbonate exchangertransporter
DB09154Sodium citrateMitochondrial 2-oxodicarboxylate carriertransporter
DB09154Sodium citrateSolute carrier family 13 member 2transporter
DB09154Sodium citrateSolute carrier family 13 member 5transporter
DB09154Sodium citrateTricarboxylate transport protein, mitochondrialtransporter