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Status:
US Approved Rx
(2017)
Source:
ANDA202294
(2017)
Source URL:
First approved in 1995
Source:
NDA020406
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Dexlansoprazole (trade names Kapidex, Dexilant) is a proton pump inhibitor (PPI) that is marketed by Takeda Pharmaceuticals for the treatment of erosive esophagitis and gastro-oesophageal reflux disease. Dexlansoprazole is used to heal and maintain healing of erosive esophagitis and to treat heartburn associated with gastroesophageal reflux disease (GERD). It lasts longer than lansoprazole, to which it is chemically related, and needs to be taken less often. Dexlansoprazole is supplied for oral administration as a dual delayed-release formulation in capsules and orally disintegrating tablets. The capsules and tablets contain dexlansoprazole in a mixture of two types of enteric-coated granules with different pH-dependent dissolution profiles. The most significant adverse reactions (≥2%) reported in clinical trials were diarrhea, abdominal pain, nausea, upper respiratory tract infection, vomiting, and flatulence.
Status:
US Approved Rx
(2016)
Source:
ANDA204068
(2016)
Source URL:
First approved in 1989
Source:
PRILOSEC by ASTRAZENECA
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Esomeprazole strontium is a proton pump inhibitor. It suppresses gastric acid secretion by specific inhibition H+/K+ ATPase in the gastric parietal cell. The S- and R-isomers of omeprazole are protonated and converted in the acidic compartment of the parietal cell forming the active inhibitor, the achiral sulphenamide. By acting specifically on the proton pump, esomeprazole blocks the final step in acid production, thus reducing gastric acidity. The drug is indicated for the treatment of gastroesophageal reflux disease, reduction the risk of NSAID-associated gastric ulcer, eradication of H.pylori, and pathological hypersecretory conditions.
Status:
US Approved Rx
(2011)
Source:
ANDA090618
(2011)
Source URL:
First approved in 1988
Source:
AXID by SMITHKLINE BEECHAM
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Nizatidine, chemically N-[2-[[[2- [(dimethylamino)methyl]-4-thiazolyl]methyl]thio]ethyl]-N’ -methyl-2-nitro-1,1-ethenediamine, is a histamine H2-receptor antagonist.
Nizatidine reduced gastric acid secretion for up to 8 h suggesting that this compound could be used in with a once or twice daily dosage regime. Nizatidine was rapidly and well-absorbed orally, was widely distributed in tissues and the majority of the dose was excreted in the urine within 24 h. Nizatidine is indicated for duodenal and gastric ulcer as well as for the treatment of endoscopically diagnosed esophagitis, including erosive and ulcerative esophagitis, and associated heartburn due to gastroesophageal reflux disease.
Status:
US Approved Rx
(2014)
Source:
ANDA201995
(2014)
Source URL:
First approved in 1986
Source:
PEPCID by BAUSCH
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Famotidine, a competitive histamine H2-receptor antagonist, is used to treat gastrointestinal disorders such as gastric or duodenal ulcer, gastroesophageal reflux disease, and pathological hypersecretory conditions. Famotidine inhibits many of the isoenzymes of the hepatic CYP450 enzyme system. Other actions of Famotidine include an increase in gastric bacterial flora such as nitrate-reducing organisms. Famotidine binds competitively to H2-receptors located on the basolateral membrane of the parietal cell, blocking histamine affects. This competitive inhibition results in reduced basal and nocturnal gastric acid secretion and a reduction in gastric volume, acidity, and amount of gastric acid released in response to stimuli including food, caffeine, insulin, betazole, or pentagastrin.
Status:
US Approved Rx
(2000)
Source:
ANDA075294
(2000)
Source URL:
First approved in 1983
Source:
ZANTAC 150 by GLAXO GRP LTD
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Ranitidine, a histamine H2-receptor antagonist, is now well established as a potent inhibitor of gastric acid secretion effective in the treatment and prophylaxis of gastrointestinal lesions aggravated by gastric acid secretion.
Status:
US Approved Rx
(2008)
Source:
ANDA078807
(2008)
Source URL:
First approved in 1979
Source:
REGLAN by HIKMA
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Metoclopramide is a dopamine D2 antagonist that is used as an antiemetic. Metoclopramide inhibits gastric smooth muscle relaxation produced by dopamine, therefore increasing cholinergic response of the gastrointestinal smooth muscle. It accelerates intestinal transit and gastric emptying by preventing relaxation of gastric body and increasing the phasic activity of antrum. Simultaneously, this action is accompanied by relaxation of the upper small intestine, resulting in an improved coordination between the body and antrum of the stomach and the upper small intestine. Metoclopramide also decreases reflux into the esophagus by increasing the resting pressure of the lower esophageal sphincter and improves acid clearance from the esophagus by increasing amplitude of esophageal peristaltic contractions. Metoclopramide's dopamine antagonist action raises the threshold of activity in the chemoreceptor trigger zone and decreases the input from afferent visceral nerves. Studies have also shown that high doses of metoclopramide can antagonize 5-hydroxytryptamine (5-HT) receptors in the peripheral nervous system in animals. Metoclopramide is used for the treatment of gastroesophageal reflux disease (GERD). It is also used in treating nausea and vomiting, and to increase gastric emptying.
Status:
US Approved Rx
(2024)
Source:
ANDA218997
(2024)
Source URL:
First approved in 1977
Source:
TAGAMET by GLAXOSMITHKLINE
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Cimetidine is a histamine H2-receptor antagonist. It reduces basal and nocturnal gastric acid secretion and a reduction in gastric volume, acidity, and amount of gastric acid released in response to stimuli including food, caffeine, insulin, betazole, or pentagastrin. It is used to treat gastrointestinal disorders such as gastric or duodenal ulcer, gastroesophageal reflux disease, and pathological hypersecretory conditions. Cimetidine inhibits many of the isoenzymes of the hepatic CYP450 enzyme system. Other actions of Cimetidine include an increase in gastric bacterial flora such as nitrate-reducing organisms. Cimetidine binds to an H2-receptor located on the basolateral membrane of the gastric parietal cell, blocking histamine effects. This competitive inhibition results in reduced gastric acid secretion and a reduction in gastric volume and acidity.
Status:
US Approved Rx
(1992)
Source:
ANDA073556
(1992)
Source URL:
First approved in 1964
Source:
AVENTYL by RANBAXY
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Nortriptyline is a second-generation tricyclic antidepressant (TCA) marketed as the hydrochloride salt under the trade names Sensoval, Aventyl, Pamelor, Norpress, Allegron, Noritren and Nortrilen. Nortriptyline is used in the treatment of depression and childhood nocturnal enuresis. Its off-label uses include treatment of postherpetic neuralgia, angioedema and smoking Cessation, and attention deficit hyperactivity disorder in some neurological disorders. It is believed that nortriptyline either inhibits the reuptake of the neurotransmitter serotonin at the neuronal membrane or acts at beta-adrenergic receptors. Nortriptyline is US FDA-approved for the treatment of major depression. In the United Kingdom, it may also be used for treating nocturnal enuresis, with courses of treatment lasting no more than three months. The most common side effects include dry mouth, sedation, constipation, and increased appetite, mild blurred vision, tinnitus, occasionally hypomania or mania. An occasional side effect is a rapid or irregular heartbeat. Alcohol may exacerbate some of its side effects. However, fewer and milder side effects occur with nortriptyline than tertiary tricyclic antidepressants such as imipramine and amitriptyline. For this reason, nortriptyline is preferred to other tricyclic antidepressants, particularly with older adults, which also improves compliance.
Status:
US Approved OTC
Source:
21 CFR 331.11(a)(2) antacid:aluminum-containing aluminum hydroxide-magnesium trisilicate, co-dried gel
Source URL:
First marketed in 1921
Source:
Aluminum Hydroxide U.S.P.
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Algeldrate (Aluminium hydroxide) is the amphoteric inorganic compound used as an antacid in the treatment of Duodenal, Peptic and Stomach Ulcer and some other conditions. Aluminium hydroxide is preferred over other alternatives such as sodium bicarbonate because Al(OH)3, being insoluble, does not increase the pH of stomach above 7 and hence, does not trigger secretion of excess acid by the stomach. Brand names include Alu-Cap, Aludrox, Gaviscon or Pepsamar. It reacts with the excess acid in the stomach, reducing the acidity of the stomach content, which may relieve the symptoms of ulcers, heartburn or dyspepsia. Such products can cause constipation, because the aluminum ions inhibit the contractions of smooth muscle cells in the gastrointestinal tract, slowing peristalsis and lengthening the time needed for stool to pass through the colon. Some such products (such as Maalox) are formulated to minimize such effects through the inclusion of equal concentrations of magnesium hydroxide or magnesium carbonate, which have counterbalancing laxative effects. This compound is also used to control phosphate (phosphorus) levels in the blood of people suffering from kidney failure. Precipitated aluminum hydroxide is included as an adjuvant in some vaccines (e.g. anthrax vaccine). One of the well-known brands of aluminum hydroxide adjuvant is Alhydrogel, made by Brenntag Biosector. Since it absorbs protein well, it also functions to stabilize vaccines by preventing the proteins in the vaccine from precipitating or sticking to the walls of the container during storage. Aluminium hydroxide is sometimes mistakenly called "alum", which properly refers to aluminum potassium sulfate. Vaccine formulations containing aluminum hydroxide stimulate the immune system by inducing the release of uric acid, an immunological danger signal. This strongly attracts certain types of monocytes which differentiate into dendritic cells. The dendritic cells pick up the antigen, carry it to lymph nodes, and stimulate T cells and B cells. It appears to contribute to induction of a good Th2 response, so is useful for immunizing against pathogens that are blocked by antibodies. In the 1960s and 1970s, it was speculated that aluminum was related to various neurological disorders including Alzheimer's disease. Since then, multiple epidemiological studies have found no connection between exposure to aluminum and neurological disorders.
Status:
Investigational
Source:
NCT00857623: Phase 2 Interventional Completed Pain
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
AstraZeneca was developing AZD-2066, a metabotropic glutamate receptor 5 (mGLUR5) antagonist, for the oral treatment of pain indications (e.g. chronic neuropathic pain and painful diabetic neuropathies), depressive disorders and gastro-oesophageal reflux disease. AZD-2066 had been in phase II clinical trials by AstraZeneca for the treatment of diabetic neuropathic pain and phase I for the treatment of gastrooesophageal reflux disease (GERD). However, this reasearch had being discontinued.