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Status:
US Approved OTC
Source:
21 CFR 331.11(g)(6) antacid:magnesium-containing magnesium hydroxide
Source URL:
First marketed in 1921
Source:
Solution of Magnesium Citrate U.S.P.
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Magnesium diamide is used as a chemical intermediate. Magnesium diamide is spontaneously combustible. It is toxic by inhalation. Skin or eye contact may cause severe burns.
Status:
Investigational
Source:
NCT01161602: Phase 2 Interventional Completed Gastroesophageal Reflux Disease
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Pumosetrag is a novel, orally active and selective 5-HT 3 agonist. It is a partial agonist in rats and guinea-pig and a full agonist in the mouse, suggesting important species differences in 5-HT3 receptor structure. Pumosetrag had been in phase II clinical trials for the treatment of gastroesophageal reflux disease and irritable bowel syndrome. No serious adverse events were reported. Diarrhea was not more common on the drug and only one subject experienced pruritus. All researches on this drug candidate are discontinued.
Status:
Investigational
Source:
NCT02267525: Phase 2 Interventional Completed Gastroparesis
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Velusetrag (TD-5108) is a potent, selective high intrinsic activity serotonin 5-HT(4) receptor agonist. Velusetrag has achieved proof-of-concept in patients with chronic idiopathic constipation and was on phase II of clinical trial for the treatment of Alzheimer's disease and constipation, when studies were discontinued. In addition, velusetrag is on the phase II of clinical trial for the treatment of gastroparesis.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Neochlorogenic acid is a natural polyphenolic compound which can be found in a variety of plant sources and especially some types of dried fruit. It is an epimer of chlorogenic acid. Neochlorogenic has been investigated as a chemopreventative dietary compound for breast cancer and collorectal cancer. It has in-vitro anti-inflammatory properties, and may be responsible for the laxative effect fo prunes. Research surrounding neochlorgenic acid has often involved various plant extracts, rather than pure preparations of the compound.
Status:
US Previously Marketed
Source:
ZELNORM by ALFASIGMA
(2002)
Source URL:
First approved in 2002
Source:
ZELNORM by ALFASIGMA
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Tegaserod (3‐(5‐methoxy‐1H‐indol‐3ylmethylene)‐N‐pentyl‐carbazimidamide), an aminoguanidine indole derivative of serotonin, is a selective partial agonist highly selective for 5‐HT4 receptor with an affinity constant in the nanomolar range. Tegaserod, by acting as an agonist at neuronal 5-HT4 receptors, triggers the release of further neurotransmitters such as calcitonin gene-related peptide from sensory neurons. The activation of 5-HT4 receptors in the gastrointestinal tract stimulates the peristaltic reflex and intestinal secretion, as well as inhibits visceral sensitivity. In vivo studies showed that tegaserod enhanced basal motor activity and normalized impaired motility throughout the gastrointestinal tract. Zelnorm® (tegaserod maleate) is indicated for the short-term treatment of women with irritable bowel
syndrome (IBS) whose primary bowel symptom is constipation. In addition Zelnorm® is indicated for the treatment of patients less than 65 years of age with
chronic idiopathic constipation.
Status:
US Previously Marketed
Source:
PROPULSID by JANSSEN PHARMS
(1993)
Source URL:
First approved in 1993
Source:
PROPULSID by JANSSEN PHARMS
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Cisapride is chemically related to metoclopramide, but unlike metoclopramide, it does not cross the blood-brain barrier or have antidopaminergic effects. Cisapride is a serotonin-4 (5-HT4) receptor agonist. Cisapride was indicated for the symptomatic treatment of adult patients with nocturnal heartburn due to gastroesophageal reflux disease. The Food and Drug Administration (FDA) in America stopped the marketing of cisapride as of 14th July 2000. They had received at least 341 reports of heart rhythm abnormalities and these led to 80 deaths. Other reported adverse effects are: headache, diarrhea, abdominal pain, nausea, constipation. Cisapride for animals has been found helpful in some cases of megaesophagus and is a common treatment for feline megacolon. Clarithromycin, erythromycin, and troleandomycin markedly inhibit the metabolism of cisapride. Concurrent administration of certain anticholinergic compounds, such as belladonna alkaloids and dicyclomine, would be expected to compromise the beneficial effects of cisapride.
Status:
US Previously Marketed
Source:
PROPULSID by JANSSEN PHARMS
(1993)
Source URL:
First approved in 1993
Source:
PROPULSID by JANSSEN PHARMS
Source URL:
Class (Stereo):
CHEMICAL (MIXED)
Cisapride is chemically related to metoclopramide, but unlike metoclopramide, it does not cross the blood-brain barrier or have antidopaminergic effects. Cisapride is a serotonin-4 (5-HT4) receptor agonist. Cisapride was indicated for the symptomatic treatment of adult patients with nocturnal heartburn due to gastroesophageal reflux disease. The Food and Drug Administration (FDA) in America stopped the marketing of cisapride as of 14th July 2000. They had received at least 341 reports of heart rhythm abnormalities and these led to 80 deaths. Other reported adverse effects are: headache, diarrhea, abdominal pain, nausea, constipation. Cisapride for animals has been found helpful in some cases of megaesophagus and is a common treatment for feline megacolon. Clarithromycin, erythromycin, and troleandomycin markedly inhibit the metabolism of cisapride. Concurrent administration of certain anticholinergic compounds, such as belladonna alkaloids and dicyclomine, would be expected to compromise the beneficial effects of cisapride.
Status:
US Previously Marketed
Source:
ISADOXOL by HARVEY
(1961)
Source URL:
First approved in 1959
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Oxyphenisatin is a stimulant laxative that has been used by mouth and as an enema. Oxyphenisatin was introduced as Lavema by Winthrop in US in 1959. Oxyphenisatin was used as a cleansing enema apart
from x-ray studies and prior to urinary, gastro-intestinal and
cholecystography x-ray examination. Oxyphenisatin was also used for preoperative preparation of the large intestine and colon. May be mixed with
barium for x-ray examination of the large intestine.
Oxyphenisatin may cause jaundice. Oxyphenisatin-induced liver damage usually occurs when the
drug has been taken for at least six months and usually two years. Oxyphenisatin was withdrawn in most countries in the early 1970s.
Status:
First approved in 1958
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Bisacodyl is typically prescribed for relief of constipation and for the management of neurogenic bowel dysfunction as well as part of bowel preparation before medical examinations, such as for a colonoscopy. Some drugs (e.g., diuretics, angiotensin converting enzyme inhibitors, angiotensin receptor blockers, or non-steroidal anti-inflammatory drugs) increase risk due to fluid and electrolyte changes. Most common adverse reactions (> 3%) are overall discomfort, abdominal fullness, abdominal cramping, nausea, and vomiting.
Status:
US Previously Marketed
First approved in 1956
Class (Stereo):
CHEMICAL (MIXED)
Conditions:
Docusate, also known as docusate salts or dioctyl sulfosuccinate, prevents/relieves dry hard stool and thus is used to treat constipation. Results usually occurs 1 to 3 days after the first dose. In North America, docusate and a stimulant laxative such as sennosides are commonly used in bowel treatment protocols associated with institutionalized elderly and oncology treatments. A paucity of evidence is available to support the use of the stool softener docusate yet it continues to be prescribed in everyday clinical practice for the aforementioned populations. While the actual cost of docusate is low, additional costs associated with its administration (i.e. nursing time) and its widespread use can be significant. Docusate is absorbed into the bloodstream and excreted via the gallbladder after undergoing extensive metabolism. The effect of docusate may not necessarily be all due to its surfactant properties. Perfusion studies suggest that docusate inhibits fluid absorption or stimulates secretion in the portion of the small intestine known as the jejunum