U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 11 - 20 of 112 results

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
First approved in 2002

Class (Stereo):
CHEMICAL (ACHIRAL)


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.
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
First approved in 1959
Source:
Laverna by Winthrop
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


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:
US Previously Marketed
Source:
Dulcolax by Geigy
(1958)
Source URL:
First approved in 1958
Source:
Dulcolax by Geigy
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


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
Source:
Surfak by Lloyd Bros. (Hoechst-Roussel)
(1959)
Source URL:
First approved in 1956
Source:
Doxinate by Lloyd Bros. (Hoechst-Roussel)
Source URL:

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
Status:
Possibly Marketed Outside US
Source:
MICROLAX by Ethyl
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Sodium Lauryl Sulfoacetate is a safe skin friendly surfactant (foaming agent) for both skin and hair. Sodium Lauryl Sulfoacetate was used in 93 products in 1981, based on voluntary reports provided to FDA by industry; use concentrations ranged from >0.1% to >50%. In 2002 there were 68 uses (FDA 2002) and according to an industry survey in 2004 the current range of use concentrations is 0.6% to 21% (CTFA 2004). Asafety assessment on Sodium Lauryl Sulfoacetatewas published in 1987 with the conclusion “On the basis of the available data presented in this report, the Expert Panel concludes that Sodium Lauryl Sulfoacetate is safe as a cosmetic ingredient in the present practices of use and concentration” (Elder 1987). Studies available since that safety assessment was completed, along with updated information regarding uses and use concentrations, were considered by the CIR Expert Panel. After reviewing the available data, the Panel determined to not reopen this safety assessment.
Status:
Possibly Marketed Outside US
Source:
Wylaxine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Bisoxatin (Laxonalin, Wylaxine) acetate is a stimulant laxative that has been used in the treatment of constipation. The drug showed good effects to habitual constipation and dolichocolon but was not sufficient acting in megacolon. It seems that the drug is effective to constipation due to functional disorders but the effect is not sufficient to constipation caused chiefly by organic colonic changes. No side effect was observed even in long term administration.
Status:
Possibly Marketed Outside US
Source:
SENNA
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Sennoside B is a member of the class of sennosides that used as the laxative. Sennosides are used all over the world as a treatment for constipation. Sennosides are hydroxyanthracene glycosides derived from Senna leaves. The phytoconstituents principally responsible for its characteristic action are two anthraquinone glycosides namely; Sennoside A and Sennoside B. Sennoside A and B together are responsible for up to 40 – 60% activity of crude senna. They have identical molecular weights and formulae and are in fact diastereomers with the same substituent (H) located in opposite directions. Sennoside B has reported that it has inhibitory effects on PDGF receptor signaling and cell proliferation induced by PDGF-BB in human osteosarcoma cells.
Status:
Possibly Marketed Outside US
Source:
Senokot by Stoll, A.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Sennoside A, derived from the traditional chinese medicine plant Rheum L., has being shown to be a dual HIV-1 inhibitor effective on HIV-1 replication. Sennoside A is a kind of irritant laxative. It is also used for colonoscopy preparation. It mildly inhibits bovine serum monoamine oxidase with IC50 of 17uM.

Showing 11 - 20 of 112 results