Diloxanide furoate is an anti-protozoal drug used in the treatment of Entamoeba histolytica and some other protozoal infections. Although it is not currently approved for use in the United States, it was approved by a CDC study in the treatment of 4,371 cases of Entamoeba histolytica from 1977 to 1990.
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|Approved Prescription Products||Not Available|
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|Weight||Average: 234.08 |
Diloxanide is used alone as a primary agent in the treatment of asymptomatic (cyst passers) intestinal amebiasis caused by Entamoeba histolytica. Diloxanide may also be used concurrently, or sequentially, with other agents such as the nitroimidazoles (eg. metronidazole) in the treatment of invasive or extraintestinal forms of amebiasis.
|Structured Indications||Not Available|
Diloxanide is a luminal amebicide, however the mechanism of action of diloxanide is unknown. Diloxanide destroys the trophozoites of E. histolytica that eventually form into cysts. The cysts are then excreted by persons infected with asymptomatic amebiasis. Diloxanide furoate is a prodrug, and is hydrolyzed in the gastrointestinal tract to produce diloxanide, the active ingredient.
|Mechanism of action|
Unknown. Diloxanide may inhibit protein synthesis.
Bioavailability is 90% (in diloxanide parental form), however diloxanide furoate is slowly absorbed from the gastrointestinal tract.
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|Protein binding||Not Available|
Hydrolyzed to furoic acid and diloxanide, which undergoes extensive glucuronidation (99% of diloxanide occurs as glucuronide and 1% as free diloxanide in the systemic circulation).
|Route of elimination|
Renal (90%, rapidly excreted as glucuronide metabolite). 10% is excreted in the feces as diloxanide.
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|ATC Codes||P01AC01 — Diloxanide|
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|Predicted ADMET features|
|Mass Spec (NIST)||Not Available|
|Description||This compound belongs to the class of organic compounds known as anilides. These are organic heterocyclic compounds derived from oxoacids RkE(=O)l(OH)m (l not 0) by replacing an OH group by the NHPh group or derivative formed by ring substitution.|
|Class||Benzene and substituted derivatives|
|Alternative Parents||1-hydroxy-2-unsubstituted benzenoids / Tertiary carboxylic acid amides / Organonitrogen compounds / Organochlorides / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds / Alkyl chlorides|
|Substituents||Anilide / 1-hydroxy-2-unsubstituted benzenoid / Phenol / Tertiary carboxylic acid amide / Carboxamide group / Carboxylic acid derivative / Alkyl chloride / Hydrocarbon derivative / Organic oxide / Organooxygen compound|
|Molecular Framework||Aromatic homomonocyclic compounds|
|External Descriptors||Not Available|