Дилоксанид

Использование

Diloxanide is also active against cysts and trophozoites localized in the lumen of the intestine, and it is used for treating the carrier E. histolytica, as well as for treating asymptomatic or moderate forms of amebiasis. In the transition stage to trophozoites, the drug is less active than iodoquinol. A synonym of this drug is furamide.

Антимикробная активность

Diloxanide inhibits E. histolytica with unusually high specificity at concentrations of 0.01–0.1 mg/L.

Приобретенная устойчивость

No resistance has been reported. Patients with dysentery have lower cure rates than cyst excreters.

Фармацевтические приложения

Dichloro(hydroxyphenyl)methylacetamide. Available as an insoluble ester, the furoate, for oral administration.

Фармакокине?тика

Human pharmacokinetic data are limited. Animal data show that diloxanide furoate is rapidly absorbed from the intestine. The furoate is hydrolyzed in the gut, leaving high intraluminal concentrations of free diloxanide. About 75% is excreted via the kidney within 48 h, mostly as a glucuronide.

Клиническое использование

Furamide, or eutamide, is the 2-furoate ester of 2,2-dichloro-4 -hydroxy-N-methylacetanilide. It was developed as a resultof the discovery that various α,α-dichloroacetamidespossessed amebicidal activity in vitro. Diloxanide itself andmany of its esters are also active, and drug metabolism studiesindicate that hydrolysis of the amide is required for theamebicidal effect. Nonpolar esters of diloxanide are morepotent than polar ones. Diloxanide furoate has been used inthe treatment of asymptomatic carriers of E. histolytica. Itseffectiveness against acute intestinal amebiasis or hepaticabscesses, however, has not been established. Diloxanidefuroate is a white crystalline powder. It is administered orallyonly as 500-mg tablets and may be obtained in the UnitedStates from the CDC in Atlanta, Georgia.

Побочные эффекты

It is well tolerated, but flatulence is common, and nausea and vomiting may occur.