ジロキサニド

ジロキサニド 化学特性,用途語,生産方法

• 効能

  抗アメーバ薬, 抗原虫薬

• 使用

  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.

• 抗菌性

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

• 獲得抵抗性

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

• 応用例（製薬）

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

• 薬物動態学

  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.

• 臨床応用

  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.

• 副作用

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

ジロキサニド 生産企業

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