Luminal amoebicdes

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Chapter: Medicinal Chemistry : Antiamoebic Agents

Antiamoebic Agents - Luminal amoebicdes: Diloxanide Furoate (Furamide)


Antiamoebic Agents - Synthesis and Drug Profile

Luminal amoebicdes

 

i. Diloxanide Furoate (Furamide)


Synthesis


Metabolism: The diloxanide furoate is administered orally and is hydrolyzed in the gut to give diloxanide.


Properties and uses: Diloxanide furoate is a white crystalline powder, very slightly soluble in water, slightly soluble in ethanol and ether. It is dichloro acetamide derivative that is nontoxic, mainly used in the treatment of chronic amoebiasis. It is less effective in the treatment of acute intestinal amoebiasis.

Assay: Dissolve the sample in anhydrous pyridine and titrate against 0.1 M tetrabutylammonium hydroxide. Determine the end point potentiometrically.

Dose: The recommended oral dose is 500 mg three times daily for 10 days (Diloxanide furoate 250 mg + Tinidazole 300 mg) two tablets daily. Diloxanide furoate 250 mg + Metronidazole 250 mg two tablets thrice daily for 10 days.

Dosage forms: Diloxanide tablets B.P.

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