Diloxanide Furoate

• Approved Indications:
• Treatment of asymptomatic and symptomatic intestinal amoebiasis caused by Entamoeba histolytica cysts (luminal amoebicide)
• Eradication of cyst carriage after treatment of invasive amoebiasis with tissue amoebicides (e.g., metronidazole)
• Off-label/Clinically Accepted Uses:
• Eradication of non-pathogenic Entamoeba species colonization
• Occasionally used for intestinal protozoal infections requiring luminal eradication

• Route: Oral
• Adults:
• 500 mg three times daily (TID) for 10 days
• Pediatrics:
• 20 mg/kg/day divided into 3 doses for 10 days (not to exceed adult dose)
• Elderly:
• Use standard adult dosing; monitor for tolerance
• Renal/Hepatic Impairment:
• No established dose adjustment; use cautiously and monitor
• Administration Notes:
• Can be taken with or without food
• Complete full course to prevent recurrence or resistance

Diloxanide furoate is a luminal amebicide that acts directly on the cyst and trophozoite forms of Entamoeba histolytica in the intestinal lumen. It disrupts protozoal metabolism by interfering with energy-producing pathways, leading to decreased ATP synthesis and parasite death. Its primary action is confined to the intestinal lumen due to poor systemic absorption, making it effective at eradicating intestinal colonization but not invasive disease.

• Absorption: Poorly absorbed from the gastrointestinal tract; minimal systemic bioavailability
• Distribution: Primarily remains in the intestinal lumen
• Metabolism: Hydrolyzed in the intestinal mucosa to the active compound diloxanide, which is also poorly absorbed
• Half-life: Not well defined systemically due to poor absorption
• Elimination: Mostly eliminated unchanged in feces; negligible renal excretion
• Onset of Action: Therapeutic effects seen within days of initiation

• Pregnancy:
• FDA Category B — Animal studies have not demonstrated risk; no adequate human studies
• Use only if clearly needed and benefits outweigh risks
• Lactation:
• Data limited; use with caution during breastfeeding
• Potential for minimal excretion in breast milk

• Primary Class: Antiprotozoal agent
• Subclass: Luminal amebicide

• Known hypersensitivity to diloxanide furoate or any formulation excipients
• Acute invasive amoebiasis (tissue infection requires systemic amebicides, not luminal agents alone)
• Severe hepatic or renal impairment (use cautiously)

• Not effective as monotherapy for invasive amoebiasis; must be used after or with systemic tissue amebicides
• Monitor for signs of hypersensitivity reactions
• Use cautiously in patients with hepatic dysfunction
• Complete full treatment course to avoid relapse or resistance development
• Not suitable for treatment of infections caused by other intestinal protozoa

• Common:
• Mild gastrointestinal disturbances (nausea, abdominal discomfort, diarrhea)
• Headache
• Serious/Rare:
• Allergic reactions including rash, pruritus, or urticaria
• Rarely, jaundice or hepatic enzyme elevations
• Very rare cases of blood dyscrasias reported

• No significant drug-drug interactions reported due to minimal systemic absorption
• No known food or alcohol interactions
• Caution when co-administered with other potentially hepatotoxic drugs

• Current WHO and CDC guidelines recommend diloxanide furoate as an effective luminal agent following treatment of invasive amoebiasis to eradicate cyst carriage and prevent transmission
• No major recent changes in dosing or approved indications
• Emphasis on combined use with systemic amebicides for complete treatment of invasive disease

• Store at controlled room temperature: 20°C to 25°C (68°F to 77°F)
• Protect from moisture and light
• Keep in tightly closed container
• Keep out of reach of children