DILOXANIDE TABLETS

Indications

• Asymptomatic intestinal amebiasis
• Amebic dysentery (as part of combination therapy)

Dosage

Children: Refer to the BNF for Children for specific paediatric dosing guidelines.

Adults: Refer to the BNF for specific adult dosing guidelines.

Mechanism of action

The exact mechanism of action of diloxanide is unknown. It may inhibit protein synthesis, which contributes to its efficacy against the trophozoites of E. histolytica.

Pharmacodynamics

Diloxanide acts as a luminal amebicide, effectively destroying the trophozoites of Entamoeba histolytica. The drug's action helps in reducing the load of the organism in the intestinal lumen, thereby preventing the formation of cysts and subsequent transmission of the infection.

Pharmacokinetics

Diloxanide is administered orally and is hydrolyzed in the gastrointestinal tract to release the active ingredient. The pharmacokinetics, including absorption, distribution, metabolism, and excretion specifics, are not well-documented, indicating a need for further research in these areas.

Pregnancy

There is limited data on the use of diloxanide during pregnancy. It should only be used if clearly needed.

Breast-feeding

Diloxanide is excreted in breast milk, caution should be exercised when administering to nursing mothers.

Storage

Store in a cool, dry place, away from direct sunlight. Keep out of reach of children.

Formulations

• tablets

Indications

• Asymptomatic intestinal amebiasis
• Amoebic dysentery (mild cases)

Dosage

Children: Refer to the relevant prescribing information or guidelines.

Adults: Refer to the relevant prescribing information or guidelines.

Mechanism of action

Diloxanide furoate works by inhibiting the growth of the Entamoeba histolytica trophozoites in the intestines. The active metabolite, diloxanide, disrupts the cellular function of the protozoa, leading to cell lysis and death. It is thought to interfere with the protozoan's ability to utilize glucose and other nutrients, thereby inhibiting their metabolic processes.

Pharmacodynamics

Diloxanide furoate's effectiveness against Entamoeba histolytica is due to its ability to alter the protozoan's metabolic pathways, particularly affecting glucose metabolism. This results in a reduction of the organism's viability and ability to replicate. The drug's action is primarily localized to the intestinal lumen, minimizing systemic exposure and associated side effects.

Pharmacokinetics

After oral administration, diloxanide furoate is rapidly absorbed and metabolized to its active form, diloxanide. The drug is extensively metabolized in the liver, with a half-life of approximately 12 hours. It is excreted mainly in the feces, with minimal renal excretion. The bioavailability of diloxanide is enhanced when taken with food, leading to improved therapeutic outcomes.

Adverse effects

• Nausea
• Vomiting
• Diarrhea
• Abdominal pain
• Dizziness
• Headache

Precautions

• Use with caution in patients with a history of gastrointestinal disorders.
• Monitor liver function tests in patients with pre-existing liver conditions.

Pregnancy

There is limited data on the use of diloxanide furoate in pregnancy. It should be used only if clearly needed and the potential benefits justify the potential risks to the fetus.

Breast-feeding

It is not known whether diloxanide furoate is excreted in human milk. Caution should be exercised when administering to nursing mothers.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Oral tablet
• Oral suspension

Mechanism of action

Unknown. Diloxanide may inhibit protein synthesis.

Pharmacodynamics

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.