Skip to content

What is the drug diloxanide used for?

3 min read

According to the World Health Organization, diloxanide is on its List of Essential Medicines, underscoring its importance in treating certain parasitic infections. So, what is the drug diloxanide used for? It is an antiprotozoal medication primarily prescribed to manage intestinal amoebiasis, particularly for individuals who are asymptomatic carriers.

Quick Summary

Diloxanide is an antiprotozoal drug that functions as a luminal amebicide to treat intestinal amoebiasis, especially for carriers of Entamoeba histolytica who show no symptoms.

Key Points

  • Antiprotozoal Action: Diloxanide is a luminal amebicide, acting exclusively within the intestinal tract to target the protozoan Entamoeba histolytica.

  • Asymptomatic Carrier Treatment: Its primary use is to treat asymptomatic individuals who are passing E. histolytica cysts, preventing both the progression of disease and its transmission.

  • Prodrug Activation: The medication is administered as a prodrug, diloxanide furoate, which is hydrolyzed in the gastrointestinal tract to release the active drug.

  • Combination Therapy: For invasive or extra-intestinal amoebiasis, diloxanide is used in combination with tissue amebicides like metronidazole after the systemic infection is addressed.

  • Safety Profile: Diloxanide is generally well-tolerated, with the most common side effects being mild gastrointestinal disturbances and flatulence.

  • Limited Availability: While on the WHO's essential medicines list, diloxanide is not commercially available in many developed nations.

In This Article

Before taking any medication, it is essential to consult with a healthcare professional. Information provided here is for general knowledge and should not be considered medical advice.

Diloxanide is an antiparasitic agent that plays a crucial role in treating intestinal amoebiasis, an infection caused by the protozoan Entamoeba histolytica. The drug's most common form is diloxanide furoate, a prodrug that is hydrolyzed in the gut to release the active compound, diloxanide. Its action is localized to the intestinal lumen, making it effective against parasitic forms residing within the digestive tract but not in tissues outside the intestine.

Mechanism of Action: How Diloxanide Targets the Parasite

Diloxanide's exact mechanism of action is not completely understood, but its effects are specific to the parasite's life cycle within the intestines. The drug is believed to interfere with protein synthesis in the E. histolytica trophozoites. Trophozoites are the active, feeding stage of the amoeba that can cause tissue damage. By disrupting the trophozoites, diloxanide prevents their maturation into hardy cysts, which are then shed in stool and can infect others. Since the drug is poorly absorbed into the bloodstream, it remains highly concentrated in the gut, maximizing its effect on the parasites located there.

Clinical Applications of Diloxanide

Diloxanide's primary use is centered on intestinal amoebiasis. Its application varies depending on whether the infection is asymptomatic or invasive.

  • Treatment of Asymptomatic Carriers: For individuals who carry E. histolytica cysts in their intestines but show no symptoms, diloxanide is a first-line or second-line treatment option, depending on regional guidelines. Eradicating the cysts is vital to prevent future symptomatic disease in the carrier and to stop the spread of the infection to others.
  • Combination Therapy for Invasive Disease: When amoebiasis becomes invasive, affecting the intestinal wall (amoebic colitis) or spreading to other organs like the liver (extra-intestinal amoebiasis), diloxanide is not used alone. In these cases, a tissue-penetrating amebicide such as metronidazole is needed to treat the systemic infection. Diloxanide is then administered alongside or sequentially with the tissue amebicide to clear any remaining parasites from the intestinal lumen.

Administration

Diloxanide furoate is typically administered orally. The specific amount and duration of treatment are determined by a healthcare professional based on individual factors. It is crucial that patients complete the full course of treatment as prescribed to ensure the complete eradication of the parasite and prevent recurrence.

Common Side Effects

Diloxanide is generally well-tolerated, and side effects are usually mild and transient. The most frequently reported adverse effects include:

  • Gastrointestinal upset, such as nausea, vomiting, or abdominal pain.
  • Increased flatulence.
  • Diarrhea or cramping.
  • Skin reactions, including itchiness and hives.
  • Less common effects may include headaches or dizziness.

Serious adverse events are rare. However, patients should contact a healthcare provider if side effects are severe or persistent.

Comparison of Diloxanide with Other Amebicides

Feature Diloxanide Furoate Paromomycin Metronidazole
Drug Class Luminal Amebicide Luminal Amebicide Tissue Amebicide
Primary Indication Asymptomatic intestinal amoebiasis Asymptomatic intestinal amoebiasis Invasive amoebiasis (colitis, abscesses)
Mechanism of Action Inhibits protein synthesis (suspected) Inhibits protein synthesis Damages DNA and proteins
Location of Action Primarily within the intestinal lumen Primarily within the intestinal lumen Systemic (intestinal wall and extra-intestinal tissues)
Asymptomatic Efficacy Highly effective (cure rates around 86% historically) Considered first-line treatment Not used for asymptomatic cases
Combination Therapy Often used after metronidazole for invasive cases Less common for combination therapy Primary drug for invasive amoebiasis

Conclusion: The Place of Diloxanide in Amoebiasis Management

Diloxanide remains a critical component in the global fight against amoebiasis. Its specific action as a luminal amebicide makes it highly effective for treating asymptomatic carriers and preventing the spread of infection. Although not widely available in some developed countries, its inclusion on the WHO Essential Medicines list highlights its importance in areas where parasitic infections are more common. For invasive amoebic disease, it is effectively used in conjunction with tissue amebicides like metronidazole to ensure complete eradication of the parasite. Patients should always consult a healthcare professional to determine the appropriate treatment strategy for their specific situation.

For more detailed prescribing information, refer to the drug's profile on PubMed: Diloxanide in amoebiasis management: Unravelling the mechanism....

Frequently Asked Questions

Diloxanide is used to treat asymptomatic carriers of intestinal amoebiasis caused by Entamoeba histolytica, eliminating cysts from the gut and preventing the spread of infection.

Diloxanide furoate is hydrolyzed into the active drug, diloxanide, in the intestine. It works as a luminal amebicide, likely by inhibiting protein synthesis in the E. histolytica trophozoites, and has little to no activity outside the gut.

No, diloxanide is not effective against extra-intestinal forms of amoebiasis, such as liver abscesses, because it does not penetrate body tissues. It must be used alongside a tissue amebicide like metronidazole for such conditions.

Common side effects include gastrointestinal issues such as flatulence, nausea, vomiting, abdominal pain, and sometimes skin reactions like rash or itching.

No, diloxanide is not currently approved for commercial use in the United States, although it has been used in the past via the CDC. Availability varies by country, and it has been discontinued in some regions like the UK.

A typical treatment course with diloxanide furoate is ten days. It is important to complete the entire prescribed course to ensure the infection is fully cleared.

Diloxanide is generally contraindicated during pregnancy (especially the first trimester) and lactation. Patients who are pregnant, breastfeeding, or planning to become pregnant should consult their doctor.

References

  1. 1
  2. 2
  3. 3
  4. 4
  5. 5
  6. 6

Medical Disclaimer

This content is for informational purposes only and should not replace professional medical advice.