Diloxide500 mg

Diloxide is a luminal-acting amoebicide indicated for the treatment of intestinal amoebiasis caused by Entamoeba histolytica. Its indications, by strength of evidence, are:

• Established use — asymptomatic intestinal amoebiasis (cyst passers): Diloxide is used to eradicate E. histolytica cysts from the bowel lumen in patients who are passing cysts but have no invasive symptoms.
• Guideline-supported adjunct use — follow-up after invasive amoebiasis: after a tissue-acting agent (e.g., metronidazole) has been used to treat invasive intestinal amoebiasis (amoebic dysentery) or amoebic liver abscess, Diloxide is given as a follow-up course to eradicate any residual luminal organisms and reduce the risk of relapse or continued transmission.

Diloxide is not effective as monotherapy for invasive or extraintestinal amoebiasis (e.g., amoebic liver abscess or amoebic dysentery) because it acts only within the bowel lumen and is poorly absorbed into tissue; invasive disease requires a tissue-acting amoebicide first.

Each tablet contains Diloxanide Furoate INN 500 mg as the active ingredient, along with standard pharmaceutical excipients.

Diloxide is a synthetic dichloroacetamide derivative that acts as a luminal amoebicide. Unlike tissue-acting amoebicides such as metronidazole, Diloxide exerts its antiparasitic effect primarily within the lumen of the large intestine, where it is only minimally absorbed. It is used mainly to eliminate the cyst stage of Entamoeba histolytica from the bowel.

Diloxide is hydrolyzed in the gut to diloxanide (the active moiety) and furoic acid. A portion of the diloxanide is absorbed and later excreted mainly as the glucuronide conjugate in urine, while the unabsorbed fraction remains in the gut lumen where it exerts its amoebicidal action.

Diloxide belongs to the therapeutic class of amoebicides, specifically the subclass of luminal-acting antiprotozoal agents used in the management of intestinal amoebiasis.

The precise mechanism of action of Diloxanide Furoate has not been fully elucidated, but it is believed to act directly on amoebic trophozoites within the intestinal lumen, interfering with protein synthesis and preventing encystation, which leads to the death of the organism before cyst formation and passage in the stool.

Pharmacokinetics: After oral administration, Diloxanide Furoate is rapidly hydrolyzed by intestinal esterases into diloxanide and furoic acid. Approximately 90% of the diloxanide fraction is absorbed from the gut, rapidly conjugated with glucuronic acid, and excreted in the urine within 24-48 hours; the remainder stays in the bowel lumen, where it produces the amoebicidal effect. Peak plasma concentrations of diloxanide occur roughly 1-2 hours after dosing.

Diloxide tablets should be swallowed with a glass of water, preferably with meals, to reduce the chance of gastrointestinal discomfort. Doses should be spaced evenly (e.g., every 8 hours) across the day, and the complete prescribed course should be finished even if the patient feels better before it ends.

No well-established, clinically significant drug interactions have been documented for Diloxide in the medical literature. As with any medicine, patients should inform their physician of all other medications, supplements, or herbal products they are taking so that any theoretical interaction can be assessed on an individual basis.

Diloxide is generally well tolerated. The most common adverse effect is:

• Flatulence — the most frequently reported side effect, occurring in a substantial proportion of patients.
• Mild gastrointestinal upset, including nausea, vomiting, abdominal cramps, and loose stools.
• Less commonly: pruritus, urticaria (skin rash/itching), and dizziness.

Most side effects are mild and self-limiting and do not usually require discontinuation of therapy.

Pregnancy: Safety data on the use of Diloxide in pregnancy are limited. Diloxide should be used during pregnancy, particularly in the first trimester, only if clearly needed and if the potential benefit justifies the potential risk to the fetus; a physician should be consulted before use.

Lactation: It is not well established whether Diloxide or its metabolites pass into breast milk. Use during breastfeeding should occur only under medical supervision, weighing the benefit to the mother against any potential risk to the nursing infant.

Diloxide is a luminal-acting agent only and is not effective as monotherapy for invasive or extraintestinal amoebiasis (e.g., amoebic liver abscess or fulminant amoebic dysentery); such cases require a tissue-acting amoebicide (e.g., metronidazole), with Diloxide used afterward to clear residual luminal cysts.

Take Diloxide exactly as prescribed; do not stop, extend, skip doses, or share this medicine with others without medical advice, since an incomplete course may fail to eradicate luminal cysts and can contribute to continued transmission.

Safety and efficacy in children under 2 years of age have not been well established. No well-established dose adjustment exists for renal or hepatic impairment; such patients should be treated with caution and under close medical supervision.

Specific data on Diloxide overdose are limited. In the event of a suspected overdose, seek immediate medical attention or contact a poison control center/emergency services right away. Management is generally supportive, based on the patient's symptoms and clinical condition; do not attempt specific home treatment without professional medical guidance.

Store at room temperature (below 30°C), away from light and moisture. Keep out of reach of children.

Renal impairment: No well-established dose adjustment is available for Diloxide in renal impairment; use with caution and physician oversight.

Hepatic impairment: No well-established dose adjustment is available for Diloxide in hepatic impairment; use with caution and physician oversight.

Elderly: No specific dose adjustment has been established for elderly patients; the standard adult dose is generally used.

Children under 2 years: Safety and efficacy of Diloxide have not been established in this age group.

Pregnancy and lactation: See Pregnancy and Lactation section above.

The standard course of Diloxide is 10 days, regardless of indication. The full course should always be completed, and a follow-up stool examination is typically recommended after treatment to confirm eradication of cysts; the course may be repeated once on medical advice if cysts persist.

Diloxanide Furoate belongs to the drug class of amoebicides (luminal-acting antiprotozoal agents).

Diloxanide Furoate is hydrolyzed in the intestine to diloxanide, its active amoebicidal moiety. Diloxanide acts directly on Entamoeba histolytica trophozoites within the bowel lumen, interfering with the organism's protein synthesis and preventing normal encystation, which leads to death of the parasite. Because most of the drug's effect occurs within the gut lumen and systemic absorption is limited, Diloxanide Furoate is effective against luminal (cyst) forms of the parasite but not against tissue-invasive disease.

In children aged 2 years and older, Diloxide may be used for asymptomatic intestinal amoebiasis or as follow-up after treatment of invasive amoebiasis, at a dose of 20 mg/kg/day in three divided doses for 10 days (not exceeding the adult dose of 500 mg per dose).

Safety and efficacy of Diloxide in children under 2 years of age have not been established; use in this age group should only occur under close specialist supervision if considered essential.