diloxanide

Action and Spectrum

Actions and Spectrum: 

diloxanide is a medication primarily used to treat infections caused by protozoa, specifically amoebas. It is commonly used to manage and eliminate Entamoeba histolytica infections, which can cause amoebic dysentery and other gastrointestinal problems.  

Action:  

diloxanide works by inhibiting the growth and reproduction of protozoa, particularly Entamoeba histolytica. Its mechanism of action is not entirely understood, but it is believed to interfere with the parasites’ energy metabolism and cell membrane function. Doing so prevents the amoebas from multiplying and causing further harm to the host. 

Spectrum:  

diloxanide has a relatively narrow spectrum of activity, primarily targeting Entamoeba histolytica. It is not effective against a wide range of protozoa or other microorganisms. Therefore, it is not used to treat infections caused by other protozoa or bacteria. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Flatulence 

Urticaria 

Anorexia 

Pruritus  

Nausea 

Vomiting 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

• Hypersensitivity: Individuals with a known hypersensitivity or allergy to diloxanide or its components should not use this medication. 
• Severe Liver Disease: diloxanide is primarily metabolized by the liver, so individuals with severe liver disease should use this medication cautiously or avoid it altogether. Liver function should be monitored during treatment. 
• Pregnancy and Breastfeeding: The safety of diloxanide during pregnancy and breastfeeding has not been well-established.  
• Pediatric Use: diloxanide is typically not recommended for use in infants below the age of 2 years unless prescribed by a pediatrician and carefully monitored. 
• Alcohol Consumption: diloxanide is usually taken with alcohol-free beverages. Some formulations of the medication may contain alcohol, so it’s important to check the product label and avoid alcohol consumption while taking diloxanide. 
• Renal Impairment: While the liver primarily metabolizes diloxanide, it is excreted by the kidneys. Individuals with significant renal impairment may need dosage adjustments or monitoring while using this medication. 
• Drug Interactions: diloxanide may interact with other medications, including certain anticoagulants and drugs that affect liver function.  
• Neurological Disorders: Although rare, there have been reports of neurological adverse effects associated with diloxanide, particularly at high doses or during prolonged treatment. Patients with pre-existing neurological disorders should use diloxanide cautiously and be monitored for neurological symptoms. 

Caution 

• Liver Function: diloxanide is primarily metabolized by the liver. Individuals with pre-existing liver conditions should use this medication cautiously, and liver function should be monitored during treatment. If liver abnormalities occur, the use of diloxanide may need to be reevaluated. 
• Renal Function: While the liver primarily metabolizes diloxanide, it is excreted by the kidneys. Individuals with significant renal impairment may need dosage adjustments or monitoring while using this medication. 
• Pediatric Use: diloxanide is typically not recommended for use in infants below the age of 2 years unless prescribed by a pediatrician and carefully monitored. 
• Pregnancy and Breastfeeding: The safety of diloxanide during pregnancy and breastfeeding has not been well-established.  
• Alcohol Consumption: Some formulations of diloxanide may contain alcohol. It’s important to check the product label and avoid alcohol consumption while taking diloxanide to prevent potential interactions or adverse effects. 
• Neurological Disorders: Although rare, there have been reports of neurological adverse effects associated with diloxanide, particularly at high doses or during prolonged treatment. Patients with pre-existing neurological disorders should use diloxanide cautiously and be monitored for neurological symptoms. 
• Drug Interactions: diloxanide may interact with other medications, including certain anticoagulants and drugs that affect liver function.  
• Allergies: Patients with known allergies or hypersensitivity to diloxanide or its components should not use this medication. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: Not assigned. 

Lactation:   

Excreted into human milk: Not known. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• <b>Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence, these categories of drugs need to be avoided by pregnant women.    
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

diloxanide is an antiprotozoal medication primarily used to treat infections caused by Entamoeba histolytica, a protozoan parasite responsible for amoebic dysentery and gastrointestinal infections. diloxanide’s exact mechanism of action is not fully understood. Still, it is generally thought to interfere with the parasites’ energy metabolism and cell membrane function, inhibiting their growth and replication. The medication is administered orally, typically in the form of tablets or suspension, and it is primarily metabolized by the liver before being excreted.

diloxanide is often used with other antimicrobial agents like metronidazole or tinidazole to effectively treat amoebiasis. It has a limited spectrum of activity primarily targeting Entamoeba histolytica and is ineffective against a wide range of protozoa or other microorganisms. diloxanide should be used under the guidance of a healthcare professional, with dosing and duration of treatment determined based on the individual’s condition and the severity of the infection. 

Pharmacodynamics: 

Mechanism of action: The exact mechanism of action of diloxanide is not fully understood, but it is believed to primarily target protozoan parasites, particularly Entamoeba histolytica, which causes amoebic infections, including amoebic dysentery.  

• Interference with Energy Metabolism: diloxanide is thought to interfere with the energy metabolism of protozoa like Entamoeba histolytica. Protozoa, similar to other organisms, rely on various metabolic processes to generate energy for their survival and reproduction. diloxanide may disrupt key metabolic pathways within the parasites, potentially affecting their ability to produce energy. 
• Cell Membrane Function: diloxanide may also affect the integrity and function of cell membranes in these parasites. Cell membranes are crucial for various cellular processes, including maintaining cell structure and regulating the passage of ions and molecules in and out of the cell. Disruption of these functions could impair the parasites’ ability to survive and reproduce. 

Pharmacokinetics: 

Absorption 

diloxanide is usually administered orally in the form of tablets or suspension. It is believed to be well-absorbed from the gastrointestinal tract, primarily in the small intestine. The exact details of its absorption, including factors affecting it, are not extensively documented in the literature. 

Distribution 

diloxanide’s distribution in the body is not well-documented, but it is thought to be distributed to various tissues and fluids. It may reach therapeutic concentrations in the gastrointestinal tract, primarily acting against Entamoeba histolytica. 

Metabolism 

diloxanide undergoes hepatic metabolism (metabolism in the liver). The exact metabolic pathways and metabolites are poorly elucidated in the available literature. However, the liver metabolizes many drugs, and diloxanide is likely subject to various enzymatic transformations in this organ. 

Elimination and Excretion 

The excretion of diloxanide and its metabolites is primarily through the urine. The kidneys filter the drug and its breakdown products from the bloodstream and excrete them in the urine. The exact excretion pathways and the elimination half-life of diloxanide may vary among individuals and may be influenced by factors like renal function. 

Adminstartion

Administration: 

diloxanide is typically administered orally in the form of tablets or suspension.  

Dosage: The appropriate dosage of diloxanide can vary based on factors such as the specific formulation of the medication, the age and weight of the patient, and the severity of the infection.  

Timing: diloxanide is usually taken two or three times a day. It’s important to space out the doses evenly throughout the day to maintain a consistent level of drug in your system. Follow your healthcare provider’s recommendations for the timing of doses. 

Food and Beverage: diloxanide can typically be taken with or without food. However, some formulations may be more effective when taken with food or a specific type of beverage. Check the product label/ask your healthcare provider for guidance on whether you should take diloxanide with food or a particular type of liquid. 

Suspension (Liquid Form): If you use a liquid form of diloxanide, shake the bottle well before each use to ensure the medication is evenly mixed. Use an appropriate measuring device, such as a dosing syringe or measuring cup, to accurately measure the prescribed dose. 

Complete the Full Course: Even if you start feeling better before you’ve finished the entire course of diloxanide, it’s crucial to complete the full prescribed treatment course. Stopping the medication prematurely can lead to the recurrence of the infection or the development of antibiotic resistance. 

Alcohol: Some diloxanide formulations may contain alcohol, so checking the product label is essential. If your medication contains alcohol, avoid consuming alcoholic beverages while taking it to prevent potential interactions. 

Follow-up: Depending on the nature of the infection and your healthcare provider’s recommendations, you may be asked to return for follow-up appointments to ensure the infection has been successfully treated. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: diloxanide 

Why do we use diloxanide? 

diloxanide is a medication primarily used to treat infections caused by certain protozoa, particularly Entamoeba histolytica.  

• Amoebiasis: diloxanide is commonly used to treat infections caused by Entamoeba histolytica, a protozoan parasite responsible for amoebic dysentery and other gastrointestinal problems. Amoebiasis is characterized by symptoms such as diarrhea, abdominal pain, and fever. diloxanide is often prescribed with other medications like metronidazole or tinidazole to effectively treat this infection. 
• Asymptomatic Carriers: In some cases, individuals may carry the cysts of Entamoeba histolytica in their intestines without displaying any symptoms of amoebiasis. diloxanide can be prescribed to asymptomatic carriers to prevent the development of symptomatic disease. 
• Post-Travel Prophylaxis: diloxanide may be used as a preventive measure in individuals who have traveled to regions with a high prevalence of amoebiasis. Travelers to endemic areas may be at risk of exposure to Entamoeba histolytica, and diloxanide can help prevent the development of infection.