Usage
- This combination medication is primarily prescribed for the treatment of intestinal amoebiasis, a parasitic infection caused by Entamoeba histolytica. It is also effective against giardiasis, and sometimes used for amebic liver abscess, trichomoniasis, and bacterial vaginosis. It addresses not only the infection itself, but also helps alleviate the associated gastrointestinal symptoms like bloating, flatulence, and stomach cramps.
- Pharmacological Classification: Antiprotozoal, Antibiotic, Antiflatulent.
- Mechanism of Action: Diloxanide furoate acts as a luminal amoebicide, targeting the parasite within the intestinal lumen. Tinidazole, a nitroimidazole antibiotic, disrupts the parasite’s DNA, leading to its demise. Simethicone, an anti-foaming agent, reduces gas bubbles in the GI tract, providing relief from bloating and discomfort.
Alternate Names
- No widely recognized alternate names exist for this specific combination.
- Brand Names: Tinilox-MPS, Entrogyl, Metrodif MPS (Note: Brand availability may vary regionally.)
How It Works
- Pharmacodynamics: Diloxanide furoate exerts its antiamoebic action primarily in the intestinal lumen. Tinidazole exhibits broad-spectrum activity against various protozoa and anaerobic bacteria. Simethicone decreases the surface tension of gas bubbles, aiding their coalescence and expulsion.
- Pharmacokinetics: Diloxanide furoate is poorly absorbed from the GI tract, which concentrates its action within the intestines. Tinidazole achieves good systemic absorption after oral administration, reaching peak plasma levels in about two hours. It is metabolized in the liver and excreted primarily in the urine. Simethicone is not absorbed systemically, and is eliminated unchanged in the feces.
- Mode of Action: Diloxanide furoate’s precise mode of action is not fully elucidated, but may involve interference with the parasite’s energy metabolism. Tinidazole is reduced intracellularly within the microorganism, forming cytotoxic free radicals that damage DNA, thus inhibiting microbial growth. Simethicone acts physically to reduce gas formation and accumulation, without affecting chemical processes.
- Elimination Pathways: Diloxanide furoate is mostly excreted unchanged in the feces. Tinidazole is predominantly eliminated via renal excretion, while simethicone passes through the GI tract and is eliminated in the feces.
Dosage
Standard Dosage
Adults:
- Tablets: One tablet (Diloxanide 250mg + Tinidazole 300mg + Simethicone 25mg or similar strength) three times daily for 5-10 days.
- Suspension: 5ml containing a proportionated pediatric dose, based on age or weight, three times daily for 5-10 days, or as prescribed by a doctor.
Children:
- Dosage is weight or age-dependent and should be determined by a physician. Suspension formulations are typically used for children.
- Pediatric Safety Considerations: Use with caution in children younger than 3 years. Close monitoring for adverse effects is crucial.
Special Cases:
- Elderly Patients: Dose adjustment might be necessary depending on renal and hepatic function. Start with lower doses and adjust based on clinical response.
- Patients with Renal Impairment: Administer with caution. Dose reduction may be necessary based on creatinine clearance.
- Patients with Hepatic Dysfunction: Administer with caution. Dose adjustment might be needed due to reduced metabolic capacity.
- Patients with Comorbid Conditions: Evaluate for potential drug interactions and consider any underlying diseases that could influence drug metabolism or clearance.
Clinical Use Cases
The provided sources focus primarily on amebiasis and giardiasis treatment. Dosing for other specific clinical situations like intubation, surgical procedures, mechanical ventilation, or ICU use is not provided. Dosage recommendations for these cases should be made on a patient-specific basis by the attending physician.
Dosage Adjustments
Dosage should be individualized according to the patient’s clinical condition, age, weight, and renal/hepatic function. Therapeutic drug monitoring may be beneficial in certain cases to ensure efficacy and minimize adverse effects.
Side Effects
Common Side Effects:
Nausea, vomiting, headache, diarrhea, dry mouth, metallic taste, dizziness, fatigue, abdominal pain, skin rash.
Rare but Serious Side Effects:
Severe skin rash, hives, difficulty breathing, unusual tiredness or weakness, paresthesias, ataxia, seizures, blood dyscrasias, and other hypersensitivity reactions.
Long-Term Effects:
Long-term use of tinidazole can lead to peripheral neuropathy.
Adverse Drug Reactions (ADR):
Serious ADRs require immediate medical attention and may include anaphylaxis, Stevens-Johnson syndrome, and blood dyscrasias.
Contraindications
- Hypersensitivity to any of the components (diloxanide furoate, tinidazole, or simethicone), other nitroimidazole derivatives or any component of the formulation.
- First trimester of pregnancy.
- Patients with active neurological disorders, blood dyscrasias, or severe hepatic impairment.
- History of seizures or other neurological conditions that might be exacerbated by the medication.
Drug Interactions
- Alcohol: Avoid alcohol during therapy and for at least 72 hours after the last dose due to disulfiram-like reactions (flushing, headache, nausea, vomiting, abdominal cramps, and palpitations).
- Anticoagulants (e.g., warfarin): Enhanced anticoagulant effect. Monitor INR closely and adjust warfarin dose as needed.
- Lithium: Tinidazole can increase lithium levels. Monitor lithium levels and adjust dosage as needed.
- Phenytoin: Tinidazole may elevate phenytoin levels. Monitor phenytoin serum concentrations and adjust its dosage accordingly.
- Disulfiram: Concurrent use may result in neurotoxicity.
- CYP450 substrates: Tinidazole is a CYP3A4 inhibitor and could affect the metabolism of drugs metabolized by this pathway.
Pregnancy and Breastfeeding
- Pregnancy: Use only if clearly needed and after careful assessment of the risks and benefits. Avoid use during the first trimester.
- Breastfeeding: Tinidazole is excreted in breast milk. Interrupt breastfeeding during therapy and for at least 72 hours after the last dose.
Drug Profile Summary
- Mechanism of Action: Diloxanide furoate is a luminal amoebicide; Tinidazole damages DNA of microorganisms; Simethicone reduces gas accumulation.
- Side Effects: Nausea, metallic taste, diarrhea, vomiting, headache. Rarely, severe skin reactions and blood dyscrasias.
- Contraindications: Hypersensitivity, first trimester of pregnancy, neurological disorders, blood dyscrasias, hepatic impairment.
- Drug Interactions: Alcohol, anticoagulants, lithium, phenytoin.
- Pregnancy & Breastfeeding: Not recommended during the first trimester and while breastfeeding.
- Dosage: Refer to the dosage section. Varies based on age, weight, and clinical indication.
- Monitoring Parameters: Liver function tests, complete blood count (especially during long-term therapy), renal function tests.
Popular Combinations
- This specific combination itself is a common formulation. Additional agents might be added to address specific symptoms, such as antiemetics for nausea and vomiting.
Precautions
- Assess for underlying liver or kidney disease, blood disorders, and hypersensitivity.
- Advise patients to avoid alcohol during and after treatment.
- Caution patients about potential dizziness and drowsiness and recommend avoiding driving or operating machinery.
- Encourage adequate hydration, especially in patients with diarrhea.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Diloxanide + Simethicone + Tinidazole?
A: Refer to the Dosage section. It varies depending on age, weight, and the specific medical condition being treated. A physician should determine the appropriate dosage regimen.
Q2: What are the most common side effects?
A: Nausea, metallic taste, diarrhea, dry mouth, vomiting, headache, fatigue, and dizziness.
Q3: Is it safe to drink alcohol while taking this medication?
A: No, alcohol should be strictly avoided during treatment and for at least 72 hours after the last dose due to potential disulfiram-like reactions.
Q4: Can pregnant or breastfeeding women take this medication?
A: It’s generally contraindicated during the first trimester of pregnancy and should be used cautiously during later stages only if the benefits clearly outweigh the risks. Breastfeeding should be interrupted during treatment and for 72 hours after the last dose.
Q5: How long does the treatment usually last?
A: The usual duration is 3-10 days, depending on the infection and severity. Always complete the full course prescribed, even if symptoms improve earlier.
Q6: What should I do if I miss a dose?
A: Take the missed dose as soon as you remember. If it’s almost time for the next dose, skip the missed dose and continue with your regular schedule. Do not double the dose.
Q7: Are there any dietary restrictions while taking this medication?
A: No specific dietary restrictions are usually required, but maintaining good hydration is important, especially in patients with diarrhea. Avoid foods that trigger GI discomfort.
Q8: Can this combination be used in children?
A: Yes, it can be used in children, with adjustments in dosage based on age or weight. Liquid formulations are typically preferred for children under the age of three. Closely monitor children for adverse reactions.
Q9: What are the signs of an allergic reaction to this medication?
A: Watch for signs like skin rash, itching, hives, swelling (especially of the face, tongue, or throat), severe dizziness, and difficulty breathing. Seek immediate medical attention if any of these occur.
