Usage
- This combination medication is prescribed for the treatment of intestinal amoebiasis, a parasitic infection of the intestines caused by Entamoeba histolytica. It is effective against both symptomatic and asymptomatic cases. It also provides relief from gas, bloating, and abdominal discomfort associated with these conditions.
- Pharmacological Classification: Antiamoebic, Antiprotozoal, Antimicrobial, Antiflatulent
- Mechanism of Action: Diloxanide furoate acts as a luminal amoebicide, directly targeting amoebae in the intestinal lumen. Ornidazole is a nitroimidazole derivative that disrupts DNA synthesis and protein synthesis in anaerobic bacteria and protozoa. Simethicone is an anti-foaming agent that reduces the surface tension of gas bubbles, aiding their expulsion and relieving bloating.
Alternate Names
- There are no officially recognized alternate names for this specific combination. However, the individual components are sometimes referred to as:
- Diloxanide furoate: Diloxanide
- Ornidazole: Ornidazol
- Simethicone: Activated dimethicone
- Brand Names: Amicline Plus, Amirid, Entrogyl-OZ, Metrogyl Compound Plus
How It Works
- Pharmacodynamics: Diloxanide furoate acts directly on amoebae within the intestinal lumen, exhibiting amoebicidal activity. Ornidazole, a prodrug, enters the microbial cell where it is reduced to its active form. This active form interacts with the organism’s DNA, causing strand breakage, inhibition of DNA repair and ultimately cell death. Simethicone reduces the surface tension of gas bubbles, facilitating their coalescence and promoting passage. It does not reduce the formation of gas but alleviates its effects.
- Pharmacokinetics: Diloxanide furoate is absorbed from the gastrointestinal tract after oral administration. It is then hydrolyzed to diloxanide, the active form. Ornidazole is also well-absorbed orally. Both diloxanide and ornidazole are metabolized in the liver and excreted primarily in the urine. Simethicone is not absorbed and is eliminated unchanged in the feces.
- Mode of Action: Diloxanide’s exact mechanism of action is not completely understood, but it appears to act directly on amoebae. Ornidazole interacts with microbial DNA to cause cellular damage. Simethicone physically alters the surface tension of gas bubbles.
- Receptor Binding/Enzyme Inhibition/Neurotransmitter Modulation: Not applicable for this combination. Simethicone works through a physical mechanism and does not involve receptor binding, enzyme inhibition, or neurotransmitter modulation. The exact mechanism for diloxanide is uncertain. Ornidazole inhibits DNA synthesis.
- Elimination Pathways: Diloxanide and Ornidazole are metabolized in the liver and excreted primarily through the kidneys. Simethicone, being unabsorbed, is eliminated via the feces.
Dosage
Standard Dosage
Adults: One tablet containing Diloxanide furoate 375mg, Ornidazole 250mg, and Simethicone 25mg, taken three times a day, for 10 days.
Children: For children weighing more than 25 kg, Diloxanide can be given at a dose of 20 mg/kg body weight per day, divided into three doses, for 10 days. Ornidazole pediatric dosing needs to be determined based on clinical guidelines.
Special Cases:
- Elderly Patients: No specific dosage adjustments are typically necessary, but monitor for adverse effects.
- Patients with Renal Impairment: Use with caution. Dosage adjustment may be needed.
- Patients with Hepatic Dysfunction: Use with caution as both diloxanide and ornidazole are metabolized in the liver.
- Patients with Comorbid Conditions: Evaluate on a case-by-case basis, considering potential drug interactions.
Clinical Use Cases The drug combination is not typically used in the listed scenarios (Intubation, Surgical Procedures, Mechanical Ventilation, Intensive Care Unit (ICU) Use, Emergency Situations)
Dosage Adjustments Adjust the dosage for patients with renal or hepatic impairment based on clinical assessment and laboratory parameters.
Side Effects
Common Side Effects
- Nausea
- Vomiting
- Headache
- Dizziness
- Flatulence
- Metallic taste
- Loss of appetite
Rare but Serious Side Effects
- Peripheral neuropathy (Ornidazole)
- Seizures (Ornidazole)
Long-Term Effects
Generally, this combination is used for a short duration, so long-term effects are uncommon.
Adverse Drug Reactions (ADR)
- Severe skin reactions (rare)
Contraindications
- Hypersensitivity to any of the components, including other nitroimidazole derivatives.
- First trimester of pregnancy (Ornidazole)
- Certain neurological disorders (Ornidazole)
- Severe hepatic impairment
Drug Interactions
- Alcohol (Ornidazole): Disulfiram-like reaction.
- Anticoagulants (Ornidazole): Enhanced anticoagulant effects.
- Anti-seizure medications (Ornidazole): Altered drug metabolism.
- Lithium (Ornidazole): Increased lithium levels.
- Cimetidine (Ornidazole): Altered drug metabolism.
Pregnancy and Breastfeeding
- Pregnancy: Diloxanide is generally considered safe, but ornidazole should be avoided, especially during the first trimester.
- Breastfeeding: Both drugs are excreted in breast milk; use with caution during breastfeeding. Consider the benefits and risks.
Drug Profile Summary
- Mechanism of Action: Diloxanide: Direct-acting amoebicide; Ornidazole: Inhibits DNA and protein synthesis in anaerobes and protozoa; Simethicone: Reduces surface tension of gas bubbles.
- Side Effects: Nausea, vomiting, headache, dizziness, flatulence, metallic taste, loss of appetite. Rarely: severe skin reactions, peripheral neuropathy, seizures.
- Contraindications: Hypersensitivity, first trimester of pregnancy (Ornidazole), certain neurological disorders, severe hepatic impairment.
- Drug Interactions: Alcohol, anticoagulants, anti-seizure medications, lithium, cimetidine.
- Pregnancy & Breastfeeding: Use with caution. Avoid ornidazole in the first trimester.
- Dosage: Adults: Diloxanide 500 mg TID for 10 days; Ornidazole: varies based on indication; Children: Diloxanide 20 mg/kg/day divided TID for 10 days.
- Monitoring Parameters: Stool examination, liver function tests (if necessary).
Popular Combinations
This specific combination (Diloxanide + Ornidazole + Simethicone) is itself a common formulation. Other combinations might include Diloxanide + Metronidazole + Simethicone or Diloxanide + Tinidazole + Simethicone.
Precautions
- General Precautions: Assess for allergies, hepatic and renal function, and neurological status.
- Pregnant Women: Avoid ornidazole, particularly in the first trimester.
- Breastfeeding Mothers: Use with caution.
- Children & Elderly: Monitor for adverse reactions.
- Lifestyle Considerations: Avoid alcohol during and for at least three days after completing ornidazole therapy.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Diloxanide + Ornidazole + Simethicone?
A: The standard adult dosage is one tablet (Diloxanide 375mg + Ornidazole 250mg + Simethicone 25mg) three times a day for 10 days. Pediatric and special case dosages should be determined based on clinical guidelines.
Q2: What are the most common side effects?
A: Nausea, vomiting, headache, dizziness, flatulence, metallic taste, and loss of appetite are common.
Q3: Can this combination be used during pregnancy?
A: Diloxanide is generally considered safe, but ornidazole should be avoided during pregnancy, especially the first trimester.
Q4: Are there any drug interactions I should be aware of?
A: Yes. Avoid alcohol. Inform patients about potential interactions with anticoagulants, anti-seizure medications, lithium, and cimetidine.
Q5: What is the mechanism of action of each component?
A: Diloxanide acts directly on amoebae in the gut lumen. Ornidazole damages microbial DNA. Simethicone reduces surface tension of gas bubbles.
Q6: How should I counsel my patients about taking this medication?
A: Advise patients to take the medication with food, complete the full course of therapy, and avoid alcohol.
Q7: What should I do if a patient misses a dose?
A: Instruct patients to take the missed dose as soon as remembered unless it is almost time for the next scheduled dose. Never double-dose.
Q8: What monitoring parameters should I consider?
A: Stool examination for clearance of the infection. Liver function tests if clinically indicated.
Q9: What is the difference between this combination and other amoebiasis treatments?
A: This combination addresses amoebiasis, bacterial infections, and gas/bloating, offering a comprehensive approach to managing symptoms and infection.
Q10: When should I suspect an adverse drug reaction, and what should I do?
A: Be vigilant for rare but serious side effects like peripheral neuropathy or seizures (related to ornidazole) or severe skin reactions. Immediately discontinue the medication if these occur and provide appropriate medical care.
