Usage
This combination medication is prescribed for the treatment of various gastrointestinal infections, particularly diarrhea, dysentery, and other infections caused by susceptible bacteria and parasites. It is also effective against amoebiasis, giardiasis, and antibiotic-associated colitis. The simethicone component helps alleviate bloating and gas associated with these conditions.
Pharmacological Classification:
- Metronidazole: Antibacterial, Antiprotozoal
- Ofloxacin: Fluoroquinolone antibiotic
- Simethicone: Anti-flatulent (Gastrointestinal agent)
Mechanism of Action:
Metronidazole disrupts DNA synthesis and integrity in anaerobic bacteria and protozoa. Ofloxacin inhibits bacterial DNA gyrase and topoisomerase IV, essential enzymes for bacterial DNA replication and repair. Simethicone reduces the surface tension of gas bubbles in the gastrointestinal tract, facilitating their passage and relieving bloating.
Alternate Names
No widely recognized alternate names exist for this specific three-drug combination. The individual drugs, however, are sometimes referred to by other names (e.g., metronidazole may be known as Flagyl). Various brand names exist depending on the manufacturer and region. Some examples include:
- Oflofresh M
- Binflox M
- Ellfo-M-DS
- Ofzor-MZ
- Sanflox-MS
- MICROBID M
How It Works
Pharmacodynamics:
Metronidazole exerts its antibacterial and antiprotozoal effects by disrupting DNA structure and function, leading to microbial cell death. Ofloxacin interferes with bacterial DNA replication, preventing bacterial growth and leading to cell death. Simethicone acts physically to reduce surface tension of gas bubbles, promoting their coalescence and expulsion.
Pharmacokinetics:
- Absorption: All three drugs are absorbed orally. Metronidazole has nearly complete oral bioavailability. Ofloxacin absorption can be affected by antacids and multivitamins containing divalent cations (calcium, magnesium, aluminum, iron, zinc). Simethicone is not absorbed systemically.
- Metabolism: Metronidazole is metabolized primarily in the liver. Ofloxacin is also partially metabolized hepatically. Simethicone is not metabolized.
- Elimination: Metronidazole and its metabolites are primarily excreted in the urine. Ofloxacin is excreted both in urine and feces. Simethicone is eliminated unchanged in the feces.
Mode of Action (Cellular/Molecular):
Metronidazole enters the microbial cell and forms cytotoxic metabolites that damage DNA, disrupting cell function. Ofloxacin binds to bacterial DNA gyrase and topoisomerase IV, interfering with DNA supercoiling and strand breakage-reunion, leading to cell death. Simethicone reduces the surface tension of gas bubbles by altering the interface between gas and liquid in the gut.
Elimination Pathways:
- Metronidazole: Primarily renal excretion
- Ofloxacin: Renal and hepatic excretion
- Simethicone: Fecal excretion (unchanged)
Dosage
The dosage of this combination product is determined by the child’s weight and the severity of the infection. Always follow the prescribed dosage.
Standard Dosage
Adults:
This combination is primarily intended for pediatric use and thus, adult dosage is not well-established. Ofloxacin and metronidazole can be prescribed individually for adults, with their respective adult dosages.
Children:
Pediatric dosing varies by weight and age. Consult a pediatrician for precise dosing instructions.
Special Cases:
- Elderly Patients: Use with caution due to potential age-related decline in renal function.
- Patients with Renal Impairment: Dose adjustment may be necessary.
- Patients with Hepatic Dysfunction: Dose modification is advisable due to potential impact on drug metabolism.
- Patients with Comorbid Conditions: Careful monitoring is necessary for patients with conditions such as epilepsy, central nervous system disorders, and QT prolongation.
Clinical Use Cases
This drug combination is not typically employed in the listed medical settings.
Dosage Adjustments
Dose modifications may be required for patients with renal or hepatic impairment.
Side Effects
Common Side Effects
Nausea, vomiting, diarrhea, abdominal pain, headache, metallic taste in the mouth, dizziness.
Rare but Serious Side Effects
Seizures, peripheral neuropathy, severe allergic reactions (rash, itching, swelling, shortness of breath), QT prolongation, Clostridium difficile associated diarrhea.
Long-Term Effects
Peripheral neuropathy with prolonged metronidazole use.
Adverse Drug Reactions (ADR)
Severe allergic reactions, Stevens-Johnson syndrome, toxic epidermal necrolysis.
Contraindications
Hypersensitivity to metronidazole, ofloxacin, simethicone or any component of the formulation. History of seizures or central nervous system disorders. First trimester of pregnancy (metronidazole is contraindicated, and ofloxacin should be avoided).
Drug Interactions
Antacids, iron supplements, multivitamins containing divalent cations (calcium, magnesium, aluminum, iron, zinc) can decrease ofloxacin absorption. Alcohol should be avoided during and 48 hours after metronidazole treatment due to a disulfiram-like reaction. Metronidazole can potentiate the effects of warfarin and other anticoagulants. Ofloxacin may interact with theophylline, warfarin, and some antiarrhythmics. Concomitant use of ofloxacin and metronidazole may increase the risk of QT prolongation.
Pregnancy and Breastfeeding
Pregnancy: Metronidazole is contraindicated in the first trimester. Use with caution during other trimesters only if clearly needed. Ofloxacin should be avoided during pregnancy.
Breastfeeding: Metronidazole is excreted in breast milk. Breastfeeding should be interrupted during and for a period after treatment. Ofloxacin should also be avoided during breastfeeding.
Drug Profile Summary
- Mechanism of Action: Ofloxacin inhibits bacterial DNA gyrase. Metronidazole damages DNA of anaerobic bacteria and protozoa. Simethicone reduces the surface tension of gas bubbles.
- Side Effects: Nausea, vomiting, diarrhea, headache, metallic taste, dizziness. Serious side effects: seizures, peripheral neuropathy.
- Contraindications: Hypersensitivity, seizures, first trimester of pregnancy.
- Drug Interactions: Antacids, alcohol, warfarin, theophylline.
- Pregnancy & Breastfeeding: Contraindicated or should be avoided.
- Dosage: Pediatric use only. Consult pediatrician.
- Monitoring Parameters: Liver function, renal function, complete blood count, ECG (if at risk of QT prolongation).
Popular Combinations
The combination of ofloxacin, metronidazole, and simethicone itself is frequently used in pediatrics.
Precautions
- General Precautions: Screen for allergies, liver/renal dysfunction, history of seizures.
- Specific Populations: Avoid or use with extreme caution during pregnancy and breastfeeding. Caution in children and the elderly, adjusting dose as needed.
- Lifestyle Considerations: Avoid alcohol. May impair alertness; caution with driving or operating machinery.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Metronidazole + Ofloxacin + Simethicone?
A: Dosage is weight-based and specific to pediatric patients. Consult a pediatrician for the appropriate dose based on the child’s weight and the severity of infection.
Q2: What are the common side effects?
A: Common side effects include nausea, vomiting, diarrhea, abdominal pain, headache, metallic taste, and dizziness.
A: Seizures, peripheral neuropathy, severe allergic reactions, and QT prolongation are serious side effects that require immediate medical attention.
Q4: Can this medication be given to pregnant or breastfeeding women?
A: This medication should generally be avoided in pregnant and breastfeeding women. The first trimester of pregnancy is a definite contraindication for both metronidazole and ofloxacin. Discuss the risk versus benefits with a doctor if the infection warrants treatment during pregnancy or lactation.
Q5: What other medications should be avoided while taking this combination?
A: Avoid antacids, iron supplements, multivitamins containing divalent cations, alcohol, warfarin, theophylline, and certain antiarrhythmics. Consult a doctor or pharmacist for a comprehensive list.
Q6: How should this medication be administered?
A: This medication is available as a suspension for oral administration. It can be given with or without food, but administering it with food may help prevent gastrointestinal upset.
Q7: What if a dose is missed?
A: If a dose is missed, administer it as soon as remembered. However, if it is almost time for the next dose, skip the missed dose and continue with the regular dosing schedule. Do not double the dose.
Q8: What should I do if a child overdoses on this medication?
A: In case of a suspected overdose, seek immediate medical attention.
Q9: Can this medication be used for long-term treatment?
A: Long-term use of metronidazole, specifically, can lead to peripheral neuropathy. The duration of treatment should be determined by a physician and ideally kept as short as possible while effectively treating the infection.
Q10: How does simethicone help in this combination?
A: Simethicone relieves bloating and gas, which are common symptoms associated with gastrointestinal infections. While it does not treat the infection itself, it helps improve patient comfort.
