Usage
Flupirtine + Paracetamol is prescribed for the management of moderate to severe acute and chronic pain, including musculoskeletal pain (e.g., back pain, osteoarthritis, fibromyalgia), neuropathic pain (e.g., sciatica, diabetic neuropathy), postoperative pain, headaches (migraines, tension headaches), dental pain, and pain associated with dysmenorrhea (period pain) or myalgia (muscle pain). It also possesses antipyretic properties due to the presence of paracetamol.
It is classified pharmacologically as a non-opioid analgesic and antipyretic combination.
Flupirtine works primarily as a selective neuronal potassium channel opener, reducing neuronal excitability and thus decreasing pain transmission. Paracetamol’s mechanism involves inhibition of prostaglandin synthesis, reducing pain and fever. The combination offers synergistic pain relief.
Alternate Names
While “Flupirtine + Paracetamol” is the standard generic name, regional variations may exist. Brand names for this combination include Flupitime P, Flupinex-Plus, Lupirtin P, FLUPIRIN P, and FLUMera-P. Ketadol is a brand name for Flupirtine alone.
How It Works
Pharmacodynamics: Flupirtine acts centrally as a selective neuronal potassium channel opener (SNEPCO). By opening these channels, it hyperpolarizes neurons, making them less excitable and reducing pain signal transmission. It also shows NMDA receptor antagonist activity, contributing to its neuroprotective effects. Paracetamol inhibits cyclooxygenase (COX) enzymes in the central nervous system, primarily COX-3, reducing prostaglandin synthesis, which are mediators of pain and fever. The combination results in synergistic pain relief. Flupirtine may also have some muscle relaxant properties.
Pharmacokinetics: Flupirtine is well-absorbed orally. It is metabolized in the liver, primarily to 2-amino-3-acetylamino-6-(para-fluorobenzylamino) pyridine. Elimination is primarily renal (72%), with a smaller fraction excreted in feces. Paracetamol is rapidly absorbed, with peak plasma concentrations occurring within 30-60 minutes. It undergoes hepatic metabolism, mainly through glucuronidation and sulfation pathways. A small amount is metabolized by CYP2E1 to a hepatotoxic metabolite, N-acetyl-p-benzoquinone imine (NAPQI), which is normally detoxified by glutathione. Elimination is primarily renal.
Receptor Binding, Enzyme Inhibition, or Neurotransmitter Modulation: Flupirtine: SNEPCO, NMDA receptor antagonist. Paracetamol: COX, primarily COX-3 inhibitor.
Elimination Pathways: Flupirtine: Primarily renal excretion. Paracetamol: Primarily renal excretion of metabolites.
Dosage
Standard Dosage
Adults:
The typical adult dose is one tablet (Flupirtine 100mg + Paracetamol 325mg) taken orally two to three times daily, preferably after meals. The maximum daily dose should not exceed three tablets.
Children:
Use in children younger than 6 years is not recommended as safety and efficacy have not been established. For children above 6 years, please consult a healthcare professional for appropriate dosing guidance. One suggested guideline is 50 mg of flupirtine, three to four times a day. For paracetamol dosing in children, refer to pediatric dosing charts based on age and weight, and do not exceed the recommended maximum daily dose.
Special Cases:
- Elderly Patients: Initiate therapy with the lowest effective dose. Monitor liver and kidney function. Dose adjustment may be necessary.
- Patients with Renal Impairment: Reduce dosage and monitor renal function.
- Patients with Hepatic Dysfunction: Use with caution and monitor liver function. Dose adjustment may be necessary.
- Patients with Comorbid Conditions: Caution is advised in patients with chronic malnutrition, alcoholism, myasthenia gravis, and cardiovascular disease.
Clinical Use Cases
Dosage for clinical use cases like Intubation, Surgical Procedures, Mechanical Ventilation, ICU Use, and Emergency Situations should be determined by a qualified anesthesiologist or critical care specialist based on individual patient needs and in accordance with established clinical protocols.
Dosage Adjustments
Dosage adjustments are required in elderly patients, and those with hepatic or renal impairment.
Side Effects
Common Side Effects:
Nausea, vomiting, constipation, dry mouth, dizziness, headache, sleepiness, fatigue, abdominal discomfort, diarrhea, gas, heartburn, increased sweating, loss of appetite, sleep disturbances, shakiness.
Rare but Serious Side Effects:
Liver damage (hepatotoxicity), jaundice, allergic reactions (including Steven-Johnson syndrome and anaphylactic reactions), anemia, edema, erythema.
Long-Term Effects:
Potential for liver damage with prolonged high doses of paracetamol.
Adverse Drug Reactions (ADR):
Hepatotoxicity, severe allergic reactions.
Contraindications
Hypersensitivity to flupirtine or paracetamol, severe hepatic impairment (hepatic encephalopathy, cholestasis), myasthenia gravis, chronic alcoholism, primary biliary cirrhosis.
Drug Interactions
Anticoagulants (e.g., warfarin): Increased risk of bleeding. Alcohol: Increased risk of drowsiness and liver damage. CNS depressants (e.g., benzodiazepines): Increased sedation. Carbamazepine: Reduced efficacy of flupirtine. Other hepatotoxic drugs: Increased risk of liver damage.
Pregnancy and Breastfeeding
Flupirtine + Paracetamol is generally not recommended during pregnancy and breastfeeding due to limited safety data. Consult a healthcare professional to weigh the potential benefits against the risks.
Drug Profile Summary
- Mechanism of Action: Flupirtine: SNEPCO, NMDA antagonist. Paracetamol: COX inhibitor.
- Side Effects: Nausea, dizziness, drowsiness, liver toxicity (rare).
- Contraindications: Liver disease, hypersensitivity, myasthenia gravis, alcoholism.
- Drug Interactions: Anticoagulants, alcohol, CNS depressants.
- Pregnancy & Breastfeeding: Not recommended.
- Dosage: Adults: One tablet 2-3 times daily.
- Monitoring Parameters: Liver function tests, especially with prolonged use.
Popular Combinations
This information is not available from the current sources.
Precautions
- General Precautions: Assess liver and kidney function, history of allergies.
- Pregnant Women: Avoid unless absolutely necessary.
- Breastfeeding Mothers: Avoid.
- Children & Elderly: Use with caution, lower doses.
- Lifestyle Considerations: Avoid alcohol. Driving may be impaired.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Flupirtine + Paracetamol?
A: The standard adult dose is one tablet (Flupirtine 100mg + Paracetamol 325mg) two to three times daily.
Q2: What are the common side effects?
A: Common side effects include nausea, dizziness, drowsiness, constipation, and dry mouth.
Q3: Can I take this medication if I have liver disease?
A: No, it’s contraindicated in patients with severe liver disease. Use with caution in mild to moderate liver impairment with close monitoring of liver function.
Q4: Can I drink alcohol while taking this medication?
A: No, alcohol should be avoided as it can increase the risk of drowsiness and liver damage.
Q5: Is it safe to take during pregnancy or breastfeeding?
A: Generally not recommended. Consult a healthcare professional.
Q6: How long can I take this medication?
A: The duration of treatment should be as short as possible and as directed by the physician. Prolonged paracetamol use should be monitored due to the risk of hepatotoxicity.
Q7: Can I drive while taking Flupirtine + Paracetamol?
A: Use caution as it may cause dizziness and drowsiness. Avoid driving if these symptoms occur.
Q8: What should I do if I experience any side effects?
A: Report any persistent or bothersome side effects to your doctor immediately.
Q9: What if I miss a dose?
A: Take the missed dose as soon as you remember, unless it is almost time for your next dose. Do not double the dose to catch up.
Q10: Can I take this with other painkillers?
A: Consult your doctor before combining with other painkillers, especially those containing paracetamol, to avoid exceeding the maximum daily dose.
