Usage
- Medical Conditions: Paracetamol + Tolperisone is prescribed for the symptomatic treatment of painful muscle spasms and musculoskeletal conditions such as sprains, strains, and rigidity. It is also indicated for the symptomatic treatment of post-stroke spasticity associated with pain in adults.
- Pharmacological Classification: This drug is a combination of an analgesic (Paracetamol) and a centrally acting skeletal muscle relaxant (Tolperisone).
- Mechanism of Action: Tolperisone acts on the central nervous system to reduce muscle tone and spasticity. Paracetamol provides analgesic and antipyretic effects by inhibiting cyclooxygenase (COX) enzymes in the brain, reducing the production of prostaglandins, which are chemical messengers involved in pain and fever.
Alternate Names
- No widely recognized alternate names exist for the combination product itself.
- Brand Names: Reladol-P, Myotop-P.
How It Works
- Pharmacodynamics: Tolperisone’s primary effect is the reduction of muscle tone and spasm. Paracetamol reduces pain and fever.
- Pharmacokinetics: Both drugs are absorbed orally. Tolperisone is metabolized in the liver and excreted renally. Paracetamol is also primarily metabolized in the liver, with most being excreted in the urine as glucuronide and sulfate conjugates. A small portion is metabolized by CYP450 enzymes to a potentially hepatotoxic metabolite, NAPQI. This metabolite is usually detoxified by glutathione.
- Mode of Action: Tolperisone is believed to block sodium and calcium channels in the spinal cord, reducing muscle tone. Paracetamol inhibits COX enzymes, primarily in the CNS.
- Elimination Pathways: Both drugs are primarily eliminated through hepatic metabolism and subsequent renal excretion.
Dosage
Standard Dosage
Adults:
- The recommended adult dose is one tablet (containing 150mg Tolperisone and 325mg or 500mg of Paracetamol), three times a day.
Children:
- This combination is not recommended for children.
Special Cases:
- Elderly Patients: Caution is advised, and dose adjustments based on renal and hepatic function might be necessary. Start with lower doses and monitor closely.
- Patients with Renal Impairment: Close monitoring is advised. Reduce the dose in patients with moderate to severe renal impairment.
- Patients with Hepatic Dysfunction: Use with caution. Closely monitor liver function and adjust the dose as needed.
- Patients with Comorbid Conditions: Exercise caution in patients with cardiovascular disease, especially heart failure, and monitor blood pressure and cardiovascular status.
Clinical Use Cases
- The provided sources did not give specific dosage recommendations for clinical settings such as intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. Dosage adjustments should be made on a case-by-case basis by the attending physician considering patient-specific factors and the clinical scenario.
Dosage Adjustments
- Dose adjustments may be needed based on individual patient factors like renal/hepatic dysfunction, other medical conditions, and drug interactions.
Side Effects
Common Side Effects:
- Nausea, vomiting, dry mouth, dizziness, weakness, sleepiness, headache, abdominal discomfort.
Rare but Serious Side Effects:
- Allergic reactions (itching, skin rash, dyspnea, angioedema, anaphylactic shock), hepatotoxicity (with Paracetamol overdose), muscular weakness, hypotension.
Long-Term Effects:
- Long-term effects are not well established, but chronic use of Paracetamol at high doses can contribute to liver damage.
Adverse Drug Reactions (ADR):
- Severe allergic reactions, hepatotoxicity (Paracetamol), significant hypotension, effects related to pre-existing conditions.
Contraindications
- Hypersensitivity to any component of the product.
- Myasthenia gravis.
- Severe hepatic impairment.
- Severe renal impairment.
Drug Interactions
- No specific drug interactions are listed in the sources for this particular combination, but consider interactions of the individual drugs.
- Paracetamol: Alcohol, other hepatotoxic drugs, drugs that induce liver enzymes.
- Tolperisone: Other muscle relaxants, CNS depressants.
Pregnancy and Breastfeeding
- This combination is contraindicated in the first trimester of pregnancy and during breastfeeding. In the second and third trimesters, use only if the benefit outweighs the risk.
Drug Profile Summary
- Mechanism of Action: Tolperisone: Centrally acting muscle relaxant; Paracetamol: Analgesic and antipyretic.
- Side Effects: Nausea, vomiting, dizziness, drowsiness, allergic reactions.
- Contraindications: Hypersensitivity, Myasthenia Gravis, severe hepatic or renal impairment.
- Drug Interactions: Potential interactions with other medications metabolized by the liver, including alcohol.
- Pregnancy & Breastfeeding: Contraindicated in the first trimester and during breastfeeding. Use with caution later in pregnancy.
- Dosage: Adults: One tablet (150mg/325-500mg) three times a day. Not recommended for children.
- Monitoring Parameters: Liver and kidney function tests.
Popular Combinations
- Information not found in the given source.
Precautions
- Pre-existing medical conditions (liver/kidney disease, cardiovascular disease).
- Pregnancy/Breastfeeding: Avoid in the first trimester and during breastfeeding.
- Children & Elderly: Not for children, elderly patients may require lower doses.
- Lifestyle: Avoid alcohol, as it may increase the risk of liver damage with Paracetamol.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Paracetamol + Tolperisone?
A: The usual adult dose is one tablet (150mg tolperisone + 325/500mg paracetamol) three times a day. Dosage should be adjusted based on individual patient needs and not recommended for children.
Q2: What are the common side effects?
A: Common side effects include nausea, vomiting, dry mouth, dizziness, weakness, and sleepiness.
Q3: Can pregnant or breastfeeding women take this medication?
A: Contraindicated during the first trimester of pregnancy and breastfeeding. Use with caution during the later stages of pregnancy only if benefits outweigh the risks.
Q4: Are there any drug interactions I should be aware of?
A: Potential interactions exist with alcohol and medications metabolized by the liver. Inform your doctor about all other medications you are taking.
Q5: What conditions is this medicine used to treat?
A: Painful muscle spasms, musculoskeletal conditions (sprains, strains, rigidity), post-stroke spasticity with associated pain.
Q6: How does this medication work?
A: Tolperisone relaxes muscles, while Paracetamol reduces pain and fever.
Q7: What should I do 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.
Q8: Are there any contraindications for this medication?
A: Yes, contraindications include myasthenia gravis, severe liver or kidney impairment, and hypersensitivity to the components.
Q9: What precautions should I take while on this medication?
A: Inform your doctor about all pre-existing conditions, especially liver or kidney problems. Avoid alcohol. Exercise caution while driving or operating machinery, as the medication can cause drowsiness.
Q10: How should this medicine be stored?
A: Store in a cool, dry place away from direct sunlight and out of reach of children.
