Usage
Nimesulide + Tolperisone is prescribed for the relief of painful muscle spasms associated with musculoskeletal conditions such as:
- Rigidity
- Tension
- Stiffness
- Skeletal muscle spasms
- Ankylosing spondylitis
- Osteoarthritis
- Back pain
Pharmacological Classification:
- Tolperisone: Centrally acting skeletal muscle relaxant
- Nimesulide: Non-steroidal anti-inflammatory drug (NSAID)
Mechanism of Action:
- Tolperisone: Acts centrally on the brain and spinal cord, reducing muscle tone and spasms. It also improves peripheral blood flow to muscles, thereby reducing pain.
- Nimesulide: Primarily inhibits COX-2, reducing prostaglandin synthesis and inflammation. It also inhibits COX-1, cartilage breakdown, and cytokine formation.
Alternate Names
The combination may be referred to by various brand names depending on the manufacturer and region.
How It Works
Pharmacodynamics:
- Tolperisone: Reduces muscle tone and spasms by acting on the central nervous system. It also improves peripheral blood flow to muscles, alleviating pain.
- Nimesulide: Exerts analgesic and anti-inflammatory effects through COX-2 inhibition. It also offers some cartilage protection by inhibiting COX-1 and reduces cytokine formation.
Pharmacokinetics:
- Tolperisone: Well absorbed orally, metabolized in the liver, and primarily eliminated in urine.
- Nimesulide: Rapidly absorbed orally, highly protein-bound, extensively metabolized in the liver (primarily to 4-hydroxynimesulide), and excreted in urine and feces.
Mode of Action:
- Tolperisone: Blocks sodium and calcium channels in the spinal cord, inhibiting spinal reflexes through presynaptic blockade of neurotransmitter release.
- Nimesulide: Inhibits COX-2 enzymes, thus reducing prostaglandin production, which are mediators of pain and inflammation.
Elimination Pathways:
- Tolperisone: Renal excretion (primarily).
- Nimesulide: Hepatic metabolism (primarily) followed by renal and fecal excretion.
Dosage
Standard Dosage
Adults:
One tablet (150 mg Tolperisone + 100 mg Nimesulide) twice daily, orally, after meals. Treatment duration should not typically exceed 7 days.
Children:
Not recommended for children below 12 years of age.
Special Cases:
- Elderly Patients: Use with caution due to increased risk of adverse effects. Dose adjustment may be necessary.
- Patients with Renal Impairment: Use with caution. Dose adjustment may be required in severe renal impairment.
- Patients with Hepatic Dysfunction: Contraindicated in severe hepatic impairment. Use cautiously in mild to moderate impairment; dose adjustment may be necessary.
- Patients with Comorbid Conditions (e.g., cardiovascular disease, diabetes, gastrointestinal disorders): Consult a doctor.
Clinical Use Cases
This combination is typically not indicated for Intubation, Surgical Procedures, Mechanical Ventilation, ICU use, or Emergency Situations.
Dosage Adjustments
Dosage modifications are based on patient-specific factors, such as renal/hepatic dysfunction, after careful evaluation.
Side Effects
Common Side Effects:
- Nausea
- Vomiting
- Diarrhea
- Dizziness
- Headache
- Skin rashes
- Drowsiness
- Muscular weakness
Rare but Serious Side Effects:
- Liver damage (hepatotoxicity)
- Stevens-Johnson syndrome
- Blood disorders
- Allergic reactions (anaphylaxis)
- Renal impairment
Long-Term Effects:
- Potential for liver and renal damage with prolonged use.
Adverse Drug Reactions (ADR):
- Hepatotoxicity
- Severe skin reactions (Stevens-Johnson Syndrome)
- Blood dyscrasias
- Anaphylaxis
- Renal failure
Contraindications
- Hypersensitivity to Nimesulide or Tolperisone.
- Severe hepatic impairment.
- Active peptic ulcer or gastrointestinal bleeding.
- Severe heart failure.
- Severe renal impairment.
- Pregnancy (especially the first trimester).
- Breastfeeding.
- Children under 12 years old.
- Myasthenia gravis (for Tolperisone).
Drug Interactions
- Other NSAIDs
- Anticoagulants (e.g., warfarin)
- Antihypertensives
- Diuretics (e.g., furosemide)
- Methotrexate
- Cyclosporine
- Alcohol
- CYP450 interacting drugs (Nimesulide inhibits CYP2C9).
- Methocarbamol
- Fenofibrate
- Valproic acid
- Tolbutamide
Pregnancy and Breastfeeding
Contraindicated in both pregnancy (especially first trimester, potential for birth defects and effects on fetal circulation) and breastfeeding (Nimesulide may be excreted in breast milk).
Drug Profile Summary
- Mechanism of Action: Tolperisone: Centrally acting muscle relaxant. Nimesulide: COX-2 inhibitor, analgesic, and antipyretic.
- Side Effects: Nausea, vomiting, diarrhea, dizziness, headache, liver toxicity (rare).
- Contraindications: Severe liver disease, pregnancy, breastfeeding, children under 12.
- Drug Interactions: Other NSAIDs, anticoagulants, antihypertensives.
- Pregnancy & Breastfeeding: Contraindicated.
- Dosage: Adults: One tablet (150mg/100mg) twice daily after meals.
- Monitoring Parameters: Liver function tests (LFTs), renal function tests (RFTs) if used for extended periods.
Popular Combinations
Not applicable – this is a combination product.
Precautions
- Assess liver and kidney function before initiating therapy.
- Monitor for signs of gastrointestinal bleeding or ulceration.
- Avoid alcohol.
- Use cautiously in elderly patients.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Nimesulide + Tolperisone?
A: One tablet (150 mg Tolperisone + 100 mg Nimesulide) twice daily, orally, after meals for adults. Dosage adjustments might be necessary for elderly patients and those with renal or hepatic impairment.
Q2: Can Nimesulide + Tolperisone be used in children?
A: No, it is contraindicated in children under 12 years old.
Q3: Is Nimesulide + Tolperisone safe during pregnancy and breastfeeding?
A: No, it’s contraindicated during pregnancy and breastfeeding.
Q4: What are the common side effects of this combination?
A: Common side effects include nausea, vomiting, diarrhea, dizziness, headache, skin rashes, drowsiness, and muscular weakness.
Q5: Are there any serious side effects I should be aware of?
A: Yes, rare but serious side effects include liver damage, Stevens-Johnson syndrome, blood disorders, allergic reactions, and renal impairment.
Q6: What should I do if I miss a dose?
A: Take the missed dose as soon as you remember, unless it is close to the next scheduled dose. Do not double the dose.
Q7: Can I consume alcohol while taking this medication?
A: No, alcohol should be avoided, as it can exacerbate side effects.
Q8: How long should I take Nimesulide + Tolperisone?
A: The treatment duration should typically not exceed 7 days. Consult your doctor regarding the duration of treatment.
Q9: What are the signs of an allergic reaction to this medication?
A: Signs of an allergic reaction can include skin rash, itching, swelling (especially of the face, tongue, or throat), severe dizziness, and trouble breathing. Seek immediate medical help if these occur.
Q10: What if I have pre-existing liver or kidney problems?
A: Inform your doctor about any pre-existing liver or kidney conditions before starting Nimesulide + Tolperisone. Dose adjustment or alternative medications might be necessary.
