Usage
Diclofenac + Tolperisone is prescribed for acute musculoskeletal pain and spasms. This includes conditions such as low back pain, neck pain, muscle strains and sprains, and muscle spasms related to neurological disorders (e.g., multiple sclerosis, stroke) or resulting from trauma or surgery.
It is classified pharmacologically as a combination of a Nonsteroidal Anti-inflammatory Drug (NSAID) and a centrally acting muscle relaxant.
The mechanism of action involves two components: Diclofenac inhibits prostaglandin synthesis, reducing pain and inflammation, while Tolperisone acts on the central nervous system to decrease muscle stiffness and spasms by interfering with spinal reflexes.
Alternate Names
There is no officially recognized alternate name for the combination itself. However, the individual components have various names: Diclofenac is sometimes referred to as diclofenac sodium or diclofenac potassium depending upon the salt used, and Tolperisone is known as tolperisone hydrochloride.
Brand names under which this combination is marketed include Myotop-D, Tolperitas-DSR, Tolifast D, Reladol-D, and various others depending upon the manufacturer and region.
How It Works
Pharmacodynamics: Diclofenac, the NSAID component, inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis. This leads to decreased pain and inflammation. Tolperisone, a centrally acting muscle relaxant, is believed to decrease muscle tone by inhibiting voltage-gated sodium and calcium channels in the central nervous system. It also may block spinal reflexes that mediate muscle contractions, reducing spasms and rigidity without affecting muscle strength.
Pharmacokinetics:
- Diclofenac: Well absorbed orally. Peak plasma concentrations occur in 1-2 hours. Metabolized primarily in the liver by CYP2C9 to several metabolites. Primarily excreted renally.
- Tolperisone: Well absorbed orally. Peak plasma levels are reached in about 0.5 to 1 hour. Extensively metabolized in the liver, mostly by CYP2D6. Excreted primarily in the urine.
Mode of Action (Cellular/Molecular): Diclofenac blocks COX-1 and COX-2 enzymes at the cellular level. This inhibition prevents the conversion of arachidonic acid to prostaglandins, which mediate inflammation and pain. Tolperisone acts centrally, possibly at the brainstem reticular formation, by influencing neuronal transmission to reduce muscle tone. Its specific binding sites and molecular targets aren’t entirely understood, but modulation of voltage-gated sodium and calcium channels and interference with polysynaptic spinal reflexes have been suggested. It does not directly affect neuromuscular transmission or muscle contractility.
Elimination Pathways: Diclofenac is mostly excreted in the urine as metabolites, with some biliary excretion. Tolperisone undergoes extensive hepatic metabolism, primarily by CYP2D6, followed by renal excretion of the metabolites.
Dosage
Standard Dosage
Adults:
The typical dose is one tablet containing 150mg Tolperisone and 50mg Diclofenac, taken two to three times daily. It’s crucial to swallow tablets whole with water and preferably after a meal.
Children:
This combination is generally not recommended for children under 18, as safety and efficacy haven’t been established.
Special Cases:
- Elderly Patients: Start with lower doses due to potential age-related decline in hepatic and renal function. Close monitoring is necessary.
- Patients with Renal Impairment: Dose adjustment might be required. Monitor renal function carefully.
- Patients with Hepatic Dysfunction: Dose reduction may be necessary. Closely monitor liver function.
- Patients with Comorbid Conditions: Use cautiously in patients with cardiovascular disease, gastrointestinal problems, or asthma. Dose adjustments may be needed.
Clinical Use Cases
Diclofenac + Tolperisone is not typically used in clinical settings like intubation, surgical procedures, mechanical ventilation, ICU, or emergency situations. Its primary role is in the outpatient management of musculoskeletal pain and spasm. Other medications are preferred in acute medical or surgical settings.
Dosage Adjustments
Adjustments are made based on patient response, tolerance, and organ function (renal/hepatic). Genetic polymorphisms affecting drug metabolism, especially related to CYP2D6 for Tolperisone and CYP2C9 for Diclofenac, should be considered if available.
Side Effects
Common Side Effects:
Nausea, vomiting, diarrhea, abdominal pain, dizziness, drowsiness, headache, weakness, loss of appetite, heartburn.
Rare but Serious Side Effects:
Allergic reactions (rash, itching, swelling, difficulty breathing), gastrointestinal bleeding, peptic ulcer, liver damage, kidney problems, cardiovascular events (heart attack, stroke), blood disorders.
Long-Term Effects:
Chronic use can lead to gastrointestinal issues, renal impairment, and cardiovascular problems.
Adverse Drug Reactions (ADR):
Anaphylaxis, Stevens-Johnson syndrome, toxic epidermal necrolysis, severe gastrointestinal bleeding, acute renal failure, hepatotoxicity.
Contraindications
- Hypersensitivity to either diclofenac or tolperisone.
- Active peptic ulcer or gastrointestinal bleeding.
- Severe hepatic or renal impairment.
- History of asthma, urticaria, or allergic-type reactions after taking NSAIDs or aspirin.
- Myasthenia gravis.
- Pregnancy (especially the third trimester).
- Breastfeeding.
- Severe heart failure.
- Recent heart surgery.
Drug Interactions
- Other NSAIDs: Increased risk of gastrointestinal bleeding.
- Anticoagulants (e.g., warfarin): Increased bleeding risk.
- Antiplatelets (e.g., clopidogrel): Increased bleeding risk.
- Corticosteroids: Increased risk of gastrointestinal ulcers.
- SSRIs: Increased risk of gastrointestinal bleeding.
- Diuretics: Decreased diuretic effect, increased risk of renal impairment.
- Digoxin: Increased digoxin levels.
- Methotrexate: Increased methotrexate toxicity.
- Cyclosporine: Increased risk of nephrotoxicity.
- Lithium: Increased lithium levels.
- Alcohol: Increased drowsiness and risk of gastrointestinal bleeding.
- CYP450 interactions: Tolperisone is primarily metabolized by CYP2D6, and diclofenac by CYP2C9. Drugs affecting these enzymes can change the drugs’ levels and effects.
Pregnancy and Breastfeeding
Contraindicated during pregnancy, especially the third trimester, as it can cause premature closure of the ductus arteriosus in the fetus and other complications. Also contraindicated during breastfeeding due to potential adverse effects on the neonate.
Drug Profile Summary
- Mechanism of Action: Diclofenac: COX inhibitor reducing pain and inflammation. Tolperisone: Centrally acting muscle relaxant reducing muscle spasm and spasticity.
- Side Effects: Nausea, vomiting, diarrhea, dizziness, drowsiness, GI bleeding, peptic ulcer, liver/kidney dysfunction, cardiovascular events.
- Contraindications: Hypersensitivity, active peptic ulcer, severe hepatic/renal impairment, pregnancy, breastfeeding.
- Drug Interactions: Other NSAIDs, anticoagulants, antiplatelets, corticosteroids, SSRIs, diuretics, digoxin, methotrexate, cyclosporine, lithium, alcohol.
- Pregnancy & Breastfeeding: Contraindicated.
- Dosage: Adults: One tablet (150mg tolperisone/50mg diclofenac) 2-3 times/day. Adjustments needed for elderly and patients with hepatic/renal dysfunction.
- Monitoring Parameters: Liver and renal function tests, blood pressure, signs of gastrointestinal bleeding.
Popular Combinations
It is often used as a standalone combination product. Co-prescription with other analgesics or muscle relaxants may be done with caution if deemed necessary by the physician.
Precautions
- General Precautions: Assess for allergies, hepatic and renal function, cardiovascular history, and gastrointestinal issues before starting.
- Specific Populations: Use with extreme caution in the elderly, those with hepatic or renal impairment, and patients with cardiovascular risks.
- Pregnant Women: Contraindicated.
- Breastfeeding Mothers: Contraindicated.
- Children & Elderly: Not recommended for children. Use cautiously with reduced dose in the elderly.
- Lifestyle Considerations: Avoid alcohol. Caution while driving or operating machinery due to the possibility of dizziness and drowsiness.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Diclofenac + Tolperisone?
A: The standard adult dosage is one tablet (150mg tolperisone/50mg diclofenac) two to three times daily, taken after meals. Dosage adjustments may be needed based on individual patient characteristics and conditions.
Q2: What are the primary uses of this drug combination?
A: It is mainly used for the symptomatic relief of acute musculoskeletal pain and spasms.
Q3: Can it be used for chronic pain conditions?
A: While it can provide relief, it’s generally prescribed for short-term use in acute conditions. Long-term use carries increased risks of side effects.
Q4: Is this medication safe for patients with a history of stomach ulcers?
A: No, it’s contraindicated in patients with active or a history of recurrent peptic ulcers/gastrointestinal bleeding.
Q5: What are the common side effects patients should be aware of?
A: Common side effects include nausea, dizziness, drowsiness, vomiting, diarrhea, and abdominal discomfort.
Q6: Are there any serious drug interactions I should be aware of?
A: Yes. It interacts with other NSAIDs, anticoagulants, and some antidepressants, increasing the risk of bleeding. It can also interact with certain heart medications and other drugs metabolized by the liver. Always check for potential interactions.
Q7: Can this medication be used during pregnancy or breastfeeding?
A: No, it is contraindicated in both pregnancy, especially the third trimester, and breastfeeding due to potential harm to the fetus or infant.
Q8: Can I take this medication with alcohol?
A: No, alcohol should be avoided as it can exacerbate side effects like drowsiness and increase the risk of gastrointestinal issues.
Q9: How should I manage potential gastrointestinal side effects?
A: Taking the medication with food or milk can minimize stomach upset. If persistent, consult a physician.
Q10: 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.
