Usage
Diclofenac + Metaxalone is prescribed for the relief of pain and inflammation associated with muscle spasms and musculoskeletal conditions like strains, sprains, and other injuries.
Pharmacological Classification:
- Diclofenac: Nonsteroidal anti-inflammatory drug (NSAID)
- Metaxalone: Skeletal muscle relaxant
Mechanism of Action: Diclofenac inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis, thereby decreasing pain and inflammation. Metaxalone’s exact mechanism is unclear, but it is thought to depress the central nervous system, leading to muscle relaxation and reduced pain perception.
Alternate Names
No widely recognized alternate names exist for the combination product itself. The individual components have various salt forms (e.g., Diclofenac potassium, Diclofenac sodium) and may be marketed internationally under different names.
Brand Names: Several brand names exist for Diclofenac + Metaxalone, varying by region and manufacturer (e.g., Mobiswift-D, Movidase-D).
How It Works
Pharmacodynamics: Diclofenac exerts its anti-inflammatory and analgesic effects through COX inhibition. Metaxalone’s muscle relaxant properties likely stem from its action on the central nervous system, potentially by inhibiting nerve impulse transmission.
Pharmacokinetics:
- Absorption: Both drugs are absorbed orally.
- Metabolism: Primarily hepatic metabolism, potentially involving CYP450 enzymes.
- Elimination: Renal and hepatic excretion.
Mode of Action: Diclofenac acts by inhibiting COX-1 and COX-2 enzymes, reducing prostaglandin synthesis. Metaxalone is believed to work on the spinal cord and brain centers, but the precise molecular mechanism remains unclear.
Receptor binding, enzyme inhibition, or neurotransmitter modulation: Diclofenac inhibits COX enzymes. Metaxalone’s exact mode of action at the cellular level is yet to be fully elucidated.
Elimination Pathways: Diclofenac and Metaxalone undergo hepatic metabolism and are excreted through both renal and hepatic pathways.
Dosage
Standard Dosage
Children: Safety and efficacy have not been established in children. Use is generally not recommended.
Special Cases:
- Elderly Patients: Start with the lowest effective dose due to increased risk of adverse effects. Close monitoring is recommended.
- Patients with Renal Impairment: Dose adjustment may be necessary. Caution is advised.
- Patients with Hepatic Dysfunction: Dose adjustment may be needed. Close monitoring of liver function is recommended, especially with prolonged use.
- Patients with Comorbid Conditions: Caution is advised in patients with cardiovascular disease, hypertension, gastrointestinal disorders, or bleeding tendencies.
Clinical Use Cases
The use of Diclofenac + Metaxalone in specific clinical settings like intubation, surgical procedures, mechanical ventilation, ICU use, and emergency situations is generally not indicated. Its primary role is in the management of musculoskeletal pain and spasms.
Dosage Adjustments
Dose adjustments may be required based on patient-specific factors, including renal or hepatic dysfunction, other medical conditions, and concomitant medications.
Side Effects
Common Side Effects:
Nausea, vomiting, stomach pain, heartburn, diarrhea, dizziness, headache, drowsiness, loss of appetite.
Rare but Serious Side Effects:
Gastrointestinal bleeding, ulcers, renal impairment, hepatic dysfunction, cardiovascular events (heart attack, stroke), allergic reactions.
Long-Term Effects:
Chronic use of NSAIDs like diclofenac carries an increased risk of gastrointestinal and cardiovascular complications.
Adverse Drug Reactions (ADR):
Severe allergic reactions, gastrointestinal bleeding, Stevens-Johnson syndrome.
Contraindications
- Hypersensitivity to diclofenac or metaxalone.
- Active peptic ulcer disease or gastrointestinal bleeding.
- Severe heart failure.
- Recent coronary artery bypass graft (CABG) surgery.
- Aspirin triad (asthma, nasal polyps, aspirin sensitivity).
Drug Interactions
- Anticoagulants (warfarin, heparin) – Increased bleeding risk.
- Other NSAIDs (aspirin, ibuprofen) – Increased risk of gastrointestinal and renal side effects.
- Corticosteroids (prednisone) – Increased risk of gastrointestinal bleeding.
- Antihypertensives – May reduce the effectiveness of antihypertensive medications.
- Alcohol – Increased risk of drowsiness and gastrointestinal bleeding.
Pregnancy and Breastfeeding
- Pregnancy: Diclofenac + Metaxalone should be avoided during the third trimester due to the risk of premature closure of the ductus arteriosus in the fetus. Use in other trimesters should be carefully considered and only if the benefits outweigh the potential risks.
- Breastfeeding: The use of Diclofenac + Metaxalone during breastfeeding is generally not recommended.
Drug Profile Summary
- Mechanism of Action: Diclofenac inhibits COX enzymes, reducing prostaglandin synthesis. Metaxalone’s mechanism is unclear, but it acts as a muscle relaxant.
- Side Effects: Nausea, vomiting, stomach pain, heartburn, diarrhea, dizziness, drowsiness. Serious side effects include gastrointestinal bleeding and cardiovascular events.
- Contraindications: Hypersensitivity, active peptic ulcer, severe heart failure, recent CABG surgery.
- Drug Interactions: Anticoagulants, other NSAIDs, corticosteroids, antihypertensives, alcohol.
- Pregnancy & Breastfeeding: Generally avoided during pregnancy, especially in the third trimester, and during breastfeeding.
- Dosage: One tablet (50mg/400mg) once or twice daily. Adjustments may be necessary for elderly patients or those with renal/hepatic impairment.
- Monitoring Parameters: Liver function tests, renal function, blood pressure, signs of gastrointestinal bleeding.
Popular Combinations
Diclofenac + Metaxalone is itself a combination product. It is sometimes prescribed alongside physical therapy and other non-pharmacological interventions.
Precautions
- Use the lowest effective dose for the shortest duration possible.
- Monitor for signs of gastrointestinal bleeding, renal or hepatic dysfunction, and cardiovascular events.
- Caution in patients with a history of cardiovascular disease, hypertension, or gastrointestinal disorders.
- Avoid alcohol during treatment.
- Avoid driving or operating heavy machinery if drowsiness occurs.
FAQs (Frequently Asked Questions)
A: The typical dose is one tablet (Diclofenac 50mg + Metaxalone 400mg) once or twice daily. Dosage adjustments might be necessary based on the individual patient’s condition.
A: Safety and efficacy have not been established in children. Use is generally not recommended.
A: Common side effects include nausea, vomiting, stomach pain, heartburn, diarrhea, dizziness, headache, and drowsiness.
A: Consult your doctor before using this medication if you are pregnant, breastfeeding, or planning to become pregnant. It’s generally best to avoid it, particularly during the third trimester of pregnancy and while breastfeeding.
A: Avoid alcohol consumption as it can increase the risk of drowsiness and gastrointestinal bleeding.
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 time for your next scheduled dose. Do not double the dose to catch up.
Q7: Can I drive while taking this medication?
A: Diclofenac + Metaxalone can cause dizziness and drowsiness. Avoid driving or operating heavy machinery until you know how this medication affects you.
Q8: Are there any drug interactions I should be aware of?
A: Yes, several drug interactions are possible. Inform your doctor about all other medications, including over-the-counter drugs and supplements, that you are currently taking.
Q9: What should I do if I experience any adverse effects?
A: Contact your doctor immediately if you experience any severe or persistent side effects, such as stomach pain, signs of bleeding, allergic reactions, or changes in your vision.
A: Long-term use of NSAIDs like diclofenac carries potential risks, particularly for cardiovascular and gastrointestinal complications. Your doctor will carefully evaluate the benefits and risks before prescribing long-term use. Discuss any concerns you have about the duration of treatment with your physician.
