Chlormezanone + Diclofenac + Paracetamol

Usage

• This combination medication is prescribed for the relief of pain, inflammation, and muscle spasms associated with musculoskeletal conditions such as low back pain, sprains, strains, myalgia (muscle pain), osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, post-operative pain, traumatic muscle injuries, and cervical root and disc syndrome.
• Pharmacological Classification:
  • Diclofenac: Nonsteroidal anti-inflammatory drug (NSAID)
  • Paracetamol: Analgesic and antipyretic
  • Chlormezanone: Centrally acting skeletal muscle relaxant
• Mechanism of Action: This combination targets different pain pathways for enhanced relief. Diclofenac reduces inflammation by inhibiting cyclooxygenase (COX) enzymes. Paracetamol provides central pain and fever relief. Chlormezanone acts on the central nervous system to reduce muscle spasms.

Alternate Names

• Diclofenac + Paracetamol + Chlorzoxazone
• Diclopar
• Diclomec Plus
• Other regional brand names may exist. Some brand names may include vitamins in addition to the three base ingredients, such as Dolo-Neurobion Forte (B Vitamins).

How It Works

• Pharmacodynamics: Diclofenac inhibits COX enzymes, reducing prostaglandin synthesis. Paracetamol acts centrally on pain and temperature regulation. Chlormezanone suppresses polysynaptic reflexes, causing muscle relaxation.
• Pharmacokinetics:
  • Absorption: All three drugs are well-absorbed orally.
  • Metabolism: Diclofenac is highly protein-bound and undergoes hepatic metabolism primarily through CYP2C9. Paracetamol is mostly conjugated in the liver via glucuronidation and sulfation pathways with a minor fraction metabolized by CYP enzymes (CYP2E1, CYP1A2, and CYP3A4) to a reactive metabolite that is normally detoxified by glutathione. Chlorzoxazone undergoes hepatic metabolism through hydroxylation and oxidation primarily by CYP2E1 and to a lesser extent CYP1A2.
  • Elimination: Diclofenac metabolites are excreted in urine and bile. Paracetamol metabolites are primarily excreted in the urine. Chlorzoxazone is predominantly excreted in urine, both as unchanged drug and as its metabolites.
• Mode of Action: Diclofenac: COX inhibition reduces prostaglandin production. Paracetamol: acts centrally on pain and temperature regulation. Chlorzoxazone: Suppresses polysynaptic reflexes in the spinal cord and subcortical areas of the brain.

Dosage

Standard Dosage

Adults: One tablet (Diclofenac 50 mg, Paracetamol 325 mg, Chlorzoxazone 250/500 mg) two to three times daily. Maximum daily doses are Diclofenac 150mg, Paracetamol 4000mg, and Chlorzoxazone 3000mg.

Children: This combination is generally not recommended for children due to lack of safety and efficacy data.

Special Cases:

• Elderly Patients: Initiate therapy at the lowest effective dose and monitor closely for adverse effects. Dose reduction may be necessary.
• Patients with Renal Impairment: Exercise caution and consider dose reduction.
• Patients with Hepatic Dysfunction: Adjust dosage based on the severity of impairment.
• Patients with Comorbid Conditions: Careful evaluation is needed; dose adjustments may be necessary.

Clinical Use Cases Dosage guidelines for specific medical settings are generally the same as standard dosage guidelines. If more frequent dosing is needed, increase the dosing frequency to every 6 hours but make sure not to exceed the daily maximum dose for any of the three drugs.

Dosage Adjustments

Dose modifications are based on patient-specific factors such as renal/hepatic dysfunction, other medical conditions, and potential drug interactions.

Side Effects

Common Side Effects

• Drowsiness, dizziness, nausea, vomiting, stomach upset, constipation, diarrhea, skin rash, weakness.

Rare but Serious Side Effects

• Allergic reactions, liver injury, gastrointestinal bleeding, cardiovascular events, renal impairment, blood dyscrasias, Stevens-Johnson syndrome.

Long-Term Effects

• Prolonged use can increase the risk of gastrointestinal bleeding, ulcers, and kidney problems.

Adverse Drug Reactions (ADR)

• Severe allergic reactions, severe liver injury, severe gastrointestinal bleeding, cardiovascular events.

Contraindications

• Hypersensitivity to any component; active peptic ulcer disease; severe hepatic or renal impairment; history of gastrointestinal bleeding or perforation associated with NSAID use; aspirin triad; last trimester of pregnancy; porphyria.

Drug Interactions

• NSAIDs, anticoagulants, antihypertensives, diuretics, methotrexate, lithium, alcohol, other medications containing paracetamol, CYP450 enzyme inducers/inhibitors.

Pregnancy and Breastfeeding

• Avoid during the third trimester. Use with caution during the first and second trimesters. Consult a physician before use.

Drug Profile Summary (See above sections for expanded details.)

Popular Combinations

This drug is a combination of three ingredients, so the most popular combination includes all three. Diclofenac and Paracetamol are often used together as a dual therapy for pain. The synergistic effects of Diclofenac and Paracetamol can enhance pain and fever relief.

Precautions

(See sections on side effects, contraindications, drug interactions, pregnancy and breastfeeding).

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Chlormezanone + Diclofenac + Paracetamol?

A: The typical adult dosage is one tablet (Diclofenac 50 mg, Paracetamol 325 mg, and Chlorzoxazone 250/500 mg) two to three times daily.

Q2: Can children take this combination?

A: No, it’s generally not recommended for children due to a lack of established safety and efficacy data.

Q3: What are the common side effects?

A: Drowsiness, dizziness, nausea, and gastrointestinal upset are common.

Q4: Are there serious side effects to be aware of?

A: Yes, rare but serious side effects include allergic reactions, liver damage, gastrointestinal bleeding, and cardiovascular issues.

Q5: Can pregnant or breastfeeding women use this medication?

A: It is contraindicated in the third trimester and should be used cautiously under medical supervision during the first and second trimesters. Its use during breastfeeding should also be assessed by a physician.

Q6: Does this medication interact with other drugs?

A: Yes, it can interact with NSAIDs, anticoagulants, antihypertensives, and other medications. Alcohol should also be avoided. Be sure to list any existing medication before taking this drug.

Q7: Should this medicine be taken with food?

A: Yes, it should be taken with food or milk to minimize stomach upset.

Q8: What conditions is this medication contraindicated in?

A: It’s contraindicated in individuals with hypersensitivity to the components, active peptic ulcer disease, severe liver or kidney impairment, and certain other conditions.

Q9: What should patients with renal or hepatic impairment do?

A: They should consult a physician before using this medication. Dosage adjustments are often necessary.