Usage
This combination medication is prescribed for the relief of pain, inflammation, and muscle spasms associated with musculoskeletal disorders such as sprains, strains, osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, and other painful conditions.
Pharmacological Classification:
- Aceclofenac: Non-Steroidal Anti-inflammatory Drug (NSAID)
- Paracetamol: Analgesic and Antipyretic
- Chlorzoxazone: Centrally-acting Skeletal Muscle Relaxant
Mechanism of Action: Aceclofenac inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis, which are mediators of pain and inflammation. Paracetamol acts centrally to relieve pain and fever. Chlorzoxazone acts on the central nervous system to depress reflexes and relax skeletal muscles, reducing muscle spasms.
Alternate Names
There is no internationally recognized non-proprietary name for this specific combination. It is generally referred to by its constituent generic names. Several brand names exist depending on the manufacturer and region.
How It Works
Pharmacodynamics: Aceclofenac reduces inflammation and pain by inhibiting COX-1 and COX-2 enzymes. Paracetamol’s mechanism is not fully understood but involves central inhibition of prostaglandin synthesis and other pathways. Chlorzoxazone depresses polysynaptic reflexes in the spinal cord and subcortical areas of the brain, leading to muscle relaxation.
Pharmacokinetics:
- Aceclofenac: Well absorbed orally. Metabolized in the liver, primarily by CYP2C9. Excreted in urine and bile.
- Paracetamol: Rapidly absorbed orally. Metabolized in the liver. Excreted in urine, primarily as glucuronide and sulfate conjugates.
- Chlorzoxazone: Rapidly and completely absorbed orally. Metabolized in the liver. Excreted in urine, primarily as metabolites.
Receptor Binding/Enzyme Inhibition: Aceclofenac inhibits COX-1 and COX-2 enzymes. Paracetamol’s mechanism may involve TRPA1 receptor antagonism and endocannabinoid system modulation. Chlorzoxazone does not directly bind to muscle receptors but acts centrally.
Elimination Pathways: Aceclofenac is primarily eliminated by hepatic metabolism followed by renal and biliary excretion. Paracetamol is mainly eliminated by hepatic metabolism followed by renal excretion. Chlorzoxazone is mainly eliminated by hepatic metabolism followed by renal excretion of metabolites.
Dosage
Standard Dosage
Adults: One tablet two to three times a day, preferably after meals. The maximum daily dose should not exceed 200mg aceclofenac, 4g paracetamol, and 3g Chlorzoxazone.
Children: This combination is not recommended for children.
Special Cases:
- Elderly Patients: Use with caution. Initiate therapy at the lowest effective dose and monitor closely for adverse effects. Dose adjustment may be necessary.
- Patients with Renal Impairment: Use with caution. Dosage adjustment may be required based on the degree of impairment.
- Patients with Hepatic Dysfunction: Use with caution. A lower initial dose of aceclofenac is recommended. Dosage adjustment may be required.
- Patients with Comorbid Conditions: Careful consideration is required in patients with cardiovascular disease, gastrointestinal disorders, or other relevant conditions. Individualized dosing and close monitoring are necessary.
Clinical Use Cases
This combination is not typically used in clinical settings like intubation, surgical procedures, mechanical ventilation, ICU, or emergency situations. Its primary use is for the management of musculoskeletal pain on an outpatient basis.
Dosage Adjustments
Dosage adjustments may be necessary based on patient-specific factors like renal or hepatic impairment, other medical conditions, concomitant medications, and response to therapy. Individualized dosing is essential to maximize efficacy and minimize adverse effects.
Side Effects
Common Side Effects: Nausea, vomiting, heartburn, stomach pain, diarrhea, loss of appetite, dizziness, drowsiness, fatigue, headache, skin rash, itching.
Rare but Serious Side Effects: Allergic reactions (e.g., angioedema, anaphylaxis), gastrointestinal bleeding or perforation, liver damage (especially with high doses of paracetamol), Stevens-Johnson syndrome, toxic epidermal necrolysis.
Long-Term Effects: Chronic use of NSAIDs like aceclofenac can increase the risk of cardiovascular events and renal impairment. Long-term use of high doses of paracetamol can cause liver damage.
Contraindications
- Hypersensitivity to any of the components.
- Active peptic ulcer or gastrointestinal bleeding.
- Severe hepatic or renal impairment.
- Severe heart failure.
- Last trimester of pregnancy.
- History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs.
Drug Interactions
- Anticoagulants (e.g., warfarin): Increased risk of bleeding.
- Methotrexate: Increased risk of methotrexate toxicity.
- Lithium: Increased lithium levels.
- Digoxin: Increased digoxin levels.
- Diuretics: Reduced diuretic effect and increased risk of renal impairment.
- Alcohol: Increased risk of gastrointestinal bleeding and drowsiness.
Pregnancy and Breastfeeding
Aceclofenac and Chlorzoxazone are contraindicated during pregnancy, especially in the third trimester. Aceclofenac is contraindicated during breastfeeding. Paracetamol is generally considered safe during pregnancy and breastfeeding, but its use should be limited to the lowest effective dose for the shortest possible duration.
Drug Profile Summary
- Mechanism of Action: Aceclofenac: COX inhibitor; Paracetamol: Central analgesic and antipyretic; Chlorzoxazone: Central muscle relaxant.
- Side Effects: Nausea, vomiting, dizziness, drowsiness, liver damage (paracetamol), gastrointestinal bleeding (aceclofenac).
- Contraindications: Hypersensitivity, active peptic ulcer, severe hepatic/renal impairment, pregnancy (third trimester), severe heart failure.
- Drug Interactions: Anticoagulants, methotrexate, lithium, digoxin, diuretics, alcohol.
- Pregnancy & Breastfeeding: Contraindicated (aceclofenac and chlorzoxazone in pregnancy, aceclofenac in breastfeeding).
- Dosage: Adults: 1 tablet 2-3 times/day.
- Monitoring Parameters: Liver function tests, renal function tests, signs of gastrointestinal bleeding.
Popular Combinations
This combination itself is a popular combination for musculoskeletal pain. Sometimes, it may be combined with other medications depending on the specific needs of the patient.
Precautions
- General Precautions: Monitor liver and renal function, especially with prolonged use.
- Specific Populations: Use with caution in the elderly, patients with renal/hepatic impairment, and pregnant/breastfeeding women (paracetamol only if necessary).
- Lifestyle Considerations: Avoid alcohol, monitor for drowsiness and avoid driving or operating machinery if affected.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Aceclofenac + Chlorzoxazone + Paracetamol?
A: The recommended dosage for adults is one tablet two to three times a day. It should not be used in children.
Q2: Can this combination be used in patients with a history of peptic ulcers?
A: No, it is contraindicated in patients with active or a history of recurrent peptic ulcers.
Q3: Can pregnant women take this combination?
A: No, aceclofenac and chlorzoxazone are contraindicated in pregnancy, especially in the third trimester. Paracetamol can be used with caution if clearly necessary, but should be limited to the lowest effective dose for the shortest duration.
Q4: What are the potential side effects of this medication?
A: Common side effects include nausea, vomiting, heartburn, dizziness, drowsiness, and fatigue. Serious side effects include allergic reactions, gastrointestinal bleeding, and liver damage.
Q5: What are the signs of liver damage associated with paracetamol?
A: Signs of liver damage can include yellowing of the skin and eyes (jaundice), dark urine, abdominal pain, and nausea.
Q6: Can patients with kidney disease use this medication?
A: Use with caution in patients with renal impairment. Dose adjustment may be necessary.
Q7: Does this medication interact with alcohol?
A: Yes, alcohol can increase the risk of gastrointestinal bleeding and drowsiness. Alcohol should be avoided while taking this medication.
Q8: Are there any dietary restrictions while taking this medication?
A: No specific dietary restrictions are associated with this medication. However, it is generally recommended to take it with food to minimize gastrointestinal side effects.
Q9: Can this combination be used long-term?
A: Long-term use should be avoided unless deemed absolutely necessary and under close medical supervision, due to the potential risks associated with chronic NSAID and paracetamol use. Regular monitoring of liver and renal function is essential.
Q10: What should a patient do if they miss a dose?
A: If a dose is missed, take it as soon as remembered. If it is close to the time for the next dose, skip the missed dose and take the next dose as scheduled. Do not double the dose to catch up.
