Usage
Aceclofenac + Cyclobenzaprine is prescribed for the relief of muscle spasm associated with acute, painful musculoskeletal conditions such as:
- Osteoarthritis
- Rheumatoid arthritis
- Ankylosing spondylitis
- Acute pain
- Chronic low back pain
- Muscle spasms
- Gouty arthritis
Pharmacological Classification:
- Aceclofenac: Non-Steroidal Anti-Inflammatory Drug (NSAID)
- Cyclobenzaprine: Skeletal Muscle Relaxant
Mechanism of Action: Aceclofenac inhibits cyclooxygenase (COX) enzymes, reducing pain and inflammation. Cyclobenzaprine acts centrally to reduce muscle spasm, possibly by affecting serotonin, norepinephrine, and dopamine levels in the central nervous system. It also affects brain stem and spinal cord decreasing muscle contractions.
Alternate Names
This medication may be marketed under various brand names, including Flexabenz Plus, Zorifen MR, CycloVib Plus and others. Several brand names may exist regionally.
How It Works
Pharmacodynamics: Aceclofenac reduces inflammation and pain by inhibiting COX enzymes. Cyclobenzaprine acts centrally to reduce muscle spasm, possibly by affecting serotonin, norepinephrine, and dopamine levels in the central nervous system.
Pharmacokinetics:
- Aceclofenac: Well-absorbed orally, metabolized in the liver, primarily by CYP2C9.
- Cyclobenzaprine: Extensively metabolized, primarily by CYP3A4 and 1A2, eliminated through the kidneys. It may undergo glucuronidation.
Mode of Action: Aceclofenac blocks COX enzymes, reducing prostaglandin synthesis, leading to decreased pain and inflammation. Cyclobenzaprine’s exact mechanism isn’t fully understood, but it’s believed to work centrally in the brain and spinal cord to decrease muscle contractions.
Receptor Binding/Enzyme Inhibition/Neurotransmitter Modulation: Aceclofenac inhibits COX enzymes. Cyclobenzaprine may affect serotonin, norepinephrine, and dopamine levels.
Elimination Pathways: Aceclofenac is eliminated primarily through hepatic metabolism, with a smaller portion excreted in the urine as unchanged drug. For Cyclobenzaprine, metabolites and unchanged drug are excreted in urine.
Dosage
Standard Dosage
Adults: One tablet of Aceclofenac 200mg + Cyclobenzaprine 15mg once daily, taken orally with food. Some patients may require 30mg of Cyclobenzaprine daily.
Children: Use in children below 18 years is not recommended due to lack of established safety and efficacy data.
Special Cases:
- Elderly Patients: Extended-release formulations are not recommended. Dosage adjustments may be necessary for standard formulations.
- Patients with Renal Impairment: Dose adjustment may be required. Avoid in severe renal impairment.
- Patients with Hepatic Dysfunction: Use with caution. Dose adjustment may be needed. Avoid in moderate to severe hepatic impairment.
- Patients with Comorbid Conditions: Use with caution in patients with cardiovascular disease, hypertension, diabetes, stomach ulcers, bleeding disorders, hyperthyroidism, asthma, and porphyria.
Clinical Use Cases
Dosage for these settings should be determined on a case-by-case basis in consultation with a specialist, as the standard formulation might not be appropriate.
Dosage Adjustments
Adjustments may be necessary based on renal/hepatic function, other medical conditions, and concomitant medications.
Side Effects
Common Side Effects:
- Nausea
- Dry mouth
- Dizziness
- Stomach pain
- Drowsiness
- Sleepiness
- Heartburn
- Diarrhea
- Loss of appetite
Rare but Serious Side Effects:
- Allergic reactions (e.g., rash, itching, swelling, severe dizziness, trouble breathing)
- Serotonin syndrome (e.g., agitation, hallucinations, fever, sweating, shivering, fast heart rate, muscle stiffness, twitching, loss of coordination, nausea, vomiting, diarrhea)
- Cardiac events
Long-Term Effects:
- Potential for gastrointestinal issues with prolonged NSAID use.
Contraindications
- Hypersensitivity to aceclofenac, cyclobenzaprine, or other NSAIDs
- Recent heart attack (myocardial infarction)
- Heart block or arrhythmias
- Hyperthyroidism
- Moderate to severe hepatic impairment
- Moderate to severe renal impairment
- Concurrent use of MAO inhibitors
- Third trimester of pregnancy
- Asthma
- Porphyria
Drug Interactions
- Alcohol: Increased risk of drowsiness and gastrointestinal bleeding
- MAO inhibitors: Hypertensive crisis
- Tricyclic antidepressants: Enhanced effects and side effects
- CNS depressants: Additive sedative effects
- CYP3A4 inhibitors or inducers: Altered metabolism of cyclobenzaprine
- Digoxin
- Aspirin and other NSAIDs
- Morphine
- Clopidogrel
- Selegiline
- Lithium
- Captopril
- Amiloride
- Tacrolimus
- Chlorpheniramine
- Zolpidem
Pregnancy and Breastfeeding
- Pregnancy: Not recommended, particularly in the third trimester. Use only if benefits clearly outweigh the risks.
- Breastfeeding: Small amounts may pass into breast milk. Use with caution and monitor infant for drowsiness and adequate weight gain. Safer alternatives may be preferred.
Drug Profile Summary
- Mechanism of Action: Aceclofenac: COX inhibitor, reduces pain and inflammation. Cyclobenzaprine: Central muscle relaxant, reduces muscle spasm.
- Side Effects: Nausea, dry mouth, dizziness, stomach pain, drowsiness, sleepiness.
- Contraindications: Hypersensitivity, recent MI, heart block, hyperthyroidism, hepatic/renal impairment, MAO inhibitor use, third-trimester pregnancy, asthma, porphyria.
- Drug Interactions: Alcohol, MAO inhibitors, tricyclic antidepressants, CNS depressants, CYP3A4 modulators, several other medications (see detailed list above).
- Pregnancy & Breastfeeding: Use with caution, consult physician. Generally not recommended.
- Dosage: Adults: Aceclofenac 200mg/Cyclobenzaprine 15mg once daily. Adjust for renal/hepatic impairment.
- Monitoring Parameters: Liver function, kidney function, cardiovascular status.
Popular Combinations
This combination itself is commonly used. Individual components may be combined with other analgesics or muscle relaxants as needed.
Precautions
- Monitor for cardiovascular events and gastrointestinal bleeding.
- Caution in patients with pre-existing heart, liver, or kidney conditions.
- Avoid alcohol.
- Avoid driving or operating machinery if experiencing drowsiness or dizziness.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Aceclofenac + Cyclobenzaprine?
A: The standard adult dosage is one tablet of Aceclofenac 200mg + Cyclobenzaprine 15mg once a day, taken orally with food.
Q2: Can this medication be used in children?
A: No, its use is not recommended in children under 18 due to lack of safety and efficacy data.
Q3: What are the common side effects?
A: Common side effects include nausea, dry mouth, dizziness, stomach pain, drowsiness, and sleepiness.
Q4: Are there any serious side effects?
A: Yes, though rare, serious side effects like allergic reactions, serotonin syndrome, and cardiovascular events can occur. Seek immediate medical attention if these develop.
Q5: Can I drink alcohol while taking this medication?
A: No, alcohol should be avoided as it can increase the risk of drowsiness, dizziness, and gastrointestinal bleeding.
Q6: What should I do if I miss a dose?
A: If you miss a dose, take it as soon as you remember, unless it’s almost time for your next dose. Do not double the dose to catch up.
Q7: Can pregnant or breastfeeding women take this medication?
A: This medication is generally not recommended during pregnancy, especially in the third trimester, and should be used with caution during breastfeeding. Consult a doctor for guidance.
A: Inform your doctor if you have any history of heart, liver, or kidney problems, stomach ulcers, bleeding disorders, hyperthyroidism, asthma, porphyria, or allergies to any medications. Also, inform your doctor about all other medications you are currently taking.
Q9: What is the mechanism by which Cyclobenzaprine reduce muscle spasm?
A: Cyclobenzaprine reduce muscle spasm through central action: It possibly by affecting serotonin, norepinephrine, and dopamine levels in the central nervous system. It also through its action on brain stem and spinal cord decrease muscle contractions
