Usage
- Medical Conditions: This combination medication is primarily prescribed for the relief of pain and inflammation associated with muscle spasms in musculoskeletal conditions like low back pain, sprains, and strains. It can also be used for osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis.
- Pharmacological Classification: Analgesic, anti-inflammatory, and muscle relaxant.
- Mechanism of Action: Aceclofenac, a nonsteroidal anti-inflammatory drug (NSAID), works by inhibiting the production of prostaglandins, chemical messengers that cause pain and inflammation. Paracetamol is an analgesic and antipyretic that acts centrally to reduce pain and fever. Tolperisone is a centrally acting muscle relaxant that works on the spinal cord and brain to relieve muscle stiffness and spasms without affecting muscle strength.
Alternate Names
- No internationally recognized alternate generic names exist. Regional variations may occur.
- Brand Names: Various brands exist depending on the manufacturer, including but not limited to TEEPRAX-AP, Set-N, Brudol-MR, and Dolset-TP.
How It Works
- Pharmacodynamics: Aceclofenac inhibits COX enzymes, reducing prostaglandin synthesis and thus inflammation and pain. Paracetamol acts centrally on the nervous system, reducing pain perception and fever. Tolperisone inhibits sodium and calcium channels in neuronal tissue, suppressing reflex activity and pain perception, leading to muscle relaxation.
- Pharmacokinetics:
- Absorption: All three components are absorbed orally. Taking it with food may help with absorption and reduce gastrointestinal side effects.
- Metabolism: Aceclofenac is metabolized in the liver, primarily by CYP2C9. Paracetamol is mainly metabolized in the liver, with a small portion undergoing glucuronidation and sulfation. Tolperisone is extensively metabolized in the liver.
- Elimination: Aceclofenac is excreted primarily through the kidneys. Paracetamol metabolites are also excreted through the kidneys. Tolperisone is excreted through the urine and bile.
Dosage
Standard Dosage
Adults:
- One tablet twice daily, typically after meals.
Children:
- Not generally recommended for children under 18 years of age. Some sources state use is possible from 12 or even 6 years, depending on the exact formulation. Safety and efficacy in pediatric populations haven’t been well-established.
Special Cases:
- Elderly Patients: Start with a lower dose and monitor closely for adverse effects, considering potential age-related decline in hepatic and renal function.
- Patients with Renal Impairment: Reduce the dose based on the degree of impairment. Use with caution in moderate to severe renal impairment.
- Patients with Hepatic Dysfunction: Reduce the dose based on the degree of impairment. Use with caution in moderate to severe hepatic impairment.
- Patients with Comorbid Conditions: Assess potential drug interactions with other medications the patient is taking. Exercise caution in patients with cardiovascular disease or a history of peptic ulcer.
Clinical Use Cases
- The combination isn’t specifically indicated for procedures such as intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. Its use is primarily limited to managing pain associated with musculoskeletal conditions.
Dosage Adjustments
- Adjust dosages based on renal and hepatic function, co-existing medical conditions, and other medications the patient is taking.
Side Effects
Common Side Effects:
- Nausea, vomiting, dizziness, drowsiness, headache, dyspepsia, abdominal pain, diarrhea, dry mouth, weakness.
Rare but Serious Side Effects:
- Allergic reactions (skin rash, itching, breathing difficulty, swelling of face), gastrointestinal bleeding, liver damage, kidney problems.
Long-Term Effects:
- Prolonged use of NSAIDs can increase the risk of cardiovascular events and gastrointestinal complications.
Adverse Drug Reactions (ADR):
- Any signs of allergic reactions or severe gastrointestinal problems require immediate intervention. Monitor for liver or renal dysfunction.
Contraindications
- Hypersensitivity to any component, active peptic ulcer, severe heart/liver/renal impairment, third trimester of pregnancy.
Drug Interactions
- NSAIDs: Concomitant use of multiple NSAIDs can increase the risk of gastrointestinal side effects.
- Anticoagulants: Aceclofenac can enhance the effects of anticoagulants like warfarin, potentially increasing bleeding risk.
- Antihypertensives: May reduce the efficacy of antihypertensive medications.
- Alcohol: Increases the risk of gastrointestinal side effects and liver damage.
- Other potential interactions: Metoclopramide, domperidone, cholestyramine, liver enzyme-inducing medications (carbamazepine, phenytoin), digoxin, lithium.
Pregnancy and Breastfeeding
- Pregnancy: Contraindicated in the third trimester. Use with caution during the first and second trimesters.
- Breastfeeding: Exercise caution, as small amounts of the drugs may be excreted in breast milk. Potential effects on the neonate are unknown.
Drug Profile Summary
- Mechanism of Action: Aceclofenac: COX inhibitor, Paracetamol: central analgesic and antipyretic, Tolperisone: central muscle relaxant.
- Side Effects: Nausea, dizziness, drowsiness, dyspepsia, abdominal pain, allergic reactions, GI bleeding.
- Contraindications: Hypersensitivity, active peptic ulcer, severe heart/liver/renal impairment, third trimester of pregnancy.
- Drug Interactions: NSAIDs, anticoagulants, antihypertensives, alcohol.
- Pregnancy & Breastfeeding: Use with caution. Contraindicated in the third trimester of pregnancy.
- Dosage: Adults: 1 tablet twice daily. Adjustments required in special populations.
- Monitoring Parameters: Liver and renal function, blood pressure.
Popular Combinations
- Often prescribed alone. Combination therapy is generally not recommended.
Precautions
- General Precautions: Assess for allergies, medical history, and concomitant medications. Monitor renal and liver function.
- Specific Populations: As described above.
- Lifestyle Considerations: Avoid alcohol. Caution when driving or operating machinery.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Aceclofenac + Paracetamol + Tolperisone?
A: One tablet twice daily for adults. Adjustments may be needed based on individual patient conditions. Not recommended for children.
Q2: Can this medication be taken with food?
A: Yes, it is recommended to take this medication with or after food to reduce the risk of gastrointestinal upset.
Q3: What are the common side effects?
A: Common side effects include nausea, dizziness, drowsiness, dyspepsia, and abdominal pain.
Q4: Is it safe to take during pregnancy?
A: It is contraindicated in the third trimester of pregnancy and should be used with caution during the first and second trimesters, only if clearly needed.
Q5: Are there any drug interactions I should be aware of?
A: Yes, this medication can interact with other NSAIDs, anticoagulants, antihypertensives, and alcohol. It can also potentially interact with other medications such as metoclopramide, domperidone, and cholestyramine. Always inform your doctor about all other medications you are taking.
Q6: What should I do if I miss a dose?
A: Take the missed dose as soon as you remember. However, if it is close to the time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not double the dose to catch up.
Q7: How long does it take to see the effects of this medication?
A: Some effects, like pain relief, may be noticeable within a few hours. However, the full benefits, particularly the anti-inflammatory effects of aceclofenac, may take several days or weeks to become apparent.
Q8: Can I drink alcohol while taking this medication?
A: No, it is not recommended to consume alcohol while taking this medication, as it can increase the risk of gastrointestinal side effects and liver damage.
Q9: Can I drive while taking this medication?
A: This medication may cause dizziness or drowsiness. It’s advisable to avoid driving or operating machinery if you experience these side effects.
