Usage
Aceclofenac + Tizanidine is prescribed for the relief of pain and inflammation associated with musculoskeletal and joint disorders, such as osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, low back pain, muscle spasms, and spasticity. It can also provide relief from dental pain, menstrual cramps, and headaches. This combination medication falls under the pharmacological classifications of Nonsteroidal Anti-inflammatory Drugs (NSAIDs) and Skeletal Muscle Relaxants. Aceclofenac works by inhibiting cyclooxygenase (COX) enzymes, reducing prostaglandin production, which are responsible for pain and inflammation. Tizanidine acts as a centrally acting muscle relaxant by inhibiting the release of excitatory neurotransmitters in the spinal cord and brain.
Alternate Names
While there are no widely recognized alternate generic names for this specific drug combination, various brand names exist depending on the manufacturer and region. Some examples include Tizanac AC, Zerodol-MR, and others.
How It Works
Pharmacodynamics: Aceclofenac exerts its analgesic and anti-inflammatory effects by inhibiting COX enzymes, primarily COX-2, thereby reducing prostaglandin synthesis. Tizanidine acts as an α2-adrenergic agonist, primarily within the central nervous system, leading to inhibition of excitatory neurotransmitter release and subsequent muscle relaxation.
Pharmacokinetics: Aceclofenac is well-absorbed orally, reaching peak plasma concentrations within 1-3 hours. It is extensively metabolized in the liver, primarily by CYP2C9, and excreted mainly through the kidneys. Tizanidine is also well-absorbed orally, with peak plasma levels achieved within 1-2 hours and a half-life of approximately 2-4 hours. It undergoes extensive hepatic metabolism, primarily via CYP1A2, and is primarily eliminated through the kidneys.
Mode of Action: Aceclofenac inhibits COX enzymes, responsible for prostaglandin formation at sites of injury and inflammation. This leads to reduced pain and swelling. Tizanidine binds to α2-adrenergic receptors in the central nervous system, modulating the release of excitatory neurotransmitters like glutamate and aspartate. This reduces muscle tone, relieves spasms, and improves muscle movement.
Dosage
Standard Dosage
Adults: The usual adult dose is one tablet containing 100 mg of Aceclofenac and 2 mg of Tizanidine, taken twice daily after meals. The maximum daily dose is two tablets.
Children: This combination is not recommended for children under 12 years of age due to limited safety and efficacy data.
Special Cases:
- Elderly Patients: Use with caution and initiate treatment at lower doses. Monitor for adverse effects and adjust dose as needed.
- Patients with Renal Impairment: Exercise caution and reduce the dose as needed. Monitor renal function closely.
- Patients with Hepatic Dysfunction: Use with caution and reduce the dose. Monitor liver function tests.
- Patients with Comorbid Conditions: Consider potential drug interactions and adjust dose accordingly.
Clinical Use Cases
The provided sources do not offer specific dosage guidelines for intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. Dosages in these scenarios should be determined based on individual patient needs and clinical context.
Dosage Adjustments
Dose adjustments may be necessary based on patient factors such as renal or hepatic dysfunction, comorbid conditions, and potential drug interactions. Always consider individual patient characteristics and clinical response when determining optimal dosing.
Side Effects
Common Side Effects:
Nausea, vomiting, stomach pain, diarrhea, dizziness, drowsiness, loss of appetite, heartburn.
Rare but Serious Side Effects:
Allergic reactions (anaphylaxis, skin rash), altered heart rate, hepatotoxicity, gastrointestinal bleeding.
Long-Term Effects:
Chronic use of NSAIDs like Aceclofenac may increase the risk of gastrointestinal complications.
Adverse Drug Reactions (ADR):
Severe allergic reactions, liver dysfunction, gastrointestinal bleeding require immediate intervention.
Contraindications
- Hypersensitivity to Aceclofenac or Tizanidine.
- Active or recent peptic ulcer or gastrointestinal bleeding.
- Severe heart failure, severe liver impairment, severe kidney impairment.
- Pregnancy (especially the third trimester).
Drug Interactions
- Other NSAIDs (increased risk of gastrointestinal side effects).
- Corticosteroids (increased risk of gastrointestinal bleeding).
- Blood thinners (increased risk of bleeding).
- Antihypertensives (may reduce the effectiveness of these medications).
- CYP1A2 inhibitors (fluvoxamine, ciprofloxacin; can increase Tizanidine levels).
- Alcohol (increased risk of drowsiness and gastrointestinal problems).
Pregnancy and Breastfeeding
Aceclofenac + Tizanidine should be avoided during pregnancy, especially in the third trimester, due to potential risks to the fetus. It is also not recommended during breastfeeding, as it may be excreted in breast milk and could potentially harm the infant. Consult with a physician for alternative pain management options.
Drug Profile Summary
- Mechanism of Action: Aceclofenac: COX inhibitor (primarily COX-2), reduces prostaglandin synthesis. Tizanidine: α2-adrenergic agonist, inhibits excitatory neurotransmitter release.
- Side Effects: Nausea, vomiting, stomach pain, diarrhea, dizziness, drowsiness.
- Contraindications: Hypersensitivity, active peptic ulcer, severe heart, liver, or kidney impairment, pregnancy.
- Drug Interactions: Other NSAIDs, corticosteroids, blood thinners, antihypertensives, CYP1A2 inhibitors.
- Pregnancy & Breastfeeding: Avoid during pregnancy, especially the third trimester, and breastfeeding.
- Dosage: Adults: One tablet (100 mg Aceclofenac + 2 mg Tizanidine) twice daily after meals.
- Monitoring Parameters: Liver function tests, renal function, blood pressure.
Popular Combinations
Aceclofenac is sometimes combined with Paracetamol for enhanced pain relief. However, combining multiple NSAIDs is generally not recommended.
Precautions
- Evaluate patients for pre-existing medical conditions, including heart, liver, and kidney function.
- Screen for allergies to NSAIDs or muscle relaxants.
- Exercise caution in elderly patients and those with renal or hepatic impairment.
- Advise patients against driving or operating machinery while taking this medication due to potential drowsiness.
- Avoid alcohol consumption during treatment.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Aceclofenac + Tizanidine?
A: The standard adult dose is one tablet (100 mg Aceclofenac + 2 mg Tizanidine) twice daily after meals.
Q2: Can Aceclofenac + Tizanidine be used in children?
A: No, this combination is generally not recommended for children under 12 years old.
Q3: What are the common side effects of Aceclofenac + Tizanidine?
A: Common side effects include nausea, vomiting, stomach pain, diarrhea, dizziness, and drowsiness.
Q4: Are there any serious side effects to watch out for?
A: Yes, rare but serious side effects can include allergic reactions, liver dysfunction, and gastrointestinal bleeding. Seek immediate medical attention if these occur.
Q5: Can I drink alcohol while taking Aceclofenac + Tizanidine?
A: It’s advisable to avoid alcohol as it can exacerbate drowsiness and increase the risk of gastrointestinal problems.
Q6: Can pregnant or breastfeeding women take this medication?
A: It’s contraindicated during pregnancy, especially the third trimester, and not recommended during breastfeeding. Consult a doctor for safer alternatives.
Q7: What should I do if I miss a dose?
A: Take the missed dose as soon as you remember. If it’s near the time of your next dose, skip the missed dose and continue your regular dosing schedule. Do not double the dose.
Q8: Does Aceclofenac + Tizanidine interact with other medications?
A: Yes, it can interact with other NSAIDs, corticosteroids, blood thinners, and certain antihypertensives. It’s crucial to inform your doctor about all other medications you are taking, including over-the-counter drugs and supplements.
Q9: Can I drive while taking Aceclofenac + Tizanidine?
A: It’s best to avoid driving or operating heavy machinery as this medication can cause drowsiness and dizziness.
Q10: What should I do if I experience any side effects?
A: Contact your doctor immediately if you experience any persistent or bothersome side effects, especially if they are severe.
