Usage
- Medical Conditions: Aceclofenac + Tramadol is prescribed for the symptomatic treatment of moderate to severe acute pain, such as postoperative pain, trauma, and other painful conditions where a combination of NSAID and opioid analgesic is warranted. It is effective for both acute and chronic pain conditions such as osteoarthritis.
- Pharmacological Classification: Analgesic (combining a non-steroidal anti-inflammatory drug (NSAID) and an opioid analgesic).
- Mechanism of Action: Aceclofenac inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis, thereby decreasing inflammation and pain. Tramadol acts as a centrally acting analgesic. Its primary metabolite, O-desmethyltramadol (M1) binds to mu-opioid receptors, inhibiting pain signal transmission. Tramadol also inhibits serotonin and norepinephrine reuptake, further contributing to pain relief.
Alternate Names
- No widely recognized alternate generic names exist.
- Brand Names: Various brand names are available depending on the region/country, often combining prefixes or suffixes with the generic components (e.g., Aceclo + Tram, Tramadol/Aceclofenac).
How It Works
- Pharmacodynamics: Aceclofenac exerts its anti-inflammatory and analgesic effects by inhibiting COX-1 and COX-2 enzymes, which are responsible for the production of prostaglandins. Tramadol and its metabolite M1 exert their analgesic effects by binding to mu-opioid receptors in the central nervous system, thus modulating pain perception. Tramadol also inhibits the reuptake of serotonin and norepinephrine, which contributes to its analgesic effect.
- Pharmacokinetics:
- Absorption: Aceclofenac is rapidly absorbed after oral administration, reaching peak plasma concentrations within 1-3 hours. Tramadol is also well-absorbed orally, with peak plasma concentrations occurring in approximately 2 hours. Food can delay the rate but not the extent of tramadol absorption.
- Metabolism: Aceclofenac is extensively metabolized in the liver, primarily by CYP2C9. Tramadol undergoes hepatic metabolism, primarily by CYP2D6 and CYP3A4. M1 (O-desmethyltramadol) is a more potent mu-opioid agonist than tramadol.
- Elimination: Aceclofenac is primarily eliminated renally as metabolites. Tramadol and its metabolites are primarily excreted in the urine.
- Mode of Action: Aceclofenac inhibits COX enzymes, decreasing prostaglandin synthesis. Tramadol binds to mu-opioid receptors and inhibits reuptake of serotonin and norepinephrine. M1 has a greater affinity for mu-opioid receptors than tramadol, contributing significantly to the analgesic effect.
Dosage
Standard Dosage
Adults: One tablet of Aceclofenac 100 mg + Tramadol 37.5 mg twice daily, administered orally with or after meals. The maximum daily dose should not exceed two tablets.
Children: Not recommended for children under 12 years of age. For adolescents 12 years and older, dosage should be determined by a physician and carefully monitored.
Special Cases:
- Elderly Patients: Start with the lowest effective dose and monitor closely for adverse effects. Dose adjustments may be necessary based on renal and hepatic function.
- Patients with Renal Impairment: Use with caution. Dose adjustment is necessary in patients with moderate to severe renal impairment.
- Patients with Hepatic Dysfunction: Use with caution. Dose reduction may be necessary in patients with moderate hepatic impairment. Avoid use in patients with severe hepatic impairment.
- Patients with Comorbid Conditions: Use with caution in patients with a history of seizures, respiratory depression, substance abuse, or gastrointestinal disorders.
Clinical Use Cases
The combination is not typically used in the clinical scenarios presented due to the potential for respiratory depression and the availability of more suitable alternatives:
- Intubation: Alternatives preferred.
- Surgical Procedures: Alternatives preferred for intraoperative and postoperative analgesia.
- Mechanical Ventilation: Avoid, due to the risk of respiratory depression.
- Intensive Care Unit (ICU) Use: Alternatives preferred.
- Emergency Situations: Other analgesics are generally more suitable.
Dosage Adjustments
Dose adjustments are required for patients with renal or hepatic impairment.
Side Effects
Common Side Effects
Nausea, vomiting, dizziness, drowsiness, constipation, headache, dry mouth, indigestion.
Rare but Serious Side Effects
Allergic reactions (e.g., skin rash, itching, swelling), seizures, respiratory depression, serotonin syndrome, hepatotoxicity.
Long-Term Effects
Potential for tolerance, dependence, and opioid withdrawal syndrome with prolonged use.
Adverse Drug Reactions (ADR)
Serotonin syndrome, respiratory depression, anaphylaxis, Stevens-Johnson syndrome.
Contraindications
Hypersensitivity to aceclofenac or tramadol, severe respiratory depression, acute or severe bronchial asthma, gastrointestinal obstruction, acute intoxication with alcohol or opioids, concomitant use of MAO inhibitors, severe hepatic impairment, severe renal impairment, known epilepsy uncontrolled by treatment.
Drug Interactions
MAO inhibitors, other opioids, CNS depressants (e.g., alcohol, benzodiazepines), serotonergic drugs (e.g., SSRIs, triptans), anticoagulants (e.g., warfarin), CYP2D6 and CYP3A4 inhibitors or inducers.
Pregnancy and Breastfeeding
Tramadol is not recommended during pregnancy. Aceclofenac should be avoided in the third trimester. Tramadol is excreted in breast milk; use caution during breastfeeding.
Drug Profile Summary
- Mechanism of Action: Aceclofenac: COX inhibitor, Tramadol: mu-opioid agonist, serotonin and norepinephrine reuptake inhibitor.
- Side Effects: Nausea, vomiting, dizziness, drowsiness, constipation. Serious: Seizures, respiratory depression, serotonin syndrome.
- Contraindications: Hypersensitivity, respiratory depression, GI obstruction, acute intoxication with alcohol or opioids, severe hepatic/renal impairment.
- Drug Interactions: MAOIs, other opioids, CNS depressants, SSRIs, anticoagulants, CYP2D6 and CYP3A4 inhibitors/inducers.
- Pregnancy & Breastfeeding: Avoid tramadol during pregnancy. Avoid aceclofenac in the third trimester. Use caution with breastfeeding.
- Dosage: Adults: One tablet of Aceclofenac 100 mg + Tramadol 37.5 mg twice daily.
- Monitoring Parameters: Respiratory rate, mental status, pain level, liver and renal function.
Popular Combinations
While Aceclofenac + Tramadol is itself a combination, it is not generally combined with other drugs due to the risk of interactions and additive adverse effects.
Precautions
- General Precautions: Monitor for adverse reactions, especially respiratory depression and serotonin syndrome. Assess for substance abuse history.
- Specific Populations: Adjust dosage for renal/hepatic impairment. Avoid in pregnancy/breastfeeding unless absolutely necessary. Not recommended for children under 12.
- Lifestyle Considerations: Avoid alcohol. Avoid operating machinery until effects are known.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Aceclofenac + Tramadol?
A: One tablet of Aceclofenac 100 mg + Tramadol 37.5 mg twice daily, orally with or after food.
Q2: Can this combination be used for long-term pain management?
A: Prolonged use should be avoided due to the risk of tolerance, dependence, and withdrawal symptoms. Re-evaluate the need for continued use regularly.
Q3: What are the serious side effects to watch out for?
A: Respiratory depression, seizures, serotonin syndrome, allergic reactions, and gastrointestinal bleeding.
Q4: Can this combination be used during pregnancy or breastfeeding?
A: Generally avoided unless the benefits clearly outweigh the risks. Tramadol can cause neonatal withdrawal symptoms. Consult with a specialist.
Q5: What are the key drug interactions with this combination?
A: MAOIs, alcohol, other opioids, benzodiazepines, SSRIs, triptans, and anticoagulants can interact significantly.
Q6: How should the dosage be adjusted for patients with renal or hepatic impairment?
A: Reduce the dose or avoid use altogether in moderate to severe renal or hepatic impairment. Consult prescribing information or a specialist.
Q7: What are the symptoms of tramadol overdose?
A: Pinpoint pupils, respiratory depression, loss of consciousness, and seizures. Administer naloxone if opioid overdose is suspected.
Q8: Is Aceclofenac + Tramadol addictive?
A: Yes, Tramadol, an opioid component of the medication, has the potential for addiction and dependence. Use for the shortest duration possible and monitor closely.
Q9: Can this drug be crushed or chewed?
A: It’s generally recommended to swallow the tablets whole with water. Crushing or chewing may alter the release of the medication.
Q10: What should patients do if they miss a dose?
A: Take the missed dose as soon as remembered, unless it’s close to the next scheduled dose. Do not double the dose.
