Usage
Aceclofenac + Diacerein is prescribed for the relief of pain and inflammation associated with osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis. It falls under the pharmacological classifications of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) and anti-rheumatic agents. The combination works by inhibiting cyclooxygenase (COX) enzymes, reducing prostaglandin production (which causes pain and inflammation), and blocking interleukin-1 beta (IL-1β), a protein that contributes to cartilage degradation.
Alternate Names
There are no widely recognized alternate generic names for the combination product itself. However, the individual components have other names. Aceclofenac is sometimes referred to as aclofenac, and diacerein is also known as diacetylrhein. Various brand names exist for this combination, including Onisrin-A, Sagasrin-A, and Protecfenac.
How It Works
Pharmacodynamics: Aceclofenac inhibits COX-1 and COX-2 enzymes, thereby reducing prostaglandin synthesis and mitigating pain and inflammation. Diacerein, a prodrug, metabolizes into rhein, which inhibits IL-1β, a key mediator in cartilage destruction and inflammation in osteoarthritis.
Pharmacokinetics: Aceclofenac is well-absorbed orally, reaching peak plasma concentrations within 1-3 hours. It is highly protein-bound and metabolized in the liver, primarily by CYP2C9. Elimination occurs through both renal and biliary routes. Diacerein is also absorbed orally but undergoes extensive first-pass metabolism to its active metabolite, rhein. Rhein’s elimination is primarily through the kidneys.
Mode of Action: Aceclofenac exerts its effects through non-selective COX inhibition. Diacerein, through its active metabolite rhein, reduces cartilage destruction by decreasing the expression of matrix metalloproteinases (MMP)-1 and -3 and diminishing interleukin-1 beta activity.
Dosage
Standard Dosage
Adults: The typical dose is 100 mg aceclofenac + 50 mg diacerein twice daily, taken orally with or after meals.
Children: Use in children is not recommended due to a lack of clinical data establishing safety and efficacy.
Special Cases:
- Elderly Patients: Due to the increased risk of adverse effects, careful monitoring of renal, cardiovascular, and hepatic function is required. The lowest effective dose should be used for the shortest possible duration. Dose adjustment might be necessary.
- Patients with Renal Impairment: Caution is advised, and dose reduction may be necessary in patients with moderate to severe renal impairment. Contraindicated in severe renal impairment.
- Patients with Hepatic Dysfunction: Dose reduction is recommended for patients with hepatic impairment. Contraindicated in severe hepatic dysfunction.
- Patients with Comorbid Conditions: Patients with a history of peptic ulcers, gastrointestinal bleeding, asthma, cardiovascular disease, or those undergoing heart surgery should be closely monitored.
Clinical Use Cases
The combination is not typically used for intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. Its primary indication is for the long-term management of osteoarthritis and other inflammatory joint conditions.
Dosage Adjustments
Dose adjustments are needed based on patient-specific factors like renal or hepatic dysfunction and other medical conditions. Regular monitoring of liver and kidney function, blood sugar levels, and blood components is advisable during long-term therapy.
Side Effects
Common Side Effects:
- Nausea
- Vomiting
- Diarrhea
- Abdominal pain
- Indigestion
- Heartburn
- Flatulence
- Loss of appetite
- Intense yellow urine
- Dizziness
- Rash, itching
- Eczema
Rare but Serious Side Effects:
- Gastrointestinal bleeding or perforation
- Severe allergic reactions (anaphylaxis)
- Liver damage (hepatitis)
- Kidney damage
- Stevens-Johnson syndrome
- Toxic epidermal necrolysis
- Meningitis
Long-Term Effects:
- Chronic gastrointestinal issues
- Renal dysfunction
- Hepatic impairment
Adverse Drug Reactions (ADR): Severe skin reactions, signs of meningitis, gastrointestinal bleeding, liver or kidney damage.
Contraindications
- Hypersensitivity to aceclofenac, diacerein, or any components.
- Active peptic ulcer, recent gastrointestinal bleeding or perforation.
- Severe liver or kidney failure.
- Severe heart failure.
- Inflammatory bowel disease (e.g., Crohn’s disease, ulcerative colitis)
- Intestinal obstruction
- Pregnancy (especially the last trimester) and breastfeeding.
- History of asthma, urticaria, or hypersensitivity reactions to NSAIDs.
- Coronary artery bypass graft surgery.
Drug Interactions
- Other NSAIDs (aspirin, ibuprofen)
- Anticoagulants (warfarin, dabigatran)
- Antiplatelet drugs (clopidogrel, ticagrelor)
- Corticosteroids (prednisone)
- SSRIs (fluoxetine, citalopram)
- Diuretics (furosemide, torsemide)
- ACE inhibitors/ARBs (lisinopril, benazepril)
- Lithium
- Methotrexate
- Cyclosporine
- Antacids (aluminum hydroxide, magnesium hydroxide)
- Antibiotics (amoxicillin/clavulanic acid)
- Cardiac glycosides (digoxin)
- Alcohol
Pregnancy and Breastfeeding
Aceclofenac + Diacerein is contraindicated during pregnancy, especially the last trimester, and while breastfeeding. It can have adverse effects on the fetus and may be excreted in breast milk.
Drug Profile Summary
- Mechanism of Action: Aceclofenac inhibits COX enzymes; diacerein (metabolized to rhein) inhibits IL-1β.
- Side Effects: Nausea, vomiting, diarrhea, abdominal pain, gastrointestinal bleeding, liver/kidney damage.
- Contraindications: Hypersensitivity, peptic ulcer, severe liver/kidney/heart failure, pregnancy, breastfeeding.
- Drug Interactions: NSAIDs, anticoagulants, diuretics, lithium, methotrexate.
- Pregnancy & Breastfeeding: Contraindicated.
- Dosage: 100 mg/50 mg twice daily (adult), adjustments needed for specific populations.
- Monitoring Parameters: Liver and kidney function, blood counts, blood sugar.
Popular Combinations
The combination of aceclofenac and diacerein itself is a common pairing for managing osteoarthritis. It is not generally combined with other drugs for this indication, though other medications may be used to manage comorbidities.
Precautions
- Pre-screening for allergies, hepatic/renal dysfunction, and relevant medical history is crucial.
- Avoid alcohol consumption during treatment.
- Monitor for gastrointestinal and other side effects.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Aceclofenac + Diacerein?
A: The standard adult dosage is 100 mg aceclofenac + 50 mg diacerein twice daily, taken orally with food. Dosages may need adjustments based on patient-specific conditions.
Q2: How does Aceclofenac + Diacerein work for osteoarthritis?
A: Aceclofenac reduces pain and inflammation, while diacerein slows the progression of cartilage degradation.
Q3: What are the common side effects of this combination?
A: Common side effects include nausea, diarrhea, abdominal pain, and altered urine color.
Q4: Who should avoid taking Aceclofenac + Diacerein?
A: Pregnant or breastfeeding women, individuals with severe liver/kidney issues, and those with active peptic ulcers should not take it.
Q5: Are there any drug interactions I should be aware of?
A: Yes, this drug interacts with several other medications, including NSAIDs, anticoagulants, and some diuretics. It’s essential to inform your physician about all other medications you are taking.
Q6: Can I drink alcohol while taking Aceclofenac + Diacerein?
A: Alcohol is not advised as it can increase the risk of stomach problems.
Q7: What if I miss a dose?
A: Take the missed dose as soon as you remember unless it is close to your next dose. Do not double the dose.
Q8: Can Aceclofenac + Diacerein cure osteoarthritis?
A: It does not cure osteoarthritis but helps manage pain and slow down disease progression.
Q9: How long should I take this medication?
A: The duration of treatment should be determined by your doctor based on your specific condition and response to therapy.
