Diacerein: Targeted Joint Support for Osteoarthritis Management
| Product dosage: 50 mg | |||
|---|---|---|---|
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| 180 | $0.92
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Synonyms | |||
Diacerein is a disease-modifying osteoarthritis drug (DMOAD) specifically formulated to address the underlying pathophysiology of osteoarthritis rather than merely masking symptoms. As an interleukin-1 inhibitor, it works by modulating the biochemical processes responsible for cartilage degradation and inflammation. This prescription medication offers a unique mechanism of action distinct from conventional analgesics and NSAIDs, making it particularly valuable for long-term joint health management. Clinical evidence supports its ability to slow disease progression while providing sustained symptomatic relief.
Features
- Active ingredient: Diacerein 50mg
- Pharmaceutical form: Capsules or tablets
- Mechanism: Selective interleukin-1β inhibitor
- Bioavailability: Approximately 35-56%
- Half-life: Approximately 4-6 hours (diacerein), 25-30 hours (active metabolite rhein)
- Metabolism: Hepatic hydrolysis to active metabolite rhein
- Excretion: Primarily renal (60-70%), fecal (20-25%)
Benefits
- Modifies disease progression by inhibiting cartilage-degrading enzymes
- Reduces joint pain and stiffness through anti-inflammatory mechanisms
- Improves physical function and mobility in osteoarthritis patients
- Provides sustained therapeutic effects that persist after treatment discontinuation
- Demonstrates chondroprotective properties by promoting cartilage matrix synthesis
- Offers favorable gastrointestinal safety profile compared to traditional NSAIDs
Common use
Diacerein is primarily indicated for the symptomatic treatment of osteoarthritis, particularly affecting weight-bearing joints such as knees and hips. It is prescribed for patients experiencing mild to moderate osteoarthritis where disease modification is clinically desirable. The medication is typically considered when conventional first-line treatments provide insufficient relief or cause unacceptable side effects. Medical practitioners may recommend diacerein for patients who would benefit from its disease-modifying properties, especially those showing early radiographic evidence of joint space narrowing. The therapeutic effects become clinically apparent after 2-4 weeks of continuous treatment, with maximum benefits typically observed after 3-4 months of therapy.
Dosage and direction
The standard adult dosage is 50mg twice daily, taken with meals to enhance absorption and minimize gastrointestinal discomfort. Treatment initiation typically begins with 50mg once daily for the first 2-4 weeks to assess tolerance before increasing to the maintenance dose. For elderly patients or those with renal impairment, dosage adjustment may be necessary based on creatinine clearance levels. The capsules should be swallowed whole with a full glass of water and not crushed or chewed. Treatment duration is generally long-term, often extending for several months to years, with regular medical supervision to assess therapeutic response and potential side effects. Discontinuation should be gradual rather than abrupt to maintain therapeutic benefits.
Precautions
Patients with pre-existing gastrointestinal conditions, particularly those with history of inflammatory bowel disease, should exercise caution when using diacerein. Regular monitoring of renal function is recommended during prolonged therapy, especially in elderly patients or those with pre-existing renal impairment. Hepatic function should be assessed periodically, as the medication undergoes significant hepatic metabolism. Diacerein may cause photosensitivity reactions, necessitating sun protection measures during treatment. Patients should be advised that the medication may cause a harmless reddish discoloration of urine due to its metabolite excretion. Use during pregnancy should be avoided unless clearly necessary, and breastfeeding is not recommended during therapy.
Contraindications
Diacerein is contraindicated in patients with known hypersensitivity to diacerein, rhein, or any excipients in the formulation. It should not be used in patients with severe hepatic impairment (Child-Pugh class C) or severe renal impairment (creatinine clearance <30 mL/min). The medication is contraindicated in patients with active inflammatory bowel disease, such as Crohn’s disease or ulcerative colitis. It should not be administered to children or adolescents under 18 years of age due to insufficient safety data. Concomitant use with potent CYP3A4 inducers or inhibitors may require alternative therapy selection.
Possible side effects
The most frequently reported adverse effects involve the gastrointestinal system, including diarrhea (occurring in approximately 30-40% of patients), abdominal pain, and soft stools. These symptoms are typically dose-dependent and often diminish with continued treatment. Other reported side effects include nausea, vomiting, and epigastric discomfort. Dermatological reactions such as pruritus, rash, and photosensitivity may occur in some patients. Hepatic enzyme elevations have been observed in clinical trials, though significant hepatotoxicity is rare. Urine discoloration (yellow-orange to red) is a common, harmless effect related to metabolite excretion. Serious adverse effects including severe diarrhea requiring hospitalization occur in approximately 2-4% of patients.
Drug interaction
Diacerein may interact with anticoagulants like warfarin, potentially enhancing their anticoagulant effect and requiring closer INR monitoring. Concomitant use with other hepatically metabolized drugs may require dosage adjustments due to potential metabolic interactions. The absorption of diacerein may be reduced when taken with antacids containing aluminum or magnesium. CYP3A4 inhibitors such as ketoconazole may increase diacerein concentrations, while inducers like rifampicin may decrease its efficacy. Concurrent administration with other anti-osteoarthritis medications should be carefully monitored for additive therapeutic effects or increased adverse reactions.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is nearly time for the next scheduled dose. In that case, the missed dose should be skipped, and the regular dosing schedule resumed. Patients should not double the dose to make up for a missed administration. Consistent dosing is important for maintaining therapeutic levels, but occasional missed doses are unlikely to significantly impact overall treatment efficacy. If multiple doses are missed, patients should consult their healthcare provider before resuming therapy to determine if any dosage adjustment is necessary.
Overdose
Symptoms of overdose may include severe diarrhea, abdominal cramps, nausea, and vomiting. In cases of significant overdose, electrolyte imbalance and dehydration may occur due to persistent diarrhea. There is no specific antidote for diacerein overdose. Management should focus on symptomatic and supportive care, including fluid and electrolyte replacement. Gastric lavage may be considered if ingestion occurred within one hour. Activated charcoal administration may help reduce further absorption. Patients should seek immediate medical attention if overdose is suspected, particularly if severe gastrointestinal symptoms develop or persist.
Storage
Diacerein capsules should be stored at room temperature (15-30°C) in their original packaging to protect from light and moisture. The medication should be kept in a secure location away from direct sunlight and heat sources. Keep the container tightly closed when not in use to prevent degradation. Do not store in bathrooms or other areas with high humidity. Keep out of reach of children and pets. Do not use beyond the expiration date printed on the packaging. Proper storage conditions help maintain pharmaceutical stability and efficacy throughout the shelf life.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Diacerein is a prescription medication that should only be used under the supervision of a qualified healthcare professional. Individual response to treatment may vary, and not all patients will experience the same benefits or side effects. The prescribing physician should make dosage decisions based on individual patient characteristics and medical history. Patients should not discontinue or modify their treatment regimen without consulting their healthcare provider. Always follow the specific instructions provided by your prescribing physician and refer to the official prescribing information for complete details.
Reviews
Clinical studies demonstrate that diacerein provides significant improvement in pain scores and functional capacity compared to placebo, with effects sustained beyond treatment discontinuation. Meta-analyses of randomized controlled trials show moderate efficacy in reducing joint space narrowing progression over 2-3 years of treatment. Patient-reported outcomes indicate improved quality of life measures, particularly regarding mobility and daily activities. Gastroenterological side effects remain the primary limitation, though many patients develop tolerance with continued use. The delayed onset of action (2-4 weeks) is frequently noted as a consideration in treatment planning. Long-term studies suggest maintained efficacy with acceptable safety profile over extended treatment periods.