Diacerein: Targeted Joint Health Support for Osteoarthritis
| Product dosage: 50 mg | |||
|---|---|---|---|
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| 180 | $0.93
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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 a non-opioid, non-steroidal anti-inflammatory alternative, it offers a unique mechanism of action by inhibiting interleukin-1β, a key pro-inflammatory cytokine involved in cartilage degradation. This prescription medication is indicated for the symptomatic slow-acting treatment of osteoarthritis in adults, particularly for large joints such as the knees and hips. Clinical evidence supports its potential to modify disease progression by reducing cartilage breakdown and stimulating cartilage matrix synthesis.
Features
- Active ingredient: Diacerein 50mg
- Pharmaceutical form: Capsules or tablets
- Mechanism: Selective interleukin-1β inhibitor
- Prescription status: Rx-only in most jurisdictions
- Onset of action: 2-4 weeks for initial symptomatic effect
- Treatment duration: Long-term therapy recommended (minimum 3-6 months)
- Metabolism: Hepatic transformation to active metabolite rhein
- Excretion: Primarily renal (95%) and fecal (3%)
Benefits
- Reduces joint pain and stiffness through cytokine modulation
- Slows radiographic progression of joint space narrowing
- Improves physical function and mobility scores in osteoarthritis patients
- Demonstrates carry-over effect with sustained benefits after treatment discontinuation
- Favorable safety profile compared to traditional NSAIDs regarding gastrointestinal and renal adverse events
- May reduce need for rescue analgesia and potentially delay surgical intervention
Common use
Diacerein is primarily indicated for the symptomatic treatment of osteoarthritis, particularly affecting weight-bearing joints such as knees and hips. It is commonly prescribed for patients with mild to moderate osteoarthritis who have inadequate response to simple analgesics or who cannot tolerate NSAIDs due to gastrointestinal, cardiovascular, or renal concerns. The medication is often used as part of a comprehensive osteoarthritis management plan that includes non-pharmacological interventions such as weight management, physical therapy, and exercise programs. Clinical trials have demonstrated efficacy in reducing Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) scores and improving patient global assessment.
Dosage and direction
The recommended adult dosage is 50mg twice daily, taken with meals to minimize gastrointestinal discomfort. Treatment initiation typically begins with one 50mg capsule daily for the first 2-4 weeks to assess tolerance before increasing to the full maintenance dose. The full therapeutic effect may take several weeks to manifest due to the drug’s slow-acting nature. Treatment should be continued for at least 3-6 months to assess clinical response adequately. For elderly patients or those with hepatic impairment, dosage reduction to 50mg once daily may be necessary. Capsules should be swallowed whole with water and not chewed or crushed.
Precautions
Hepatic function should be monitored periodically during treatment, as diacerein is metabolized in the liver. Patients with pre-existing liver conditions require careful supervision and possibly dosage adjustment. Renal function assessment is recommended before initiation and periodically during treatment, particularly in elderly patients or those with pre-existing renal impairment. Gastrointestinal tolerability should be monitored, especially during the initial weeks of therapy. Patients with history of inflammatory bowel disease or chronic diarrhea should use with extreme caution. Pregnancy and breastfeeding contraindicate use due to insufficient safety data.
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 (eGFR <30 mL/min/1.73m²). Contraindications include patients with active peptic ulcer disease, chronic diarrhea, or inflammatory bowel diseases such as Crohn’s disease or ulcerative colitis. The medication is not recommended during pregnancy (Category C) or lactation due to potential transfer to breast milk and lack of adequate human safety data.
Possible side effects
The most commonly reported adverse reactions involve the gastrointestinal system, including diarrhea (occurring in approximately 20-30% of patients), abdominal pain, and soft stools. These effects are typically dose-dependent and often diminish with continued treatment. Less frequent side effects include mild elevation of liver enzymes, skin reactions such as pruritus or rash, and discoloration of urine (yellow-orange hue, which is harmless). Serious adverse events are rare but may include severe hepatitis, significant weight loss, or exacerbation of pre-existing bowel conditions. Most side effects are mild to moderate in severity and often transient.
Drug interactions
Diacerein may potentiate the effects of oral anticoagulants such as warfarin, requiring closer monitoring of INR values. Concurrent use with other hepatically metabolized drugs warrants caution due to potential metabolic interactions. The combination with magnesium-, aluminum-, or calcium-containing antacids may reduce diacerein absorption and should be administered at least 2 hours apart. Concomitant use with other laxatives or drugs that cause diarrhea may exacerbate gastrointestinal adverse effects. Limited data exists regarding interactions with cytochrome P450 substrates, though theoretical interactions are possible given hepatic metabolism.
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. Doubling the dose to make up for a missed dose is not recommended due to increased risk of gastrointestinal side effects. Patients should be advised to maintain consistent dosing timing to ensure stable therapeutic levels, though the drug’s long half-life provides some forgiveness for occasional missed doses.
Overdose
Cases of acute overdose are rare due to the drug’s favorable safety margin. Symptoms would likely manifest as exaggerated pharmacological effects, particularly severe diarrhea, abdominal cramps, and possible electrolyte imbalances. Management should be supportive and symptomatic, including maintenance of hydration and electrolyte balance. Gastric lavage may be considered if ingestion occurred within 1-2 hours. There is no specific antidote, and hemodialysis is unlikely to be effective due to high protein binding. Medical attention should be sought for significant overdose, particularly in elderly or debilitated patients.
Storage
Store at room temperature (15-30°C/59-86°F) in the original container, protected from light and moisture. Keep tightly closed and away from direct sunlight. Do not store in bathroom cabinets where humidity levels may fluctuate. Keep out of reach of children and pets. Do not use beyond the expiration date printed on the packaging. Proper disposal of unused medication should follow local regulations for pharmaceutical waste.
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 therapeutic decisions should be based on professional medical judgment considering the patient’s complete medical history. Always consult with a healthcare provider before starting, stopping, or changing any medication regimen.
Reviews
Clinical studies demonstrate that approximately 60-70% of patients experience meaningful symptomatic improvement with diacerein therapy. Systematic reviews and meta-analyses have shown consistent benefits in pain reduction and functional improvement compared to placebo, with effect sizes comparable to NSAIDs but with better gastrointestinal tolerability. Long-term extension studies suggest sustained benefits over 2-3 years of treatment. Patient-reported outcomes indicate improved quality of life measures, particularly regarding mobility and daily activities. The delayed onset of action is frequently noted as a limitation, though most patients who persist beyond the initial month report satisfactory outcomes.