Diacerein: Targeted Osteoarthritis Symptom and Disease Modification
| Product dosage: 50 mg | |||
|---|---|---|---|
| Package (num) | Per cap | Price | Buy |
| 30 | $1.43 | $43.00 (0%) | 🛒 Add to cart |
| 60 | $1.06 | $86.00 $63.64 (26%) | 🛒 Add to cart |
| 90 | $0.95 | $129.00 $85.14 (34%) | 🛒 Add to cart |
| 120 | $0.87 | $172.00 $104.06 (39%) | 🛒 Add to cart |
| 180 | $0.79
Best per cap | $258.00 $141.90 (45%) | 🛒 Add to cart |
Synonyms | |||
Diacerein is a non-steroidal, disease-modifying osteoarthritis drug (DMOAD) belonging to the class of anthraquinones. Unlike conventional rapid-acting analgesics, its primary mechanism of action involves the inhibition of interleukin-1 beta (IL-1β), a key pro-inflammatory cytokine implicated in the pathogenesis of osteoarthritis. This targeted approach not only alleviates symptoms like pain and stiffness but also demonstrates a potential to slow the structural progression of the disease by reducing cartilage degradation. Its delayed onset of action is complemented by a sustained therapeutic effect that persists even after treatment cessation, making it a unique agent in the long-term management of osteoarthritis.
Features
- Active Pharmaceutical Ingredient: Diacerein.
- Pharmacological Class: Interleukin-1 inhibitor; Disease-Modifying Osteoarthritis Drug (DMOAD).
- Available Formulations: Typically 50 mg capsules.
- Primary Metabolite: Rhein, which is largely responsible for the pharmacological activity.
- Mechanism: Selective inhibition of interleukin-1 beta (IL-1β) synthesis and activity.
- Onset of Action: Clinical effects are typically observed after 2-4 weeks of continuous administration.
Benefits
- Provides sustained relief from osteoarthritis pain and improves joint function by targeting the underlying inflammatory process.
- Demonstrates a disease-modifying potential by inhibiting enzymes that break down cartilage, potentially slowing disease progression.
- Offers a favorable safety profile for long-term use, being non-acidic and not associated with the gastrointestinal or renal risks common with traditional NSAIDs.
- Exhibits a carry-over effect, where therapeutic benefits persist for a period after the cessation of treatment.
- Does not mask pain in an acute, non-specific manner, allowing for a more natural assessment of joint load and rehabilitation progress.
Common use
Diacerein is indicated for the symptomatic treatment of osteoarthritis, particularly of the hip and knee joints. It is used in the management of chronic osteoarthritis pain, reduction of joint stiffness, and improvement of physical function. Its use is most appropriate for patients requiring long-term therapy where the goal is not only symptomatic relief but also potential retardation of cartilage destruction.
Dosage and direction
The standard adult dosage is 50 mg (one capsule) taken twice daily, typically with meals to enhance gastrointestinal tolerance. For elderly patients or those with mild hepatic impairment, a starting dose of 50 mg once daily may be recommended, with a possible increase to the full dose based on tolerability. The full therapeutic effect is achieved gradually. Treatment should be continued as long as symptomatic benefit is observed, as prescribed by a physician.
Precautions
Use with caution in patients with a history of gastrointestinal disorders, particularly those prone to diarrhea. Liver function tests should be considered before and during prolonged therapy, especially in patients with pre-existing hepatic conditions. Its use during pregnancy and lactation is not recommended due to a lack of sufficient safety data. Patients should be advised that the medication may cause a reddish discoloration of urine, which is harmless.
Contraindications
Diacerein is contraindicated in patients with known hypersensitivity to diacerein, rhein, or any of the excipients in the formulation. It is also contraindicated in patients with severe hepatic impairment or severe renal impairment (creatinine clearance < 30 mL/min). It should not be used in children or adolescents under 18 years of age.
Possible side effect
The most commonly reported side effect is diarrhea or soft stools, which often occurs at the beginning of treatment and is usually transient. Other less frequent adverse reactions may include:
- Abdominal pain and discomfort
- Nausea
- Epigastric pain
- Mild and transient increases in liver transaminases
- Skin reactions such as pruritus or rash
- Reddish discoloration of urine (benign)
Drug interaction
Concomitant use with laxatives may exacerbate diarrhea and is not recommended. While not extensively documented, caution is advised when co-administering with other hepatically metabolized drugs. Its interaction with potent CYP450 enzyme inducers or inhibitors is possible but not well-established. Always inform your healthcare provider of all medications you are taking, including over-the-counter drugs and herbal supplements.
Missed dose
If a dose is missed, it should be taken as soon as remembered. However, if it is almost time for the next scheduled dose, the missed dose should be skipped. Do not take a double dose to make up for a missed one. Maintaining a consistent dosing schedule is important for achieving the desired therapeutic effect.
Overdose
There is limited data on acute overdose. Symptoms would likely be an extension of the known adverse effects, primarily severe diarrhea, abdominal cramps, and possibly dehydration. There is no known specific antidote. Treatment should be symptomatic and supportive, with a focus on maintaining hydration and electrolyte balance. Gastric lavage may be considered if ingestion was very recent. In case of suspected overdose, seek immediate medical attention.
Storage
Store at room temperature (15°C - 25°C / 59°F - 77°F) in a dry place, protected from light and moisture. Keep the container tightly closed. Keep all medications out of the reach of children and pets. Do not use the medicine after the expiration date printed on the packaging.
Disclaimer
This information is for educational and informational purposes only and does not constitute medical advice. It is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here.
Reviews
(Compilation of typical expert and clinical trial conclusions) “Diacerein presents a well-tolerated and effective option for the long-term management of osteoarthritis, offering a unique mechanism of action focused on disease modification. Clinical trials, such as those published in Annals of the Rheumatic Diseases, have consistently shown its superiority over placebo in reducing pain and improving function, with a notable carry-over effect. While the onset of action is slower than NSAIDs, its sustained benefit and potential to alter disease course make it a valuable part of a comprehensive osteoarthritis management strategy. Gastrointestinal events, primarily mild diarrhea, are the most frequently noted adverse effects but often resolve with continued use.”