From the Guidelines
Diacerein is primarily indicated for the treatment of osteoarthritis, particularly for knee and hip osteoarthritis, as a slow-acting, symptom-modifying drug. It is an anthraquinone derivative, chemically known as 4,5-diacetyloxy-9,10-dioxo-anthracene-2-carboxylic acid, which is metabolized to its active form, rhein, in the liver 1. The typical dosage is 50 mg twice daily or 100 mg once daily, taken with food to minimize gastrointestinal side effects. Diacerein functions by inhibiting interleukin-1 (IL-1) production and activity, which plays a key role in cartilage degradation and joint inflammation, unlike NSAIDs, it doesn't directly inhibit cyclooxygenase enzymes, giving it a different safety profile 1. Some key points to consider when prescribing diacerein include:
- Common side effects include diarrhea, abdominal pain, and soft stools, particularly during the first few weeks of treatment.
- Patients with liver disease, inflammatory bowel disease, or intestinal obstruction should avoid diacerein, and liver function should be monitored during treatment.
- The medication's effects typically develop gradually over 2-4 weeks, and it may provide continued benefit for several months after discontinuation.
- Diacerein is classified as a symptomatic slow-acting drug for osteoarthritis (SYSADOA), which may possess structure modification properties, but more studies are required to confirm this 1. Given the available evidence, diacerein is a viable option for the treatment of osteoarthritis, particularly in patients who cannot tolerate NSAIDs or require a different mechanism of action.
From the Research
Diacerein Indication
- Diacerein is used for the treatment of osteoarthritis (OA) 2, 3, 4, 5, 6.
- It is a symptomatic slow-acting drug in osteoarthritis (SYSADOA) with anti-inflammatory, anti-catabolic and pro-anabolic properties on cartilage and synovial membrane 2.
Diacerein Chemical
- Diacerein is a semi-synthetic anthraquinone derivative 5.
- It inhibits the interleukin-1-beta (IL-1β) cytokine, which plays a key role in the pathogenesis of OA 5.
Efficacy and Safety
- Diacerein has shown modest efficacy and acceptable tolerability in a number of trials of low to moderate quality 5.
- It has a small, consistent benefit in improvement in pain 3, 4, 6.
- The most frequent adverse event is diarrhea, affecting 42% of participants 3.
- Diacerein is associated with an increased risk of diarrhea and some withdrawal from therapy following adverse events 4.
- The European Medicines Agency (EMA) has restricted the use of diacerein-containing medicines due to concerns about the frequency and severity of diarrhea and liver disorders in OA patients 5, 6.