Capsule

Mechanism

Diacerein is a slow-acting anti-osteoarthritic agent that is converted to its active metabolite, rhein. Diacerein/rhein is thought to exert its effects primarily by modulating the interleukin-1β (IL-1β) pathway, an important mediator involved in inflammation and cartilage degradation in osteoarthritis. Experimental evidence suggests that rhein can reduce IL-1β-associated signalling and the expression of certain cartilage-degrading mediators, while influencing the metabolism of extracellular-matrix components. Unlike conventional NSAIDs, Diacerein does not primarily act through inhibition of prostaglandin synthesis. Its therapeutic effect develops gradually and is intended for symptomatic management of osteoarthritis.

Pharmacokinetics
Absorption → Oral bioavailability ~50–60%; food increases absorption.
Conversion → Rapidly deacetylated to active metabolite rhein.
Distribution → High plasma protein binding (~99%); penetrates synovial fluid.
Metabolism → Hepatic conjugation to glucuronide and sulfate forms.
Excretion → Mainly renal (conjugates); ~20% unchanged; half‑life ~7–8 hours.
Renal impairment → Requires dose reduction due to accumulation risk.

Dosage

• As directed by the physician.

Side Effects

• Loose stools
• Vomiting

Contraindications

• Hypersensitivity to Diacerein or any component of the formulation.
• Current liver disease or a history of liver disease.
• Patients for whom Diacerein is otherwise contraindicated according to the approved prescribing information.

Drug Interactions

• Diuretics, because diarrhoea-related dehydration may increase the risk of complications.
• Cardiac glycosides, particularly where hypokalaemia may occur.
• Laxatives, because concurrent use may increase gastrointestinal effects.
• Other medicines associated with hepatic injury, where clinically relevant.

Warning and Precautions

• Stop treatment and contact the physician if diarrhoea develops.
• Maintain adequate hydration if gastrointestinal symptoms occur.
• Keep out of reach of children.
• Patients should limit alcohol intake during treatment where advised by the treating physician.
• Store in a cool, dry place away from direct sunlight and moisture.
• Patients with current or previous liver disease should not use Diacerein under the applicable contraindication.