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Pharmacology: Pharmacodynamics: Diacerein is a prodrug. After metabolism in the liver, the active metabolite rhein is formed. Rhein is a selective inhibitor of Interleukin - 1 (IL-1). This unique mode of action make diacerein superior to the conventionally used NSAIDs for the treatment of OA. Diacerein has beneficial effects on the anabolic processes that occur in the cartilage. It increases the production of transforming growth factor-β (TGF-β) that triggers chondrocyte proliferation and stimulates the production of collagen & proteoglycan.
Pharmacokinetics: Absorption: Diacerein is well absorbed following oral dosing. Diacerein is taken with food, there is an increase in the absorption by 24%.
Distribution: Total protein binding of rhein is about 99%. It achieves synovial fluid concentration of 0.3 to 3.0 milligrams/liter. Peak plasma concentration of rhein was reached 15-30 minutes after dosing.
Metabolism: Diacerein is metabolized extensively (100%) in liver following oral dosing, to the deacetylated active metabolite rhein, prior to entering systemic circulation. Major active metabolites include Rhein glucuronide and Rhein sulfate with half-life being 7 to 8 hours. In healthy adults, rhein has plasma half life of 4.2 hours after the first 50mg dose.
Excretion: Diacerein is eliminated mainly by the kidneys (20% unchanged form, 60% glucuronide and 20% sulphate derivatives).
