Diacerein : a New Class of Anti-Osteoarthritic Drugs

Abstract

Osteoarthritis, an articular cartilage degenerative disease, is the most common form of joint diseases. The overall disease prevalence increases with age. The pathophysiology of the cartilage degeneration is complex and multifactorial. Cytokines such as interleukins and tumor necrosis factors, inflammatory mediators such as prostaglandins and nitric oxide, and metalloproteinases greatly contribute to it. Pharmacologic therapy mainly includes simple analgesics and NSAIDs. New therapies which may prevent further joint progression are being developed. Diacerein is a slow-acting, symptom-modifying, anti-osteoarthritic drug. It inhibits the production and activity of cytokines, especially interleukin-1 which is the well-known inflammatory cytokine, and also stimulates the production of TGF-β. This drug is effective in relieving symptoms in osteoarthritis patients with a good gastric safety profile. It is given orally as 50 mg twice daily. Diacerein is entirely converted into rhein, the active metabolite, before reaching the systemic circulation. Both in vitro and in vivo studies suggest that this drug may have disease-modifying effects. ·