Summary
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▲ Rhein, the active metabolite of diacerein, inhibits interleukin-1 activity. Consequently, collagenase production in articular cartilage is reduced.
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▲ Rhein dose-dependently inhibits Superoxide anion production, chemotaxis and phagocytic activity of neutrophils, and macrophage migration and phagocytosis.
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▲ Articular cartilage damage is reduced by diacerein in animal models of osteoarthritis.
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▲ Diacerein does not alter renal or platelet cyclo-oxygenase activity and may therefore be tolerated by patients with prostaglandin-dependent renal function.
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▲ In clinical trials of ≤6 months’ duration, oral diacerein 50mg twice daily was associated with improvement in 57 to 85% of patients with osteoarthritis. Pain scores and measures of joint function were generally reduced compared with baseline and placebo.
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▲ Diacerein had similar efficacy to NSAIDs, but a slower onset of action, in comparative trials of ▲2 months’ duration conducted in patients with osteoarthritis.
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▲ The predominant adverse effects of diacerein are diarrhoea and related disorders.
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Spencer, C.M., Wilde, M.I. Diacerein. Drugs 53, 98–106 (1997). https://doi.org/10.2165/00003495-199753010-00007
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DOI: https://doi.org/10.2165/00003495-199753010-00007