Diacerein
- 1 January 1997
- journal article
- review article
- Published by Springer Nature in Drugs
- Vol. 53 (1), 98-106
- https://doi.org/10.2165/00003495-199753010-00007
Abstract
▲ Rhein, the active metabolite of diacerein, inhibits interleukin-1 activity. Consequently, collagenase production in articular cartilage is reduced. ▲ Rhein dose-dependently inhibits Superoxide anion production, chemotaxis and phagocytic activity of neutrophils, and macrophage migration and phagocytosis. ▲ Articular cartilage damage is reduced by diacerein in animal models of osteoarthritis. ▲ Diacerein does not alter renal or platelet cyclo-oxygenase activity and may therefore be tolerated by patients with prostaglandin-dependent renal function. ▲ 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. ▲ Diacerein had similar efficacy to NSAIDs, but a slower onset of action, in comparative trials of ▲2 months’ duration conducted in patients with osteoarthritis. ▲ The predominant adverse effects of diacerein are diarrhoea and related disorders. ▲ Rhein, the active metabolite of diacerein, inhibits interleukin-1 activity. Consequently, collagenase production in articular cartilage is reduced. ▲ Rhein dose-dependently inhibits Superoxide anion production, chemotaxis and phagocytic activity of neutrophils, and macrophage migration and phagocytosis. ▲ Articular cartilage damage is reduced by diacerein in animal models of osteoarthritis. ▲ Diacerein does not alter renal or platelet cyclo-oxygenase activity and may therefore be tolerated by patients with prostaglandin-dependent renal function. ▲ 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. ▲ Diacerein had similar efficacy to NSAIDs, but a slower onset of action, in comparative trials of ▲2 months’ duration conducted in patients with osteoarthritis. ▲ The predominant adverse effects of diacerein are diarrhoea and related disorders.Keywords
This publication has 31 references indexed in Scilit:
- Anin vivo investigation of the effect of anthraquinones on the turnover of aggrecans in spontaneous osteoarthritis in the guinea pigInflammation Research, 1995
- Using inhibitors of metalloproteinases to treat arthritis. Easier said than done?Arthritis & Rheumatism, 1994
- Pharmacokinetics of diacerein in patients with liver cirrhosisBiopharmaceutics & Drug Disposition, 1993
- Diacetylrhein and rhein:In vivo andin vitro effect on lymphocyte membrane fluidityPharmacological Research, 1990
- Factors involved in the regulation of proteoglycan metabolism in articular cartilageArthritis & Rheumatism, 1989
- The Biology of OsteoarthritisNew England Journal of Medicine, 1989
- Effects of Diacerein on the Quantity and Phagocytic Activity of Thioglycollate-Elicited Mouse Peritoneal MacrophagesPharmacology, 1989
- Rhein: an anthraquinone that modulates superoxide anion production from human neutrophilsJournal of Pharmacy and Pharmacology, 1987
- The influence of rhein on the biosynthesis of prostaglandin-like substances in-vitroJournal of Pharmacy and Pharmacology, 1983
- Preliminary experience with diacetylrhein in the treatment of osteoarthritisCurrent Medical Research and Opinion, 1980