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Application of diacerein for management of patients with osteoarthritis



Application of diacerein for management of patients with osteoarthritis



Reumatologia 41(2): 184-189



Diacerein or diacetylrein (4,5-diacetooxy-9,10-antrachoni-2-carboxylic acid) is a derivate of antrachinone, applied orally in management of patients with osteoarthritis. The drug is classified as chondroprotective and symptomatic slow-acting agent. Diacerein and its active metabolite, rein are strong inhibitors of cytokine synthesis, especially interleukin-1beta as well as they inhibits metalloproteinase production in vitro. The drug stimulates production of transforming growth factor beta and tissue inhibitor of metalloproteinases. In this way, diacerein inhibits destruction of the cartilage matrix and facilitates regeneration processes. Additionally, it has been shown that rein inhibits supraoxygen radical formation, synthesis of nitric oxide, chemotaxis and phagocytic activity of neutrophils as well as migration of macrophages and their phagocytic activity. Animal model and clinical studies revealed that diacerein decreases destruction of the articular cartilage and protects against lost of the bone mass and alternations in subchondral layer of the bone. It also has anti-inflammatory properties. Clinical efficacy of the drug is found about 4 weeks after introduction of management and is lasting longer than the period of the drug application. Decrease in pain intensity is the main clinical effect of the drug. Diacerein was found to be synergistic with non-steroidal anti-inflammatory anti-rheumatic drugs. The drug was also applied as supportive agent in patients with rheumatoid arthritis. Diacerein is given orally. It is deacetylated to rein, and metabolized in the liver. Majority of the drug derivates is eliminated though the kidneys. The pick plasma concentration of rein is found 2 hr after administration of a single dose. Diacerein is well tolerated, it does not produce gastric hemorrhages, has no toxic influence on the bone marrow, kidneys or liver.

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