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Orthocer
Diacerein
Diacerein is newly introduced one of the symptomaticslow acting drug for OA. It is a semi-syntheticanthraquinone derivative extracted from certain plants.
Mechanism of Action :
It directly inhibits IL-1synthesis and release in vitro and down modulate IL-1induced activities and have been shown to posses disease modifying effect in experimental models of osteoarthritisand in human subjects with finger joint and knee steoarthritis . IL-1 plays a fundamental role inosteoarthritis pathophysiology and cartilage destructionIL-1 also promotesexpression of inducible nitric oxide synthase , increaserelease of prostaglandin E2, IL-6,IL-8 in human osteoarthritis chondrocytes, which promote jointdegradation . Hence, by inhibiting IL-1 diacereinretards all pathological prepossess initiated in OA. iacerein also inhibits IL-1 induced expression ofcartilage degrading enzymes. It also enhances expression of TGF BETA-1 and TGF BETA 2 thus favoring matrixsynthesis and turnover in articular chondrocytes, therebyaccounting for disease modifying property of diacerein.It also inhibits superoxideproduction, chemotaxis and phagocytic activity ofneutrophils in addition to effect on macrophage migrationand phagocytosis. In contrast to NSAIDS diacerein dose not inhibit ynthis of prostaglandins; hence no gastroduednal toxicity has been observed with diacerein.It is also demonstrated to be involved in preventionof loss of hydroxiproline and proteoglycans in the jointcartilage, an effect not observed with conventionalNSAIDS or COX-2 inhibitors.
Pharmacology :
Diacerein has efficacy on functionalmanifestations of osteoarthritis and on structuralcomponent. It exerts its pharmacologic action through itsactive metabolite-rhein . Diacerien is entirelyconverted to rhien before reaching systemic circulation and rhein later gets eliminated by renal route (20%) orconjugated in liver to rhein glucronide (60%) and rheinsulphate (20%),these metabolites are mainly eliminated by renal route.The pharmokinetics after a single oral doseare linear in normal therapeutic doses with equal efficacyin normal young and elderly volunteers. The absorptionin systemic circulation is delayed with standard meal butis associated with 25% increase in amount absorbed. Incontrast to other NSAIDS the interactions are minimalas highly binding of rhein to plasma proteins is notsaturable. It dose not alter renal or platelet COXactivity and can be tolerated easily by patients withprostaglandin dependent renal function . Though dosemodification is required in mild to severe renalinsufficiency [50% dose reduction in severe renal failure],no reduction in initial dose is proposed in liver cirrhosis.
Structural effect : Various clinical trails haveconfirmed the efficacy of diacerein in patients with hiposteoarthritis
Safety profile : Drug watch data and clinical trailshave confirmed the safety and tolerability of diacerein.So there is no limitation on the duration of its use.
 

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