ARTROPI

Diacerein is a prodrug which is metabolized to rhein.

It is currently approved in

France for the treatment of osteoarthritis although the use of diacerein is restricted due to the side effects including severe diarrhea 6.

Diacerein is under investigation for the treatment of Insulin Resistance, Diabetes Mellitus (Type 2), and Diabetes-Related Complications.

For the treatment of osteoarthritis affecting the hip or knee 6.

Decreases inflammation and cartilage destruction and also corrects altered osteoblast acitivity 3 4 5.

Diacerein's active metabolite rhein Rhein reduces cartilage destruction by decreasing expression of matrix metalloproteinase (MMP)-1 and -3 as well as upregulating tissue inhibitor of matrix metalloproteinases which serve to reduce the activity of several MMPs 5.

The anti-inflammatory action of rhein reduces the level of interleukin-1beta activity which plays a large role in reduction of extracellular matrix production, MMP activity, and continued inflammation 4.

Rhein reduces abnormal osteoblast synthetic activity through an unknown mechanism 3.

Interleukin-1 beta inhibitor Humans U Oxysterols receptor LXR-alpha inhibitor Humans U Oxysterols receptor LXR-beta inhibitor Humans U Arylamine N-acetyltransferase inhibitor Helicobacter pylori U Polyunsaturated fatty acid 5-lipoxygenase inhibitor Humans U Cytochrome P450 1A2 inhibitor Humans U Cytochrome P450 3A Subfamily inhibitor Humans U Cytochrome P450 2E1 inhibitor Humans U Cytochrome P450 2C9 inhibitor Humans U Cytochrome P450 2D6 inhibitor Humans.

Bioavailability of 50-60% 1.

Entirely converted to the active metabolite rhein Rhein before reaching systemic circulation.

Entirely converted to rhien

Rhein through double deacetylation before reaching systemic circulation 1.

Rhein is further metabolized to rhein glucuronide and rhein sulfate.

Hover over products below to view reaction partners Diacerein Rhein.

37% excreted in urine and 53% in feces as estimated in rats 2.

CL is 1.5 L/h and renal CL is 0.1 L/h 1.

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Rhein Rhein has an oral

LD50 of >5000 mg/kg in mice.

This is equivalent to a diacerein dose of >6476 mg/kg.