DIACENE
SANAMED
Identification
- Active ingredient (INN)
- DIACEREINE
- Internal code
- 04 B 045
- Country of Origin
- Algeria
- Pharmaceutical form
- Capsule
- Prescription List
- Highly Regulated (List I)
- Packaging
- b/30
DAWA Clinical Workbench v2.0
Information may not be accurate. Always consult a physician, pharmacist, or specialist before acting on any data shown here.
Description
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.
Indications
For the treatment of osteoarthritis affecting the hip or knee 6.
Pharmacodynamics
Decreases inflammation and cartilage destruction and also corrects altered osteoblast acitivity 3 4 5.
Mechanism of Action
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.
Absorption
Bioavailability of 50-60% 1.
Entirely converted to the active metabolite rhein Rhein before reaching systemic circulation.
Metabolism
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.
Route of Elimination
37% excreted in urine and 53% in feces as estimated in rats 2.
Clearance
CL is 1.5 L/h and renal CL is 0.1 L/h 1.
Adverse Effects
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Toxicity
Rhein Rhein has an oral
LD50 of >5000 mg/kg in mice.
This is equivalent to a diacerein dose of >6476 mg/kg.