Tradename
Diacerein
Generic Name
Diacerein
Category
Musculoskeletal System
Form
Capsules
Composition
Diacerein......50 mg
Description
For the treatment of osteoarthritis
Properties/Actions
Pharmacodynamics
Diacerein has a novel mode of action that differentiate it from othe rnon-steroidal anti-inflammatory drugs and other conventional therapies. Diacerein inhibits the stimulation of interleukin-1 beta production and production of nitrous oxide. It also significantly reduces severity of pathological changes of osteoarthritis, increases the expression of transforming growth factor TGF-beta 1 and TGF-beta 2 with potential cartilage repairing properties. Diacerein does not alter renal or platelet cylcooxygenase activity and amy therefore be tolerated by patients with prostaglandin-dependant renal function. Diacerein has moderate antiinflammatory activity without an irritating effect on the stomach. Its action appears on teh 30th day of treatment and is significant on the 45th day. The effect is additive, in association with NSAIDs.

Pharmacokinetics
Absorption
After absorption of a single amount of 50 mg of Diacerein, the peak plasma concentration is achieved after 2.5 hours, and Cmax is about 3 mg/l.
For amounts ranging between 50 and 200 mg of Diacerein, all the pharmacokinetic parameters are independent on the amount. Concurrent intake of food is associated with a 25% increase in absorption. Therefore, Diacerein is best given with food.
Distribution
Total protein binding of rhein is about 99% to plasma albumin and in a lesser percentage to lipoproteins and gamma-immunoglobulins. It achieves synovial fluid concentration of 0.3 to 3.0 mg/l.
Metabolism
Diacerein is metabolized extensively (100%) in liver following oral dosing, to the deacetylated active metabolite rhein.
Excretion
Urinary excretion of Diacerein in the form of its metabolites has range between 35% and 60%, with approximately 20% as free rhein and 80% as conjugates of rhein.
Indications
Diacerein is indicated for the treatment of knee and hip osteoarthritis.
Contraindications
Hypersensitivity to Diacerein or any of the product components.
Drug Interactions
There are no interactions with drugs such as warfarin, tolbutamide, aspirin, chlopromazide and indomethacin.
Side Effects/Adverse Effects
Generally, Diacerein is well tolerated. The most common adverse reaction was diarrhea. Few cases of abdominal pain have been reported. These adverse effects may be diminished by dose adjustment. Other adverse effects are urine discoloration, rash and eczema.
Pregnancy & Lactation
Pregnancy
It is not recommended to use Diacerein in pregnancy.
Lactation
Pharmacokinetics of Diacerein has not been studied in lactating women and its administration is not recommended.
Dosage & Administration
Overdosage
Warnings
Notes
Pediatric Use
Pharmacokinetics of Diacerein has not been studied in the pediatric population and its administration is not recommended for children under 15 years.
Geriatric Use
Given the good tolerance of the prodcut, it is not necessary to modify the dose in elderly patients, despite slower elimination.
Storage
Keep in a cool, dry place. Below 30°C.
Packaging
Pack of 2 or 3 strips, containing 10 capsules each.
Manufacturer
Eva Pharma
Price
Date Added/Updated
12th October 2011 2:43 am

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