Each capsule contains:
Diacerein 50 mg
PHARMACEUTICAL FORM :
Hard gelatin capsules.
Pharmacological Actions: Diacerein has a novel mode of action that differentiate it from other non steroldal anti-lntlammatcry drugs and other conventional therapies. Diacerein inhibits the stimulation of inteneukin-t 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)-betal 1 and TGF-beta 2 with potential cartilage repairing properties. Diacereln does not alter renal or platelet cyelo-oxygenase activity and may therefore be tolerated by patients with
prostaglandin-dependent renal function. Diacerein has moderate anti-inflammatory activity without irritating effect on the stomach. Its action appears on the 30th day of treatment and is significant
on the 45th day. The effect is additive, in association with NSAIDs.
Absorption: After absorption of a single amount of 50 mg of Diacerein, the peak plasma concentration is achieved after 2.5 hours and Omax is about 3 mglL For amounts ranging between 50 and200 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 mein 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 milligrams/liter. 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 ranged between 35% and 60%, with approximately 20% as free rhein and 80% as , conjugates of rhein.
Diacerein is indicated for the treatment of knee & hip osteoarthritis.
Hypersensitivity to Diacerein or any of the product’s components.
SIDE EFFECTS :
Generally, Diacerein is welt 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 & eczema.
DRUG INTERACTION :
There is no interaction with the drugs such as: warfarin, tolbutamide, aspirin (acetylsalicylic acid), chlorpromazine, indomethacin.
Dlacerein 50 mg is to be administered oralty one capsule in the middle of a meal with a glass of water twice daily for 2 to 4 weeks (for adults over 15 years). It is recommended to continue
treatment for 6 months: the clinical studies have demonstrated that the drug can be used for 2 years without serious adverse effects.
General: Antacid use may decrease Diacerein absorption so it is advised to take antacids within an interval of two hours. Renal Impairment: Diacerein daily dose should be reduced by half in patients with severe renal insufficiency. Hepatic Impairment: Close clinical monitoring is advised for patients with hepatic insufficiency.
PREGNANCY & LACTATION :
Pregnancy: It is not recommended to use Diacereinin pregnancy. Lactation: Pharmacokinetics of Diacerein has not been studied in lactating women and its administration is not recommended.
Pediatric Use: Pharmacokinetics of Diacerein has not been
studied in pediatric population and its administration is not recommended for children under 15 years.
Geriatric Use: Among the elderly, given the good tolerance of the
product, it is not necessary to modify the dose, despite slower elimination.
Keep in a cool dry place, below 30°C.
Pack of 2 or 3 strips AUPVC each containing 10 capsules.
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