ARTRODAR

Country: Malaysia

Language: English

Source: NPRA (National Pharmaceutical Regulatory Agency, Bahagian Regulatori Farmasi Negara)

Active ingredient:

DIACEREIN

Available from:

TRB CHEMEDICA MALAYSIA SDN BHD

INN (International Name):

DIACEREIN

Units in package:

30Capsule Capsules

Manufactured by:

TRB PHARMA S.A

Patient Information leaflet

Not Applicable

Summary of Product characteristics

ARTRODAR
®
50 MG
Diacerein
Capsules
PHYSICAL CHARACTERISTICS
ARTRODAR
®
is presented as hard gelatin capsules each containing 50 mg diacerein
as the active
ingredient and excipients.
PHARMACOLOGY INFORMATION (PHARMACODYNAMICS/PHARMACOKINETICS)
PHARMACODYNAMIC PROPERTIES
_In vitro_ and _in vivo_ studies have shown that diacerein:
• inhibits the production of interleukin 1,
• decreases collagenolytic activity.
The anti-osteoarthritis properties of diacerein are due to its
capacity to inhibit the pro-inflammatory,
pro-catabolic cytokines such as interleukin 1 which plays an important
role in the degradation of
articular cartilage, for example, it inhibits cartilage production and
stimulates the liberation of
cartilage degrading enzymes (collagenase and stromelysin).
Clinical studies of 2 to 6 months duration demonstrate that diacerein
is effective in improving the
signs and symptoms of osteoarthritis (pain and joint function). These
studies show that the drug has
a slow onset of action which becomes significant after 30-45 days and
which is maintained once
treatment is interrupted. Diacerein has a good gastric tolerance.
PHARMACOKINETIC PROPERTIES
After oral administration, diacerein is hydrolysed before entering the
systemic circulation and is
absorbed, metabolised and excreted as rhein and its conjugates. All
the pharmacokinetic data that
follow refer to this active principle.
_ABSORPTION_
After oral administration diacerein undergoes a first hepatic passage
and is totally deacetylated to
rhein. After the intake of a single dose of 100 mg, the peak plasma
levels (C
max
) were 8-10 μg/ml of
free rhein. The values for T
max
were 1.8-2.0 hours after administration to fasting healthy volunteers.
The simultaneous intake of a standard meal induces a delay in the
absorption process and prolongs
the T
max
together which results in a higher bioavailability (increase of about
25% in the AUC). Given
this behaviour, it is advisable to take the drug with meals.
_DISTRIBUTION_
Nearly all the non-conjugated rhein (more th