APO-Leflunomide

Country: Australia

Language: English

Source: Department of Health (Therapeutic Goods Administration)

Active ingredient:

Leflunomide

Available from:

Apotex Pty Ltd

Class:

Medicine Registered

Patient Information leaflet

APO-LEFLUNOMIDE
TABLETS

_Contains the active ingredient leflunomide_
CONSUMER MEDICINE INFORMATION

_FOR A COPY OF A LARGE PRINT LEAFLET, PH: 1800 195 055_

WHAT IS IN THIS LEAFLET
READ THIS LEAFLET CAREFULLY BEFORE
TAKING YOUR MEDICINE.
This leaflet answers some common
questions about leflunomide. It does
not contain all the available
information.
It does not take the place of talking to
your doctor or pharmacist.
The information in this leaflet was
last updated on the date listed on the
last page. More recent information on
this medicine may be available.
ASK YOUR DOCTOR OR PHARMACIST:
•
if there is anything you do not
understand in this leaflet,
•
if you are worried about taking
your medicine, or
•
to obtain the most up-to-date
information.
You can also download the most up
to date leaflet from
www.apotex.com.au.
All medicines have risks and
benefits. Your doctor has weighed
the risks of you using this medicine
against the benefits they expect it
will have for you.
Pharmaceutical companies cannot
give you medical advice or an
individual diagnosis.
Keep this leaflet with your medicine.
You may want to read it again.
WHAT THIS MEDICINE IS
USED FOR
The name of your medicine is APO-
Leflunomide. It contains the active
ingredient leflunomide.
It is used to treat:
•
rheumatoid arthritis
Ask your doctor if you have any
questions about why this medicine
has been prescribed for you. Your
doctor may have prescribed this
medicine for another reason.
This medicine is available only with
a doctor's prescription.
_HOW IT WORKS_
Leflunomide belongs to a group of
medicines called disease-modifying
anti-rheumatic drugs (DMARDs),
which act to decrease joint damage
and disability due to rheumatoid
arthritis.
In rheumatoid arthritis, leflunomide
works by reducing the activity of the
immune system, which helps to
reduce inflammation, swelling and
pain in affected joints. It also helps to
reduce damage to those joints.
There is no evidence that this
medicine is addictive.
_USE IN CHILDREN_
There is not enou

Summary of Product characteristics

Product Information – Australia 
APO-Leflunomide Tablets 
Page 1 
APO-LEFLUNOMIDE TABLETS 

NAME OF THE MEDICINE 
Leflunomide. 

Chemical Name: 
_N_-(4-trifluoromethylphenyl)-5-methylisoxazol-4-carboxamide) 

Chemical Structure: 

Molecular Formula: 
  C
12
H
9
F
3
N
2
O
2

Molecular Weight: 
  270.2 

CAS Registry Number:  75706-12-6 

DESCRIPTION 
Leflunomide is a white to off white powder, practically insoluble in water and freely soluble in ethanol 
or acetone. 

PHARMACOLOGY 
SITE AND MODE OF ACTION 
Leflunomide is an isoxazole immunomodulatory agent which is effective in animal models of arthritis 
and other autoimmune diseases, allergy and
transplantation.  _In vivo_, leflunomide is rapidly 
metabolized to the ring opened form, A771726, which
is the active drug.  It has immunomodulating/ 
immunosuppressive characteristics, acts as an
anti-proliferative agent and displays weak anti-
inflammatory properties. The anti-proliferative activity is reversed by the addition of uridine to the cell 
culture, indicating that A771726  acts at the
level  of the pyrimidine biosynthesis pathway.  Binding 
studies using radio-labelled ligand demonstrate that the active
metabolite binds to and inhibits the 
human enzyme dihydroorotate dehydrogenase (DHODH, an enzyme
involved in _de novo_  pyrimidine 
synthesis).  Together, these data suggest that, _in vivo_, at concentrations achievable in patients 
receiving leflunomide, pyrimidine synthesis in lymphocytes and other rapidly dividing cell populations 
may be inhibited.  Further, the inhibition of tyrosine kinase activity has been reported, for both _in vitro_ 
and  _in vivo_  situations.  The  _in vitro_  activity does not seem to
be mediated directly through enzyme 
inhibition and takes place only at much
higher concentration