Entecavir Apotex entecavir (as monohydrate) 1mg tablet blister pack

Nchi: Australia

Lugha: Kiingereza

Chanzo: Department of Health (Therapeutic Goods Administration)

Viambatanisho vya kazi:

entecavir

Inapatikana kutoka:

Apotex Pty Ltd

INN (Jina la Kimataifa):

Entecavir

Idhini hali ya:

Registered

Taarifa za kipeperushi

ENTECAVIR APOTEX
_Contains the active ingredient entecavir monohydrate_
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 entecavir. 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:
•
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
Entecavir APOTEX tablets. It
contains the active ingredient
entecavir and belongs to a group of
medicines called antiviral medicines.
It is used to treat chronic hepatitis B
virus infection in adults 16 years or
older.
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_
Infection by the hepatitis B virus can
lead to damage to the liver. Entecavir
reduces the amount of virus in your
body and has been shown to improve
the condition of the liver.
It is not known how safe entecavir is
when taken for long periods.
There is no evidence that this
medicine is addictive.
_USE IN CHILDREN_
This medicine should not be used in
children under 16 years as safety and
effectiveness

Tabia za bidhaa

Product Information – Australia
Entecavir APOTEX Tablets
Page 1
ENTECAVIR APOTEX TABLETS
NAME OF THE MEDICINE
Entecavir monohydrate
Chemical Name:
2-amino-1,9-dihydro-9-[(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-
methylenecyclopentyl]-6H-purin-6-one, monohydrate.
Structural Formula:
Molecular Formula:
C
12
H
15
N
5
O
3

H
2
O,
Molecular Weight:
295.3
CAS Registry Number:
209216-23-9
DESCRIPTION
Entecavir monohydrate is a white to off-white powder. It is slightly
soluble in water (2.4 mg/mL), and
the pH of the saturated solution in water is 7.9 at 25

±
0.5

C.
Each tablet contains entecavir (as monohydrate) as the active
ingredient. In addition, each tablet
contains
the
following
inactive
ingredients:
lactose,
microcrystalline
cellulose,
copovidone,
crospovidone, magnesium stearate, hypromellose,
hydroxypropylcellulose, macrogol 8000, titanium
dioxide and iron oxide red (1.0mg only).
PHARMACOLOGY
PHARMACOLOGICAL ACTIONS
Mechanism of action
Entecavir monohydrate is a guanosine nucleoside analogue with activity
against HBV polymerase. It is
phosphorylated to the active triphosphate (TP) form, which has an
intracellular half-life of 15 hours.
Intracellular TP levels are directly related to extracellular
entecavir monohydrate concentrations, with
no significant accumulation beyond initial plateau levels. By
competing with the natural substrate
deoxyguanosine-TP,
entecavir
monohydrate-TP
inhibits
all
3
functional
activities
of
the
viral
polymerase: (1) priming of the HBV polymerase, (2) reverse
transcription of the negative strand from
the pregenomic messenger RNA, and (3) synthesis of the positive strand
of HBV DNA. Entecavir
monohydrate-TP K
i
value for inhibition of HBV DNA polymerase is 1.2 nM. Entecavir
monohydrate-TP
is a weak inhibitor of cellular DNA polymerases α, ß,

and ε with K
i
values of 18 to 40 µM. It did not
inhibit mitochondrial γ polymerase (K
i
>160μM) and did not affect the mitochondrial DNA content of
human
hepatoma
cells
_in _
_vitro_.
Entecavir
monohydrate
inhibited
HBV
DNA