BOSENTAN APOTEX bosentan (as monohydrate) 62.5mg tablets bottle
Country: Australia
Language: English
Source: Department of Health (Therapeutic Goods Administration)
Patient Information leaflet
(PIL)
15-06-2017
Summary of Product characteristics
(SPC)
15-06-2017
Public Assessment Report
(PAR)
26-11-2017
Active ingredient:
bosentan monohydrate
Available from:
Apotex Pty Ltd
INN (International Name):
bosentan monohydrate
Authorization status:
Registered
Patient Information leaflet
BOSENTAN APOTEX
_Contains the active ingredient bosentan (as 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 bosentan. 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
Bosentan APOTEX tablets. It
contains the active ingredient
bosentan (as monohydrate).
It is used to treat high blood pressure
in the blood vessels between the
heart and the lungs. This condition is
called pulmonary arterial
hypertension.
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_
Bosentan acts to reduce abnormally
high blood pressure by widening the
blood vessels between the heart and
lungs. It belongs to the class of
medicines known as endothelin
antagonists.
There is no evidence that this
medicine is addictive.
_USE IN CHILDREN_
There is limited experience with the
use of this medicine in children.
BEFORE YOU TAKE THIS
MEDICINE
_WHEN YOU MU
Read the complete document
Summary of Product characteristics
Product Information – Australia
APOTEX Bosentan tablets
Page 1
BOSENTAN APOTEX TABLETS
Bosentan may cause birth defects and is contraindicated in pregnancy
(see CONTRAINDICATIONS
and PRECAUTIONS).
Rare cases of hepatic cirrhosis and hepatic failure have been reported
in patients using bosentan
(see PRECAUTIONS).
NAME OF THE MEDICINE
Bosentan (as monohydrate)
Chemical Name:
Benzenesulphonamide,
4-(1,1-dimethylethyl)-_N_-[6-(2hydroxyethoxy)-5-(2-
methoxyphenoxy)[2,2’-bipyrimidin]-4-yl]-, monohydrate.
Structural Formula:
Molecular Formula:
C
27
H
29
N
5
O
6
S•H
2
O
Molecular Weight:
569.64
CAS Registry Number: 157212-55-0
DESCRIPTION
Bosentan is the first of a new class of medicines, an endothelin
receptor antagonist. Bosentan
belongs to a class of highly substituted pyrimidine derivatives, with
no chiral centres.
Bosentan monohydrate, a white to off-white powder, is practically
insoluble at low pH (0.1 mg/100 mL
at pH 1.1 and 4.0; 0.2 mg/100 mL at pH 5.0). Solubility increases at
higher pH values (43 mg/100 mL
at pH 7.5). In the solid state, bosentan monohydrate is very stable,
is not hygroscopic and shows no
light sensitivity.
Each tablet contains 62.5 mg or 125 mg bosentan (as monohydrate) as
the active ingredient. In
addition,
each
tablet
contains
the
following
inactive
ingredients:
methylcellulose,
poloxamer,
crospovidone,
silicon
dioxide,
magnesium
stearate
and
a
coating
containing
hypromellose,
hydroxypropylcellulose, macrogol 8000, titanium dioxide, iron oxide
red and iron oxide yellow.
PHARMACOLOGY
PHARMACOLOGICAL ACTIONS
The neurohormone endothelin-1 (ET-1) is a potent vasoconstrictor. ET-1
concentrations are elevated
in plasma and lung tissue of patients with pulmonary arterial
hypertension (PAH), suggesting a
pathogenic role for ET-1 in this disease.
Bosentan
is a specific and competitive antagonist at endothelin receptor types
ET
A
and ET
B
.
Bosentan has a slightly higher affinity for ET
A
receptors than for ET
B
receptors.
Product Information – Australia
APOTEX Bosentan tablets
Page 2
PHARMACO
Read the complete document
