BOSENTAN ACTELION bosentan 125mg (as monohydrate) tablet bottle

Country: Australia

Language: English

Source: Department of Health (Therapeutic Goods Administration)

Active ingredient:

bosentan monohydrate

Available from:

Janssen-Cilag Pty Ltd

INN (International Name):

bosentan monohydrate

Authorization status:

Registered

Patient Information leaflet

BOSENTAN
ACTELION (BOZ-
EN-TAN - ACT-
TEE-LEON )
_Bosentan 62.5 mg/125 mg film-coated tablets _
CONSUMER MEDICINE
INFORMATION
WHAT IS IN THIS LEAFLET
This leaflet answers some common
questions about Bosentan Actelion.
It does not contain all the available
information. It does not take the place of
talking to your doctor or pharmacist.
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.
IF YOU HAVE ANY CONCERNS ABOUT USING
THIS MEDICINE, ASK YOUR DOCTOR OR
PHARMACIST.
KEEP THIS LEAFLET WITH THE MEDICINE.
You may need to read it again.
WHAT BOSENTAN ACTELION IS USED
FOR
Bosentan Actelion is used for the
treatment of high blood pressure in the
blood vessels between the heart and the
lungs. This condition is called
pulmonary arterial hypertension.
This medicine acts to reduce abnormally
high blood pressure by widening these
blood vessels. It belongs to the class of
medicines known as endothelin receptor
antagonists.
Your doctor however, may prescribe
Bosentan Actelion for another purpose.
ASK YOUR DOCTOR IF YOU HAVE ANY
QUESTIONS WHY IT HAS BEEN PRESCRIBED
FOR YOU.
This medicine is only available with a
doctor’s prescription.
BEFORE YOU TAKE BOSENTAN
ACTELION
_WHEN YOU MUST NOT TAKE BOSENTAN _
_ACTELION _
DO NOT TAKE THIS MEDICINE IF YOU ARE:
•
PREGNANT OR INTEND TO BECOME
PREGNANT. YOU MUST STOP
TAKING THE MEDICINE AT LEAST 3
MONTHS BEFORE TRYING TO
BECOME PREGNANT.
I
t
is known
that this medicine causes harm
to the developing baby if you
take it during pregnancy and in
the three months before
b
ecoming pregnant.
•
BREASTFEEDING:
Tell your doctor
immediately if you are
breastfeeding. You are advised
to stop breastfeeding if this
medicine is prescribed for you
because it is not known if this
drug passes into the milk in
women who are taking this
medicine.
•
B
eing treated with cyclosporine
A (a medicine used after a
transplant or to treat psoriasis)
•
Being treated with
glibenclamide (a medicine used
for d

Summary of Product characteristics

1/26
PRODUCT INFORMATION
BOSENTAN ACTELION 62.5 MG & 125 MG TABLETS
Bosentan Actelion 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
Active: Bosentan (as monohydrate)
The chemical name of bosentan monohydrate is benzenesulphonamide,
4-(1,1-
dimethylethyl)-N-[6-(2hydroxyethoxy)-5-(2-methoxyphenoxy)[2,2’-bipyrimidin]-4-yl]-,
monohydrate.
The structural formula is:
The molecular formula is:
C
27
H
29
N
5
O
6
S
Anhydrous
MW: 551.62
C
27
H
29
N
5
O
6
S.H
2
O
Monohydrate
MW: 569.64
CAS 147536-97-8 (anhydrous substance)
Bosentan is the first of a new drug class, an endothelin receptor
antagonist.
Bosentan belongs to a class of highly substituted pyrimidine
derivatives, with no
chiral centres.
DESCRIPTION
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.
Inactive: maize
starch
, pregelatinised maize starch, sodium starch glycollate,
povidone, glyceryl behenate, magnesium stearate, hypromellose,
triacetin, talc,
titanium dioxide, iron oxide yellow, iron oxide red, ethylcellulose.
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PHARMACOLOGY
PHARMACODYNAMIC PROPERTIES
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, suggesting a pathogenic role for ET-1 in this
disease.
Bosentan is a specific and competitive antagonist at endothelin
receptor types ETA
and ETB. Bosentan has a slightly higher affinity for ETA receptors
than for ETB
receptors.
PHARMACOKINETICS
_General _
After oral administration, maximum plasma concentrations of bosentan
found in a
study of the 125 mg tablets taken as a sing