BOSENTAN INTAS Bosentan (as monohydrate) 62.5 mg film-coated tablets blister pack

Country: Australia

Language: English

Source: Department of Health (Therapeutic Goods Administration)

Active ingredient:

bosentan monohydrate, Quantity: 64.54 mg (Equivalent: bosentan, Qty 62.5 mg)

Available from:

Accord Healthcare Pty Ltd

INN (International Name):

bosentan monohydrate

Pharmaceutical form:

Tablet, film coated

Composition:

Excipient Ingredients: sodium starch glycollate type A; maize starch; povidone; magnesium stearate; purified water; pregelatinised maize starch; titanium dioxide; hypromellose; purified talc; triacetin; iron oxide yellow; iron oxide red

Administration route:

Oral

Units in package:

112 tablets in blister pack, 56 tablets in blister pack, 14 tablets in blister pack

Prescription type:

(S4) Prescription Only Medicine

Therapeutic indications:

Bosentan Intas is indicated for the treatment of ? idiopathic pulmonary arterial hypertension ? familial pulmonary arterial hypertension ? pulmonary arterial hypertension associated with scleroderma or ? pulmonary arterial hypertension associated with congenital systemic to pulmonary shunts including Eisenmenger?s physiology,in patients with WHO functional Class II, III or IV symptoms.

Product summary:

Visual Identification: Orange-white, round, biconvex, film-coated tablets, debossed with IB1 on one side and plain on other side.; Container Type: Blister Pack; Container Material: PVC/PE/PVDC/Al; Container Life Time: 21 Months; Container Temperature: Store below 25 degrees Celsius

Authorization status:

Licence status A

Authorization date:

2016-03-22

Patient Information leaflet

BOSENTAN INTAS
CONSUMER MEDICINE INFORMATION
Version: 2.0
‐2016‐ Page 1 of 5
BOSENTAN INTAS
(BOSENTAN FILM‐COATED TABLETS 62.5 MG AND 125 MG)
_Bosentan monohydrate _
CONSUMER MEDICINE INFORMATION
WHAT IS IN THIS LEAFLET
This leaflet answers some
common questions about
Bosentan Intas.
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
taking Bosentan Intas against
the benefits this medicine is
expected to have for you.
IF YOU HAVE ANY CONCERNS
ABOUT USING BOSENTAN INTAS
ASK YOUR DOCTOR OR
PHARMACIST.
KEEP THIS LEAFLET WITH YOUR
MEDICINE.
You may need to read it
again.
WHAT BOSENTAN INTAS IS USED
FOR
Bosentan Intas 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 Intas for
another purpose.
ASK YOUR DOCTOR IF YOU HAVE
ANY QUESTIONS ABOUT WHY IT
HAS BEEN PRESCRIBED FOR YOU.
This medicine is only
available with a doctor's
prescription.
BEFORE YOU TAKE BOSENTAN
INTAS
_WHEN YOU MUST NOT TAKE _
_BOSENTAN INTAS _
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. It is known that
this medicine causes harm
to the developing baby if
you
take it during
pregnancy and in the three
months before becoming
pregnant.
•
BREAST‐FEEDING: Tell your
doctor immediately if you
are breast‐feeding. You are
advised to stop breast‐
feeding 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.
•
Being treated with
cyclosporine A (a medicine
used after a transplant o

Summary of Product characteristics

Bosentan Intas (Bosentan Film-coated Tablets 62.5 mg and 125 mg)
Version 2.0
-2016-
Page 1 of 27
PRODUCT INFORMATION
Bosentan Intas
(bosentan film-coated tablets 62.5 mg and 125 mg)
BOSENTAN INTAS 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 Intas (bosentan film-coated tablets 62.5 mg and 125 mg).
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
molecular weight: 551.62
C
27
H
29
N
5
O
6
S.H
2
O
Monohydrate
molecular weight: 569.63
CAS 147536-97-8 (anhydrous substance)
Bosentan is the first of a new drug class, an endothelin receptor
antagonist.
Bosentan Intas (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.
Bosentan Intas (Bosentan Film-coated Tablets 62.5 mg and 125 mg)
Version 2.0
-2016-
Page 2 of 27
Inactive:
maize
starch,
pregelatinised
maize
starch,
sodium
starch
glycollate
type
A,
povidone, magnesium stearate, hypromellose, glycerol triacetate,
purified talc, titanium
dioxide, iron oxide yellow and iron oxide red.
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 spec