BOSENTAN-DRLA bosentan (as monohydrate) 62.5 mg tablet blister pack

Country: Australia

Language: English

Source: Department of Health (Therapeutic Goods Administration)

Active ingredient:

bosentan monohydrate, Quantity: 64.541 mg

Available from:

Dr Reddys Laboratories Australia Pty Ltd

INN (International Name):

bosentan monohydrate

Pharmaceutical form:

Tablet, film coated

Composition:

Excipient Ingredients: maize starch; pregelatinised maize starch; sodium starch glycollate type A; povidone; glycerol dibehenate; magnesium stearate; hypromellose; titanium dioxide; triacetin; purified talc; iron oxide yellow; iron oxide red; ethylcellulose; cetyl alcohol; sodium lauryl sulfate

Administration route:

Oral

Units in package:

60

Prescription type:

(S4) Prescription Only Medicine

Therapeutic indications:

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: Light orange, film-coated, round biconvex tablet debossed with '62.5' on one side and plain on the other side; Container Type: Blister Pack; Container Material: PVC/PE/PVDC/Al; Container Life Time: 24 Months; Container Temperature: Store below 25 degrees Celsius; Container Closure: Neither child resistant closure nor restricted flow insert

Authorization status:

Licence status A

Authorization date:

2016-12-21

Patient Information leaflet

Bosentan‐DRLA CMI
Page 1 of 3
BOSENTAN-
DRLA
_Bosentan (BOZ-en-tan) 62.5 mg/125 _
_mg film- coated tablets_
CONSUMER MEDICINE
INFORMATION
WHAT IS IN THIS LEAFLET
This leaflet answers some common
questions about Bosentan-DRLA.
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-DRLA IS
USED FOR
Bosentan-DRLA 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-DRLA 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-
DRLA
_WHEN YOU MUST NOT TAKE BOSENTAN-_
_DRLA_
_ _
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 diabete

Summary of Product characteristics

1/29
PRODUCT INFORMATION
BOSENTAN-DRLA
BOSENTAN (AS MONOHYDRATE) 62.5 MG & 125 MG TABLETS
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)
CAS 157212-55-0 (monohydrate)
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,
cetyl alcohol,
sodium lauryl sulfate.
BOSENTAN-DRLA 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
2/29
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 pla