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BOSENTAN 125 MG FILM-COATED TABLETS

Active substance(s): BOSENTAN MONOHYDRATE

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BOSENTAN
62.5 mg AND 125 mg
FILM-COATED TABLETS
Package leaflet: Information for the user

Read all of this leaflet carefully before
you start taking this medicine because it
contains important information for you.
• Keep this leaflet. You may need to read
it again.
• If you have any further questions, ask
your doctor or pharmacist.
• This medicine has been prescribed for
you only. Do not pass it on to others. It
may harm them, even if their signs of
illness are the same as yours.
• If you get any side effects, talk to your
doctor or pharmacist. This includes any
possible side effects not listed in this
leaflet. See section 4.
What is in this leaflet:

1. What Bosentan is and what it is used
for
2. What you need to know before you
take Bosentan
3. How to take Bosentan
4. Possible side effects
5. How to store Bosentan
6. Contents of the pack and other
information

1 What Bosentan is and what it
is used for
Bosentan tablets contain bosentan, which
blocks a naturally occurring hormone
called endothelin-1 (ET-1), which causes
blood vessels to narrow. Bosentan
therefore causes blood vessels to expand
and belongs to the class of medicines
called “endothelin receptor antagonists”.
Bosentan is used to treat:
• Pulmonary arterial hypertension (PAH):
PAH is a disease of severe narrowing
of the blood vessels in the lungs
resulting in high blood pressure in the
blood vessels (the pulmonary arteries)
that carry blood from the heart to the
lungs. This pressure reduces the
amount of oxygen that can get into the
blood in the lungs, making physical
activity more difficult. Bosentan
widens the pulmonary arteries, making
it easier for the heart to pump blood
through them. This lowers the blood
pressure and relieves the symptoms.
Bosentan is used to treat patients with
class III pulmonary arterial hypertension
(PAH) to improve exercise capacity (the
ability to carry out physical activity) and
symptoms. The ‘class’ reflects the
seriousness of the disease: ‘class III’
involves marked limitation of physical
activity. Some improvements have also
been shown in patients with class II PAH.
‘Class II’ involves slight limitation of
physical activity. The PAH for which
Bosentan is indicated can be:
• primary (with no identified cause or
familial)
• caused by scleroderma (also called
systemic sclerosis, a disease where
there is abnormal growth of the
connective tissue that supports the
skin and other organs)
• caused by congenital (inborn) heart
defects with shunts (abnormal
passageways) causing abnormal flow
of blood through the heart and lungs.

write the date of your most recent test
and also of your next test (ask your
doctor for the date) on the Patient Alert
Card, to help you remember when your
next test is due.
Blood tests for liver function
These will be done every month for the
duration of treatment with Bosentan.
After an increase in dose an additional
test will be done after 2 weeks.
Blood tests for anaemia
These will be done every month for the
first 4 months of treatment, then every
3 months after that, as patients taking
Bosentan may get anaemia.
If these results are abnormal, your doctor
may decide to reduce your dose or stop
treatment with Bosentan and to perform
further tests to investigate the cause.
Children and adolescents
Bosentan is not recommended in
paediatric patients with systemic
sclerosis and ongoing digital ulcer
disease. Please see also section 3 “How
to take Bosentan”.
Other medicines and Bosentan
Please tell your doctor or pharmacist if
you are taking or have recently taken any
other medicines, including medicines
obtained without a prescription. It is
especially important to tell your doctor if
you are taking:
• cyclosporine A (a medicine used after
transplants and to treat psoriasis),
which must not be used together with
Bosentan
• sirolimus or tacrolimus, which are
medicines used after transplants, as
these are not recommended to be
used together with Bosentan
• glibenclamide (a diabetes medicine),
rifampicin (a tuberculosis medicine),
fluconazole and ketoconazole
(medicines against fungal infections),
nevirapine (an HIV medicine) as these
medicines are not recommended to be
used together with Bosentan
• other medicines for the treatment of
HIV infection, which may require
special monitoring if used together
with Bosentan
• hormonal contraceptives, which are
not effective as the sole method of
contraception when you take
Bosentan. Inside your pack of
Bosentan tablets you will find a Patient
Alert Card which you should read
carefully. Your doctor and/or
gynaecologist will establish the
contraception which is appropriate for
you
• other medications for the treatment of
pulmonary hypertension: sildenafil and
tadalafil
• warfarin (an anticoagulant agent)
• simvastatin (used to treat
hypercholesterolemia).
Women of child-bearing age
Do not take Bosentan if you are pregnant
or planning to become pregnant.
Pregnancy tests
Bosentan may harm unborn babies
conceived before starting or during
treatment. If you are a woman who could
become pregnant, your doctor will ask
you to take a pregnancy test before you
start taking Bosentan, and regularly while
you are taking Bosentan.

• Digital ulcers: (sores on the fingers
and toes) in adult patients with a
condition called scleroderma.
Bosentan reduces the number of new
finger and toe ulcers that appear.

Contraceptives
If it is possible that you could become
pregnant, use a reliable form of birth
control (contraception) while you are
taking Bosentan. Your doctor or
gynaecologist will advise you about
What
you
need
to
know
before
reliable contraceptive methods while
2
you take Bosentan
taking Bosentan. Because Bosentan may
make hormonal contraception (e.g., oral,
Do not take Bosentan if you:
injection, implant, or skin patches)
• are allergic to bosentan or any of the
ineffective, this method on its own is not
other ingredients of this medicine
reliable. Therefore, if you use hormonal
(listed in section 6)
contraceptives you must also use a
• have liver problems (ask your doctor) barrier method (e.g., female condom,
• are pregnant, or could get pregnant
diaphragm, contraceptive sponge, or
because you are not using reliable
your partner must also use a condom).
contraceptive methods. Please read
Inside your pack of Bosentan tablets you
the information under
will find a Patient Alert Card. You should
“Contraceptives” and “Other
complete this card and take it to your
medicines and Bosentan”
doctor at your next visit so that your
• are taking cyclosporine A (a medicine doctor or gynaecologist can assess
used after a transplant or to treat
whether you need additional or
psoriasis).
alternative reliable contraceptive
methods. Monthly pregnancy tests are
If any of these apply to you, tell your
recommended while you are taking
doctor.
Bosentan and are of child-bearing age.
Warnings and precautions
Tests your doctor will do before
treatment:
• a blood test to check your liver
function
• a blood test to check for anaemia (low
haemoglobin)
• a pregnancy test if you are a woman of
child-bearing potential.
Some patients taking Bosentan have
been found to have abnormal liver
function tests and anaemia (low
haemoglobin).
Tests your doctor will do during
treatment
During treatment with Bosentan, your
doctor will arrange for regular blood tests
to check for changes in your liver function
and haemoglobin level.
For all these tests please refer also to the
Patient Alert Card (inside your pack of
Bosentan tablets). It is important that you
have these regular blood tests as long as
you are taking Bosentan. We suggest you

Tell your doctor immediately if you
become pregnant while you are taking
Bosentan, or plan to become pregnant in
the near future.
Breast-feeding
Tell your doctor immediately if you are
breast-feeding. You are advised to stop
breast-feeding if Bosentan is prescribed
for you, because it is not known whether
this medicine passes into breast milk.
Fertility
If you are a man taking Bosentan, it is
possible that this medicine may lower
your sperm count. It cannot be excluded
that this may affect your ability to father a
child. Talk to your doctor if you have any
questions or concerns about it.
Driving and using machines
Bosentan has no or negligible influence
on the ability to drive and use machines.
However, Bosentan can induce
hypotension (decrease of your blood
pressure) which can make you feel dizzy,

affect your vision and affect your ability
to drive and use machines. Therefore, if
you feel dizzy or that your vision is
blurred while taking Bosentan, do not
drive or operate any tools or machines.

Uncommon: may
people
• thrombocytope
blood platelets)
• neutropenia/leu
of white blood
How to take Bosentan
• elevated liver fu
hepatitis (inflam
including possi
Treatment with Bosentan should only be
underlying hep
started and monitored by a doctor who
(yellowing of th
has experience in the treatment of PAH or
the eyes).
systemic sclerosis. Always take this
medicine exactly as your doctor has told
you. Check with your doctor or
pharmacist if you are not sure.
Bosentan with food and drink
Bosentan can be taken with or without
food.
Recommended dose
Adults
The treatment in adults is usually started
for the first 4 weeks with 62.5 mg twice
daily (morning and evening), from then
your doctor will usually advise you to
take a 125 mg tablet twice daily,
depending on how you react to Bosentan.
Use in children and adolescents
The dose recommendation in children is
only for PAH. For children 1 year and
older, treatment with bosentan is usually
started with 2 mg per kg bodyweight
twice daily (morning and evening). Your
doctor will advise you on your dosing.
Please note that bosentan is also
available as a dispersible 32 mg tablet
formulation, which may make correct
dosing easier for children and patients
with low body weight or difficulties to
swallow film-coated tablets.
If you have the impression that the effect
of Bosentan is too strong or too weak,
talk to your doctor in order to find out
whether your dose needs to be changed.

Rare: may affect u
• anaphylaxis (ge
angioedema (sw
commonly arou
tongue or throa
• cirrhosis (scarri
failure (serious
function).

Not known: frequ
estimated from th
• blurred vision.

Side effects in chil
The side effects th
in children treated
same as those in a

Reporting of side
If you get any side
doctor or pharmac
possible side effec
leaflet. You can als
directly via the Yel
www.mhra.gov.uk
By reporting side
provide more info
this medicine.

How to stor

Keep this medicin
reach of children.

Do not use this m
date which is state
blister after EXP. T
How to take Bosentan
the last day of tha
Tablets should be taken (morning and
evening), swallowed with water. The
Store below 30°C.
tablets can be taken with or without food.
Do not throw awa
If you take more Bosentan than you
wastewater or hou
should
pharmacist how to
If you take more tablets than you have
you no longer use
been told to take, contact your doctor
help protect the en
immediately.

Contents of

If you forget to take Bosentan
information
If you forget to take Bosentan, take a
dose as soon as you remember, then
What Bosentan co
continue to take your tablets at the usual • The active subs
times. Do not take a double dose to make
• Each 62.5 mg
up for forgotten tablets.
contains 62.5
monohydrat
If you stop taking Bosentan
• Each 125 mg
Suddenly stopping your treatment with
contains 125
Bosentan may lead to your symptoms
monohydrat
getting worse. Do not stop taking
• The other ingre
Bosentan unless your doctor tells you to.
• Tablet core: m
Your doctor may tell you to reduce the
pregelatinize
dose over a few days before stopping
glycolate (ty
completely.
glycerol dibe
magnesium
If you have any further questions on the

Film-coat:
hy
use of this medicine, ask your doctor or
talc, titanium
pharmacist.
oxide (E172)
and ethylcell
Possible side effects
dispersion (c
ethylcellulos
Like all medicines, this medicine can
sulphate and
cause side effects, although not
everybody gets them.
What Bosentan lo
the pack
The most serious side effects with
Each 62.5 mg Bos
bosentan are:
tablets are pink-or
• abnormal liver function which may
diameter), biconve
affect more than 1 in 10 people
on one side.
• anaemia (low blood value) which may Each 125 mg Bose
affect up to 1 in 10 people. Anaemia may are pink-orange, o
occasionally require blood transfusion. dimensions), with
Your liver and blood values will be
side.
monitored during treatment with
Bosentan (see section 2). It is important
Bosentan 62.5 mg
that you have these tests as ordered by
sizes of 7, 14, 28, 5
your doctor.
film-coated tablets
14x1, 28x1, 56 x1,
Signs that your liver may not be working film-coated tablets
properly include:
unit-dose blisters.
• nausea (urge to vomit)
Bosentan 125 mg
• vomiting
sizes of 7, 14, 28, 5
• fever (high temperature)
film-coated tablets
• pain in your stomach (abdomen)
14x1, 28x1, 56 x1,
• jaundice (yellowing of your skin or the film-coated tablets
whites of your eyes)
unit-dose blisters.
• dark-coloured urine
• itching of your skin
Not all pack sizes
• lethargy or fatigue (unusual tiredness
Marketing Authori
or exhaustion)
TEVA UK Limited,
• flu-like syndrome (joint and muscle
UK
pain with fever).
If you notice any of these signs tell your
doctor immediately.
Other side effects:

Manufacturer
PLIVA Hrvatska d.
Ltd.), Prilaz baruna
10000, Croatia

Very common: may affect more than one This leaflet was la
in 10 people
PL 00289/1847
• headache
PL 00289/1848
• oedema (swelling of the legs and
ankles or other signs of fluid retention).
Common: may affect up to one in 10
people
• flushed appearance or redness of skin
• hypersensitivity reactions (including
skin inflammation, itching and rash)
• gastroesophageal reflux disease (acid
reflux)
• diarrhoea
• syncope (fainting)
• palpitations (fast or irregular heart
beats)
• low blood pressure
• nasal congestion.

TAN
D 125 mg
D TABLETS

arefully before
dicine because it
rmation for you.
may need to read

er questions, ask
acist.
en prescribed for
it on to others. It
n if their signs of
s yours.
ects, talk to your
This includes any
not listed in this

d what it is used

ow before you

n

an
and other

s and what it

n bosentan, which
ing hormone
1), which causes
. Bosentan
vessels to expand
of medicines
tor antagonists”.

t:
pertension (PAH):
vere narrowing
n the lungs
d pressure in the
lmonary arteries)
the heart to the
educes the
at can get into the
aking physical
. Bosentan
y arteries, making
to pump blood
wers the blood
the symptoms.

write the date of your most recent test
and also of your next test (ask your
doctor for the date) on the Patient Alert
Card, to help you remember when your
next test is due.
Blood tests for liver function
These will be done every month for the
duration of treatment with Bosentan.
After an increase in dose an additional
test will be done after 2 weeks.
Blood tests for anaemia
These will be done every month for the
first 4 months of treatment, then every
3 months after that, as patients taking
Bosentan may get anaemia.
If these results are abnormal, your doctor
may decide to reduce your dose or stop
treatment with Bosentan and to perform
further tests to investigate the cause.
Children and adolescents
Bosentan is not recommended in
paediatric patients with systemic
sclerosis and ongoing digital ulcer
disease. Please see also section 3 “How
to take Bosentan”.
Other medicines and Bosentan
Please tell your doctor or pharmacist if
you are taking or have recently taken any
other medicines, including medicines
obtained without a prescription. It is
especially important to tell your doctor if
you are taking:
• cyclosporine A (a medicine used after
transplants and to treat psoriasis),
which must not be used together with
Bosentan
• sirolimus or tacrolimus, which are
medicines used after transplants, as
these are not recommended to be
used together with Bosentan
• glibenclamide (a diabetes medicine),
rifampicin (a tuberculosis medicine),
fluconazole and ketoconazole
(medicines against fungal infections),
nevirapine (an HIV medicine) as these
medicines are not recommended to be
used together with Bosentan
• other medicines for the treatment of
HIV infection, which may require
special monitoring if used together
with Bosentan
• hormonal contraceptives, which are
not effective as the sole method of
contraception when you take
Bosentan. Inside your pack of
Bosentan tablets you will find a Patient
Alert Card which you should read
carefully. Your doctor and/or
gynaecologist will establish the
contraception which is appropriate for
you
• other medications for the treatment of
pulmonary hypertension: sildenafil and
tadalafil
• warfarin (an anticoagulant agent)
• simvastatin (used to treat
hypercholesterolemia).

t patients with
ial hypertension
se capacity (the
cal activity) and
eflects the
se: ‘class III’
on of physical
ments have also
with class II PAH.
limitation of
H for which
n be:
Women of child-bearing age
tified cause or
Do not take Bosentan if you are pregnant
or planning to become pregnant.
ma (also called
disease where
Pregnancy tests
wth of the
Bosentan may harm unborn babies
t supports the
conceived before starting or during
s)
treatment. If you are a woman who could
(inborn) heart
become pregnant, your doctor will ask
abnormal
you to take a pregnancy test before you
g abnormal flow start taking Bosentan, and regularly while
heart and lungs. you are taking Bosentan.

on the fingers
ients with a
oderma.
number of new
that appear.

Contraceptives
If it is possible that you could become
pregnant, use a reliable form of birth
control (contraception) while you are
taking Bosentan. Your doctor or
gynaecologist will advise you about
o know before reliable contraceptive methods while
an
taking Bosentan. Because Bosentan may
make hormonal contraception (e.g., oral,
you:
injection, implant, or skin patches)
an or any of the
ineffective, this method on its own is not
his medicine
reliable. Therefore, if you use hormonal
contraceptives you must also use a
ask your doctor) barrier method (e.g., female condom,
d get pregnant
diaphragm, contraceptive sponge, or
using reliable
your partner must also use a condom).
ds. Please read
Inside your pack of Bosentan tablets you
r
will find a Patient Alert Card. You should
“Other
complete this card and take it to your
tan”
doctor at your next visit so that your
ne A (a medicine doctor or gynaecologist can assess
nt or to treat
whether you need additional or
alternative reliable contraceptive
methods. Monthly pregnancy tests are
you, tell your
recommended while you are taking
Bosentan and are of child-bearing age.

ns
o before

your liver

Tell your doctor immediately if you
become pregnant while you are taking
Bosentan, or plan to become pregnant in
the near future.

or anaemia (low

Breast-feeding
Tell your doctor immediately if you are
u are a woman of breast-feeding. You are advised to stop
al.
breast-feeding if Bosentan is prescribed
sentan have
for you, because it is not known whether
ormal liver
this medicine passes into breast milk.
mia (low
Fertility
If you are a man taking Bosentan, it is
o during
possible that this medicine may lower
your sperm count. It cannot be excluded
osentan, your
that this may affect your ability to father a
egular blood tests child. Talk to your doctor if you have any
your liver function questions or concerns about it.

e refer also to the
e your pack of
mportant that you
d tests as long as
. We suggest you

Driving and using machines
Bosentan has no or negligible influence
on the ability to drive and use machines.
However, Bosentan can induce
hypotension (decrease of your blood
pressure) which can make you feel dizzy,

affect your vision and affect your ability
to drive and use machines. Therefore, if
you feel dizzy or that your vision is
blurred while taking Bosentan, do not
drive or operate any tools or machines.

Uncommon: may affect up to one in 100
people
• thrombocytopenia (low number of
blood platelets)
• neutropenia/leukopenia (low number
of white blood cells)
• elevated liver function tests with
3 How to take Bosentan
hepatitis (inflammation of the liver)
including possible exacerbation of
Treatment with Bosentan should only be
underlying hepatitis and/or jaundice
started and monitored by a doctor who
(yellowing of the skin or the whites of
has experience in the treatment of PAH or
the eyes).
systemic sclerosis. Always take this
medicine exactly as your doctor has told
you. Check with your doctor or
pharmacist if you are not sure.
Bosentan with food and drink
Bosentan can be taken with or without
food.
Recommended dose
Adults
The treatment in adults is usually started
for the first 4 weeks with 62.5 mg twice
daily (morning and evening), from then
your doctor will usually advise you to
take a 125 mg tablet twice daily,
depending on how you react to Bosentan.
Use in children and adolescents
The dose recommendation in children is
only for PAH. For children 1 year and
older, treatment with bosentan is usually
started with 2 mg per kg bodyweight
twice daily (morning and evening). Your
doctor will advise you on your dosing.
Please note that bosentan is also
available as a dispersible 32 mg tablet
formulation, which may make correct
dosing easier for children and patients
with low body weight or difficulties to
swallow film-coated tablets.
If you have the impression that the effect
of Bosentan is too strong or too weak,
talk to your doctor in order to find out
whether your dose needs to be changed.

Rare: may affect up to one in 1000 people
• anaphylaxis (general allergic reaction),
angioedema (swelling, most
commonly around the eyes, lips,
tongue or throat)
• cirrhosis (scarring) of the liver, liver
failure (serious disturbance of liver
function).
Not known: frequency cannot be
estimated from the available data
• blurred vision.
Side effects in children and adolescents
The side effects that have been reported
in children treated with Bosentan are the
same as those in adults.
Reporting of side effects
If you get any side effects, talk to your
doctor or pharmacist. This includes any
possible side effects not listed in this
leaflet. You can also report side effects
directly via the Yellow Card Scheme at:
www.mhra.gov.uk/yellowcard
By reporting side effects you can help
provide more information on the safety of
this medicine.

5 How to store Bosentan
Keep this medicine out of the sight and
reach of children.

Do not use this medicine after the expiry
date which is stated on the carton and
blister after EXP. The expiry date refers to
How to take Bosentan
the last day of that month.
Tablets should be taken (morning and
evening), swallowed with water. The
Store below 30°C.
tablets can be taken with or without food.
Do not throw away any medicines via
If you take more Bosentan than you
wastewater or household waste. Ask your
should
pharmacist how to throw away medicines
If you take more tablets than you have
you no longer use. These measures will
been told to take, contact your doctor
help protect the environment.
immediately.

Contents of the pack and other

6
If you forget to take Bosentan
information
If you forget to take Bosentan, take a
dose as soon as you remember, then
What Bosentan contains
continue to take your tablets at the usual • The active substance is bosentan.
times. Do not take a double dose to make
• Each 62.5 mg film-coated tablet
up for forgotten tablets.
contains 62.5 mg bosentan (as
monohydrate).
If you stop taking Bosentan
• Each 125 mg film-coated tablet
Suddenly stopping your treatment with
contains 125 mg bosentan (as
Bosentan may lead to your symptoms
monohydrate).
getting worse. Do not stop taking
• The other ingredients are
Bosentan unless your doctor tells you to.
• Tablet core: maize starch,
Your doctor may tell you to reduce the
pregelatinized starch, sodium starch
dose over a few days before stopping
glycolate (type A), povidone,
completely.
glycerol dibehenate and
magnesium stearate.
If you have any further questions on the

Film-coat:
hypromellose, triacetin,
use of this medicine, ask your doctor or
talc, titanium dioxide, yellow iron
pharmacist.
oxide (E172), red iron oxide (E172)
and ethylcellulose aqueous
4 Possible side effects
dispersion (containing
ethylcellulose, sodium lauryl
Like all medicines, this medicine can
sulphate and cetyl alcohol).
cause side effects, although not
everybody gets them.
What Bosentan looks like and contents of
the pack
The most serious side effects with
Each 62.5 mg Bosentan film-coated
bosentan are:
tablets are pink-orange, round (6 mm in
• abnormal liver function which may
diameter), biconvex, with debossing 62.5
affect more than 1 in 10 people
on one side.
• anaemia (low blood value) which may Each 125 mg Bosentan film-coated tablets
affect up to 1 in 10 people. Anaemia may are pink-orange, oval (11 mm x 5 mm in
occasionally require blood transfusion. dimensions), with debossing 125 on one
Your liver and blood values will be
side.
monitored during treatment with
Bosentan (see section 2). It is important
Bosentan 62.5 mg is available in pack
that you have these tests as ordered by
sizes of 7, 14, 28, 56, 60 and 112
your doctor.
film-coated tablets in blisters or 7x1,
14x1, 28x1, 56 x1, 60x1 and 112x1
Signs that your liver may not be working film-coated tablets in perforated
properly include:
unit-dose blisters.
• nausea (urge to vomit)
Bosentan 125 mg is available in pack
• vomiting
sizes of 7, 14, 28, 56, 60, 112 and 120
• fever (high temperature)
film-coated tablets in blisters or 7x1,
• pain in your stomach (abdomen)
14x1, 28x1, 56 x1, 60x1 and 112x1
• jaundice (yellowing of your skin or the film-coated tablets in perforated
whites of your eyes)
unit-dose blisters.
• dark-coloured urine
• itching of your skin
Not all pack sizes may be marketed.
• lethargy or fatigue (unusual tiredness
Marketing Authorisation Holder
or exhaustion)
TEVA UK Limited, Eastbourne, BN22 9AG,
• flu-like syndrome (joint and muscle
UK
pain with fever).
If you notice any of these signs tell your
doctor immediately.
Other side effects:

Manufacturer
PLIVA Hrvatska d.o.o. (PLIVA Croatia
Ltd.), Prilaz baruna Filipovica 25, Zagreb,
10000, Croatia

Very common: may affect more than one This leaflet was last revised in 10/2017.
in 10 people
PL 00289/1847
• headache
PL 00289/1848
• oedema (swelling of the legs and
ankles or other signs of fluid retention).
Common: may affect up to one in 10
people
• flushed appearance or redness of skin
• hypersensitivity reactions (including
skin inflammation, itching and rash)
• gastroesophageal reflux disease (acid
reflux)
• diarrhoea
• syncope (fainting)
• palpitations (fast or irregular heart
beats)
• low blood pressure
• nasal congestion.

EAS1411b

180 x 600

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