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BOSENTAN 62.5 MG FILM-COATED TABLETS

Active substance(s): BOSENTAN MONOHYDRATE

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


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.

2.

What you need to know before you take Bosentan

Do not take Bosentan if you:

are allergic to bosentan or any of the other ingredients of this medicine (listed in section 6)

have liver problems (ask your doctor)

are pregnant, or could get pregnant because you are not using reliable contraceptive methods.
Please read the information under “Contraceptives” and “Other medicines and Bosentan”



are taking cyclosporine A (a medicine used after a transplant or to treat psoriasis).

If any of these apply to you, tell your doctor.
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 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) or fluconazole (a medicine
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.
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.
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 reliable contraceptive methods
while taking Bosentan. Because Bosentan may make hormonal contraception (e.g., oral, injection, implant,
or skin patches) ineffective, this method on its own is not reliable. Therefore, if you use hormonal
contraceptives you MUST also use a barrier method (e.g., female condom, diaphragm, contraceptive sponge,
or your partner must also use a condom). Inside your pack of Bosentan tablets you will find a Patient Alert
Card. You should complete this card and take it to your doctor at your next visit so that your doctor or
gynaecologist can assess whether you need additional or alternative reliable contraceptive methods. Monthly
pregnancy tests are recommended while you are taking Bosentan and are of child-bearing age.
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 and affect your ability
to drive and use machines. Therefore, if you feel dizzy while taking Bosentan, do NOT drive or operate any
tools or machines.
3.

How to take Bosentan

Treatment with Bosentan should only be started and monitored by a doctor who has experience in the
treatment of PAH or 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.
How to take Bosentan
Tablets should be taken (morning and evening), swallowed with water. The tablets can be taken with or
without food.
If you take more Bosentan than you should
If you take more tablets than you have been told to take, contact your doctor immediately.
If you forget to take Bosentan
If you forget to take Bosentan, take a dose as soon as you remember, then continue to take your tablets at the
usual times. Do NOT take a double dose to make up for forgotten tablets.
If you stop taking Bosentan
Suddenly stopping your treatment with Bosentan may lead to your symptoms getting worse. Do NOT stop
taking Bosentan unless your doctor tells you to. Your doctor may tell you to reduce the dose over a few days
before stopping completely.
If you have any further questions on the use of this medicine, ask your doctor or pharmacist.
4.

Possible side effects

Like all medicines, this medicine can cause side effects, although not everybody gets them.
The most serious side effects with bosentan are:

abnormal liver function which may affect more than 1 in 10 people

anaemia (low blood value) which may affect up to 1 in 10 people. Anaemia may occasionally require
blood transfusion.
Your liver and blood values will be monitored during treatment with Bosentan (see section 2). It is important
that you have these tests as ordered by your doctor.
Signs that your liver may not be working properly include:

nausea (urge to vomit)

vomiting

fever (high temperature)

pain in your stomach (abdomen)

jaundice (yellowing of your skin or the whites of your eyes)

dark-coloured urine

itching of your skin

lethargy or fatigue (unusual tiredness or exhaustion)

flu-like syndrome (joint and muscle pain with fever).
If you notice any of these signs tell your doctor immediately
Other side effects:
Very common: may affect more than one in 10 people

headache

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)


gastrooesophageal reflux disease (acid reflux)







diarrhoea
syncope (fainting)
palpitations (fast or irregular heart beats)
low blood pressure
nasal congestion.

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 hepatitis (inflammation of the liver) including possible exacerbation
of underlying hepatitis and/or jaundice (yellowing of the skin or the whites of the eyes).
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).
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 the last day of that month.
Store below 30°C.
Do not throw away any medicines via wastewater or household waste. Ask your pharmacist how to throw
away medicines you no longer use. These measures will help protect the environment.
6.

Contents of the pack and other information

What Bosentan contains
 The active substance is bosentan.

Each 62.5 mg film-coated tablet contains 62.5 mg bosentan (as monohydrate).

Each 125 mg film-coated tablet contains 125 mg bosentan (as monohydrate).
 The other ingredients are

Tablet core: maize starch, pregelatinized starch, sodium starch glycolate (type A), povidone,
glycerol dibehenate and magnesium stearate

Film-coat: hypromellose, triacetin, talc, titanium dioxide, yellow iron oxide (E172), red iron
oxide (E172) and ethylcellulose aqueous dispersion (containing ethylcellulose, sodium lauryl
sulphate and cetyl alcohol).
What Bosentan looks like and contents of the pack
Each 62.5 mg Bosentan film-coated tablets are pink-orange, round (6 mm in diameter), biconvex, with
debossing 62.5 on one side.
Each 125 mg Bosentan film-coated tablets are pink-orange, oval (11 mm x 5 mm in dimensions), with
debossing 125 on one side.

Bosentan 62.5 mg is available in pack sizes of 7, 14, 56, 60 and 112 film-coated tablets in blisters or 7x1,
14x1, 56 x1, 60x1 and 112x1 film-coated tablets in perforated unit-dose blisters.
Bosentan 125 mg is available in pack sizes of 7, 14, 56, 60 and 112 film-coated tablets in blisters or 7x1,
14x1, 56 x1, 60x1 and 112x1 film-coated tablets in perforated unit-dose blisters.
Not all pack sizes may be marketed.
Marketing Authorisation Holder
TEVA UK Limited, Eastbourne, BN22 9AG, UK
Manufacturer
PLIVA Hrvatska d.o.o. (PLIVA Croatia Ltd.), Prilaz baruna Filipovica 25, Zagreb, 10000, Croatia
*OR
Teva Pharma B.V., Swensweg 5, Haarlem, 2031 GA, The Netherlands
This leaflet was last revised in 03/2016.
PL 00289/1847
PL 00289/1848
* Only the actual site of batch release will appear on the printed version of the leaflet

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Source: Medicines and Healthcare Products Regulatory Agency

Disclaimer: Every effort has been made to ensure that the information provided here is accurate, up-to-date and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. This information has been compiled for use by healthcare practitioners and consumers in the United States. The absence of a warning for a given drug or combination thereof in no way should be construed to indicate that the drug or combination is safe, effective or appropriate for any given patient. If you have questions about the substances you are taking, check with your doctor, nurse or pharmacist.

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