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BOSENTAN ZENTIVA 62.5 MG FILM-COATED TABLETS

Active substance(s): BOSENTAN MONOHYDRATE / BOSENTAN MONOHYDRATE / BOSENTAN MONOHYDRATE

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FILM TAB.ORT.TRF.(GB)

PM TYPE:
ARTWORK VERSION:
ARTWORK CREATION DATE:
ARTWORK REVISION DATE:
REASON OF REVISION:

LEAFLET
02
07.04.2017
10.04.2017

PLANT NAME:
ARTWORK BY:

LULEBURGAZ
AK

TECHNICAL INFORMATION

GENERAL INFORMATION

PRODUCT NAME: BOSENTAN

FORMAT (size):

PM CODE: 11030014685

OLD PM CODE: 11030014438

148 x 500 ± 0.5 mm

NUMBER OF COLORS:

1

Black
LEATUS (optical code/pharma code):

(475)

TECHNICAL DRAWING NUMBER:

B10075

MINIMAL SIZE OF TEXT:

9 pt

FONTS:

Helvetica Neue

PACKAGE LEAFLET: INFORMATION FOR THE USER

Bosentan 62.5 mg film-coated tablets
Bosentan 125 mg film-coated tablets
bosentan
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
The name of your medicine is Bosentan 62.5 mg film-coated
tablets or Bosentan 125 mg film-coated tablets (called bosentan
throughout this leaflet). 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).
• if you have liver problems (ask your doctor).
• if you 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”.

Children and adolescents
Bosentan is not recommended in paediatric patients with
systemic sclerosis and ongoing digital ulcer disease. Please see
If any of these apply to you, tell your doctor.
also section 3. How to take Bosentan.
Other medicines and bosentan
Warnings and precautions
Tell your doctor or pharmacist if you are taking, have recently
Tests your doctor will do before treatment
taken or might take any other medicines, including medicines
• a blood test to check your liver function.
obtained without a prescription. It is especially important to tell
• a blood test to check for anaemia (low haemoglobin).
• a pregnancy test if you are a woman of child-bearing potential. your doctor if you are taking:
− Cyclosporin A (a medicine used after transplants and to treat
Some patients taking bosentan have been found to have
psoriasis), which must not be used together with bosentan
abnormal liver function tests and anaemia (low haemoglobin).
− Sirolimus or tacrolimus, which are medicines used after
transplants, as these are not recommended to be used
Tests your doctor will do during treatment
together with bosentan
During treatment with bosentan, your doctor will arrange for
− Glibenclamide (a diabetes medicine), rifampicin (a tuberculosis
regular blood tests to check for changes in your liver function
medicine), fluconazole or ketoconazole (medicines against
and haemoglobin level.
fungal infections), nevirapine (an HIV medicine) as these
medicines are not recommended to be used together with
For all these tests please refer also to the Patient Alert Card
bosentan
(inside your pack of bosentan tablets). It is important that you
− Other medicines for the treatment of HIV infection such as
have these regular blood tests as long as you are taking
lopinavir and ritonavir, which may require special monitoring if
bosentan. We suggest you write the date of your most recent test
used together with bosentan
and also of your next test (ask your doctor for the date) on the
− Hormonal contraceptives, which are not effective as the sole
Patient Alert Card, to help you remember when your next test is
method of contraception when you take bosentan. Inside your
due.
pack of bosentan tablets you will find a Patient Alert Card
Blood tests for liver function
which you should read carefully. Your doctor and/or
gynaecologist will establish the contraception which is
These will be done every month for the duration of treatment with
appropriate for you.
bosentan. After an increase in dose an additional test will be
− Warfarin (a medicine used to prevent blood clotting), which
done after 2 weeks.
requires more frequent monitoring if used together with
Blood tests for anaemia
bosentan
These will be done every month for the first 4 months of
− Sildenafil (a medicine used to treat erectile dysfunction and
treatment, then every 3 months after that, as patients taking
pulmonary arterial hypertension), which requires caution when
bosentan may get anaemia.
used with bosentan
If these results are abnormal, your doctor may decide to reduce
− Simvastatin (a medicine used to decrease elevated lipid levels
your dose or stop treatment with bosentan and to perform further
in blood), which may require monitoring of cholesterol levels
and a dose adjustment if it’s necessary.
tests to investigate the cause.
• if you are taking cyclosporin A (a medicine used after a
transplant or to treat psoriasis).

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.
Bosentan with food and drink
Bosentan can be taken with or without food.
Pregnancy, breast-feeding and fertility
If you are pregnant or breast-feeding, think you may be pregnant
or are planning to have a baby, ask your doctor or pharmacist for
advice before taking bosentan.
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 this.
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.

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.

• Hypersensitivity reactions (including skin inflammation, itching
and rash).
• Gastrooesophageal reflux disease (acid reflux).
• Diarrhoea.
• Syncope (fainting).
• Palpitations (fast or irregular heartbeats).
• Low blood pressure.
• Nasal congestion.

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.

Rare (may affect up to 1 in 1,000 people):
• Angioedema (swelling, most commonly around the eyes, lips,
tongue or throat).
• Cirrhosis (scarring) of the liver.

If you have any further questions on the use of this medicine, ask
your doctor or pharmacist

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.

4. POSSIBLE SIDE EFFECTS

Other side effects:

Like all medicines, this medicine can cause side effects, although
not everybody gets them.

Very common (may affect more than 1 in 10 people)
• Headache.
• Oedema (swelling of the legs and ankles or other signs of fluid
The most serious side effects with bosentan are:
retention).
• Abnormal liver function which may affect more than 1 in 10 people.
• Allergic (hypersensitivity) reaction with signs such as itching,
Common (may affect up to 1 in 10 people):
rash or swelling of the hands, feet, ankles, face, lips or throat
• Flushed appearance or redness of skin.

Uncommon (may affect up to 1 in 100 people):
• 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).

Blurred vision have also been reported at an unknown frequency
(frequency cannot be estimated from the available data).
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.

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 film-coated tablets contain
The active substance is bosentan.
Each 62.5 mg tablet contains 62.5 mg of bosentan (as monohydrate).
Each 125 mg tablet contains 125 mg of bosentan (as monohydrate).
The other ingredients are maize starch, povidone (K-30), sodium
starch glycolate (type B), pregelatinized maize starch, glycerol
dibehenate, magnesium stearate, opadry II 85F230061 orange (a
mixture consisting of polyvinyl alcohol, titanium dioxide,
macrogol 3350, talc , iron oxide yellow (E 172) and iron oxide red
(E 172)).
What Bosentan film-coated tablets look like and contents of
the pack
Bosentan 62.5 mg film-coated tablets are round,
biconvex-shaped, light orange coloured film-coated tablets with
the diameter approx. 6.1 mm.
Bosentan 125 mg film-coated tablets are oval,
biconvex-shaped, light orange coloured film-coated tablets with
length approx. 11.1 mm and width approx. 5.1 mm.
Size of packing: 14, 56 and 112 film-coated tablets.
Not all pack sizes may be marketed.
Marketing Authorisation Holder and Manufacturer

By reporting side effects you can help provide more information
on the safety of this medicine.

Marketing Authorisation Holder
Zentiva, One Onslow Street, Guildford, Surrey, GU1 4YS, UK.

5. HOW TO STORE BOSENTAN

Manufacturer
Zentiva, k.s., U kabelovny 130, Dolni Mecholupy,
102 37 Prague, Czech Republic

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 package. The expiry date refers to the last day of that month.

This leaflet was last updated in April 2017

148x500
475

Children and adolescents
The dose recommendation in children is only for PAH. For
children 1 year and older, treatment with bosentan is usually

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.

which may cause difficulty in swallowing or breathing. May
affect up to 1 in 10 people.
• Anaemia (low blood value) with signs as pale skin and
weakness or breathlessness which may affect up to 1 in 10
people. Anaemia may occasionally require blood transfusion.
• Changes in blood cells (platelets and white blood cells) with
signs of infection, unexplained bruising or bleeding which may
affect up to 1 in 100 people.
• Anaphylaxis (serious allergic reaction) which causes difficulty in
breathing or dizziness may affect up to 1 in 1,000 people.
• Serious disturbances of liver function which may affect up to
1 in 1,000 people.

11030014685

Recommended dose
Adult
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.

started with 2 mg per kg bodyweight twice daily (morning and
evening). Your doctor will advise you on your dosing.
Bosentan should not be administered to children with a body
weight below 31 kg, and an alternative product containing
bosentan should be used.

Expand Transcript

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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