Consumer medicine information

Tracleer 62.5 mg Tablets

Bosentan

BRAND INFORMATION

Brand name

Tracleer

Active ingredient

Bosentan

Schedule

S4

 

Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using Tracleer 62.5 mg Tablets.

What is in this leaflet


This leaflet answers some common questions about Tracleer.
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 Tracleer is used for


Tracleer (TRAK-leer) 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 Tracleer 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 Tracleer

When you must not take Tracleer


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.
  • breastfeeding:
    Tell your doctor immediately if you are breastfeeding. You are advised to stop breastfeeding if this medicine is prescribed for you because it has been reported that this drug passes into the milk in a woman who was taking this medicine.

• being treated with cyclosporine A (a medicine used after a transplant or to treat psoriasis)
• being treated with glibenclamide (a medicine used for diabetes)
Do not take Tracleer if you are allergic to it or any of the ingredients listed at the end of this leaflet.
Do not take Tracleer if you have moderate to severe liver disorder.
Do not take it after the expiry date (EXP) printed on the pack.
If you take it after the expiry date has passed, it may not work as well.
Do not take it if the packaging is torn or shows signs of tampering.

Before you start to take Tracleer


Tracleer may harm sperm. All men should use effective birth control while taking this medicine and for 3 months after they stop taking it.
If sexually active, you must use a hormonal and barrier method of contraception.
This medicine may reduce the effectiveness of hormone contraceptives such as the pill and hormone patches, implants or injection. It is important to use other contraceptives, like condoms or an intrauterine device.
Your doctor will advise you about using reliable contraceptives before taking this medicine.
You must have a negative pregnancy test at the time of starting treatment if you are sexually active.
Your doctor will need evidence that you are not pregnant.
Tell your doctor if:
1. you are a woman of childbearing potential and not using reliable contraceptive methods. You must have a negative pregnancy test before beginning treatment. The test should be performed on the second day of a normal menstrual period or 11 days after the last unprotected sexual intercourse, whichever is later. Your doctor will advise you about using reliable contraception before taking or whilst taking this medicine.
Hormonal contraception on its own is not a reliable option because this medicine may make this method ineffective in preventing pregnancy. Hormonal contraceptives include ones you take orally (the pill), patches you put on your skin, ones that are injected and implants. You should ALWAYS use additional methods of contraception such as condoms and IUDs and not rely just on hormonal contraception. You should have a pregnancy test every month while you are taking this medicine. You must stop taking this medicine for at least 3 months prior to becoming pregnant.
2. you are breastfeeding or planning to breastfeed.
It is not known whether Tracleer passes into breast milk.
3. you have allergies to:
• any other medicines
• any other substances such as foods, preservatives or dyes.
4. you have or have had any medical conditions, especially the following:
• pulmonary arterial hypertension or lung disease/ condition
• anaemia
• hypotension
• liver or renal disorders
• heart failure or disease
• HIV infection
If you have not told your doctor about any of the above, tell them before you use Tracleer.

While taking Tracleer


Do not become pregnant while taking this medicine. You must have a pregnancy test every month while you are taking this medicine.
If there is any delay in getting period or any other reason to suspect pregnancy, you must tell your doctor immediately for pregnancy testing. Tracleer may harm unborn babies.
Your doctor will need evidence that you are not pregnant before prescribing this medicine again.
Your doctor may arrange for regular blood tests to check for changes in your liver function and haemoglobin level.

Interactions with other medicines


Tell your doctor if you are taking any other medicines including any that you buy without a prescription from your pharmacy, supermarket or health food shop.
Some medicines may interfere with Tracleer. These include:
  • hormonal contraceptives (oral, injectable, transdermal and implantable)
  • simvastatin, medicines for lowering blood fats
  • medicines for diabetes such as glibenclamide and tolbutamide
  • medicines for fungal infections such as ketoconazole, itraconazole, fluconazole and voriconazole
  • medicines for bacterial infections such as rifampicin
  • medicine to prevent organ transplantation rejection such as cyclosporine A, tacrolimus and sirolimus
  • medicines for rheumatoid arthritis or psoriasis / dermatitis
  • lopinavir+ritonavir or other ritonavir-boosted protease inhibitors and nevirapine (used to treat HIV);
  • warfarin (used as anti-clotting medicines)
  • digoxin (used to treat heart rhythm disorders)
  • sildenafil or tadalafil (used to treat erectile dysfunction and/or pulmonary arterial hypertension)
  • phenytoin, carbamazepine or phenobarbital (medicines for seizures)
  • nimodipine
  • St John's Wort

These medicines may be affected by Tracleer or may affect how well it works. You may need to use different amounts of your medicines, or take different medicines.
Your doctor will advise you.
Your doctor or pharmacist has more information on medicines to be careful with or to avoid while taking Tracleer.

How to take Tracleer

How much to take


Always take this medicine exactly as your doctor has instructed you.
You should check with your doctor or pharmacist if you are unsure.
Adults
The usual dose is one tablet, twice daily. For the first 4 weeks you will take a 62.5 mg tablet twice daily.
Depending on how you respond to the medicine, your doctor may increase the dosage after four weeks to a 125 mg tablet twice daily.
Patients with low body weight
If you have body weight less than 40 kg but are over 12 years old, your doctor may advise you take a 62.5 mg tablet twice daily.
Children aged 3 years and over
The dose will be determined by your doctor depending on the weight of the child.
If you do not think the medicine is working or you think it is working too well, talk to your doctor. Your doctor may need to change the dose you are taking.

How to take this medicine


Tracleer is taken by mouth, in the morning and evening, and can be taken with or without food.

How long to take it


Do not stop taking this medicine unless your doctor tells you to.
Stopping your treatment may lead to a worsening of your symptoms. Your doctor may tell you to reduce the dose over a few days before stopping completely.

If you forget to take it


If it is almost time for your next dose, skip the dose you missed and take the next dose when you are meant to.
Do not take a double dose to make up for the dose you have missed.
This may increase the chance of getting an unwanted side effect.
If there is still a long time to go before your next dose, take it as soon as you remember and then go back to taking it as you would normally.
If you are not sure what to do, ask your doctor or pharmacist.
If you have trouble remembering when to take your medicine, ask your pharmacist for hints.

If you take too much (overdose)


Immediately telephone your doctor or the Poisons Information Centre or go to Accident and Emergency at your nearest hospital if you think you or anyone else may have taken too much Tracleer.
Do this even if there are no signs of discomfort or poisoning.
Poison Information Centre telephone numbers:
  • Australia: 13 11 26
  • New Zealand: 0800 POISON or 0800 764 766

You may need urgent medical attention.

While you are using Tracleer

Things you must do


It is very important that you have a liver function blood test before you start treatment and every month after that.
Tracleer can cause liver damage if it is not found early. Because this side effect may not cause symptoms at first, only a blood test can show that you have early liver damage. Regular blood tests let your doctor change or stop your therapy before there is permanent damage.
You should have a blood test for anaemia after 1 and 3 months, and then every 3 months for the rest of your treatment.
You need to have pregnancy tests monthly if you are a female of childbearing age

Things you must not do


Do not give the tablets to anyone else even if they have the same symptoms as you.

Things to be careful of


If you feel dizzy or that your vision is blurred whilst taking this medicine, do not drive or operate any tools or machinery.

Side Effects


Tell your doctor immediately or go to Accident and Emergency at your nearest hospital if you notice any of the following:

  • shortness of breath or difficulty in breathing
  • anaphylaxis and/ or swelling, most commonly around the eyes, lips, tongue or throat
  • nausea
  • vomiting
  • fever
  • unusual tiredness
  • stomach pain
  • yellowing of your skin or the whites of your eyes (jaundice)
  • dark-coloured urine
  • chest pain

These may be serious side effects of Tracleer. You may need urgent medical attention.
Serious side effects are uncommon.
Other side effects of this medicine include:
  • headache
  • respiratory tract infection
  • dizziness or fainting
  • anaemia
  • abnormal liver function test or liver disorders
  • inflamed throat and irritated nasal passages
  • flushing (hot flashes)
  • swelling of ankle, leg and joint or other signs of fluid retention
  • joint pain
  • low blood pressure
  • blood disorders
  • fast heart beat
  • tiredness
  • hypersensitivity reactions including itching, rash and skin inflammation
  • blocked or runny nose
  • heartburn or acid reflux
  • diarrhoea
  • redness of the skin
  • blurred vision
  • nosebleed
  • body ache and pain
  • worsening of existing lung disease

See your doctor if any of these worry you.
Tell your doctor if you notice anything else that is making you feel unwell.
Other side effects not listed above may occur in some consumers.
Do not be alarmed by this list of possible side effects.
You may not experience any of them.

After using Tracleer

Storage


Store this medicine in the original bottle, in a cool, dry place where the temperature stays below 25°C.
Keep out of reach of children.

Disposal


Medicines should not be disposed of in wastewater or household waste.
Ask your pharmacist how to dispose of medicines you no longer require. These measures will help to protect the environment.

Product description

What it looks like


Tracleer 62.5 mg tablets are orange-white, round tablets, embossed with "62.5" on one side.
Tracleer 125 mg tablets are orange-white, oval tablets, embossed with "125" on one side.

Pack size


Bottles of 60 tablets.

Ingredients


Active ingredient:
Tracleer 62.5 mg: 62.5 mg bosentan (as monohydrate) per tablet.
Tracleer 125 mg: 125 mg bosentan (as monohydrate) per tablet.
Inactive ingredients:
  • 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.

Sponsor


JANSSEN-CILAG Pty Ltd
1-5 Khartoum Road
Macquarie Park NSW 2113 Australia
Telephone: 1800 226 334
NZ Office: Auckland New Zealand
Telephone: 0800 800 806
This leaflet was prepared in January 2024.
Australian Register Number:
Tracleer 62.5 mg - AUST R 91919
Tracleer 125 mg - AUST R 91920

BRAND INFORMATION

Brand name

Tracleer

Active ingredient

Bosentan

Schedule

S4

 

Boxed Warnings

Causes birth defects and is contraindicated in pregnancy. See Section 4.3 Contraindications; Section 4.4 Special Warnings and Precautions for Use.
Rare cases of hepatic cirrhosis and hepatic failure have been reported in patients using Tracleer. See Section 4.4 Special Warnings and Precautions for Use.

1 Name of Medicine

Tracleer (bosentan).

2 Qualitative and Quantitative Composition

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.
See Section 6.1 List of Excipients.

3 Pharmaceutical Form

Tracleer 62.5 mg film-coated, round, biconvex, orange-white tablets, embossed with identification marking '62.5'.
Tracleer 125 mg film-coated, oval, biconvex, orange-white tablets, embossed with identification marking '125'.

4 Clinical Particulars

4.9 Overdose

Bosentan has been given as a single dose of up to 2,400 mg in normal volunteers, or up to 2,000 mg/day for 2 months in patients, without any major clinical consequences. The most common side effect was headache of mild to moderate intensity. In the cyclosporine A interaction study, in which doses of 500 mg and 1000 mg twice daily of bosentan were given concomitantly with cyclosporine A, trough plasma concentrations of bosentan increased 30-fold, resulting in severe headache, nausea and vomiting, but not serious adverse events. Mild decreases in blood pressure and increases in heart rate were observed.
Massive overdosage may result in pronounced hypotension requiring active cardiovascular support. In the postmarketing period there was one reported overdose of 10,000 mg of bosentan taken by an adolescent male patient. He had symptoms of nausea, vomiting, hypotension, dizziness, sweating and blurred vision. He recovered completely within 24 hours with blood pressure support.
Note. Bosentan is not removed through dialysis.
For information on the management of overdose, contact the Poison Information Centre on 131126 (Australia).

5 Pharmacological Properties

5.3 Preclinical Safety Data

Genotoxicity. See Section 4.6 Fertility, Pregnancy and Lactation.
Carcinogenicity. Two years of dietary administration of bosentan to mice produced an increased incidence of hepatocellular adenomas and combined adenomas and carcinomas in males at doses as low as 450 mg/kg/day (about 8 times the maximum recommended human dose (MRHD) of 12 mg twice daily on a mg/m2 basis). In the same study, doses greater than 2,000 mg/kg/day (about 32 times the [MRHD]) were associated with an increased incidence of colon adenomas in both males and females. In rats, dietary administration of bosentan for two years was associated with an increased incidence of brain astrocytomas in males at doses as low as 500 mg/kg/day (about 16 times the [MRHD]; no-effect dose of 125 mg/kg/day, about 4 times the MRHD) and females at doses of 3,000 mg/kg/day (no-effect dose of 2,000 mg/kg/day, about 128 times the MRHD). An increased incidence of thyroid follicular adenomas was also observed in male rats at doses as low as 2,000 mg/kg/day (about 32 times the MRHD). However, the relevance of these findings to humans is not known.
There was no evidence for mutagenic or clastogenic activity of bosentan in a standard battery of in vitro tests (the microbial mutagenesis assay, the unscheduled DNA synthesis assay, the V-79 mammalian cell mutagenesis assay, and human lymphocyte assay) and an in vivo mouse micronucleus assay.

6 Pharmaceutical Particulars

6.7 Physicochemical Properties

Active: Bosentan (as monohydrate).
The chemical name of bosentan monohydrate is benzenesulphonamide, 4-(1,1-dimethylethyl)-N-[6(2-hydroxyethoxy)-5-(2-methoxyphenoxy) [2,2'-bipyrimidin]-4-yl]-, monohydrate.
The molecular formula is C27H29N5O6S (anhydrous); C27H29N5O6S.H2O (monohydrate). MW: 551.62 (anhydrous); 569.64 (monohydrate).
Bosentan is the first of a new drug class, an endothelin receptor antagonist.
Tracleer (bosentan) belongs to a class of highly substituted pyrimidine derivatives, with no chiral centres.
Chemical structure.
https://stagingapi.mims.com/au/public/v2/images/fullchemgif/CSBOSENT.gif CAS number. 147536-97-8 (anhydrous substance).

7 Medicine Schedule (Poisons Standard)

Schedule 4 - Prescription Only Medicine.

Summary Table of Changes

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