SUMMARY CMI

Dostinex^®

Consumer Medicine Information (CMI) summary

The full CMI on the next page has more details. If you are worried about using this medicine, speak to your doctor or pharmacist.

1. Why am I using Dostinex?

Dostinex contains the active ingredient cabergoline. Dostinex may be needed if your levels of a hormone known as prolactin are abnormally high (hyperprolactinaemia). Dostinex can also be prescribed to prevent the production of milk in women after birth. For more information, see Section 1. Why am I using Dostinex? in the full CMI.

2. What should I know before I use Dostinex?

Before starting treatment your doctor will need to do some tests to detect any underlying heart, lung or kidney disease. Do not take if you have or have had any scarring or thickening of the lungs with shortness of breath; heart valve disorder; any swelling or inflammation around the heart or lungs; or any abnormal formation of tissue outside the stomach wall.

Do not take if you have an allergy to any medicine containing cabergoline, ergot alkaloids or any of the ingredients listed. For more information, see Section 2. What should I know before I use Dostinex? in the full CMI.

3. What if I am taking other medicines?

Some medicines may interfere with cabergoline and affect how it works. A list of these medicines is in Section 3. What if I am taking other medicines? in the full CMI.

4. How do I use Dostinex?

To treat hyperprolactinaemia the recommended starting dose is half a tablet taken twice a week. Your doctor will generally start you on a low dose and may gradually increase your dose.

To prevent the production of breast milk, the recommended dose is two tablets taken as a single dose, on the first day after delivery of your baby. More instructions can be found in Section 4. How do I use Dostinex? in the full CMI.

5. What should I know while using Dostinex?

For more information, see Section 5. What should I know while using Dostinex? in the full CMI.

6. Are there any side effects?

Some common side effects include dizziness, fainting, headache, nausea or vomiting, unusual sleepiness, abdominal pain or heartburn or pain in the stomach, constipation, nosebleed, weakness or tiredness, temporary impairment of vision, breast pain, hot flushes, rash or hair loss. For more serious side effects and further information, including what to do if you have any side effects, see Section 6. Are there any side effects? in the full CMI.

FULL CMI

Dostinex^® (doss-tee-nex)

Active ingredient(s): cabergoline (ca-ber-go-lean)

Consumer Medicine Information (CMI)

This leaflet provides important information about using Dostinex. You should also speak to your doctor or pharmacist if you would like further information or if you have any concerns or questions about using Dostinex.

Where to find information in this leaflet:

1. Why am I using Dostinex?
2. What should I know before I use Dostinex?
3. What if I am taking other medicines?
4. How do I use Dostinex?
5. What should I know while using Dostinex?
6. Are there any side effects?
7. Product details

1. Why am I using Dostinex?

Dostinex contains the active ingredient cabergoline.

Dostinex may be prescribed by your doctor to reduce your body's level of a hormone known as prolactin. Dostinex may be needed if your levels of prolactin are abnormally high (hyperprolactinaemia).

Abnormally high prolactin may cause menstrual changes in women, impotence in men and breast changes in both sexes.

Dostinex can also be prescribed to prevent the production of milk in women after birth, if breast-feeding is to be prevented for medical reasons.

2. What should I know before I use Dostinex?

Warnings

Before starting treatment with Dostinex, your doctor will need to do some tests to detect any underlying heart, lung or kidney disease.

These tests include chest x-rays, physical examinations, blood tests and heart monitoring.

Your doctor will repeat these tests regularly if you are taking Dostinex for a long period of time.

While you are taking Dostinex report anything unusual to your doctor such as difficulty in breathing, chest pain, swelling of your hands or feet, or anything else that is making you feel unwell.

Do not take Dostinex if you have or have had:

• any scarring or thickening of the lungs with shortness of breath
• heart valve disorder
• any swelling or inflammation around the heart or lungs
• any abnormal formation of tissue outside the stomach wall.
• an allergy to any medicine containing cabergoline, ergot alkaloids (medicines used to treat migraine) or any of the ingredients listed at the end of this leaflet.
  Some of the symptoms of an allergic reaction may include:
  - shortness of breath
  - wheezing or difficulty breathing
  - swelling of the face, lips, tongue or other parts of the body
  - rash, itching or hives on the skin.

Do not give this medicine to a child under the age of 16 years.

The safety and effectiveness in children have not been established.

Check with your doctor if you:

• have or have had any of the following medical conditions:
  - kidney, heart or liver problems
  - lung disease or problems with your breathing
  - Raynaud's syndrome (associated with extreme numbness, tingling and colour changes in the fingers due to cold)
  - ulcer or bleeding in the stomach or intestines
  - low blood pressure
  - high blood pressure after childbirth
  - history of severe mental illness.
• take any medicines for any other condition.

During treatment, you may be at risk of developing certain side effects. It is important you understand these risks and how to monitor for them. See additional information under Section 6. Are there any side effects?

Pregnancy and breastfeeding

Tell your doctor if you are pregnant or plan to become pregnant.

Your doctor will discuss with you the risks and benefits involved.

It is recommended that women who plan to become pregnant stop taking Dostinex at least one month before becoming pregnant.

Tell your doctor if you are breastfeeding or plan to breastfeed.

This medicine prevents the flow of breast milk.

3. What if I am taking other medicines?

Tell your doctor or pharmacist if you are taking any other medicines, including any medicines, vitamins or supplements that you buy without a prescription from your pharmacy, supermarket or health food shop.

Some medicines may be affected by Dostinex or may affect how well it works. You may need different amounts of your medicines, or you may need to take different medicines. Your doctor will advise you.

Tell your doctor or pharmacist if you are taking any of the following:

• medicines used to treat mental illness e.g. antipsychotic medicines for schizophrenia
• medicines used to treat high blood pressure
• ergot alkaloids, medicines used to treat migraine
• medicines used to prevent nausea and vomiting (e.g. metoclopramide)
• medicines called macrolide antibiotics which are used to treat bacterial infections (e.g. erythromycin).

Check with your doctor or pharmacist if you are not sure about what medicines, vitamins or supplements you are taking and if these affect Dostinex.

4. How do I use Dostinex?

How much to take

To treat high levels of prolactin (hyperprolactinaemia), the recommended starting dose is half a tablet taken twice a week. Your doctor will generally start you on a low dose and may gradually increase your dose.

To prevent the production of breast milk, the recommended dose is two tablets taken as a single dose, on the first day after delivery of your baby.

Follow all instructions from your doctor and pharmacist carefully.

How to take it

Swallow Dostinex tablets with a glass of water.

When to take Dostinex

Take your medicine with food or a meal.

Taking it with food will lessen any side effects you may experience.

Take your medicine at about the same time each day.

Taking it at the same time each day will have the best effect. It will also help you remember when to take it.

If you are not sure of how to take Dostinex, ask your doctor or pharmacist.

How long to take it

Continue taking your medicine for as long as your doctor tells you.

This medicine helps to control your condition, but does not cure it. It is important to keep taking your medicine even if you feel well.

If you forget to take it

If it is almost time for your next dose, skip the dose you missed and take your next dose when you are meant to.

Otherwise, take it as soon as you remember, then go back to taking your medicine as you normally would.

Do not take a double dose to make up for the dose that you missed.

This may increase the chance of you getting an unwanted side effect.

If you are not sure what to do, ask your doctor or pharmacist.

If you have trouble remembering to take your medicine, ask your pharmacist for some hints.

If you take too much Dostinex

If you think that you have taken too much Dostinex, you may need urgent medical attention.

You should immediately:

• phone the Poisons Information Centre
  (by calling 13 11 26), or
• contact your doctor, or
• go to the Emergency Department at your nearest hospital.

You should do this even if there are no signs of discomfort or poisoning.

Symptoms of an overdose may include:

• nausea
• vomiting
• stomach pains
• dizziness.

Have the Dostinex bottle or box or this leaflet available to give details if needed.

5. What should I know while using Dostinex?

Things you should do

Follow your doctor's requests for tests and report anything unusual to your doctor such as difficulty in breathing, chest pain or swelling of your hands or feet.

Tell your doctor as soon as possible if you notice an increase in your blood pressure, or you experience severe headache that is getting progressively worse (with or without changes in vision); you may need medical attention.

Call your doctor right away or go straight to the Emergency Department at your nearest hospital if you experience seizures, sudden chest pain that does not go away with rest, or stroke symptoms (including trouble walking, speaking and understanding, as well as numbness of the face, arm or leg on one side of the body).

Keep all of your doctor's appointments so that your progress can be checked.

It is important that your doctor carries out some regular tests if you are taking Dostinex for a long period of time to make sure the medicine is working and to prevent unwanted side effects. These tests may include chest x-rays, physical examinations, blood tests and heart monitoring.

If you are about to be started on any new medicine, remind your doctor and pharmacist that you are taking Dostinex.

Tell any other doctors, dentists, and pharmacists who treat you that you are taking this medicine.

Use barrier methods of contraception, such as condoms, to prevent pregnancy during and for at least one month after taking Dostinex.

Your doctor may recommend routine pregnancy tests during long periods of treatment.

Stop taking Dostinex immediately if you become pregnant and consult your doctor.

Things you should not do

Do not use Dostinex to treat any other complaints unless your doctor tells you to.

Do not stop taking your medicine until your doctor tells you to, even if you are feeling better.

Do not give Dostinex to anyone else, even if they have the same condition as you.

Things to be careful of

If you feel light-headed, dizzy or faint when getting out of bed or standing up, get up slowly.

See your doctor if you notice changes in your behaviour that result in a strong desire to either gamble, shop, eat or use medicines to excess, or you notice an increase in your sex drive.

Such compulsive behaviours have been seen with this class of medicines, including cabergoline.

Driving or using machines

Be careful before you drive or use any machines or tools until you know how Dostinex affects you.

Dostinex may cause dizziness or affect your ability to respond quickly.

If you feel sleepy while taking Dostinex, do not drive or operate machinery.

Looking after your medicine

Follow the instructions on the carton on how to take care of your medicine properly.

Keep Dostinex in its container until it is time to take it.

If you take the tablets out of the bottle they may not keep well.

Keep Dostinex in a cool dry place, where the temperature stays below 25°C.

Store it in a cool dry place away from moisture, heat or sunlight; for example, do not store it:

• in the bathroom or near a sink, or
• in the car or on window sills.

Keep Dostinex where young children cannot reach it.

Do not use this medicine after the expiry date.

Getting rid of any unwanted medicine

If you no longer need to use this medicine or it is out of date, take it to any pharmacy for safe disposal.

6. Are there any side effects?

All medicines can have side effects. If you do experience any side effects, most of them are minor and temporary. However, some side effects may need medical attention.

See the information below and, if you need to, ask your doctor or pharmacist if you have any further questions about side effects.

Common side effects

Serious side effects

Very serious side effects

Tell your doctor or pharmacist if you notice anything else that may be making you feel unwell.

Other side effects not listed here may occur in some people.

Some of these side effects (e.g. changes in liver function) can only be found when your doctor does tests from time to time to check your progress.

Reporting side effects

After you have received medical advice for any side effects you experience, you can report side effects to the Therapeutic Goods Administration online at www.tga.gov.au/reporting-problems. By reporting side effects, you can help provide more information on the safety of this medicine.

Always make sure you speak to your doctor or pharmacist before you decide to stop taking any of your medicines.

7. Product details

This medicine is only available with a doctor's prescription.

What Dostinex contains

Do not take this medicine if you are allergic to any of these ingredients.

What Dostinex looks like

Dostinex comes as capsule-shaped, flat, white tablets. One side is marked with the letter 'P' on a side of the score and the letter 'U' on the other. The other side of the tablet is marked '700' with a short score on the top and bottom of the tablet surface.
AUST R 52158

Dostinex is available in bottles of 2 and 8 tablets.

Who distributes Dostinex

Pfizer Australia Pty Ltd
Sydney NSW
Toll Free Number: 1800 675 229
www.pfizermedicalinformation.com.au

This leaflet was prepared in March 2023.

^® Registered Trademark

© Pfizer Australia Pty Ltd 2023

Published by MIMS May 2023

1 Name of Medicine

Cabergoline.

2 Qualitative and Quantitative Composition

Dostinex (cabergoline) is a dopaminergic ergoline derivative, which has a potent and long lasting prolactin (PRL)-lowering activity.
Each Dostinex tablet for oral administration contains 500 microgram cabergoline.

Excipient(s) with known effect.

3 Pharmaceutical Form

Dostinex tablets are white flat capsule shaped, with the letter 'P' on a side of a score and the letter 'U' on the other side. On the other surface the number '700' with a short score in the middle of the upper and lower extremity of the tablet surface.

4 Clinical Particulars

4.1 Therapeutic Indications

Inhibition of physiological lactation.

Treatment of hyperprolactinemic disorders.

4.2 Dose and Method of Administration

Dosage.

For the prevention of onset of physiological lactation in the puerperium.

For treatment of pathological hyperprolactinaemia.

Method of administration.

4.3 Contraindications

Hypersensitivity to cabergoline, other ergot alkaloids, or to any of the excipients.
History of pulmonary, pericardial and retroperitoneal fibrotic disorders.
Anatomical evidence of cardiac valvulopathy of any valve as determined by pre-treatment (e.g. echocardiogram showing valve leaflet thickening, valve restriction, valve mixed restriction-stenosis).

4.4 Special Warnings and Precautions for Use

General.

Renal and hepatic disease.

Fibrosis and cardiac valvulopathy.

Before initiating long-term treatment.

During long-term treatment.

Inhibition/suppression of physiological lactation.

Postural hypotension.

Treatment of hyperprolactinaemic disorders.

Somnolence/sudden sleep onset.

Psychiatric.

Use in the elderly.

Paediatric use.

Effects on laboratory tests.

4.5 Interactions with Other Medicines and Other Forms of Interactions

The concomitant use of other drugs during early puerperium, particularly of methylergometrine maleate, has not been associated with detectable interactions modifying the efficacy and safety of Dostinex.
Although there is no conclusive evidence of an interaction between Dostinex and other ergot alkaloids, the concomitant use of these medications during long-term therapy with Dostinex is not recommended.
Since Dostinex exerts its therapeutic effect by direct stimulation of dopamine receptors, it should not be concurrently administered with drugs which have dopamine antagonist activity (such as phenothiazines, butyrophenones, thioxanthenes, metoclopramide) since these might reduce the PRL-lowering effect of Dostinex.
Mono-oxygenase activity was increased 1.5 to 3-fold in female rats treated with cabergoline 100 microgram/kg/day to 1.5 mg/kg/day orally. Concomitant administration of cabergoline with drugs metabolised by mono-oxygenases may result in altered exposure and activity.
Dostinex should not be used with macrolide antibiotics (e.g. erythromycin) due to increased systemic bioavailability of cabergoline.

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

4.7 Effects on Ability to Drive and Use Machines

See Section 4.4 Special Warnings and Precautions for Use.

4.8 Adverse Effects (Undesirable Effects)

Side effects are generally dose related. In patients known to be intolerant of dopaminergic drugs, side effects may be lessened by starting Dostinex therapy with reduced doses (e.g. 250 microgram once a week) with subsequent gradual increase until the therapeutic range is reached. In case of persistent or severe adverse events, temporary reduction of dosage followed by a more gradual increase (e.g. in steps of 250 microgram per week fortnightly) may result in reversal of side effects once they have occurred.
In women treated for inhibition of physiological lactation, the most frequently occurring adverse events are asymptomatic decreases in blood pressure, dizziness/vertigo, headache, nausea, somnolence and abdominal pain. In addition, on rare occasions, palpitations, epigastric pain, epistaxis, transient hemianopia, vomiting, syncope, asthenia, and hot flushes have been reported.
Most side effects are transient and mild to moderate in severity.
In patients treated for hyperprolactinaemia, the most common symptoms in decreasing rank of frequency are nausea, headache, dizziness/vertigo, abdominal pain/dyspepsia/gastritis, asthenia/fatigue, constipation, vomiting, breast pain, hot flushes, depression and paraesthesia.
Dostinex generally exerts a hypotensive effect in patients treated chronically: however, symptomatic hypotension or fainting have been rarely reported. The symptoms are generally mild to moderate in degree, mainly appearing during the first two weeks of therapy, and mostly disappearing despite continued therapy.
Being an ergot derivative, Dostinex may also act in some patients as a vasoconstrictor: digital vasospasm and leg cramps have been occasionally reported.
Discontinuation of Dostinex because of adverse events was required in only approximately 3% of patients. Dostinex withdrawal results in reversal of side effects, usually within a few days after discontinuation.
Alterations in standard laboratory tests are uncommon during long-term therapy with Dostinex. A decrease in haemoglobin values have been observed in amenorrhoeic women during the first few months after menses resumption.
Pleuropulmonary changes (pleural effusions, pneumonitis, pleural and pulmonary fibrosis) have been reported (see Section 4.4 Special Warnings and Precautions for Use).

Postmarketing experience.

Reporting suspected adverse effects.

4.9 Overdose

There is limited experience of overdosage in humans. Symptoms of overdosage would likely be those of over-stimulation of dopamine receptors. These might include nausea, vomiting, gastric complaints, hypotension, nasal congestion, syncope, hallucinations or thought/perceptual disturbances.
Treatment of overdose is symptomatic and supportive. Supportive measures should be directed to maintain blood pressure, if necessary.
Consider administration of activated charcoal in the event of a potentially toxic ingestion. Activated charcoal is most effective when administered within 1 hour of ingestion. In patients who are not fully conscious or have impaired gag reflex, consideration should be given to administering activated charcoal via nasogastric tube once the airway is protected.
In addition, in case of pronounced central nervous system effects, the administration of dopamine antagonist drugs may be advisable.
For information on the management of overdose, contact the Poison Information Centre on 131126 (Australia).

5 Pharmacological Properties

5.1 Pharmacodynamic Properties

Mechanism of action.

Clinical trials.

5.2 Pharmacokinetic Properties

The pharmacokinetic and metabolic profiles of Dostinex have been studied in healthy volunteers of both sexes and in female hyperprolactinaemic patients.
After oral administration of the labelled compound, radioactivity was rapidly absorbed from the gastrointestinal tract, and the peak of radioactivity in plasma was between 0.5 and 4 hours. Ten days after administration about 18% and 72% of the radioactive dose was recovered in urine and faeces respectively. Unchanged drug in urine accounted for 2-3% of the dose.
In urine, the main metabolite identified was 6-allyl-8β-carboxy-ergoline, which accounted for 4-6% of the dose. Three additional metabolites were identified in urine, which accounted overall for less than 3% of the dose. The metabolites have been found to be much less potent than Dostinex in inhibiting PRL secretion in vitro.
The low urinary excretion of unchanged Dostinex has been confirmed also in studies with non-radioactive product. The elimination half-life of Dostinex, estimated from urinary excretion rates, is long (63-68 hours in healthy volunteers, 79-115 hours in hyperprolactinaemic patients).
On the basis of the elimination half-life, steady state conditions should be achieved after 4 weeks, as confirmed by the mean peak plasma levels of Dostinex obtained after a single 1 mg dose (37 ± 8 picogram/mL) and after a 4 week regimen of 1 mg/week (101 ± 43 picogram/mL).
In vitro experiments showed that the drug, at concentrations of 100 microgram/mL to 10 mg/mL, is 41-42% bound to plasma proteins.
In limited studies, food did not appear to have an effect on the absorption of Dostinex.
In rats, Dostinex and/or its metabolites are excreted in milk; no information on its excretion in maternal milk in humans is available.

5.3 Preclinical Safety Data

Genotoxicity.

Carcinogenicity.

6 Pharmaceutical Particulars

6.1 List of Excipients

Lactose, leucine.

6.2 Incompatibilities

Incompatibilities were either not assessed or not identified as part of the registration of this medicine.

6.3 Shelf Life

In Australia, information on the shelf life can be found on the public summary of the Australian Register of Therapeutic Goods (ARTG). The expiry date can be found on the packaging.

6.4 Special Precautions for Storage

Store below 25°C.

6.5 Nature and Contents of Container

Dostinex is supplied as 500 microgram tablets in bottles of 2 or 8 tablets.

6.6 Special Precautions for Disposal

In Australia, any unused medicine or waste material should be disposed of by taking to your local pharmacy.

6.7 Physicochemical Properties

Chemical structure.

CAS number.

7 Medicine Schedule (Poisons Standard)

Prescription Only Medicine (S4).

Summary Table of Changes