Dostinex

New Zealand - English - Medsafe (Medicines Safety Authority)

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Active ingredient:
Cabergoline 0.5 mg
Available from:
Pfizer New Zealand Limited
INN (International Name):
Cabergoline 0.5 mg
Dosage:
0.5 mg
Pharmaceutical form:
Tablet
Composition:
Active: Cabergoline 0.5 mg Excipient: Lactose Leucine
Units in package:
Bottle, glass, 2 tablets
Class:
Prescription
Prescription type:
Prescription
Manufactured by:
Olon SpA
Therapeutic indications:
Prevention of the onset of lactation in the puerperium only for clearly defined medical reasons: DOSTINEX is indicated for the inhibition of physiological lactation soon after delivery. 1. After parturition, when breast feeding is contraindicated due to medical reasons related to the mother or the new-born. 2.After stillbirth or abortion.
Product summary:
Package - Contents - Shelf Life: Bottle, glass, amber, with tamper resistant aluminium screw cap - 2 tablets - 24 months from date of manufacture stored at or below 25°C - Bottle, glass, amber, with tamper resistant aluminium screw cap - 8 tablets - 24 months from date of manufacture stored at or below 25°C - Bottle, plastic, HDPE bottle PP child resistant cap (inner cap desiccant) - 2 tablets - 24 months from date of manufacture stored at or below 25°C - Bottle, plastic, HDPE bottle PP child resistant cap (inner cap desiccant) - 8 tablets - 24 months from date of manufacture stored at or below 25°C
Authorization number:
TT50-5317
Authorization date:
1993-03-18

DOSTINEX

DOSTINEX

®

Cabergoline 500 microgram

Consumer Medicine Information

What is in this leaflet

This leaflet answers some common

questions about Dostinex. 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 taking Dostinex

against the expected benefits.

If you have any concerns about

taking this medicine, ask your

doctor or pharmacist.

Keep this leaflet with the medicine.

You may need to read it again.

What Dostinex is used

for

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.

Ask your doctor if you have any

questions about why this medicine

has been prescribed for you.

Your doctor may have prescribed it

for another reason.

Dostinex is available only with a

doctor's prescription.

Before you start to

take Dostinex

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.

When you must not take it

Do not take Dostinex if you have

an allergy to:

any medicine containing

cabergoline

any of the ingredients listed at the

end of this leaflet

ergot alkaloids (medicines used to

treat migraine).

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 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.

Do not take this medicine if you

are pregnant.

It may affect your developing baby if

you take it during pregnancy.

Do not give this medicine to a child

under the age of 16 years.

The safety and effectiveness in

children has not been established.

Do not take this medicine after the

expiry date printed on the pack or

if the packaging is torn or shows

signs of tampering.

If it has expired or is damaged, return

it to your pharmacist for disposal.

If you are not sure whether you

should start taking this medicine,

talk to your doctor.

Before you start to take it

Tell your doctor if you have or

have had any of the following

medical conditions:

kidney, heart and 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

DOSTINEX

low blood pressure

high blood pressure after

childbirth

history of severe mental illness.

Tell your doctor if you are

pregnant or plan to become

pregnant.

Your doctor can 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 breast-

feeding or intend to breastfeed.

This medicine prevents the flow of

breast milk.

If you have not told your doctor or

pharmacist about any of the above,

tell them before you start to take

Dostinex.

Taking other medicines

Tell your doctor if you are taking

any other medicines, including

medicines you buy without a

prescription from a pharmacy,

supermarket or health food shop.

Some medicines and Dostinex may

interfere with each other. These

include:

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).

These medicines may be affected by

Dostinex or may affect how well it

works. You may need different

amounts of your medicine or you

may need to take different medicines.

Your doctor or pharmacist has more

information on medicines to be

careful with or avoid while taking

Dostinex.

How to take Dostinex

Follow all directions given to you

by your doctor or pharmacist

carefully.

The directions given to you by your

doctor or pharmacist on how to take

Dostinex may differ from the

information contained in this leaflet.

You may be given a different dosage

depending on your condition or how

you react to the medicine.

If you do not understand the

instructions on the label, ask your

doctor or pharmacist for help.

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.

How to take it

Swallow Dostinex tablets with a

glass of water.

When to take it

Take your medicine with food or a

meal.

How long to take it

Continue taking Dostinex until

your doctor tells you to stop.

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,

speak to your doctor or

pharmacist.

If you have trouble remembering

to take your medicine, ask your

pharmacist for some hints.

If you take too much

(overdose)

Immediately telephone your doctor

or the Poisons Information Centre

for advice (telephone 0800

POISON or 0800 764 766) or go to

the Accident and Emergency

department (Casualty) at your

nearest hospital if you think you or

anyone else may have taken too

much Dostinex. Do this even if

there are no signs of discomfort or

poisoning.

You may need urgent medical

attention. Keep telephone numbers

for these services handy. Have the

medicine or this leaflet available to

give details if needed.

The symptoms of taking too much

Dostinex may include nausea,

vomiting, stomach pains and

dizziness.

While you are taking

Dostinex

Things you must 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.

Keep all of your doctor's

appointments while taking

DOSTINEX

Dostinex 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 must not do

Do not use Dostinex to treat any

other medical 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.

Be careful driving or operating

machinery 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.

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 medicine,

including cabergoline.

Side effects

Tell your doctor as soon as possible

if you do not feel well while taking

Dostinex, even if you do not think

the problems are connected with

the medicine or they are not listed

in this leaflet.

Like many medicines, Dostinex may

cause side effects. If they occur, they

are likely to be minor and temporary.

However, some may be serious and

need medical attention.

It can be difficult to tell whether side

effects are the result of taking

Dostinex, effects of your condition or

side effects of other medicines you

may be taking. For this reason it is

important to tell your doctor of any

change in your condition.

Do not be alarmed by the following

list of possible side effects.

You may not experience any of them.

Ask your doctor or pharmacist

about any questions you may have.

Tell your doctor if...

Tell your doctor if you notice any

of the following and they worry

you:

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

hair loss.

The side effects listed above are

usually mild and short lived.

Tell your doctor as soon as

possible if...

Tell your doctor as soon as possible

if you notice any of the following:

irregular heart beat

leg cramps or pain in the fingers

or toes

aggressive behaviour

depression, feelings of deep

sadness

changes in behaviour such as

increased sex drive, a compelling

desire to gamble, shop, eat or take

medicines

any breathing problems.

The above list includes serious side

effects, which may require medical

attention.

Go to hospital if...

Tell your doctor immediately or go

to Accident and Emergency at

your nearest hospital, if you notice

any of the following:

chest pain with shortness of

breath

sudden signs of allergy such as

rash, itching or hives, swelling of

the face, lips, tongue or other

parts of the body, shortness of

breath, wheezing or difficulty

breathing.

The above list includes very serious

side effects. You may need urgent

medical attention or hospitalisation.

These side effects are very rare.

Tell your doctor if you notice

anything else that is making you

feel unwell when you are taking, or

soon after you have finished taking

Dostinex.

DOSTINEX

Other side effects not listed above

may also occur in some patients.

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.

After taking Dostinex

Storage

Keep Dostinex in its container until

it is time to take it.

Keep Dostinex in a cool dry place,

where the temperature stays below

25 °C.

Do not store Dostinex, or any

medicines, in a bathroom or near

the sink. Do not leave Dostinex in

the car or on window sills.

Heat and dampness can destroy some

medicines.

Keep Dostinex where children

cannot reach it.

A locked cupboard at least one-and-

a-half metres above the ground is a

good place to store medicines.

Disposal

Ask your pharmacist what to do

with any Dostinex which is left

over, or if the medicine has passed

its expiry date.

Product Description

What it 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.

Dostinex is available in bottles of 2

and 8 tablets.

Ingredients

Active Ingredient

The active ingredient is cabergoline

500 microgram.

Inactive Ingredients

Each tablet also contains: lactose and

leucine.

Supplier

Pfizer New Zealand Limited

PO Box 3998

Auckland

New Zealand

Toll free number: 0800 736 363

This leaflet was revised in July 2020.

© Pfizer Australia Pty Ltd

® Registered Trademark

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NEW ZEALAND DATA SHEET

1.

PRODUCT NAME

DOSTINEX

2.

QUALITATIVE AND QUANTITATIVE COMPOSITION

Each DOSTINEX tablet contains 0.5 mg cabergoline.

Excipient(s) with known effect

Lactose anhydrous

For the full list of excipients, see section 6.1.

3.

PHARMACEUTICAL FORM

Tablet.

Cabergoline 0.5 mg tablets are flat, capsule shaped tablets, 4 x 8 mm, scored, white tablets,

engraved “PU” on one side and “700” on the reverse side.

4.

CLINICAL PARTICULARS

4.1 Therapeutic indications

Prevention of the onset of lactation in the puerperium only for clearly defined medical

reasons:

DOSTINEX is indicated for the inhibition of physiological lactation soon after

delivery.

1. After parturition, when breast feeding is contraindicated due to medical reasons related to

the mother or the new-born.

2. After stillbirth or abortion.

Treatment of hyperprolactinaemic disorders

: DOSTINEX is indicated for the treatment of

dysfunctions associated with hyperprolactinaemia, including amenorrhoea, oligomenorrhoea,

anovulation and galactorrhoea. DOSTINEX is indicated in patients with prolactin-secreting

pituitary adenomas (micro- and macroprolactinomas), idiopathic hyperprolactinaemia, or

empty

sella

syndrome

with

associated

hyperprolactinaemia,

which

represent

basic

underlying pathologies contributing to the above clinical manifestations.

4.2 Dose and method of administration

DOSTINEX is to be administered by the oral route. Since in clinical studies DOSTINEX has

been mainly administered with food since the tolerability of this class of compound is

improved with food, it is recommended that DOSTINEX be preferably taken with meals.

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Inhibition of physiological lactation

: DOSTINEX should be administered during the first day

post-partum. The recommended therapeutic dose is 1 mg (two 0.5 mg tablets) as a single

dose.

Treatment

of

hyperprolactinaemic

disorders

recommended

initial

dosage

DOSTINEX is 0.5 mg per week given in one or two (½ of a 0.5 mg tablet) doses (e.g. on

Monday and Thursday) per week. The weekly dose should be increased gradually preferably

by adding 0.5 mg per week at monthly intervals until the optimal therapeutic response is

achieved. The therapeutic dosage is usually 1 mg per week and ranges from 0.25 to 2 mg per

week. Doses of DOSTINEX up to 4.5 mg per week have been used in hyperprolactinaemic

patients.

The weekly dose may be given as a single administration or divided into two or more doses

per week according to patient tolerability. Division of the weekly dose into multiple

administrations is advised when doses higher than 1 mg per week are to be given since the

tolerability of doses greater than 1 mg given as a single weekly dose has been evaluated in

only a few patients. Patients should be evaluated during dose escalation to determine the

lowest

dosage

that

produces

required

therapeutic

response.

Monitoring

serum

prolactin levels at monthly intervals is advised since; once the effective dosage regimen has

been reached serum prolactin normalisation is usually observed within two to four weeks.

After

DOSTINEX

withdrawal,

recurrence

hyperprolactinaemia

usually

observed.

However persistent suppression of prolactin levels has been observed for several months in

some

patients.

most

women,

ovulatory

cycles

persist

least

months

after

DOSTINEX discontinuation.

Severe hepatic insufficiency

: Lower doses should be considered in patients with severe

hepatic insufficiency who receive prolonged treatment with DOSTINEX. (See section 4.4).

Children

: The safety and efficacy of DOSTINEX has not been established in subjects less

than 16 years of age.

Elderly

: As a consequence of the indications for which DOSTINEX is presently proposed,

the experience in the elderly is very limited. Available data do not indicate a special risk.

4.3 Contraindications

Hypersensitivity to cabergoline, any other component of the product, or any ergot alkaloid.

History of pulmonary, pericardial and retroperitoneal fibrotic disorders. (See section 4.4).

Anatomical evidence of cardiac valvulopathy of any valve as determined by pre-treatment

echocardiogram showing valve leaflet thickening, valve restriction, valve mixed restriction-

stenosis. (See section 4.4).

4.4 Special warnings and precautions for use

General

The safety and efficacy of DOSTINEX have not yet been established in patients with renal

and hepatic disease. Since available data indicate that biliary excretion represents the main

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route of elimination of the drug, it is advisable not to administer the drug to subjects with

severe liver insufficiency.

Lower doses should be considered in patients with severe hepatic insufficiency who receive

prolonged treatment with DOSTINEX. Compared to normal volunteers and those with lesser

degrees of hepatic insufficiency, an increase in AUC has been seen in patients with severe

hepatic insufficiency (Child-Pugh score>10) who received a single 1 mg dose.

As with other ergot derivatives, DOSTINEX should be given with caution to patients with

severe cardiovascular disease, Raynaud's syndrome, liver disease, renal insufficiency, peptic

ulcer or gastrointestinal bleeding, or with a history of serious, particularly psychotic, mental

disorders.

Postural hypotension can occur following administration of cabergoline. Care should be

exercised when administering DOSTINEX concomitantly with other drugs known to lower

blood pressure.

Fibrosis and Cardiac Valvulopathy

As with other ergot derivatives, fibrotic and serosal inflammatory disorders such as pleuritis,

pleural effusion, pulmonary fibrosis, pericarditis, pericardial effusion, cardiac valvulopathy

or retroperitoneal fibrosis have occurred after prolonged usage of cabergoline. The valvular

effects were predominantly seen at doses exceeding the maximum recommended dose for

treatment of hyperprolactinaemic disorders and maybe associated with cumulative dose.

Some reports were in patients previously treated with ergotinic dopamine agonists. In some

cases,

following

diagnosis

pleural

effusion/pulmonary

fibrosis

valvulopathy,

discontinuance of cabergoline has been reported to result in improvement of signs and

symptoms. Progression of signs and symptoms may continue for a time before improvement

occurs. Erythrocyte sedimentation rate (ESR) has been found to be abnormally increased in

association with pleural effusion/fibrosis. Chest x-ray examination is recommended in cases

of unexplained ESR increases to abnormal values. Serum creatinine measurements can also

be used to help in the diagnosis of fibrotic disorder.

Before initiating long-term treatment:

It is recommended that before initiating treatment with cabergoline all patients undergo a

cardiovascular evaluation, including an echocardiogram, to assess potential presence of an

occult

valvular

disease.

also

appropriate

perform

baseline

investigations

erythrocyte sedimentation rate or other inflammatory markers, lung function/chest X-ray and

renal function prior to initiation of therapy. In patients with valvular regurgitation, it is not

known whether

cabergoline treatment might

worsen the underlying

disease.

If fibrotic

valvular disease is detected, the patient should not be treated with cabergoline.

During long-term treatment:

Fibrotic disorders can have an insidious onset and patients should be regularly monitored for

possible manifestations of progressive fibrosis. Therefore during treatment, attention should

be paid to the signs and symptoms of:

Pleuropulmonary disease such as dyspnoea, shortness of breath, persistent cough or

chest pain

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Renal insufficiency or ureteral/abdominal vascular obstruction that may occur with

pain in the loin/flank and lower limb oedema as well as any possible abdominal

masses or tenderness that may indicate retroperitoneal fibrosis.

Cardiac failure - cases of valvular and pericardial fibrosis have often manifested as

cardiac failure. Therefore, valvular fibrosis (and constrictive pericarditis) should be

excluded if such symptoms occur.

Clinical diagnostic monitoring for development of fibrotic disorders, as appropriate, is

essential. Following treatment initiation, the first echocardiogram must occur within 3-6

months; thereafter, the frequency of echocardiographic monitoring should be determined by

appropriate individual clinical assessment with particular emphasis on the above-mentioned

signs and symptoms, but must occur at least every 6 to 12 months.

Additional appropriate investigations such as erythrocyte sedimentation rate and serum

creatinine measurements should be performed if necessary to support a diagnosis of a fibrotic

disorder.

DOSTINEX

should

discontinued

fibrotic

serosal

inflammatory

disorders

diagnosed or an echocardiogram reveals valvular regurgitation, valvular restriction or valve

leaflet thickening (See section 4.3 and section 4.8).

The need for other subsequent clinical monitoring (e.g. physical examination, careful cardiac

auscultation,

x-ray,

additional

echocardiogram,

scan)

should

determined

individual basis.

Somnolence/Sudden Sleep Onset

Cabergoline has been associated with somnolence. Dopamine agonists can be associated

with sudden sleep onset episodes in patients with Parkinson’s disease. A reduction of dosage

or termination of therapy may be considered.

Inhibition/Suppression of Physiologic Lactation

As with other ergot derivatives, DOSTINEX should not be used in women with preeclampsia

or post-partum hypertension.

A single dose of 0.25 mg of DOSTINEX should not be exceeded in nursing women treated

for suppression of established lactation to avoid potential postural hypotension.

Treatment of Hyperprolactinaemic Disorders

A complete evaluation of the pituitary is indicated before treatment with DOSTINEX is

initiated.

DOSTINEX

restores

ovulation

fertility

women

with

hyperprolactinaemic

hypogonadism. Because pregnancy might occur prior to reinitiation of menses, a pregnancy

test is recommended at least every 4 weeks during the amenorrhoeic period and, once menses

are reinitiated, every time a menstrual period is delayed by more than 3 days. Women who

wish to avoid pregnancy should be advised to use mechanical contraception during treatment

with DOSTINEX and after discontinuation of DOSTINEX until recurrence of anovulation.

As a precautionary measure, women who become pregnant should be monitored to detect

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signs of pituitary enlargement since expansion of pre-existing pituitary tumours may occur

during gestation.

Psychiatric

Patients should be regularly monitored for the development of impulse control disorders.

Patients and carers should be made aware that behavioural symptoms of impulse control

disorders

including

pathological

gambling,

increased

libido,

hypersexuality,

compulsive

spending or buying, binge eating and compulsive eating can occur in patients treated with

dopamine agonists including DOSTINEX. Dose reduction/tapered discontinuation should be

considered if such symptoms develop.

4.5 Interaction with other medicines and other forms of interaction

concomitant

other

drugs

during

early

puerperium,

particularly

methylergometrine maleate, has not been associated with detectable interactions modifying

the efficacy and safety of DOSTINEX.

No information is available about interaction between cabergoline and other ergot alkaloids;

therefore,

concomitant

these

medications

during

long-term

treatment

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 that have dopamine-antagonist activity

(such as phenothiazines, butyrophenones, thioxanthenes, metoclopramide) since these might

reduce the prolactin-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.

As with other ergot derivatives, DOSTINEX should not be used with macrolide antibiotics (e.g.

erythromycin) due to increased systemic bioavailability of cabergoline.

4.6 Fertility, pregnancy and lactation

Pregnancy

Before DOSTINEX administration, pregnancy should be excluded.

Animal studies with cabergoline have not demonstrated teratogenic effects or effects on

overall reproductive performance. However, there are no adequate and well-controlled

studies in pregnant women. DOSTINEX should be used during pregnancy only if clearly

needed. If conception occurs during therapy with DOSTINEX, discontinuation of treatment

should be considered, after careful evaluation of the risks and benefits to mother and foetus.

Pregnancy should be avoided for at least one month following discontinuation of treatment

with DOSTINEX due to the long half-life of the drug and the limited data on

in utero

exposure, although the use of DOSTINEX at 0.5 to 2 mg/week for hyperprolactinaemic

disorders does not appear to be associated with an increased risk of abortion, premature

delivery, multiple pregnancy or congenital abnormalities.

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Lactation

In rats, cabergoline and/or its metabolites are excreted in milk. No information is available

on the excretion in breast milk in humans; however, mothers should be advised not to breast-

feed in case of failed lactation inhibition/suppression by DOSTINEX. Since it prevents

lactation, DOSTINEX should not be administered to mothers with hyperprolactinaemic

disorders who wish to breast-feed their infants.

Fertility

No data available.

4.7 Effects on ability to drive and use machinery

Patients being treated with cabergoline and presenting with somnolence must be informed to

refrain from driving or engaging in activities where impaired alertness may put themselves or

others at risk of serious injury or death (e.g. operating machines) unless patients have

overcome such experiences of somnolence.

4.8 Undesirable effects

Inhibition/Suppression of lactation

: Approximately 14% of women treated with a single 1

mg dose of DOSTINEX for inhibition of physiological lactation complained of at least one

side effect. All side effects were mild to moderate in severity and of a transient nature. The

most frequently occurring adverse events were dizziness/vertigo, headache, nausea and

abdominal pain. In addition rarely palpitations, epigastric pain, somnolence, epistaxis and

transient hemianopsia, vomiting, syncope, asthenia, and hot flushes were reported.

Asymptomatic decreases in blood pressure (

20 mmHg systolic and

10 mmHg diastolic)

may occur usually once during the first 3-4 days postpartum.

Adverse effects have been observed in approximately 14% of nursing women treated with

0.25 mg of DOSTINEX every 12 hours for two days for suppression of lactation. The most

frequent symptoms were dizziness/vertigo, headache, nausea, somnolence, abdominal pain.

In addition, rarely vomiting, syncope, asthenia, and hot flushes were reported. Most side

effects were transient and mild to moderate in severity.

Hyperprolactinaemic disorders

: Data obtained in a controlled clinical trial of 6 months

therapy

with

doses

ranging

between

week

given

weekly

administrations; indicate a 68% incidence of adverse effects during DOSTINEX therapy.

However, the symptoms were generally mild to moderate in degree, mainly appearing during

the first two weeks of therapy, and mostly disappearing despite continued therapy. Severe

adverse events were reported at least once during therapy by 14% of patients but therapy was

discontinued because of adverse events in only approximately 3% of patients. DOSTINEX

withdrawal results in reversal of side effects, usually within a few days after discontinuation.

The most common symptoms in decreasing rank of frequency were nausea, headache,

dizziness/vertigo,

abdominal

pain/dyspepsia/gastritis,

asthenia/fatigue,

constipation,

vomiting, breast pain, hot flushes, depression and paraesthesia.

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General:

DOSTINEX generally exerts a hypotensive effect in patients treated chronically:

however, symptomatic hypotension or fainting has been reported rarely.

Being an ergot derivative, DOSTINEX may also act in some patients as a vasoconstrictor:

digital vasospasm and leg cramps have occasionally been reported.

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.

0.25 mg 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 0.25 mg per week fortnightly) may result in reversal of

side effects once they have occurred.

Alterations

standard

laboratory

tests

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.

Post-marketing surveillance

There have been reports of fibrotic and serosal inflammatory conditions, such as pleuritis,

pleural effusion, pleural fibrosis, pulmonary fibrosis, pericarditis, pericardial effusion, cardiac

valvulopathy and retroperitoneal fibrosis in patients taking cabergoline. (See section 4.4).

The prevalence of asymptomatic valvular regurgitation is significantly greater than that of

non-ergot dopamine agonists.

following

events

have

been

reported

association

with

cabergoline:

aggression,

alopecia, blood creatinine phosphokinase increased, delusions, dyspnoea, oedema, hepatic

function abnormal, hypersensitivity reaction, liver function tests abnormal, rash, psychotic

disorder, respiratory disorder, respiratory failure,

valvulopathy and fibrosis (see section 4.4 –

Fibrosis/Valvulopathy).

Pathological gambling, increased libido, hypersexuality, compulsive spending or buying,

binge eating and compulsive eating can occur in patients treated with dopamine agonists

including DOSTINEX (see section 4.4).

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicine is important. It

allows

continued

monitoring

benefit/risk

balance

medicine.

Healthcare

professionals

asked

report

suspected

adverse

reactions https://nzphvc.otago.ac.nz/reporting/.

4.9 Overdose

There

experience

humans

overdosage

with

DOSTINEX

proposed

indications. It is likely to lead to symptoms due to over-stimulation of dopamine receptors.

These might include nausea, vomiting, gastric complaints, hypotension, nasal congestion,

confusion

hallucinations,

psychosis

thought/perception

disturbances.

Treatment

overdose is symptomatic and supportive. Supportive measures should be directed to maintain

blood pressure, if necessary.

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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 advice on the management of overdose please contact the National Poisons Centre on

0800 POISON (0800 764766).

5.

PHARMACOLOGICAL PROPERTIES

5.1 Pharmacodynamic properties

Mechanism of action

DOSTINEX is a dopaminergic ergoline derivative with potent and long-lasting Prolactin-

lowering activity. It acts by direct stimulation of the D2-dopamine receptors on pituitary

lactotrophs, thus inhibiting Prolactin secretion. In rats the compound decreases prolactin

secretion at oral doses of 3-25 µg/ml, and

in vitro

at a concentration of 45 pg/ml. In addition

DOSTINEX exerts a central dopaminergic effect via D2 receptor stimulation at oral doses

higher than those effective in lowering serum Prolactin levels. The long-lasting Prolactin-

lowering effects of DOSTINEX is probably due to its long persistence in the target organ as

suggested by the slow elimination of total radioactivity from the pituitary after a single oral

dose in rats (t

of approximately 60 hours).

The pharmacodynamic effects of DOSTINEX have been studied in healthy women, puerperal

women and hyperprolactinaemic patients. After a single oral administration of DOSTINEX

(0.3-1.5 mg), a significant decrease in serum Prolactin levels was observed in each of the

populations studied. The effect is prompt (within 3 hours from administration) and persistent

(up to 7-28 days in healthy volunteers and hyperprolactinaemic patients, and up to 14-21 days

in puerperal women). The Prolactin-lowering effect is dose related both in terms of degree of

effect and duration of action.

With regard to the endocrine effects of DOSTINEX not related to the antiprolactinaemic

effect, data available from humans confirm the experimental findings in animals indicating

that the test compound is endowed with a very selective action with no effect on basal

secretion

other

pituitary

hormones

cortisol.

pharmacodynamic

actions

DOSTINEX not correlated with the therapeutic effect only relate to blood pressure decrease.

The maximal hypotensive effect of DOSTINEX as a single dose usually occurs during the

first 6 hours after medicine intake and is dose-dependent both in terms of maximal decrease

and frequency.

Inhibition/suppression of physiological lactation

: In controlled clinical trials DOSTINEX

given as a single 1 mg administration during the first day post-partum was effective in

inhibiting milk secretion, as well as breast engorgement and pain in 70-90% of the women.

Less than 5% of women experienced rebound breast symptomatology during the third post-

partum week (which was usually mild in severity).

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Hyperprolactinaemic disorders

: On chronic therapy, DOSTINEX at doses ranging between

1 and 2 mg per week was effective in normalising serum prolactin levels in approximately

84% of hyperprolactinaemic patients. Regular cycles were resumed in 83% of previously

amenorrhoeic women. Restoration of ovulation was documented in 89% of women with

progesterone levels monitored during the luteal phase. Galactorrhoea disappeared in 90% of

cases showing this symptom before therapy. Reduction in tumour size was obtained in 50-

90% of female and male patients with micro- or macro-prolactinoma.

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

gastrointestinal

tract.

peak

radioactivity

plasma

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-8B-carboxyl-ergoline, which accounted

for 4-6% of the dose. Three additional metabolites were identified in the urine, which

accounted overall for less than 3% of the dose. The metabolites have been found to be much

less

potent

than

DOSTINEX

inhibiting

prolactin

secretion

in

vitro

DOSTINEX

biotransformation was also studied in plasma of healthy male volunteers treated with [14C]-

cabergoline. A rapid and extensive biotransformation of cabergoline was shown. The low

urinary excretion of unchanged DOSTINEX has also been confirmed in studies with non-

radioactive

product.

elimination

half

life

DOSTINEX

estimated

from

urinary

excretion

rates,

long

(63-68 hours

healthy

volunteers,

79-115 hours

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

dose (37 ± 8 pg/ml) after a 4 week multiple-regimen (101 ± 43 pg/ml).

In vitro experiments showed that the cabergoline at concentrations of 0.1-10 ng/ml is 41-42%

bound to plasma proteins.

Food does not appear to affect absorption and disposition of DOSTINEX.

5.3 Preclinical safety data

Genotoxicity

No data available.

Carcinogenicity

No data available.

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Reproductive and developmental toxicity

No data available.

6.

PHARMACEUTICAL PARTICULARS

6.1 List of excipients

Lactose anhydrous

Leucine.

6.2 Incompatibilities

No data available.

6.3 Shelf life

Two year shelf life.

6.4 Special precautions for storage

Store below 25°C.

6.5 Nature and contents of container

2 or 8 tablets packed in either glass bottles with aluminium caps or HDPE bottles with

polypropylene caps.

Not all pack sizes may be marketed.

DOSTINEX tablets are supplied in bottles with desiccant in the caps. This desiccant must

not be removed.

6.6 Special precautions for disposal

Any unused medicine or waste material should be disposed of in accordance with local

requirements.

7.

MEDICINE SCHEDULE

Prescription Medicine.

8.

SPONSOR

Pfizer New Zealand Limited

P O Box 3998

Auckland, New Zealand

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Toll Free Number: 0800 736 363

9.

DATE OF FIRST APPROVAL

17 March 1994

10. DATE OF REVISION OF THE TEXT

21 May 2019

Summary table of changes

Section changed

Summary of new information

New Data Sheet format in accordance with Medsafe guidance.

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