New Zealand - English - Medsafe (Medicines Safety Authority)
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
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
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
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
Before you start to
Before starting treatment with
Dostinex, your doctor will need to
do some tests to detect any
underlying heart, lung or kidney
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
any of the ingredients listed at the
end of this leaflet
ergot alkaloids (medicines used to
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
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
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
kidney, heart and liver problems
lung disease or problems with
Raynaud's syndrome (associated
with extreme numbness, tingling
and colour changes in the fingers
due to cold )
ulcer or bleeding in the stomach
low blood pressure
high blood pressure after
history of severe mental illness.
Tell your doctor if you are
pregnant or plan to become
Your doctor can discuss with you the
risks and benefits involved.
recommended that women who plan
to become pregnant stop taking
Dostinex at least one month before
Tell your doctor if you are breast-
feeding or intend to breastfeed.
This medicine prevents the flow of
If you have not told your doctor or
pharmacist about any of the above,
tell them before you start to take
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
medicines used to treat mental
illness, e.g. antipsychotic
medicines for schizophrenia
medicines used to treat high
ergot alkaloids, medicines used to
medicines used to prevent nausea
and vomiting (e.g.
medicines called macrolide
antibiotics which are used to treat
bacterial infections (e.g.
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
How to take Dostinex
Follow all directions given to you
by your doctor or pharmacist
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
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
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
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
Otherwise, take it as soon as you
remember, then go back to taking
your medicine as you normally
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
If you have trouble remembering
to take your medicine, ask your
pharmacist for some hints.
If you take too much
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
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
While you are taking
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 so that your progress can
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
Your doctor may recommend routine
pregnancy tests during long periods
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
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,
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
nausea or vomiting
abdominal pain, or heartburn or
pain in the stomach
weakness or tiredness
temporary impairment of vision
The side effects listed above are
usually mild and short lived.
Tell your doctor as soon as
Tell your doctor as soon as possible
if you notice any of the following:
irregular heart beat
leg cramps or pain in the fingers
depression, feelings of deep
changes in behaviour such as
increased sex drive, a compelling
desire to gamble, shop, eat or take
any breathing problems.
The above list includes serious side
effects, which may require medical
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
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
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
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
After taking Dostinex
Keep Dostinex in its container until
it is time to take it.
Keep Dostinex in a cool dry place,
where the temperature stays below
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
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.
Ask your pharmacist what to do
with any Dostinex which is left
over, or if the medicine has passed
its expiry date.
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
Dostinex is available in bottles of 2
and 8 tablets.
The active ingredient is cabergoline
Each tablet also contains: lactose and
Pfizer New Zealand Limited
PO Box 3998
Toll free number: 0800 736 363
This leaflet was revised in July 2020.
© Pfizer Australia Pty Ltd
® Registered Trademark
Page 1 of 11
NEW ZEALAND DATA SHEET
QUALITATIVE AND QUANTITATIVE COMPOSITION
Each DOSTINEX tablet contains 0.5 mg cabergoline.
Excipient(s) with known effect
For the full list of excipients, see section 6.1.
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.
4.1 Therapeutic indications
Prevention of the onset of lactation in the puerperium only for clearly defined medical
DOSTINEX is indicated for the inhibition of physiological lactation soon after
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
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
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
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
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.
However persistent suppression of prolactin levels has been observed for several months in
Severe hepatic insufficiency
: Lower doses should be considered in patients with severe
hepatic insufficiency who receive prolonged treatment with DOSTINEX. (See section 4.4).
: The safety and efficacy of DOSTINEX has not been established in subjects less
than 16 years of age.
: 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.
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
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
Postural hypotension can occur following administration of cabergoline. Care should be
exercised when administering DOSTINEX concomitantly with other drugs known to lower
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
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
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
cabergoline treatment might
worsen the underlying
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
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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
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
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
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
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
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
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;
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
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
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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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.
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.
: Data obtained in a controlled clinical trial of 6 months
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,
vomiting, breast pain, hot flushes, depression and paraesthesia.
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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.
DOSTINEX. A decrease in haemoglobin values have been observed in amenorrhoeic women
during the first few months after menses resumption.
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.
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 –
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
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,
overdose is symptomatic and supportive. Supportive measures should be directed to maintain
blood pressure, if necessary.
Page 8 of 11
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).
5.1 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
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
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
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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: 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
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
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-
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
No data available.
No data available.
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Reproductive and developmental toxicity
No data available.
6.1 List of excipients
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
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
Pfizer New Zealand Limited
P O Box 3998
Auckland, New Zealand
Page 11 of 11
Toll Free Number: 0800 736 363
DATE OF FIRST APPROVAL
17 March 1994
10. DATE OF REVISION OF THE TEXT
21 May 2019
Summary table of changes
Summary of new information
New Data Sheet format in accordance with Medsafe guidance.