Quinagolide 75microgram tablets

United Kingdom - English - MHRA (Medicines & Healthcare Products Regulatory Agency)

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Active ingredient:
Quinagolide hydrochloride
Available from:
Aspire Pharma Ltd
ATC code:
G02CB04
INN (International Name):
Quinagolide hydrochloride
Dosage:
75microgram
Pharmaceutical form:
Tablet
Administration route:
Oral
Class:
No Controlled Drug Status
Prescription type:
Valid as a prescribable product
Product summary:
BNF: 06070100; GTIN: 5060209731421
Authorization number:
PL 35533/0064

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PACKAGE LEAFLET

Quinagolide Tablets

Norprolac® Tablets

Patient Information

Read all of this leaflet carefully before you start

taking this medicine.

Keep this leaflet, you may need to use it again.

If you have further questions, please ask your doctor or pharmacist.

This medicine has been prescribed for you personally and you should not pass it on to others. It may

harm them, even if their symptoms are the same as yours.

In this leaflet:

1. What Quinagolide

is and what it is used for

2. Before you take Quinagolide

3. How to take Quinagolide

4. Possible side effects

5. How to store Quinagolide

6. Further information

1. What Quinagolide is and what it is used for

Quinagolide is for oral use only. It is available in strengths of 25 micrograms, 50 micrograms and 75

micrograms. Quinagolide contains quinagolide which decreases the production of the hormone prolactin.

Quinagolide is used to treat conditions resulting from high levels of prolactin in the blood

(hyperprolactinaemia) including:

excess production of breast milk

changes in menstrual bleeding patterns

infertility

reduced sexual drive.

2. Before you take Quinagolide

Do not take Quinagolide:

if you have a medical condition affecting your liver or kidneys

if you are allergic to any of the ingredients listed in section 6

If you are pregnant or planning a pregnancy, please refer to the pregnancy section of this leaflet.

Before taking Quinagolide:

please consult your doctor if you have ever had any mental illness.

Quinagolide may cause your blood pressure to drop when you stand up, particularly for the first few

days of treatment or following an increase in your dosage. This may result in reduced alertness or

fainting. To avoid this, stand up slowly from a sitting or lying down position. Your doctor will normally

check your blood pressure during the first few days of treatment and when increasing your dosage.

Inform your doctor if you or your family/carer notices that you are developing urges or cravings to

behave in ways that are unusual for you and you cannot resist the impulse, drive or temptation to carry

out certain activities that could harm yourself or others. These are called impulse control disorders and

can include behaviours such as addictive gambling, excessive eating or spending, an abnormally high sex

drive or an increase in sexual thoughts or feelings. Your doctor may need to adjust or stop your dose.

Taking/using other medicines:

Please inform your doctor or pharmacist if you are taking or have recently taken or used any other

medicines - even those not prescribed.

Taking Quinagolide with drink:

Drinking alcohol may increase the side effects of Quinagolide. If this happens, you should avoid drinking

alcohol while you are on treatment with Quinagolide.

Pregnancy:

Fertility may be restored while you are on Quinagolide, so women of child-bearing age who do not wish

to become pregnant should use a reliable method of contraception.

If you are planning a pregnancy, it is recommended that Quinagolide is stopped when pregnancy is

confirmed. However, some patients may need to continue treatment with Quinagolide during pregnancy.

If you become pregnant while you are on Quinagolide, tell your doctor as soon as possible.

Breast-feeding:

Quinagolide reduces production of breast-milk, so it is not normally possible to breast-feed while you are

taking it. You should not breast-feed even if it is possible to do so. This is because it is not known

whether the active ingredient in Quinagolide passes into breast-milk.

Driving and using machines:

While you are on Quinagolide, caution is advised if you drive or operate machinery. This is because

Quinagolide:

may cause your blood pressure to drop, particularly during the first few days of treatment or following

dosage increase. This may result in reduced alertness or fainting.

may also cause somnolence (drowsiness or sleepiness).

If you experience any of these effects, please do not drive or engage in any other activity (e.g. operating

machinery) where impaired alertness may put you or others at risk of serious injury or death and please

consult your doctor, as your dose may need to be adjusted.

Important information about some of the ingredients in Quinagolide:

Quinagolide contains the ingredient lactose. Therefore, if you have been told by your doctor that you have

an intolerance to some sugars (including lactose), contact your doctor before taking this medicinal

product.

3. How to take Quinagolide

Adults:

It is important to take your medicine as directed by your doctor. The label on your medicine should tell

you how much to take and when to take it. If it does not, or you are not sure, ask your doctor or

pharmacist.

Elderly:

Take this medicine only if your doctor has decided that this is appropriate for you. Follow the instructions

given to you very carefully.

The tablets should only be removed from the blister when it is time to take your medicine.

Your treatment will normally begin with the ‘starter pack’ and you will take one 25 micrograms tablet

daily (one light pink tablet) for the first three days (marked Day 1, Day 2 and Day 3 on the blister strip).

This is followed by one 50 micrograms tablet daily (one very pale blue tablet) for the next three days

(marked Day 4, Day 5 and Day 6 on the blister strip).

From Day 7, the recommended dose is one 75 micrograms tablet daily (one whitish tablet). Most

patients require a daily dose of 75 to 150 micrograms. Some patients require a daily dose of 300

micrograms or higher. Your doctor will tell you if you need a higher dose. You should not change the

dose yourself.

Quinagolide should be taken once daily at bedtime preferably with a snack. Remove the tablet from the

blister by pushing it through the foil and place it in your mouth. Swallow it with a mouthful of water.

If you take more Quinagolide than you should:

If you take more Quinagolide than you should, tell your doctor immediately or go to your nearest casualty

department.

If you forget to take Quinagolide:

If you forget to take a dose, take it as soon as you remember. However, if you do not remember until it is

nearly time for the next dose, take your next dose as usual and carry on as before. Do not take double

doses to make up for a dose that you miss.

. Possible side effects

Like all medicines, Quinagolide can have side effects. These are most common during the first few days

of treatment and tend to go away on continuing treatment.

Very common side effects (affect more than 10 of every 100 patients treated):

Nausea

Vomiting

Headache

Dizziness

Tiredness

Common side effects (affect between 1 and 10 of every 100 patients treated):

Loss of appetite

Abdominal pain

Constipation or diarrhoea

Insomnia

Increased water retention

Flushing

Nasal congestion and a drop in blood pressure, which may result in fainting.

Rare side effects (affect between 1 and 10 of every 10,000 patients treated):

Somnolence (drowsiness or sleepiness).

Very rare side effects (affect less than 1 of every 10,000 patients treated):

Treatment with Quinagolide has been associated with a change in mental status, which is reversible

when treatment is stopped.

Other side effects include:

Inability to resist the impulse, drive or temptation to perform an action that could be harmful to you or

others, which may include:

strong impulse to gamble excessively despite serious personal or family consequences.

altered or increased sexual interest and behaviour of significant concern to you or to others, for example,

an increased sexual drive.

uncontrollable excessive shopping or spending.

binge eating (eating large amounts of food in a short time period) or compulsive eating (eating more

food than normal and more than is needed to satisfy your hunger).

Tell your doctor if you experience any of these behaviours; they will discuss ways of managing or

reducing the symptoms.

Reporting of side effects

If you get any side effects, talk to your doctor or pharmacist or nurse. This includes any possible side

effects not listed in this leaflet. You can also report side effects directly via the Yellow Card Scheme

(www.mhra.gov.uk/yellowcard). By reporting side effects you can help provide more information on the

safety of this medicine.

5. Storing Quinagolide

Keep Quinagolide out of the reach and sight of children.

Do not store above 25ºC.

Do not take the tablets past the expiry date on the packaging.

If you are unsure about the storage, ask your pharmacist. It is best to return all old and unused medicines

to your pharmacist for safe disposal.

6. Further information

Your medicine is called Quinagolide Tablets. They are for oral use only.

Quinagolide contains the active ingredient, quinagolide (as quinagolide hydrochloride). It is available in

strengths of 25 micrograms, 50 micrograms and 75 micrograms quinagolide.

Quinagolide also contains: colloidal anhydrous silica, methylhydroxypropylcellulose, maize starch,

magnesium stearate, microcrystalline cellulose and lactose. In addition, the 25 microgram tablets contain

indigotin lake as colouring agents.

Treatment usually starts with a ‘starter pack’ containing 3 tablets of 25 micrograms (light pink) and 3

tablets of 50 micrograms (very pale blue) in a single blister strip. This is then followed by treatment with

75 micrograms (whitish) tablets presented in a pack of 30 tablets in blister strips of 10 tablets per strip.

Marketing Authorisation Holder:

Aspire Pharma Ltd., Unit 4 Rotherbrook Court, Bedford Road, Petersfield, Hampshire, GU32 3QG, UK

Manufacturer:

Ferring GmbH, Wittland 11,D-24109 Kiel,Germany.

Quinagolide Tablets 25 micrograms PL 35533/0062

Quinagolide Tablets 50 micrograms PL 35533/0063

Quinagolide Tablets 75 micrograms PL 35533/0064

This leaflet was last revised in September 2016.

Read the complete document

Object 1

Quinagolide 75 micrograms tablets

Summary of Product Characteristics Updated 11-Oct-2016 | Aspire Pharma Ltd

1. Name of the medicinal product

NORPROLAC® 75 micrograms Tablets

Quinagolide 75 micrograms Tablets

2. Qualitative and quantitative composition

Quinagolide, as the hydrochloride, 75 micrograms

3. Pharmaceutical form

Tablet for oral administration

4. Clinical particulars

4.1 Therapeutic indications

Hyperprolactinaemia (idiopathic or originating from a prolactin-secreting pituitary microadenoma or

macroadenoma).

4.2 Posology and method of administration

Since dopaminergic stimulation may lead to symptoms of orthostatic hypotension, the dosage of

NORPROLAC should be initiated gradually with the aid of the 'starter pack', and given only at bedtime.

Adults

The optimal dose must be titrated individually on the basis of the prolactin- lowering effect and

tolerability.

With the 'starter pack' treatment begins with 25 micrograms/day for the first 3 days, followed by 50

micrograms/day for a further 3 days. From day 7 onwards, the recommended dose is 75 micrograms/day.

If necessary, the daily dose may then be increased stepwise until the optimal individual response is

attained. The usual maintenance dosage is 75 to 150 micrograms/day.

Daily doses of 300 micrograms or higher doses are required in less than one- third of the patients.

In such cases, the daily dosage may be increased in steps of 75 to 150 micrograms at intervals not shorter

than 4 weeks until satisfactory therapeutic effectiveness is achieved or reduced tolerability, requiring the

discontinuation of treatment, occurs.

Elderly

Experience with the use of NORPROLAC in elderly patients is not available.

Children

Experience with the use of NORPROLAC in children is not available.

Method of Administration

NORPROLAC should be taken once a day with some food at bedtime.

4.3 Contraindications

Hypersensitivity to the drug.

Impaired hepatic or renal function

For procedure during pregnancy, (see section 4.6 Pregnancy and lactation).

4.4 Special warnings and precautions for use

Fertility may be restored by treatment with NORPROLAC. Women of child- bearing age who do not

wish to conceive should therefore be advised to practice a reliable method of contraception.

Since orthostatic hypotension may result in syncope, it is recommended to check blood pressure both

lying and standing during the first days of therapy and following dosage increases.

In a few cases, including patients with no previous history of mental illness, treatment with

NORPROLAC has been associated with the occurrence of acute psychosis, usually reversible upon

discontinuation. Particular caution is required in patients who have had psychotic episodes in their

previous history.

To date no data is available with the use of NORPROLAC in patients with impaired renal or hepatic

function (see Section 4.3 Contraindications).

NORPROLAC has been associated with somnolence. Other dopamine agonists can be associated with

sudden sleep onset episodes, particularly in patients with Parkinson's disease. Patients must be informed

of this and advised to exercise caution whilst driving or operating machines during treatment with

NORPROLAC.

Patients who have experienced somnolence must not drive or operate machines. Furthermore, a reduction

of dosage or termination of therapy may be considered (see Section 4.7 Effects on the ability to drive and

use machines).

Impulse control disorders

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 NORPROLAC. Dose

reduction/tapered discontinuation should be considered if such symptoms develop.

NORPROLAC should be kept out of the reach and sight of children.

4.5 Interaction with other medicinal products and other forms of interaction

No interactions between NORPROLAC and other drugs have so far been reported. On theoretical

grounds, a reduction of the prolactin-lowering effect could be expected when drugs (e.g. neuroleptic

agents) with strong dopamine antagonistic properties are used concomitantly. As the potency of

NORPROLAC for 5-HT

and 5-HT

receptors is some 100 times lower than that for D

receptors, an

interaction between NORPROLAC and 5-HT

receptors is unlikely. However, care should be taken

when using these medicaments concomitantly.

The tolerability of NORPROLAC may be reduced by alcohol.

4.6 Fertility, pregnancy and lactation

Pregnancy

Animal data provide no evidence that NORPROLAC has any embryotoxic or teratogenic potential, but

experience in pregnant women is still limited. In patients wishing to conceive, NORPROLAC should be

discontinued when pregnancy is confirmed, unless there is a medical reason for continuing therapy. No

increased incidence of abortion has been observed following withdrawal of the drug at this point.

If pregnancy occurs in the presence of a pituitary adenoma and NORPROLAC treatment has been

stopped, close supervision throughout pregnancy is essential.

Lactation

Breast-feeding is usually not possible since NORPROLAC suppresses lactation. If lactation should

continue during treatment, breast-feeding cannot be recommended because it is not known whether

quinagolide passes into human breast milk.

4.7 Effects on ability to drive and use machines

Since, especially during the first days of treatment, hypotensive reactions may occasionally occur and

result in reduced alertness, patients should be cautious when driving a vehicle or operating machinery.

Patients being treated with NORPROLAC and presenting with somnolence must be advised not to drive

or engage 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 (see 4.4

Special warnings and precautions for use).

4.8 Undesirable effects

Frequency estimate: very common 10%, common 1% to <10%, uncommon 0.1% to <1%, rare

0.01% to <0.1%, very rare <0.01%.

The adverse reactions reported with the use of NORPROLAC are characteristic for dopamine receptor

agonist therapy. They are usually not sufficiently serious to require discontinuation of treatment and tend

to disappear when treatment is continued.

Very common undesirable effects are nausea, vomiting, headache, dizziness and fatigue. They occur

predominantly during the first few days of the initial treatment or, as a mostly transient event, following

dosage increase. If necessary, nausea and vomiting may be prevented by the intake of a peripheral

dopaminergic antagonist, such as domperidone, for a few days, at least 1 hour before ingestion of

NORPROLAC.

Common undesirable effects include anorexia, abdominal pain, constipation or diarrhoea, insomnia,

oedema, flushing, nasal congestion and hypotension. Orthostatic hypotension may result in faintness or

syncope (see 4.4 Special warnings and precautions for use).

Rarely NORPROLAC has been associated with somnolence.

In very rare cases, treatment with NORPROLAC has been associated with the occurrence of acute

psychosis, reversible upon discontinuation.

Impulse control disorders

Pathological gambling, increased libido, hypersexuality, compulsive spending or buying, binge eating and

compulsive eating can occur in patients treated with dopamine agonists including NORPROLAC. (See

section 4.4. 'Special warnings and precautions for use').

4.9 Overdose

Symptoms: Acute overdosage with NORPROLAC tablets has not been reported. It would be expected to

cause severe nausea, vomiting, headache, dizziness, drowsiness, hypotension and possibly collapse.

Hallucinations could also occur.

Treatment: Should be symptomatic.

5. Pharmacological properties

5.1 Pharmacodynamic properties

Pharmacotherapeutic group: prolactin inhibitors (ATC code G02C B04)

Quinagolide, the active ingredient of NORPROLAC, is a selective dopamine D

-receptor agonist not

belonging to the chemical classes of ergot or ergoline compounds. Owing to its dopaminergic action, the

drug exerts a strong inhibitory effect on the secretion of the anterior pituitary hormone prolactin, but does

not reduce normal levels of other pituitary hormones. In some patients the reduction of prolactin secretion

may be accompanied by short- lasting, small increases in plasma growth hormone levels, the clinical

significance of which is unknown.

As a specific inhibitor of prolactin secretion with a prolonged duration of action, NORPROLAC has been

shown to be effective and suitable for once-a- day oral treatment of patients presenting with

hyperprolactinaemia and its clinical manifestations such as galactorrhoea, oligomenorrhoea,

amenorrhoea, infertility and reduced libido.

5.2 Pharmacokinetic properties

After oral administration of radiolabelled drug, quinagolide is rapidly and well absorbed. Plasma

concentration values obtained by a non-selective radio- immunoassay (RIA), measuring quinagolide

together with some of its metabolites, were close to the limit of quantification and gave no reliable

information.

The apparent volume of distribution of quinagolide after single oral administration of radiolabelled

compound was calculated to be approx. 100 L. For the parent drug, a terminal half-life of 11.5 hours has

been calculated under single dose conditions, and of 17 hours at steady state.

Quinagolide is extensively metabolised during its first pass. Studies performed with

H-labelled

quinagolide revealed that more than 95 % of the drug is excreted as metabolites. About equal amounts of

total radioactivity are found in faeces and urine.

In blood, quinagolide and its N-desethyl analogue are the biologically active but minor components. Their

inactive sulphate or glucuronide conjugates represent the major circulating metabolites. In urine, the main

metabolites are the glucuronide and sulphate conjugates of quinagolide and the N-desethyl, N,N-

didesethyl analogues. In the faeces the unconjugated forms of the three components were found.

The protein binding of quinagolide is approximately 90% and is non-specific.

The results, obtained in pharmacodynamic studies, indicate that with the recommended therapeutic

dosage a clinically significant prolactin-lowering effect occurs within 2 hours after ingestion, reaches a

maximum within 4 to 6 hours and is maintained for about 24 hours.

A definite dose-response relationship could be established for the duration, but not for the magnitude, of

the prolactin-lowering effect which, with a single oral dose of 50 micrograms was close to maximum.

Higher doses did not result in a considerably greater effect but prolonged its duration.

5.3 Preclinical safety data

Acute toxicity

The LD

of quinagolide was determined for several species after single oral administration: mice 357 to

> 500 mg/kg; rats > 500 mg/kg; rabbits > 150 mg/kg.

Chronic toxicity

Decreased cholesterol levels of treated female rats suggest that quinagoilde influences lipid metabolism.

Since similar observations have been made with other dopaminergic drugs, a causal relationship with low

prolactin levels is assumed. In several chronic studies with rats, enlarged ovaries resulting from an

increased number of corpora lutea and, additionally, hydrometra and endometritis were observed. These

changes were reversible and reflect the pharmacodynamic effect of quinagolide: suppression of prolactin

secretion inhibits luteolysis in rats and thus influences the normal sexual cycle. In humans, however,

prolactin is not involved in luteolysis.

Carcinogenic and mutagenic potential

In comprehensive in vitro and in vivo mutagenic studies there was no evidence of a mutagenic effect.

The changes which were observed in carcinogenicity studies reflect the pharmacodynamic activity of

quinagolide. The drug modulates the prolactin level as well as, specially in male rats, the level of

luteinizing hormone and, in female rodents, the ratio of progesterone to oestrogen.

Long-term studies with high doses of quinagolide revealed Leydig cell tumours in rats and mesenchymal

uterine tumours in mice. The incidence of Leydig cell tumours in a carcinogenicity study in rats was

increased even at low doses (0.01 mg/kg). These results were without relevance for the therapeutic

application in humans since there are fundamental differences between humans and rodents in the

regulation of the endocrine system.

Reproductive toxicity

Animal studies in rats and rabbits showed no evidence for embryotoxic or teratogenic effects. The

prolactin inhibiting effect led to a decrease of milk production in rats, which was associated with an

increased loss of rat pups. Possible post-natal effects of exposure during fetal development (2nd and 3rd

trimester) and effects on female fertility are not sufficiently investigated.

6. Pharmaceutical particulars

6.1 List of excipients

Silica, colloidal anhydrous; magnesium stearate; methylhydroxypropylcellulose; maize starch; cellulose,

microcrystalline; lactose.

6.2 Incompatibilities

Not applicable

6.3 Shelf life

The shelf life is 5 years. The expiry date is printed on the box. On the blister the expiry date is marked

with the letters EXP.

6.4 Special precautions for storage

The expiry date refers to original unopened boxes, which were stored below 25°C. No special warning

with respect to light sensitivity or humidity is necessary because the tablets are protected by the

packaging.

6.5 Nature and contents of container

The 75 micrograms tablets are in packs of 30 tablets (3 times 10 tablets) in aluminium blisters.

6.6 Special precautions for disposal and other handling

None

7. Marketing authorisation holder

Aspire Pharma Ltd

Unit 4 Rotherbrook Court

Bedford Road

Petersfield

Hampshire

GU32 3QG

United Kingdom

8. Marketing authorisation number(s)

PL 35533/0064

9. Date of first authorisation/renewal of the authorisation

December 2004

10. Date of revision of the text

28/09/2016

Company Contact Details

Aspire Pharma Ltd

Address

4 Rotherbrook Court, Bedford Road, Petersfield, Hampshire, GU32 3QG, UK

Telephone

+44 (0)1730 231148

Customer Care direct line

+44 (0)1730 231148

http://www.aspirepharma.co.uk

Medical Information Direct Line

+44 (0)1730 231148

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