Buscopan

New Zealand - English - Medsafe (Medicines Safety Authority)

Buy It Now

Active ingredient:
Hyoscine butylbromide 20 mg/mL
Available from:
sanofi-aventis new zealand limited
INN (International Name):
Hyoscine butylbromide 20 mg/mL
Dosage:
20 mg/mL
Pharmaceutical form:
Solution for injection
Composition:
Active: Hyoscine butylbromide 20 mg/mL Excipient: Sodium chloride Water for injection
Units in package:
Ampoule, 1ml, 5 dose units
Class:
Prescription
Prescription type:
Prescription
Manufactured by:
Boehringer Ingelheim Pharma GmbH & Co KG
Product summary:
Package - Contents - Shelf Life: Ampoule, 1ml - 5 dose units - 60 months from date of manufacture stored at or below 30°C
Authorization number:
TT50-2406/1
Authorization date:
1969-12-31

Buscopan

Tablets

Hyoscine butylbromide

Consumer Medicine Information

What is in this leaflet

This leaflet answers some common

questions about Buscopan tablets.

It does not contain all available

information. It does not take the

place of talking to your doctor or

pharmacist.

This leaflet was last updated on the

date at the end of this leaflet. More

recent information may be

available. The latest Consumer

Medicine Information is available

from your pharmacist, doctor, or

from www.medicines.org.au and

www.medsafe.govt.nz/Consumers/c

mi/CMIForm.asp (New Zealand)

and may contain important

information about the medicine and

its use of which you should be

aware.

All medicines have risks and

benefits. Your doctor has weighed

the risks of you taking Buscopan

against the benefits they expect it

will have for you.

If you have any concerns about

taking this medicine, ask your

doctor or pharmacist.

Keep this information with the

medicine.

You may need to read it again.

What Buscopan is

used for

Buscopan is known as an

anticholinergic medicine. It relieves

the pain of stomach and bowel

cramps by helping your digestive

system to relax.

Buscopan blister packs of 20 tablets

are available only at a pharmacy.

Buscopan blister packs of 100

tablets are available only with a

doctor's prescription.

Always consult your doctor or

pharmacist if the pain does not

improve within 48 hours or if

pain worsens after treatment.

Before you take

Buscopan

When you must not take it

Do not take Buscopan if you are

allergic to hyoscine butylbromide

or to any of the other ingredients

listed at the end of this leaflet.

Some of the symptoms of an

allergic reaction may include:

shortness of breath

wheezing or difficulty breathing

swelling of the face, lips, tongue

or other parts of the body

rash, itching or hives on the

skin.

Do not take this medicine if you

have fructose intolerance.

Buscopan contains sucrose as an

ingredient.

Do not take Buscopan if you

have:

myasthenia gravis - a condition

in which the muscles become

weak and tire easily

glaucoma - high pressure in the

porphyria – a rare blood

pigment disorder

a suspected or confirmed

blockage of the bowel

a condition where the bowel is

blocked and does not work

properly (paralytic or

obstructive ileus). Symptoms

include severe abdominal pain

with lack of stools and/or

nausea/vomiting

a very enlarged bowel

(megacolon)

tachyarrhythmia – a fast heart

rate

achalasia – a condition that

causes difficulty in swallowing

food

prostatic hypertrophy – prostate

problems.

Buscopan must not be used when

there is a blockage in the stomach

or bowel or in certain conditions

when there is reduced bowel

activity.

These conditions are best

explained by your doctor or

pharmacist. Do not give it to a

child under the age of 6 years.

Safety and effectiveness in children

younger than 6 years have not been

established.

Do not take it 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 immediately if

your abdominal pain continues or

worsens or occurs with symptoms

like:

fever

nausea

vomiting

changes in bowel movements

fainting

blood in faeces.

Tell your doctor if you are

pregnant or plan to become

pregnant or are breastfeeding.

There is limited information on the

use of Buscopan during pregnancy

and breastfeeding.

Your doctor can discuss with you

the risks and benefits involved.

If you have not told your doctor

about any of the above, tell

him/her before you start taking

Buscopan.

Taking other medicines

Tell your doctor or pharmacist if

you are taking any other

medicines, including any that you

get without a prescription from

your pharmacy, supermarket or

health food shop.

Some medicines and Buscopan may

interfere with each other. These

include:

medicines used to treat or

prevent nausea and vomiting

such as metoclopramide

medicines used to treat malaria

such as quinine

medicines used to treat the

symptoms of Parkinson's

disease such as amantadine

medicines used to treat some

mental conditions such as tri

and tetracyclic antidepressants

and antipsychotics

medicines used to treat allergies

such as antihistamines

medicines for the treatment of

depression, heart disease or

respiratory disease such as

tiotropium, ipratropium or

atropine-like compounds

any other medicine for the

treatment of stomach or bowel

condition.

These medicines may be affected by

Buscopan or may affect how well it

works. You may need different

amounts of your medicines, or you

may need to take different

medicines.

Your doctor and pharmacist have

more information on medicines to

be careful with or avoid while

taking this medicine.

How to take

Buscopan

Follow all directions given to you

by your doctor or pharmacist

carefully.

They may differ from the

information contained in this leaflet.

If you do not understand the

instructions on the box, ask your

doctor or pharmacist for help.

How much to take

The recommended dose for adults

and children over 6 years of age is

two tablets four times a day taken

about every 4-6 hours.

How to take it

Swallow the tablets whole with a

glass of water.

How long to take it

Continue taking your medicine

for as long as your doctor tells

you.

This medicine helps to control your

condition, but does not cure it.

Do not take it for extended

periods.

Worsening or persistent stomach

pain should be investigated by your

doctor to determine the cause of the

pain.

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, and then go back to

taking your medicine as you

would 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, ask

your doctor or pharmacist.

If you no longer have any

stomach pain it is not necessary to

finish taking all the tablets in the

pack

If you take too much

(overdose)

Seek medical advice if you have

used more than the recommended

or prescribed dose of Buscopan.

Symptoms of an overdose may

include: drowsiness, dry mouth,

difficulty passing urine, reddening

of the skin, decreased

gastrointestinal tract movement, fast

heart rate and sight disturbances.

Advice can be provided by a

doctor, pharmacist or Poisons

Information Centre (in Australia

telephone 13 11 26; in New

Zealand telephone 0800 764 766).

Do not drive a car or operate

machinery if you have taken more

than the recommended or

prescribed dose of Buscopan.

While you are taking

Buscopan

Things you must do

If you are about to be started on

any new medicine, remind your

doctor and pharmacist that you

are taking Buscopan.

Tell your doctor or pharmacist if

you begin taking any other

medicine while you are taking this

medicine.

Tell your doctor or pharmacist if

the pain is severe or does not

improve within 48 hours of taking

Buscopan.

Cramps in the stomach or bowel

may be temporary or may signal the

presence of a more serious problem.

Things to be careful of

Be careful driving or operating

machinery until you know how

Buscopan affects you.

This medicine may cause dizziness,

tiredness, drowsiness in some

people.

If you have any of these

symptoms, do not drive, operate

machinery or do anything else

that could be dangerous.

Do not drink alcohol while taking

Buscopan.

Alcohol may increase the chance of

side effects such as drowsiness.

Side effects

Tell your doctor or pharmacist as

soon as possible if you do not feel

well while you are taking

Buscopan.

All medicines can have side effects.

Sometimes they are serious, most of

the time they are not.

Ask for the advice of your doctor

or pharmacist if you have any

concerns about the effects of

taking this medicine.

Do not be alarmed by the

following lists of side effects. You

may not experience any of them.

Tell your doctor or pharmacist if

you notice any of the following

and they worry you:

dry mouth

fast heart rate

reduced sweating

rash

itching

redness of the skin

a skin condition called

dyshidrosis (small blisters on

the hands and feet)

difficulty passing urine.

There have also been very rare

isolated reports of coma,

hallucinations (seeing, feeling or

hearing things that are not there),

dystonia (unusual muscle tone

causing distortion of the body),

confusion, agitation and dizziness.

These side effects were relieved

when the patients stopped Buscopan

therapy and received appropriate

medical treatment.

If any of the following happen,

tell your doctor immediately or go

to Emergency at your nearest

hospital:

allergic reactions (such as skin

rashes, or swelling of the face

and difficulty in breathing)

sudden life-threatening allergic

reactions (anaphylaxis with

episodes of shortness of breath

and shock).

Allergic reactions can be very

serious side effects. You may need

urgent medical attention or

hospitalisation.

Tell your doctor or pharmacist if

you notice anything that is

making you feel unwell.

Other side effects not listed above

may also occur in some people.

After taking

Buscopan

Storage

Keep your tablets in the pack

until it is time to take them.

If you take the tablets out of the

pack they may not keep well.

Keep your tablets in a cool dry

place where the temperature stays

below 25°C.

Do not store Buscopan or any

other medicine in the bathroom

or near a sink.

Do not leave it on a window sill or

in the car.

Heat and dampness can damage

some medicines.

Keep it 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

If the expiry date has passed, ask

your pharmacist what to do with

any medicine that is left over.

Product Description

Buscopan is available in blister

packs of 10*

, 20

and 100 tablets.

Australian Registration number on

outer carton is AUST R 48256.

* Not currently distributed in

Australia.

# Not available in New Zealand

What it looks like

Buscopan tablets are small, shiny

and white in colour.

Buscopan blister packs of 20 tablets

are available only at a pharmacy in

Australia.

Buscopan blister packs of 100

tablets are available only with a

doctor's prescription.

Ingredients

Buscopan contains 10 mg of

hyoscine butylbromide as the active

ingredient.

It also contains in the tablet core:

calcium hydrogen phosphate

maize starch

soluble starch

colloidal anhydrous silica

tartaric acid

stearic acid.

The sugar coating contains:

sucrose

povidone, purified talc

acacia

titanium dioxide

macrogol 6000

carnauba wax

white beeswax.

Supplier

Buscopan is supplied in Australia

Sanofi Consumer Healthcare,

87 Yarraman Place, Virginia,

Qld 4014 Australia.

Toll-free: 1800 818 806

Buscopan is supplied in New

Zealand by:

Sanofi-Aventis New Zealand

Limited,

Auckland, New Zealand.

Toll-free: 0800 283 684

Date of preparation: June 2018

buscopan-ccds0057-06-cmiv11-

28jun18

New Zealand Data Sheet

Buscopan & Buscopan Forte - Hyoscine butylbromide

Property of the Sanofi group - strictly confidential

Page 1

buscopan-ccdsv0-dsv4-04oct2018

DATA SHEET

1

BUSCOPAN AND BUSCOPAN FORTE

BUSCOPAN® 10 mg tablet and 20 mg/ml injection

BUSCOPAN® FORTE 20 mg film coated tablet

2

QUALITATIVE AND QUANTITATIVE COMPOSITION

Hyoscine-N-butylbromide 10 mg tablet, 20 mg film coated tablet and 20 mg/ml injection

Excipient with known effect: Lactose*

*Only applicable for the product BUSCOPAN® FORTE 20 mg film coated tablet.

For the full list of excipients, see Section 6.1.

3

PHARMACEUTICAL FORM

Tablet 10 mg: white, unmarked, biconvex, sugar-coated.

Tablet 20 mg: white, round, biconvex, film coated tablets embossed with the letter ‘B’ on one side

and the number ‘20’ on the other side.

Injection 20 mg/ml: clear, colourless solution in glass ampoules.

4

CLINICAL PARTICULARS

4.1

THERAPEUTIC INDICATIONS

Muscle spasm of the gastrointestinal tract.

New Zealand Data Sheet

Buscopan & Buscopan Forte - Hyoscine butylbromide

Property of the Sanofi group - strictly confidential

Page 2

buscopan-ccdsv0-dsv4-04oct2018

4.2

DOSE AND METHOD OF ADMINISTRATION

Oral:

Adults and children over 6 years:

2 BUSCOPAN 10 mg tablets (20 mg) four times a day

1 BUSCOPAN FORTE 20 mg tablet four times a day.

The tablets should be swallowed whole with adequate fluid.

Parenteral:

Adults and adolescents over 12 years 1 or 2 ampoules (20 – 40 mg) may be administered by slow

intravenous, intramuscular or subcutaneous injection several

times a day. A maximum daily dose of 100mg should not be

exceeded.

Infants and young children:

In severe cases, 0.3 - 0.6 mg/kg bodyweight, to be

administered by slow intravenous, intramuscular or

subcutaneous injection several times a day.The maximum

daily dose of 1.2 mg/kg should not be exceeded.

BUSCOPAN and BUSCOPAN FORTE should not be taken on a continuous daily basis or for

extended periods without investigating the cause of abdominal pain.

4.3

CONTRAINDICATIONS

BUSCOPAN and BUSCOPAN FORTE are contraindicated in myasthenia gravis, mechanical

stenosis in the gastrointestinal tract, paralytical or obstructive ileus, megacolon and in patients who

have demonstrated prior hypersensitivity to hyoscine butylbromide or any other component of the

products.

In addition, BUSCOPAN should not be administered parenterally in the following disorders:

untreated narrow angle glaucoma; tachycardia and hypertrophy of the prostate with urinary

retention.

By intramuscular injection BUSCOPAN is contraindicated in patients being treated with

anticoagulant drugs since intramuscular haematoma may occur. In these patients, the subcutaneous

or intravenous routes may be used.

In case of rare hereditary conditions that may be incompatible with an excipient of the product

(please refer to Section 4.4) the use of the product is contraindicated.

New Zealand Data Sheet

Buscopan & Buscopan Forte - Hyoscine butylbromide

Property of the Sanofi group - strictly confidential

Page 3

buscopan-ccdsv0-dsv4-04oct2018

4.4

SPECIAL WARNINGS AND PRECAUTIONS FOR USE

In case severe, unexplained abdominal pain persists or worsens, or occurs together with symptoms

like fever, nausea, vomiting, changes in bowel movements, abdominal tenderness, decreased blood

pressure, fainting or blood in stool, medical advice should immediately be sought where appropriate

diagnostic measures are needed to investigate the etiology of the symptoms.

Hyoscine may cause drowsiness: patients so affected should not drive or operate machinery. Patients

should abstain from alcohol. However, as a quaternary ammonium compound with low lipid

solubility, BUSCOPAN cannot cross the blood/brain barrier easily and only rarely causes the central

nervous system side effects associated with atropine and hyoscine.

After parenteral administration of BUSCOPAN, patients with visual accommodation disturbances

should not drive or operate machinery until vision has normalised.

Because of the potential risk of anticholinergic complications, BUSCOPAN and BUSCOPAN

FORTE tablets should be administered with caution in patients susceptible to narrow angle

glaucoma, intestinal or urinary outlet obstruction, and those inclined to tachyarrhythmia.

Elevation of intraocular pressure may be produced by the administration of anticholinergics such as

BUSCOPAN and BUSCOPAN FORTE in patients with undiagnosed and therefore untreated narrow

angle glaucoma. Therefore, patients should seek urgent ophthalmological advice if they should

develop a painful, red eye with loss of vision after the injection of BUSCOPAN and BUSCOPAN

FORTE.

After parenteral administration of BUSCOPAN, cases of anaphylaxis including episodes of shock

have been observed. As with all drugs causing such reactions, patients receiving BUSCOPAN by

injection should be kept under observation.

Caution is needed in patients with cardiac conditions submitted to parenteral treatment with

BUSCOPAN. Monitoring of these patient is advised.

BUSCOPAN injection can cause tachycardia, hypotension and anaphylaxis, therefore use with

caution in patients with cardiac conditions such as cardiac failure, coronary heart disease, cardiac

arrhythmia or hypertension, and in cardiac surgery. Monitoring of these patients is advised.

Emergency equipment and personnel trained in its use must be readily available.

One sugar-coated tablet of 10 mg contains 41.2 mg sucrose, resulting in 329.6 mg sucrose per

maximum recommended daily dose. Patients with the rare hereditary condition of fructose

intolerance should not take this medicine.

One film-coated tablet of 20 mg contains 138.5 mg lactose, resulting in 554 mg lactose per

maximum recommended daily dose. Patients with the rare hereditary conditions of galactose

intolerance e.g. galactosaemia, the Lapp lactase deficiency or glucose-galactose malabsorption

should not take this medicine.

New Zealand Data Sheet

Buscopan & Buscopan Forte - Hyoscine butylbromide

Property of the Sanofi group - strictly confidential

Page 4

buscopan-ccdsv0-dsv4-04oct2018

Paediatric use

Refer to Section 4.2 for information on paediatric dosing.

4.5

INTERACTION WITH OTHER MEDICINES AND OTHER FORMS OF INTERACTION

The anticholinergic effect of drugs such as tri- and tetracyclic antidepressants, antihistamines,

antipsychotics, quinidine, amantadine, disopyramide and other anticholinergics (e.g. tiotropium,

ipratropium, atropine-like compounds) may be intensified by BUSCOPAN and BUSCOPAN

FORTE.

Concomitant treatment with dopamine antagonists such as metoclopramide may result in diminution

of the effects of both drugs on the gastrointestinal tract.

The tachycardic effects of beta-adrenergic agents may be enhanced by BUSCOPAN and

BUSCOPAN FORTE.

4.6

FERTILITY, PREGNANCY AND LACTATION

There is limited data from the use of hyoscine-N-butylbromide in pregnant women.

Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity

(please refer to Section 5.3).

There is insufficient information on the excretion of hyoscine-N-butylbromide and its metabolites in

human milk.

As a precautionary measure, it is preferable to avoid the use of BUSCOPAN and BUSCOPAN

FORTE during pregnancy and lactation.

No studies on the effects on human fertility have been conducted (please refer to Section 5.3).

4.7

EFFECTS ON ABILITY TO DRIVE AND USE MACHINES

No studies on the effects on the ability to drive and use machines have been performed. However,

patients should be advised that they may experience undesirable effects such as accommodation

disorder or dizziness during treatment with BUSCOPAN injection. Therefore, caution should be

recommended when driving a car or operating machinery. If patients experience accommodation

disorder or dizziness, they should avoid potentially hazardous tasks such as driving or operating

machinery.

New Zealand Data Sheet

Buscopan & Buscopan Forte - Hyoscine butylbromide

Property of the Sanofi group - strictly confidential

Page 5

buscopan-ccdsv0-dsv4-04oct2018

4.8

UNDESIRABLE EFFECTS

Many of the listed undesirable effects can be assigned to the anticholinergic properties of

BUSCOPAN and BUSCOPAN FORTE. Anticholinergic side effects of BUSCOPAN and

BUSCOPAN FORTE are generally mild and self-limited.

Adverse events have been ranked under headings of frequency using the following convention: Very

common

≥ 1/10

Common

≥ 1/100, < 1/10

Uncommon

≥ 1/1,000, <1/100

Rare

≥ 1/10,000, <1/1,000

Very rare

<1/10,000

Not known

cannot be estimated from the available data

Immune system disorders

Not known: anaphylactic shock including fatal outcome, anaphylactoidic reactions, dyspnoea, skin

reactions (e.g. urticaria, rash, erythema, pruritus) and other hypersensitivity.

Eye disorders (BUSCOPAN injection)

Common: accommodation disorders

Not known*: mydriasis, increased intraocular pressure.

Cardiac disorders

Common: tachycardia

Vascular disorders (BUSCOPAN injection)

Not known: blood pressure decreased, dizziness, flushing.

Gastrointestinal disorders

Common: dry mouth

Skin and subcutaneous tissue disorders

Not known: dyshidrosis

Renal and urinary disorders

Not known: impaired micturition, urinary retention

New Zealand Data Sheet

Buscopan & Buscopan Forte - Hyoscine butylbromide

Property of the Sanofi group - strictly confidential

Page 6

buscopan-ccdsv0-dsv4-04oct2018

Nervous system disorders

Very rarely in the national post marketing surveillance data base, there have been isolated reports

following parenteral administration of coma, hallucinations, dystonia, confusion, agitation and

dizziness from which the patient recovered after drug withdrawal and appropriate treatment. In very

rare cases, dyspnoea has been reported.

Reporting of suspected adverse reactions

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

continued monitoring of the benefit/risk balance of the medicine. Healthcare professionals are asked

to report any suspected adverse reactions https://nzphvc.otago.ac.nz/reporting/.

4.9

OVERDOSE

Symptoms

Serious signs of poisoning following acute overdosage have not been observed in man. In case of

overdose, anticholinergic symptoms such as urinary retention, dry mouth, reddening of skin,

tachycardia, inhibition of gastrointestinal motility, and transient visual disturbances may occur.

Therapy

In the case of oral poisoning, gastric lavage with activated charcoal should be followed by

magnesium sulphate (15%). Symptoms of BUSCOPAN and BUSCOPAN FORTE overdosage

respond to parasympathomimetics. For patients with glaucoma, urgent ophthalmological advice

should be sought and pilocarpine should be given locally. If necessary, parasympathomimetics

should be administered, e.g. neostigmine 0.5-2.5 mg i.m. or i.v. Cardiovascular complications as a

result of using this medicine should be treated according to usual therapeutic principles. In case of

respiratory paralysis: intubation, artificial respiration should be considered. Catheterisation may be

required for urinary retention. In addition, appropriate supportive measures should be used as

required.

In the case of overdose, immediately contact the Poisons Information Centre, in New Zealand,

called 0800 764 766.

5

PHARMACOLOGICAL PROPERTIES

5.1

PHARMACODYNAMIC PROPERTIES

Pharmacotherapeutic group: Quanternary ammonium derivate, ATC code: A03BB01 Hyoscine-N-

butylbromide exerts a spasmolytic action on the smooth muscle of the

New Zealand Data Sheet

Buscopan & Buscopan Forte - Hyoscine butylbromide

Property of the Sanofi group - strictly confidential

Page 7

buscopan-ccdsv0-dsv4-04oct2018

gastrointestinal, biliary and urinary tracts. As a quaternary ammonium derivative, hyoscine-N-

butylbromide does not enter the central nervous system. Therefore, anticholinergic side effects at the

central nervous system do not occur. Peripheral anticholinergic effects result from a ganglion-

blocking action within the visceral wall as well as from anti-muscarinic activity.

5.2

PHARMACOKINETIC PROPERTIES

Absorption

As a quaternary ammonium compound, hyoscine-N-butylbromide is highly polar and hence only

partially absorbed following oral (8%) administration. After oral administration of single doses of

hyoscine butylbromide in the range of 20 to 400 mg, mean peak plasma concentrations between

0.11 ng/mL and 2.04 ng/mL were found at approximately 2 hours. In the same dose range, the

observed mean AUC0-tz-values varied from 0.37 to 10.7 ng h/mL. The median absolute

bioavailabilities of different dosage forms, i.e. coated tablets, suppositoires and oral solution,

containing 100 mg of hyoscine butylbromide each were found to be less than 1%.

Distribution

After intravenous administration hyoscine butylbromide is rapidly distributed (t

1/2α

= 4 min, t

1/2β

29 min) into the tissues. The volume of distribution (V

) is 128 L (corresponding to approx. 1.7

L/kg).

Because of its high affinity for muscarinic receptors and nicotinic receptors, hyoscine butylbromide

is mainly distributed on muscle cells of the abdominal and pelvic area as well as in the intramural

ganglia of the abdominal organs. Plasma protein binding (albumin) of hyoscine butylbromide is

approximately 4.4%. Animal studies demonstrate that hyoscine butylbromide does not pass the

blood-brain barrier, but no clinical data to this effect is available. Hyoscine butylbromide (1 mM)

has been observed to interact with the choline transport (1.4 nM) in epithelial cells of human

placenta

in vitro

Metabolism and elimination

Following oral administration of single doses in the range of 100 to 400 mg, the terminal elimination

half-lives ranged from 6.2 to 10.6 hours. The main metabolic pathway is the hydrolytic cleavage of

the ester bond. Orally administered hyoscine butylbromide is excreted in the faeces and in the urine.

Studies in man show that 2 to 5% of radioactive doses is eliminated renally after oral, and 0.7 to

1.6% after rectal administration. Approximately 90% of recovered radioactivity can be found in the

faeces after oral administration. The urinary excretion of hyoscine butylbromide is less than 0.1% of

the dose. The mean apparent oral clearances after oral doses of 100 to 400 mg range from 881 to

1420 L/min, whereas the corresponding volumes of distribution for the same range vary from 6.13

to 11.3 x 105 L, probably due to very low systemic availability. The metabolites excreted via the

renal route bind poorly to the muscarinic receptors and are therefore not considered to contribute to

the effect of the hyoscine butylbromide

New Zealand Data Sheet

Buscopan & Buscopan Forte - Hyoscine butylbromide

Property of the Sanofi group - strictly confidential

Page 8

buscopan-ccdsv0-dsv4-04oct2018

The half-life of the terminal elimination phase (t

1/2γ

) is approximately 5 hours. The total clearance is

1.2 L/min. Clinical studies with radiolabeled hyoscine butylbromide show that after intravenous

injection 42 to 61% of the radioactive dose is excreted renally and 28.3 to 37% faecally. The portion

of unchanged active ingredient excreted in the urine is approximately 50%. The metabolites

excreted via the renal route bind poorly to the muscarinic receptors and are therefore not considered

to contribute to the effect of the hyoscine butylbromide.

5.3

PRECLINICAL SAFETY DATA

Acutely, hyoscine butylbromide has a low index of toxicity: oral LD50 values were 1000-3000

mg/kg in mice, 1040-3300 mg/kg in rats, and 600 mg/kg in dogs. Toxic signs were ataxia and

decreased muscle tone, additionally, in mice tremor and convulsions, in dogs mydriasis, dry mucous

membranes and tachycardia. Deaths from respiratory arrest occurred within 24 h. The intravenous

LD50 values of hyoscine butylbromide were 10-23 mg/kg in mice and 18 mg/kg in rats.

In repeated oral dose toxicity studies over 4 weeks, rats tolerated 500 mg/kg = "no observed adverse

effect level (NOAEL)". At 2000 mg/kg, by the action on parasympathetic ganglia of visceral area,

hyoscine butylbromide paralysed the gastrointestinal function resulting in obstipation. Eleven out of

50 rats died. Haematology and clinical chemistry results did not show dose-related variations.

Over 26 weeks, rats tolerated 200 mg/kg, while at 250 and 1000 mg/kg, the gastro-intestinal

function was depressed and deaths occurred. The NOAEL of the 39-week oral (capsule) dog study

was 30 mg/kg. The majority of clinical findings were attributable to acute effects of hyoscine

butylbromide at high dosages (200 mg/kg). No adverse histopathological findings were observed.

A repeated intravenous dose of 1 mg/kg was well tolerated by rats in a 4-week study. At 3 mg/kg,

convulsions occurred immediately after injection. Rats dosed with 9 mg/kg died from respiratory

paralysis.

Dogs treated intravenously over 5 weeks at 2 x 1, 2 x 3 and 2 x 9 mg/kg, showed a dose- dependent

mydriasis in all treated animals, in addition at 2 x 9 mg/kg, ataxia, salivation and decreased body

weight and food intake were observed. The solutions were locally well tolerated.

After repeated i.m. injection, the dose of 10 mg/kg was systemically well tolerated, but lesions of

muscles at the site of injection were distinctly increased if compared to control rats. At 60 and 120

mg/kg, mortality was high and local damages were dose-dependently increased.

Hyoscine butylbromide was neither embryotoxic nor teratogenic at oral doses of up to 200 mg/kg in

the diet (rat) and 200 mg/kg by gavage or 50 mg/kg s.c. (rabbit). Fertility was not impaired at doses

of up to 200 mg/kg p.o.

Like other cationic drugs, hyoscine butylbromide interacts with the choline transport system of

human placental epithelial cells in vitro. Transfer of hyoscine butylbromide to the foetal

compartment has not been proved.

Hyoscine butylbromide-suppositories were locally well tolerated.

New Zealand Data Sheet

Buscopan & Buscopan Forte - Hyoscine butylbromide

Property of the Sanofi group - strictly confidential

Page 9

buscopan-ccdsv0-dsv4-04oct2018

In special studies concerning local tolerability, a repeated i.m. injection of 15 mg/kg BUSCOPAN

over 28 days was studied in dogs and monkeys. Small focal necroses at the site of injection were

seen only in dogs. BUSCOPAN was well tolerated in arteries and veins of the rabbit´s ear.

In vitro

2 % BUSCOPAN injectable solution showed no haemolytic action when mixed with 0.1 ml human

blood.

Hyoscine butylbromide revealed no mutagenic or clastogenic potential in the Ames test, in the

in

vitro

gene mutation assay in mammalian V79 cells (HPRT test) and in an

in vitro

chromosome

aberration test in human peripheral lymphocytes.

In vivo

, hyoscine butylbromide was negative in the

rat bone marrow micronucleus assay.

There are no

in vivo

carcinogenicity studies. Nevertheless, hyoscine butylbromide did not show a

tumorigenic potential in two oral 26-week-studies in rats given up to 1000 mg/kg.

6

PHARMACEUTICAL PARTICULARS

6.1

LIST OF EXCIPIENTS

10 mg Tablets:

dibasic calcium phosphate, maize starch, starch soluble, aerosil 200, tartaric acid,

stearic acid, polyvidone saccharose, talc, acacia, titanium dioxide, polyethylene glycol 6000,

carnauba wax, beeswax white.

20 mg Tablets:

povidone, lactose, cellulose - microcrystalline, magnesium stearate and Opadry II

white 85G18490.

Injection:

sodium chloride, water for injection

6.2

INCOMPATIBILITIES

None known.

6.3

SHELF LIFE

10 mg Tablets:

Shelf life is 36 months (3 years) from manufacture.

20 mg Tablets:

Shelf life is 36 months (3 years) from manufacture.

Injection Ampoules:

Shelf life is 60 months (5 years) from manufacture.

6.4

SPECIAL PRECAUTIONS FOR STORAGE

10 mg Tablets:

Store below 25ºC.

20 mg Tablets:

Store below 30ºC.

New Zealand Data Sheet

Buscopan & Buscopan Forte - Hyoscine butylbromide

Property of the Sanofi group - strictly confidential

Page 10

buscopan-ccdsv0-dsv4-04oct2018

Injection Ampoules:

Store below 30ºC.

6.5

NATURE AND CONTENTS OF CONTAINER

10 mg Tablets:

100s. PVC/PVDC/Al Blister pack or Plastic Bottle

20 mg Tablets:

10s. PVC/Al Blister pack

Injection Ampoules:

20 mg/mL, 1 mL, 5s. Ampoules

Not all pack sizes or pack types may be marketed.

6.6

SPECIAL PRECAUTIONS FOR DISPOSAL AND OTHER HANDLING

Injections: For single use only. Any unused solution should be discarded

7

MEDICINE SCHEDULE

10 mg Tablets:

Prescription Medicine.

20 mg Tablets:

Restricted Medicine.

Injection Ampoules:

Prescription Medicine.

8

SPONSOR

sanofi-aventis new zealand limited

Level 8

56 Cawley Street Ellerslie,

Auckland

New Zealand

Tel: 0800 283 684

9

DATE OF FIRST APPROVAL

BUSCOPAN: 31 December1969

BUSCOPAN FORTE: 26 February 2016

10

DATE OF REVISION OF THE TEXT

4 October 2018

New Zealand Data Sheet

Buscopan & Buscopan Forte - Hyoscine butylbromide

Property of the Sanofi group - strictly confidential

Page 11

buscopan-ccdsv0-dsv4-04oct2018

BUSCOPAN® is a registered trademark.

SUMMARY TABLE OF CHANGES

Section changed

Summary of new information

4.4, 4.8, 4.9

Update with safety information in line with AU PI

6.3, 6.4, 6.5, 7

Editorial changes

Similar products

Search alerts related to this product

Share this information