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VALOID 50 MG/ML INJECTION

Active substance(s): CYCLIZINE LACTATE

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PACKAGE LEAFLET: INFORMATION FOR THE USER

Valoid® 50 mg/ml Injection
(cyclizine lactate)

Read all of this leaflet carefully before you start taking this medicine
because it contains important information for you.
 Please keep this leaflet. You may need to read it again.
 If you have any further questions, ask your doctor or pharmacist.
 This medicine has been prescribed for you. Do not pass it on to others.
It may harm them, even if their symptoms are the same as yours.
 If you get any side effects, talk to your doctor or pharmacist.
This includes any possible side effects not listed in this leaflet. See
section 4.
 The name of this medicine is Valoid® 50 mg/ml Injection but it will be
referred to as Valoid Injection throughout the remainder of this leaflet.
What is in this leaflet
1. What Valoid Injection is and what is it used for
2. What you need to know before you are given Valoid Injection
3. How to use Valoid Injection
4. Possible side effects
5. How to store Valoid Injection
6. Contents of the pack and other information
1. WHAT VALOID INJECTION IS AND WHAT IS IT USED FOR
The name of your medicine is Valoid Injection.
Valoid Injection contains the active ingredient cyclizine lactate, which
belongs to a group of medicines called antihistamines which can be used to
help stop you feeling sick (nausea) or being sick (vomiting).
Valoid Injection may be used by adults. Valoid Injection may be used if you
suffer from travel or motion sickness; nausea caused by cancer treatment
(radiotherapy) or other medicines; or if you have had an operation, as
general anaesthetics can sometimes cause sickness.
Valoid can also be used to treat sickness caused by some inner ear
problems such as Meniere’s disease.

2. WHAT YOU NEED TO KNOW BEFORE YOU ARE GIVEN VALOID
INJECTION

Taking Valoid Injection with food and drink
Alcohol should be avoided when you are being treated with Valoid
Injection.

Do not take this medicine if:
 you have ever had an allergic reaction to cyclizine or any of the other
ingredients of this medicine (allergic reactions include mild symptoms
such as itching and/or rash. More severe symptoms include swelling of
the face, lips, tongue and/or throat with difficulty in swallowing or
breathing).
 you have been drinking alcohol. The anti-vomiting properties of Valoid
Injection may increase the toxicity of alcohol.

Pregnancy and breast-feeding
You should not be given Valoid Injection if you are pregnant or planning
to become pregnant or if you are breast-feeding.

Warnings and precautions
Take special care with this medicine and tell your doctor or
pharmacist before being treated with Valoid Injection if you:
 suffer from an eye disease caused by a rise of pressure within the eye
(glaucoma);
 suffer from urinary retention (experience difficulty passing urine);
 have an obstructive bowel condition;
 have any liver problems;
 suffer from phaeochromocytoma (tumour of the medulla of the adrenal
glands);
 suffer from high blood pressure;
 have epilepsy;
 are a man and you suffer from an enlarged prostate gland (difficulty or
slowness passing urine);
 have been told your heart is not working properly (heart failure);
 suffer from an inherited disorder which can lead to a sensitivity to sunlight
(porphyria);
 suffer from low blood pressure.
Other medicines and Valoid Injection
Tell your doctor if you are taking any other medicines especially the
following:
 medicines for problems such as depression, anxiety or difficulty in
sleeping;
 strong painkillers such as pethidine;
 any medicine which belong to a group of medicines called
anticholinergics.

Driving and using machinery
You can drive while being treated with Valoid but do not drive until you
know how it affects you. It may make you feel dizzy. If it affects you in this
way, do not drive or operate any machinery.
3. HOW TO USE VALOID INJECTION
You will be given Valoid Injection under supervision and your doctor will
decide on a dose which is right for you.
Valoid injection can be given as a slow injection into a vein
(intravenously) or by injection into a muscle (intramuscularly).
The recommended dose for adults is:
 50 mg up to three times a day.
For prevention of sickness after a normal operation:
Your doctor will give the first dose of Valoid by injection into a vein,
approximately 20 minutes before the end of the operation.
The use of the injectable form of Cyclizine has been associated with cases
of transient paralysis following administration of the medicine. The onset of
paralysis is usually within minutes of administration, affects the limbs, and
fully resolves within hours of discontinuation of the medicine.
If you receive more Valoid Injection than you should
As this medicine is given to you by a doctor, it is very unlikely that an
overdose will happen. Should an overdose occur, the doctor will treat
any symptoms that follow. Symptoms of overdose include dry mouth, nose
and throat, blurred vision, fast or irregular heartbeat, difficulty passing urine,
drowsiness, dizziness, lack of balance and coordination, weakness,
excitability, disorientation, impaired judgement, hallucinations, muscle
spasm, involuntary movements, convulsions, high temperature and difficulty
breathing.

Please tell your doctor if you are taking or have recently taken any other
medicines including those you have obtained without a prescription.

4. POSSIBLE SIDE EFFECTS
Like all medicines, Valoid Injection can cause side effects, although not
everybody gets them.
If you notice:
 itching or skin rashes;
 swelling of the face, lips or throat;
 difficulty in breathing or wheeziness.
Tell your doctor immediately. These may be signs of an allergic
reaction.
Side effects may include:
 skin rashes or itching;
 muscle twitches, spasms or tremors;
 restlessness;
 decrease in muscle tone that can cause irregular body movements;
 unusual body movements, particularly of your hands, arms or legs;
 lack of coordination;
 blurred vision or involuntary rolling of the eyes;
 paralysis especially in patient who are already suffering from disorder of
nerves and muscles;
 convulsions, seizures;
 nervousness;
 seeing or hearing things that are not really there (hallucinations);
 ringing in the ears;
 euphoria;
 headache;
 fast heartbeat, irregular heartbeat;
 drowsiness or general feelings of weakness/tiredness;
 a dry mouth, nose or throat;
 heartburn (reflux);
 stomach pain;
 nausea;
 vomiting;
 diarrhoea;
 loss of appetite;
 difficulty in passing water;


SUMMARY OF PRODUCT CHARACTERISTICS
1. NAME OF THE MEDICINAL PRODUCT
Valoid 50 mg/ml Injection
2.

QUALITATIVE AND QUANTITATIVE COMPOSITION
Each 1 ml ampoule contains 50 mg cyclizine lactate.
Excipients with known effect:
None

For a full list of excipients, see section 6.1.
3.
4.

PHARMACEUTICAL FORM
Clear, colourless solution for injection.
CLINICAL PARTICULARS

4.1. Therapeutic indications
Valoid is indicated in adults for the prevention and treatment of nausea and
vomiting including: Motion sickness when the oral route cannot be used.
 Nausea and vomiting caused by narcotic analgesics and by general
anaesthetics in the post-operative period.
 Vomiting associated with radiotherapy especially for breast cancer since
cyclizine does not elevate prolactin levels.
 Valoid injection, by the intravenous route, is also indicated pre-operatively
in patients undergoing emergency surgery in order to reduce the hazard
of regurgitation and aspiration of gastric contents during induction of
general anaesthesia.
Valoid may be of value in relieving vomiting and attacks of vertigo
associated with Menière’s disease and other forms of vestibular
disturbance when the oral route cannot be used.
4.2. Posology and method of administration
Posology

When used intravenously, Valoid should be injected slowly into the
bloodstream, with only minimal withdrawal of blood into the syringe.
For the prevention of postoperative nausea and vomiting, administer the
first dose by slow intravenous injection 20 minutes before the anticipated
end of surgery.
Cyclizine given intravenously, in half the recommended dose, increases the
lower oesophageal sphincter tone and thereby reduces the hazard of
regurgitation and aspiration of gastric contents if given to patients,
undergoing emergency surgery, before induction of general anaesthesia.
Older people
There have been no specific studies of Valoid in the elderly. Experience has
indicated that normal adult dosage is appropriate.
Paediatric population
Not licensed for use in children.
Method of Administration:
Intramuscularly or intravenously
4.3. Contraindications

There have been reports of abuse of cyclizine, either oral or intravenous, for
its euphoric or hallucinatory effects. The concomitant misuse of Valoid with
large amounts of alcohol is particularly dangerous, since the antiemetic
effect of cyclizine may increase the toxicity of alcohol (see also Section 4.5).
Case reports of paralysis have been received in patients using intravenous
cyclizine. Some of the patients mentioned in these case reports had an
underlying neuromuscular disorder. Thus intravenous cyclizine, should be
used with caution in all patients and with particular care in patients with
underlying neuromuscular disorders.
4.5. Interactions with other medicinal products and other forms of
interaction

4.8. Undesirable effects

Cardiac disorders
Tachycardia palpitations, arrhythmias (see section 4.4)

Valoid may counteract the haemodynamic benefits of opioid analgesics.

Valoid may mask the warning signs of damage caused by ototoxic drugs
such as aminoglycoside antibacterials.

4.4. Special warnings and precautions for use

4.6. Fertility, pregnancy and lactation

As with other anticholinergic agents, Valoid may precipitate incipient
glaucoma and it should be used with caution and appropriate monitoring in
patients with glaucoma, urinary retention, obstructive disease of the
gastrointestinal tract, hepatic disease, phaeochromocytoma, hypertension,
epilepsy and in males with possible prostatic hypertrophy. Valoid injection,
may have a hypotensive effect.

Pregnancy
In the absence of any definitive human data, the use of Valoid in pregnancy
is not advised.

Cyclizine should be avoided in porphyria.

Although there are no data available, patients should be cautioned that
Valoid may have additive effects with alcohol and other central nervous
system depressants, e.g. hypnotics and tranquillisers.

Valoid enhances the soporific effect of pethidine.

Valoid is contraindicated in the presence of acute alcohol intoxication.
The anti-emetic properties of cyclizine may increase the toxicity of alcohol.

Adults
50 mg intramuscularly or intravenously up to three times daily.

Patients should not drive or operate machinery until they have determined
their own response.

Blood and lymphatic system disorders
Agranulocytosis, leucopenia, haemolytic anaemia, thrombocytopenia.

Hypersensitivity to the active substance or to any of the excipients listed in
section 6.1.

For the prevention of postoperative nausea and vomiting, administer the
first dose by slow intravenous injection 20 minutes before the anticipated
end of surgery.

Studies designed to detect drowsiness did not reveal sedation in healthy
adults who took a single oral therapeutic dose (50 mg) of cyclizine, sedation
of short duration was reported by subjects receiving intravenous cyclizine.

Valoid may have additive effects with alcohol and other central nervous
system depressants e.g. hypnotics, tranquillisers, anaesthetics,
antipsychotics, barbiturates.

Because of its anticholinergic activity, cyclizine may enhance the
side-effects of other anticholinergic drugs, and may have an additive
antimuscarinic action with other antimuscarinic drugs, such as atropine and
some antidepressants (both tricyclics and MAOIs).

Cyclizine should be used with caution in patients with severe heart failure or
acute myocardial infarction. In such patients, cyclizine may cause a fall in
cardiac output associated with increases in heart rate, mean arterial
pressure and pulmonary wedge pressure.

4.7. Effects on ability to drive and use machines

Breast-feeding
Cyclizine is excreted in human milk, however, the amount has not been
quantified.
Fertility
In a study involving prolonged administration of cyclizine to male and
female rats, there was no evidence of impaired fertility after continuous
treatment for 90-100 days at dose levels of approximately 15 and 25 mg/kg/
day. There is no experience of the effect of Valoid on human fertility.

Eye disorders
Blurred vision, oculogyric crisis
Gastrointestinal system disorders
Dryness of the mouth, nose and throat, constipation, increased gastric
reflux, nausea, vomiting, diarrhoea, stomach pain, loss of appetite
General disorders and administration site conditions
Asthenia
Injection site reactions including vein tracking, erythema, pain,
thrombophlebitis and blisters. A sensation of heaviness, chills, and pruritus
have been reported rarely.
Anaphylaxis has been recorded following intravenous administration of
cyclizine co-administered with propanidid in the same syringe.
Hepatobiliary disorders
Hepatic dysfunction (see section 4.4), hypersensitivity hepatitis, cholestatic
jaundice and cholestatic hepatitis have occurred in association with
cyclizine.
Immune system disorders
Hypersensitivity reactions, including anaphylaxis have occurred.


















constipation;
difficulty in sleeping;
being confused, disorientated or unaware;
dizziness;
decreased consciousness/loss of consciousness;
temporary difficulty in speaking;
high blood pressure;
low blood pressure;
pins and needles;
yellowing of the skin and the whites of your eyes (jaundice);
a red or brownish patch which appears at the same spot each time you
take the medicine;
inflammation of the liver (hepatitis) or problems with the liver;
injection site reactions such as redness, pain, swelling or blistering;
sensations of heaviness, feeling cold or agitated or experiencing a
decrease in blood pressure;
reduced rate of breathing (apnoea);
reduction in the production of a type of white blood cell making infection
more likely (agranulocytosis).

5. HOW TO STORE VALOID INJECTION

 Valoid Injection will be stored by the hospital pharmacy before is given to








you. They will follow the instructions below.
Keep out of the sight and reach of children.
Do not store above 25oC.
Store in the original package.
Protect from light.
Do not use Valoid Injection if there are any particles floating in it or after
the expiry date which is stated on the carton and ampoule. The expiry
date refers to the last day of that month.
If your medicine become it discoloured or shows any signs of
deterioration, return it to your pharmacist.
Medicines should not be disposed of via wastewater or household waste.
Ask your pharmacist how to dispose of medicines no longer required.
These measures will help protect the environment.

6. CONTENTS OF THE PACK AND OTHER INFORMATION
What Valoid Injection contains
Each 1ml ampoule contains 50mg cyclizine lactate.
Also contains lactic acid and water for injections.
What Valoid Injection looks like and contents of the pack
Valoid Injection is a clear colourless solution for injection.
Valoid Injection comes in packs of 5 neutral glass ampoules.
Manufactured by
Cenexi SAS, 52, Rue Marcel et Jacques Gaucher,
94120 Fontenay sous Bois, France
Procured from within the EU by the Product Licence holder
MPT Pharma Ltd, Westgate Business Park, Unit 5-7 Tintagel Way,
Aldridge, Walsall WS9 8ER.
Repackaged by MPT Pharma Ltd.
PL: 33532/0614

If you feel very tired, experience unexpected bruising or bleeding or more
infections (e.g. colds and sore throats) than usual please tell your doctor.
Your doctor may decide to conduct tests on your blood periodically as a
result of these symptoms.

POM

Leaflet dated 9th February 2016
Leaflet coded xxxxxxxx
Valoid® is a registered trademark of Amdipharm Mercury International
Limited.

Reporting of side effects
If you get any side effects, talk to your doctor or pharmacist. This includes
any possible side effects not listed in this leaflet.
You can also report side effects directly via the Yellow Card Scheme,
website: www.mhra.gov.uk/yellowcard.
By reporting side effects you can help provide more information on the
safety of this medicine.


Musculoskeletal and connective tissue disorders
Twitching, muscle spasms
Nervous system disorders
Effects on the central nervous system have been reported with cyclizine
these include somnolence, drowsiness, incoordination, headache, dystonia,
dyskinesia, extrapyramidal motor disturbances, tremor, convulsions,
dizziness, decreased consciousness, transient speech disorders,
paraesthesia, paralysis* and generalised chorea.
* Case reports of paralysis have been received in patients using
intravenous cyclizine. Some of the patients mentioned in these case
reports had an underlying neuromuscular disorder (see Section 4.4).
Ear and labyrinth disorders
Tinnitus.
There have been rare case reports of patients experiencing depressed
levels of consciousness/loss of consciousness.
Psychiatric disorders
Disorientation, restlessness or agitation, nervousness, euphoria, insomnia
and auditory and visual hallucinations have been reported, particularly when
dosage recommendations have been exceeded.
Renal and urinary disorders
Urinary retention
Respiratory, thoracic and mediastinal disorders
Bronchospasm, apnoea
Skin and subcutaneous tissue disorders
Urticaria, pruritus, drug rash, angioedema, allergic skin reactions, fixed drug
eruption, photosensitivity
Vascular disorders
Hypertension, hypotension
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal
product is important. It allows continued monitoring of the benefit/risk
balance of the medicinal product. Healthcare professionals are asked to
report any suspected adverse reactions via the Yellow Card Scheme,
website: www.mhra.gov.uk/yellowcard.

4.9. Overdose

5.2. Pharmacokinetic properties

6.

Symptoms
Symptoms of acute toxicity from cyclizine arise from peripheral
anticholinergic effects and effects on the central nervous system.

Distribution
In healthy adult volunteers the administration of a single oral dose of 50 mg
cyclizine resulted in a peak plasma concentration of approximately
70 ng/mL occurring at about two hours after drug administration. The
plasma elimination half-life was approximately 20 hours.

6.1. List of excipients

Peripheral anticholinergic symptoms include, dry mouth, nose and throat,
blurred vision, tachycardia and urinary retention. Central nervous system
effects include drowsiness, dizziness, incoordination, ataxia, weakness,
hyperexcitability, disorientation, impaired judgement, hallucinations,
hyperkinesia, extrapyramidal motor disturbances, convulsions, hyperpyrexia
and respiratory depression.
An oral dose of 5 mg/kg is likely to be associated with at least one of the
clinical symptoms stated above. Younger children are more susceptible to
convulsions. The incidence of convulsions, in children less than 5 years, is
about 60% when the oral dose ingested exceeds 40 mg/kg.
Management
In the management of acute overdosage with Valoid, gastric lavage and
supportive measures for respiration and circulation should be performed if
necessary. Convulsions should be controlled in the usual way with
parenteral anticonvulsant therapy.
5.

PHARMACOLOGICAL PROPERTIES

5.1. Pharmacodynamic properties
ATC Code: R06AE
Pharmacotherapeutic Group: Piperazine derivatives
Mechanism of action:
Cyclizine is a histamine H1 receptor antagonist of the piperazine class which
is characterised by a low incidence of drowsiness. It possesses
anticholinergic and antiemetic properties. The exact mechanism by which
cyclizine can prevent or suppress both nausea and vomiting from various
causes is unknown. Cyclizine increases lower oesophageal sphincter tone
and reduces the sensitivity of the labyrinthine apparatus. It may inhibit the
part of the midbrain known collectively as the emetic centre.
Pharmacodynamics effects:
Cyclizine produces its antiemetic effect within two hours and lasts
approximately four hours.

Biotransformation
The N-demethylated derivative, norcyclizine, has been identified as a
metabolite of cyclizine. Norcyclizine has little antihistaminic (H1) activity
compared to cyclizine and has a plasma elimination half life of
approximately 20 hours.
Elimination
After a single dose of 50mg cyclizine given to a single adult male volunteer,
urine collected over the following 24 hours contained less than 1% of the
total dose administered.
5.3. Preclinical safety data

PHARMACEUTICAL PARTICULARS

Lactic Acid
Water for injections
6.2. Incompatibilities
None known. In the absence of compatibility studies, this medicinal
product must not be mixed with other medicinal products.
6.3. Shelf life
Four years
6.4. Special precautions for storage
Do not store above 25oC.
Store in the original package.
Protect from light.

A. Mutagenicity
Cyclizine was not mutagenic in a full Ames test, including use of
S9-microsomes but can nitrosate in vitro to form mutagenic products.

6.5. Nature and contents of container

B. Carcinogenicity
No long term studies have been conducted in animals to determine whether
cyclizine has a potential for carcinogenesis. However, long-term studies
with cyclizine administered with nitrate have indicated no carcinogenicity.

6.6. Special precautions for disposal and other handling

C. Teratogenicity
Some animal studies are interpreted as indicating that cyclizine may be
teratogenic at dose levels up to 25 times the clinical dose level. In another
study, cyclizine was negative at oral dose levels up to 65 mg/kg in rats and
75 mg/kg in rabbits. The relevance of these studies to the human situation
is not known.
D. Fertility
In a study involving prolonged administration of cyclizine to male and
female rats there was no evidence of impaired fertility after continuous
treatment for 90-100 days at dose levels of approximately 15 and 25 mg/kg/
day. There is no experience of the effect of Valoid on human fertility.

1ml neutral glass ampoules. Five ampoules in a carton.

No special instructions.
10. DATE OF REVISION OF THE TEXT
09th February 2016

PACKAGE LEAFLET: INFORMATION FOR THE USER

Cyclizine Lactate 50 mg/ml
Injection
Read all of this leaflet carefully before you start taking this medicine
because it contains important information for you.
 Please keep this leaflet. You may need to read it again.
 If you have any further questions, ask your doctor or pharmacist.
 This medicine has been prescribed for you. Do not pass it on to others.
It may harm them, even if their symptoms are the same as yours.
 If you get any side effects, talk to your doctor or pharmacist.
This includes any possible side effects not listed in this leaflet. See
section 4.
 The name of this medicine is Cyclizine Lactate 50 mg/ml Injection but it
will be referred to as Cyclizine Lactate Injection throughout the remainder
of this leaflet.
What is in this leaflet
1. What Cyclizine Lactate Injection is and what is it used for
2. What you need to know before you are given Cyclizine Lactate Injection
3. How to use Cyclizine Lactate Injection
4. Possible side effects
5. How to store Cyclizine Lactate Injection
6. Contents of the pack and other information
1. WHAT CYCLIZINE LACTATE INJECTION IS AND WHAT IS IT USED
FOR
The name of your medicine is Cyclizine Lactate Injection.
Cyclizine Lactate Injection contains the active ingredient cyclizine lactate,
which belongs to a group of medicines called antihistamines which can be
used to help stop you feeling sick (nausea) or being sick (vomiting).

2. WHAT YOU NEED TO KNOW BEFORE YOU ARE GIVEN CYCLIZINE
LACTATE INJECTION

Taking Cyclizine Lactate Injection with food and drink
Alcohol should be avoided when you are being treated with Cyclizine
Lactate Injection.

Do not take this medicine if:
 you have ever had an allergic reaction to cyclizine or any of the other
ingredients of this medicine (allergic reactions include mild symptoms
such as itching and/or rash. More severe symptoms include swelling of
the face, lips, tongue and/or throat with difficulty in swallowing or
breathing).
 you have been drinking alcohol. The anti-vomiting properties of Cyclizine
Lactate Injection may increase the toxicity of alcohol.

Pregnancy and breast-feeding
You should not be given Cyclizine Lactate Injection if you are pregnant or
planning to become pregnant or if you are breast-feeding.

Warnings and precautions
Take special care with this medicine and tell your doctor or
pharmacist before being treated with Cyclizine Lactate Injection if you:
 suffer from an eye disease caused by a rise of pressure within the eye
(glaucoma);
 suffer from urinary retention (experience difficulty passing urine);
 have an obstructive bowel condition;
 have any liver problems;
 suffer from phaeochromocytoma (tumour of the medulla of the adrenal
glands);
 suffer from high blood pressure;
 have epilepsy;
 are a man and you suffer from an enlarged prostate gland (difficulty or
slowness passing urine);
 have been told your heart is not working properly (heart failure);
 suffer from an inherited disorder which can lead to a sensitivity to sunlight
(porphyria);
 suffer from low blood pressure.

Cyclizine Lactate Injection may be used by adults. Cyclizine Lactate
Injection may be used if you suffer from travel or motion sickness; nausea
caused by cancer treatment (radiotherapy) or other medicines; or if you
have had an operation, as general anaesthetics can sometimes cause
sickness.

Other medicines and Cyclizine Lactate Injection
Tell your doctor if you are taking any other medicines especially the
following:
 medicines for problems such as depression, anxiety or difficulty in
sleeping;
 strong painkillers such as pethidine;
 any medicine which belong to a group of medicines called
anticholinergics.

Cyclizine Lactate can also be used to treat sickness caused by some inner
ear problems such as Meniere’s disease.

Please tell your doctor if you are taking or have recently taken any other
medicines including those you have obtained without a prescription.

SUMMARY OF PRODUCT CHARACTERISTICS
1. NAME OF THE MEDICINAL PRODUCT
Cyclizine Lactate 50 mg/ml Injection

When used intravenously, Cyclizine Lactate should be injected slowly into
the bloodstream, with only minimal withdrawal of blood into the syringe.

Driving and using machinery
You can drive while being treated with Cyclizine Lactate but do not drive
until you know how it affects you. It may make you feel dizzy. If it affects
you in this way, do not drive or operate any machinery.
3. HOW TO USE CYCLIZINE LACTATE INJECTION
You will be given Cyclizine Lactate Injection under supervision and your
doctor will decide on a dose which is right for you.
Cyclizine Lactate injection can be given as a slow injection into a vein
(intravenously) or by injection into a muscle (intramuscularly).
The recommended dose for adults is:
 50 mg up to three times a day.
For prevention of sickness after a normal operation:
Your doctor will give the first dose of Cyclizine Lactate by injection into a
vein, approximately 20 minutes before the end of the operation.
The use of the injectable form of Cyclizine has been associated with cases
of transient paralysis following administration of the medicine. The onset of
paralysis is usually within minutes of administration, affects the limbs, and
fully resolves within hours of discontinuation of the medicine.
If you receive more Cyclizine Lactate Injection than you should
As this medicine is given to you by a doctor, it is very unlikely that an
overdose will happen. Should an overdose occur, the doctor will treat
any symptoms that follow. Symptoms of overdose include dry mouth, nose
and throat, blurred vision, fast or irregular heartbeat, difficulty passing urine,
drowsiness, dizziness, lack of balance and coordination, weakness,
excitability, disorientation, impaired judgement, hallucinations, muscle
spasm, involuntary movements, convulsions, high temperature and difficulty
breathing.

4. POSSIBLE SIDE EFFECTS
Like all medicines, Cyclizine Lactate Injection can cause side effects,
although not everybody gets them.
If you notice:
 itching or skin rashes;
 swelling of the face, lips or throat;
 difficulty in breathing or wheeziness.
Tell your doctor immediately. These may be signs of an allergic
reaction.
Side effects may include:
 skin rashes or itching;
 muscle twitches, spasms or tremors;
 restlessness;
 decrease in muscle tone that can cause irregular body movements;
 unusual body movements, particularly of your hands, arms or legs;
 lack of coordination;
 blurred vision or involuntary rolling of the eyes;
 paralysis especially in patient who are already suffering from disorder of
nerves and muscles;
 convulsions, seizures;
 nervousness;
 seeing or hearing things that are not really there (hallucinations);
 ringing in the ears;
 euphoria;
 headache;
 fast heartbeat, irregular heartbeat;
 drowsiness or general feelings of weakness/tiredness;
 a dry mouth, nose or throat;
 heartburn (reflux);
 stomach pain;
 nausea;
 vomiting;
 diarrhoea;
 loss of appetite;
 difficulty in passing water;


2.

QUALITATIVE AND QUANTITATIVE COMPOSITION
Each 1 ml ampoule contains 50 mg cyclizine lactate.
Excipients with known effect:
None

For a full list of excipients, see section 6.1.
3.
4.

PHARMACEUTICAL FORM
Clear, colourless solution for injection.
CLINICAL PARTICULARS

4.1. Therapeutic indications
Cyclizine Lactate is indicated in adults for the prevention and treatment of
nausea and vomiting including: Motion sickness when the oral route cannot be used.
 Nausea and vomiting caused by narcotic analgesics and by general
anaesthetics in the post-operative period.
 Vomiting associated with radiotherapy especially for breast cancer since
cyclizine does not elevate prolactin levels.
 Cyclizine Lactate injection, by the intravenous route, is also indicated
pre-operatively in patients undergoing emergency surgery in order to
reduce the hazard of regurgitation and aspiration of gastric contents
during induction of general anaesthesia.
Cyclizine Lactate may be of value in relieving vomiting and attacks of
vertigo associated with Menière’s disease and other forms of vestibular
disturbance when the oral route cannot be used.
4.2. Posology and method of administration
Posology
For the prevention of postoperative nausea and vomiting, administer the
first dose by slow intravenous injection 20 minutes before the anticipated
end of surgery.
Adults
50 mg intramuscularly or intravenously up to three times daily.

For the prevention of postoperative nausea and vomiting, administer the
first dose by slow intravenous injection 20 minutes before the anticipated
end of surgery.

There have been reports of abuse of cyclizine, either oral or intravenous, for
its euphoric or hallucinatory effects. The concomitant misuse of Cyclizine
Lactate with large amounts of alcohol is particularly dangerous, since the
antiemetic effect of cyclizine may increase the toxicity of alcohol (see also
Section 4.5).

Cyclizine given intravenously, in half the recommended dose, increases the
lower oesophageal sphincter tone and thereby reduces the hazard of
regurgitation and aspiration of gastric contents if given to patients,
undergoing emergency surgery, before induction of general anaesthesia.

Case reports of paralysis have been received in patients using intravenous
cyclizine. Some of the patients mentioned in these case reports had an
underlying neuromuscular disorder. Thus intravenous cyclizine, should be
used with caution in all patients and with particular care in patients with
underlying neuromuscular disorders.

Older people
There have been no specific studies of Cyclizine Lactate in the elderly.
Experience has indicated that normal adult dosage is appropriate.

4.5. Interactions with other medicinal products and other forms of
interaction

Paediatric population
Not licensed for use in children.

Cyclizine Lactate may have additive effects with alcohol and other central
nervous system depressants e.g. hypnotics, tranquillisers, anaesthetics,
antipsychotics, barbiturates.

Method of Administration:
Intramuscularly or intravenously

Cyclizine Lactate enhances the soporific effect of pethidine.

4.3. Contraindications

Cyclizine Lactate may counteract the haemodynamic benefits of opioid
analgesics.

Hypersensitivity to the active substance or to any of the excipients listed in
section 6.1.
Cyclizine Lactate is contraindicated in the presence of acute alcohol
intoxication. The anti-emetic properties of cyclizine may increase the toxicity
of alcohol.
4.4. Special warnings and precautions for use
As with other anticholinergic agents, Cyclizine Lactate may precipitate
incipient glaucoma and it should be used with caution and appropriate
monitoring in patients with glaucoma, urinary retention, obstructive disease
of the gastrointestinal tract, hepatic disease, phaeochromocytoma,
hypertension, epilepsy and in males with possible prostatic hypertrophy.
Cyclizine Lactate injection, may have a hypotensive effect.
Cyclizine should be used with caution in patients with severe heart failure or
acute myocardial infarction. In such patients, cyclizine may cause a fall in
cardiac output associated with increases in heart rate, mean arterial
pressure and pulmonary wedge pressure.
Cyclizine should be avoided in porphyria.

Because of its anticholinergic activity, cyclizine may enhance the
side-effects of other anticholinergic drugs, and may have an additive
antimuscarinic action with other antimuscarinic drugs, such as atropine and
some antidepressants (both tricyclics and MAOIs).
Cyclizine Lactate may mask the warning signs of damage caused by
ototoxic drugs such as aminoglycoside antibacterials.
4.6. Fertility, pregnancy and lactation
Pregnancy
In the absence of any definitive human data, the use of Cyclizine Lactate in
pregnancy is not advised.
Breast-feeding
Cyclizine is excreted in human milk, however, the amount has not been
quantified.

Fertility
In a study involving prolonged administration of cyclizine to male and
female rats, there was no evidence of impaired fertility after continuous
treatment for 90-100 days at dose levels of approximately 15 and 25 mg/kg/
day. There is no experience of the effect of Cyclizine Lactate on human
fertility.
4.7. Effects on ability to drive and use machines
Studies designed to detect drowsiness did not reveal sedation in healthy
adults who took a single oral therapeutic dose (50 mg) of cyclizine, sedation
of short duration was reported by subjects receiving intravenous cyclizine.
Patients should not drive or operate machinery until they have determined
their own response.
Although there are no data available, patients should be cautioned that
Cyclizine Lactate may have additive effects with alcohol and other central
nervous system depressants, e.g. hypnotics and tranquillisers.
4.8. Undesirable effects
Blood and lymphatic system disorders
Agranulocytosis, leucopenia, haemolytic anaemia, thrombocytopenia.
Cardiac disorders
Tachycardia palpitations, arrhythmias (see section 4.4)
Eye disorders
Blurred vision, oculogyric crisis
Gastrointestinal system disorders
Dryness of the mouth, nose and throat, constipation, increased gastric
reflux, nausea, vomiting, diarrhoea, stomach pain, loss of appetite
General disorders and administration site conditions
Asthenia
Injection site reactions including vein tracking, erythema, pain,
thrombophlebitis and blisters. A sensation of heaviness, chills, and pruritus
have been reported rarely.
Anaphylaxis has been recorded following intravenous administration of
cyclizine co-administered with propanidid in the same syringe.


















constipation;
difficulty in sleeping;
being confused, disorientated or unaware;
dizziness;
decreased consciousness/loss of consciousness;
temporary difficulty in speaking;
high blood pressure;
low blood pressure;
pins and needles;
yellowing of the skin and the whites of your eyes (jaundice);
a red or brownish patch which appears at the same spot each time you
take the medicine;
inflammation of the liver (hepatitis) or problems with the liver;
injection site reactions such as redness, pain, swelling or blistering;
sensations of heaviness, feeling cold or agitated or experiencing a
decrease in blood pressure;
reduced rate of breathing (apnoea);
reduction in the production of a type of white blood cell making infection
more likely (agranulocytosis).

5. HOW TO STORE CYCLIZINE LACTATE INJECTION

 Cyclizine Lactate Injection will be stored by the hospital pharmacy before








is given to you. They will follow the instructions below.
Keep out of the sight and reach of children.
Do not store above 25oC.
Store in the original package.
Protect from light.
Do not use Cyclizine Lactate Injection if there are any particles floating in
it or after the expiry date which is stated on the carton and ampoule. The
expiry date refers to the last day of that month.
If your medicine become it discoloured or shows any signs of
deterioration, return it to your pharmacist.
Medicines should not be disposed of via wastewater or household waste.
Ask your pharmacist how to dispose of medicines no longer required.
These measures will help protect the environment.

6. CONTENTS OF THE PACK AND OTHER INFORMATION
What Cyclizine Lactate Injection contains
Each 1ml ampoule contains 50mg cyclizine lactate.
Also contains lactic acid and water for injections.
What Cyclizine Lactate Injection looks like and contents of the pack
Cyclizine Lactate Injection is a clear colourless solution for injection.
Cyclizine Lactate Injection comes in packs of 5 neutral glass ampoules.
Manufactured by
Cenexi SAS, 52, Rue Marcel et Jacques Gaucher,
94120 Fontenay sous Bois, France
Procured from within the EU by the Product Licence holder
MPT Pharma Ltd, Westgate Business Park, Unit 5-7 Tintagel Way,
Aldridge, Walsall WS9 8ER.
Repackaged by MPT Pharma Ltd.
PL: 33532/0614

If you feel very tired, experience unexpected bruising or bleeding or more
infections (e.g. colds and sore throats) than usual please tell your doctor.
Your doctor may decide to conduct tests on your blood periodically as a
result of these symptoms.

POM

Leaflet dated 9th February 2016
Leaflet coded xxxxxxxx

Reporting of side effects
If you get any side effects, talk to your doctor or pharmacist. This includes
any possible side effects not listed in this leaflet.
You can also report side effects directly via the Yellow Card Scheme,
website: www.mhra.gov.uk/yellowcard.
By reporting side effects you can help provide more information on the
safety of this medicine.


Hepatobiliary disorders
Hepatic dysfunction (see section 4.4), hypersensitivity hepatitis, cholestatic
jaundice and cholestatic hepatitis have occurred in association with
cyclizine.
Immune system disorders
Hypersensitivity reactions, including anaphylaxis have occurred.
Musculoskeletal and connective tissue disorders
Twitching, muscle spasms
Nervous system disorders
Effects on the central nervous system have been reported with cyclizine
these include somnolence, drowsiness, incoordination, headache, dystonia,
dyskinesia, extrapyramidal motor disturbances, tremor, convulsions,
dizziness, decreased consciousness, transient speech disorders,
paraesthesia, paralysis* and generalised chorea.
* Case reports of paralysis have been received in patients using
intravenous cyclizine. Some of the patients mentioned in these case
reports had an underlying neuromuscular disorder (see Section 4.4).
Ear and labyrinth disorders
Tinnitus.
There have been rare case reports of patients experiencing depressed
levels of consciousness/loss of consciousness.
Psychiatric disorders
Disorientation, restlessness or agitation, nervousness, euphoria, insomnia
and auditory and visual hallucinations have been reported, particularly when
dosage recommendations have been exceeded.
Renal and urinary disorders
Urinary retention
Respiratory, thoracic and mediastinal disorders
Bronchospasm, apnoea
Skin and subcutaneous tissue disorders
Urticaria, pruritus, drug rash, angioedema, allergic skin reactions, fixed drug
eruption, photosensitivity
Vascular disorders
Hypertension, hypotension

Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal
product is important. It allows continued monitoring of the benefit/risk
balance of the medicinal product. Healthcare professionals are asked to
report any suspected adverse reactions via the Yellow Card Scheme,
website: www.mhra.gov.uk/yellowcard.
4.9. Overdose

Mechanism of action:
Cyclizine is a histamine H1 receptor antagonist of the piperazine class which
is characterised by a low incidence of drowsiness. It possesses
anticholinergic and antiemetic properties. The exact mechanism by which
cyclizine can prevent or suppress both nausea and vomiting from various
causes is unknown. Cyclizine increases lower oesophageal sphincter tone
and reduces the sensitivity of the labyrinthine apparatus. It may inhibit the
part of the midbrain known collectively as the emetic centre.

Symptoms
Symptoms of acute toxicity from cyclizine arise from peripheral
anticholinergic effects and effects on the central nervous system.

Pharmacodynamics effects:
Cyclizine produces its antiemetic effect within two hours and lasts
approximately four hours.

Peripheral anticholinergic symptoms include, dry mouth, nose and throat,
blurred vision, tachycardia and urinary retention. Central nervous system
effects include drowsiness, dizziness, incoordination, ataxia, weakness,
hyperexcitability, disorientation, impaired judgement, hallucinations,
hyperkinesia, extrapyramidal motor disturbances, convulsions, hyperpyrexia
and respiratory depression.

5.2. Pharmacokinetic properties

An oral dose of 5 mg/kg is likely to be associated with at least one of the
clinical symptoms stated above. Younger children are more susceptible to
convulsions. The incidence of convulsions, in children less than 5 years, is
about 60% when the oral dose ingested exceeds 40 mg/kg.
Management
In the management of acute overdosage with Cyclizine Lactate, gastric
lavage and supportive measures for respiration and circulation should be
performed if necessary. Convulsions should be controlled in the usual way
with parenteral anticonvulsant therapy.
5.

PHARMACOLOGICAL PROPERTIES

5.1. Pharmacodynamic properties
ATC Code: R06AE
Pharmacotherapeutic Group: Piperazine derivatives

Distribution
In healthy adult volunteers the administration of a single oral dose of 50 mg
cyclizine resulted in a peak plasma concentration of approximately
70 ng/mL occurring at about two hours after drug administration. The
plasma elimination half-life was approximately 20 hours.
Biotransformation
The N-demethylated derivative, norcyclizine, has been identified as a
metabolite of cyclizine. Norcyclizine has little antihistaminic (H1) activity
compared to cyclizine and has a plasma elimination half life of
approximately 20 hours.
Elimination
After a single dose of 50mg cyclizine given to a single adult male volunteer,
urine collected over the following 24 hours contained less than 1% of the
total dose administered.
5.3. Preclinical safety data
A. Mutagenicity
Cyclizine was not mutagenic in a full Ames test, including use of
S9-microsomes but can nitrosate in vitro to form mutagenic products.
B. Carcinogenicity
No long term studies have been conducted in animals to determine whether
cyclizine has a potential for carcinogenesis. However, long-term studies
with cyclizine administered with nitrate have indicated no carcinogenicity.

C. Teratogenicity
Some animal studies are interpreted as indicating that cyclizine may be
teratogenic at dose levels up to 25 times the clinical dose level. In another
study, cyclizine was negative at oral dose levels up to 65 mg/kg in rats and
75 mg/kg in rabbits. The relevance of these studies to the human situation
is not known.
D. Fertility
In a study involving prolonged administration of cyclizine to male and
female rats there was no evidence of impaired fertility after continuous
treatment for 90-100 days at dose levels of approximately 15 and 25 mg/kg/
day. There is no experience of the effect of Cyclizine Lactate on human
fertility.
6.

PHARMACEUTICAL PARTICULARS

6.1. List of excipients
Lactic Acid
Water for injections
6.2. Incompatibilities
None known. In the absence of compatibility studies, this medicinal
product must not be mixed with other medicinal products.
6.3. Shelf life
Four years
6.4. Special precautions for storage
Do not store above 25oC.
Store in the original package.
Protect from light.
6.5. Nature and contents of container
1ml neutral glass ampoules. Five ampoules in a carton.
6.6. Special precautions for disposal and other handling
No special instructions.
10. DATE OF REVISION OF THE TEXT
9th February 2016

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Source: Medicines and Healthcare Products Regulatory Agency

Disclaimer: Every effort has been made to ensure that the information provided here is accurate, up-to-date and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. This information has been compiled for use by healthcare practitioners and consumers in the United States. The absence of a warning for a given drug or combination thereof in no way should be construed to indicate that the drug or combination is safe, effective or appropriate for any given patient. If you have questions about the substances you are taking, check with your doctor, nurse or pharmacist.

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