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CYCLIZINE LACTATE 50 MG/ML INJECTION

Active substance(s): CYCLIZINE LACTATE

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Package leaflet: Information for the patient

28034640

103059/LF/3 28034640

Univers

Valoid® 50 mg/ml Injection
Cyclizine Lactate

Valoid 50mg/1ml Inj
103059/LF/3
Leaflet
148 x 630mm
Great Britain
28034640
TBC
100%
Black
18/03/2014
8 pt
2
AMCo
CNC

REGULATORY AUTHORITY
APPROVAL CONFIRMATION
Confirmation that this artwork has been approved by
the appropriate market authority (if applicable, e.g.
MHRA, IMB, etc and that Amdipharm have license
approval to distribute this component for sale in the
relevent market.
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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.
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 Valoid Injection is given
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
IT IS 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
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.
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.
Please tell your doctor if you are taking or
have recently taken any other medicines
including those you have obtained without a
prescription.
Taking Valoid Injection with food and drink
Alcohol should be avoided when you are
being treated with Valoid Injection.
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.
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 VALOID INJECTION IS GIVEN
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.
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.

SUMMARY OF PRODUCT CHARACTERISTICS
VALOID INJECTION
SUMMARY OF PRODUCT CHARACTERISTICS
1. NAME OF THE MEDICINAL PRODUCT
Valoid 50 mg/ml Injection
Cyclizine Lactate 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. PHARMACEUTICAL FORM
Clear, colourless solution for injection.
4. 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
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.
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
Hypersensitivity to the active substance or to
any of the excipients listed in section 6.1.
Valoid 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, 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.
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.
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).
There have been isolated case reports of
transient paralysis occurring in patients using
intravenous cyclizine. Two of the patients
mentioned in these reports had an underlying
neuromuscular disorder. Thus intravenous
cyclizine should be used with caution in all
patients in general, and in patients with
underlying neuromuscular disorders in
particular.
4.5. Interactions with other medicinal
products and other forms of interaction
Valoid may have additive effects with alcohol
and other central nervous system depressants
e.g. hypnotics, tranquillisers, anaesthetics,
antipsychotics, barbiturates.
Valoid enhances the soporific effect of pethidine.
Valoid may counteract the haemodynamic
benefits of opioid analgesics.
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).
Valoid 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 Valoid 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 Valoid 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 Valoid 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
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.
Hepatobiliary disorders
Hepatic dysfunction, hypersensitivity hepatitis,
cholestatic jaundice and cholestatic hepatitis
have occurred in association with cyclizine.

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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;

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;

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).

6.

CONTENTS OF THE PACK AND OTHER
INFORMATION
What Valoid Injection contains
Valoid injection comes as a 1 ml ampoule
containing 50 mg of the active ingredient,
cyclizine lactate, dissolved in sterile water.
The injection also contains the inactive
ingredient, lactic acid.
What Valoid Injection looks like and the
contents of the pack
Valoid Injection is a clear, colourless
solution. Each pack contains 5 ampoules.
Marketing Authorisation Holder and
Manufacturer responsible for release
Amdipharm UK Limited,
Capital House,
85 King William Street,
London EC4N 7BL,
UK
Valoid is a registered trademark of
Amdipharm Mercury International Limited
This leaflet was last revised in March 2014

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.
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.
5. HOW TO STORE VALOID INJECTION
Valoid Injection will be stored by the hospital
pharmacy before it is given to you. They will
follow the instructions below. Valoid Injection
should be stored in a safe place below 25°C
and protected from light. The injection
should not be used if there are any particles
floating in it or after the “use by” date on
the pack.
KEEP THIS MEDICINE OUT OF THE SIGHT
AND REACH OF CHILDREN.

28034640

Immune system disorders
Hypersensitivity reactions, including anaphylaxis
have occurred.

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

Musculoskeletal and connective tissue disorders
Twitching, muscle spasms

5.2. Pharmacokinetic properties

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 and generalised chorea.
Ear and labyrinth disorders Tinnitus.
There have been rare case reports of patients
experiencing depressed levels of consciousness/
loss of consciousness. The use of cyclizine has
been associated with cases of transient paralysis
following administration of the intravenous
formulation 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 (see also Section 4.4).
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.

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 Valoid on human fertility.

4.9. Overdose

6.

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

6.1. List of excipients
Lactic Acid
Water for Injections

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.

PHARMACEUTICAL PARTICULARS

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
Store below 25ºC
Protect from light, keep the ampoule in the
outer carton.
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.
7.

MARKETING AUTHORISATION HOLDER
Amdipharm UK Limited,
Capital House,
85 King William Street,
London EC4N 7BL, UK

8.

MARKETING AUTHORISATION NUMBER
PL 20072/0010

9.

DATE OF FIRST AUTHORISATION/
RENEWAL OF AUTHORISATION
Date of first authorisation: 05 December
2005
Date of latest renewal: 31 October 2008

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.

10. DATE OF REVISION OF THE TEXT

Page 2

March 2014

2803464

Valoid 50mg/1ml Inj
103059/LF/3
Leaflet
148 x 630mm
Great Britain
28034640
TBC
100%
Black
18/03/2014
8 pt
2
AMCo
CNC

REGULATORY AUTHORITY
APPROVAL CONFIRMATION
Confirmation that this artwork has been approved by
the appropriate market authority (if applicable, e.g.
MHRA, IMB, etc and that Amdipharm have license
approval to distribute this component for sale in the
relevent market.
Accept Artwork ................................................................
Reject Artwork .................................................................
Signature ..........................................................................
Name ................................................................................
Date ...................................................................................

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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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