VALOID 50MG TABLETS

SUMMARY OF PRODUCT CHARACTERISTICS

1

NAME OF THE MEDICINAL PRODUCT
Valoid 50 mg Tablets
Cyclizine Hydrochloride 50 mg Tablets

2

QUALITATIVE AND QUANTITATIVE COMPOSITION
Each tablet contains 50 mg of cyclizine hydrochloride.
Excipient with known effect:
Lactose.
For a full list of excipients, see section 6.1.

3

PHARMACEUTICAL FORM
White, biconvex, uncoated tablet, scored; coded T4A.

The scoreline is only to facilitate breaking for ease of swallowing and not to
divide into equal doses

4

CLINICAL PARTICULARS

4.1

Therapeutic indications
Cyclizine Hydrochloride is indicated in adults and in children aged 6 years and over
for the prevention and treatment of nausea and vomiting including:•

Motion sickness.

•

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 Hydrochloride may be of value in relieving vomiting and attacks of
vertigo associated with Menière's disease and other forms of vestibular
disturbance.

4.2

Posology and method of administration
Posology
To prevent motion sickness Cyclizine Hydrochloride should be taken about
one to two hours before departure.

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

Paediatric population
Children less than 6 years of age:
Cyclizine Hydrochloride tablets are not recommended for children less than 6
years of age.
Children 6 to 12 years of age:
25 mg orally, which may be repeated up to three times a day.
Children over 12 years of age:
50 mg orally, which may be repeated up to three times a day.
Adults
50 mg orally, which may be repeated up to three times a day.
Method of administration:
Oral

4.3

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

Cyclizine 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 Hydrochloride 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 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 2associated 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 Cyclizine
Hydrochloride with large amounts of alcohol is particularly dangerous, since
the antiemetic effect of cyclizine may increase the toxicity of alcohol (see also
sections 4.3 and 4.5).
Cyclizine Hydrochloride contains lactose
Patients with rare hereditary problems of galactose intolerance, the Lapp
lactase deficiency or glucose-galactose malabsorption should not take this
medicine.

4.5

Interaction with other medicinal products and other forms of interaction
Cyclizine Hydrochloride may have additive effects with alcohol and other central
nervous system depressants e.g. hypnotics, tranquillisers, anaesthetics antipsychotics,
barbiturates.
Cyclizine Hydrochloride enhances the soporific effect of pethidine.
Cyclizine Hydrochloride may counteract the haemodynamic benefits of opioid
analgesics.
Because of its anticholinergic activity cyclizine may enhance the side-effects of other
anticholinergic drugs, and have an additive antimuscarinic action with other
antimuscarinic drugs, such as atropine and some antidepressants (both tricyclics and
MAOIs).

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

4.6

Pregnancy and lactation
Pregnancy
In the absence of any definitive human data, the use of Cyclizine
Hydrochloride 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 Hydrochloride 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.
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
Hydrochloride 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.
Immune system disorders
Hypersensitivity reactions, including anaphylaxis have occurred
Psychiatric disorders

Disorientation, restlessness, nervousness, euphoria, insomnia and auditory and visual
hallucinations have been reported, particularly when dosage recommendations have
been exceeded.
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.
Eye disorders
Blurred vision, oculogyric crisis
Cardiac disorders
Tachycardia, palpitations, arrhythmias
Vascular disorders
Hypertension, hypotension
Respiratory, thoracic and mediastinal disorders
Bronchospasm, apnoea
Gastrointestinal disorders
Dryness of the mouth, nose and throat, constipation increased gastric reflux.
Nausea, vomiting, diarrhoea stomach pain
Loss of appetite
Hepatobiliary disorders
Hepatic dysfunction, hypersensitivity hepatitis, cholestatic jaundice and cholestatic
hepatitis have occurred in association with cyclizine.
Skin and subcutaneous tissue disorders
Urticaria, drug rash, angioedema, allergic skin reactions, fixed drug eruption
photosensitivity

Musculoskeletal and connective tissue disorders
Twitching, muscle spasms
Renal and urinary disorders
Urinary retention
General disorders and administration site conditions
Asthenia
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
Symptoms:
Symptoms of acute toxicity from cyclizine arise from peripheral anticholinergic
effects and effects on the central nervous system.
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 Cyclizine Hydrochloride, 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.
Pharmacodynamic effects:
Cyclizine produces its antiemetic effect within two hours and lasts approximately
four hours.

5.2

Pharmacokinetic properties
H1-blockers are well absorbed from the GI tract. Following oral administration
effects develop within 30 minutes, are maximal within 1-2 hours and last, for
cyclizine, for 4-6 hours.
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.
The N-demethylated derivative, norcyclizine, has been identified as a metabolite of
cyclizine. Norcyclizine has little antihistaminic (H1) activity compared to cyclizine.
It is widely distributed throughout the tissues and has a plasma elimination half-life of
approximately 20 hours.
After a single dose of 50 mg 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.
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. There is no experience of the effect of Cyclizine Hydrochloride Tablets on
human fertility.

6

PHARMACEUTICAL PARTICULARS

6.1

List of excipients
Lactose
Potato starch
Acacia
Magnesium stearate

6.2

Incompatibilities
None known

6.3

Shelf life
60 months

6.4

Special precautions for storage
Store below 25°C.

6.5

Nature and contents of container
Amber glass or polyethylene bottles with polyethylene tamper evident caps for
pack size 100 tablets.

6.6

Special precautions for disposal
No special instructions

7

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

8

MARKETING AUTHORISATION NUMBER(S)
PL 20072/0241

9

DATE OF FIRST AUTHORISATION/RENEWAL OF THE
AUTHORISATION
01/1/2001 / 05/12/2005

10

DATE OF REVISION OF THE TEXT
27/03/2015