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STELAZINE 1MG TABLETS

Active substance(s): TRIFLUOPERAZINE HYDROCHLORIDE / TRIFLUOPERAZINE HYDROCHLORIDE / TRIFLUOPERAZINE HYDROCHLORIDE

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SUMMARY OF PRODUCT CHARACTERISTICS

1

NAME OF THE MEDICINAL PRODUCT
Stelazine 1mg Tablets or Trifluoperazine 1mg Tablets

2

QUALITATIVE AND QUANTITATIVE COMPOSITION

Each tablet contains Trifluoperazine hydrochloride equivalent to 1mg of
trifluoperazine

3

PHARMACEUTICAL FORM
Tablet
Blue aqueous film coated tablets marked ‘FW231’.

4

CLINICAL PARTICULARS

4.1

Therapeutic indications
Low dosage: ‘Stelazine’ is indicated as an adjunct in the short-term
management of anxiety states, depressive symptoms secondary to anxiety, and
agitation. It is also indicated in the symptomatic treatment of nausea and
vomiting.
High dosage: Treatment of symptoms and prevention of relapse in
schizophrenia and in other psychoses, especially of the paranoid type, but not
in depressive psychoses. It may also be used as an adjunct in the short-term
management of severe psychomotor agitation and of dangerously impulsive
behaviour in, for example, mental subnormality.

4.2

Posology and method of administration
Dosage:

Adults: Low dosage: 2-4 mg a day, given in divided doses, according to the
severity of the patient’s condition. If necessary, dosage may be increased to 6
mg a day, but above this level extrapyramidal symptoms are more likely to
occur in some patients.
High dosage: The recommended starting dose for physically fit adults is 5 mg
twice a day; after a week this may be increased to 15 mg a day. If necessary,
further increases of 5 mg may be made at three-day intervals, but not more
often. When satisfactory control has been achieved, dosage should be reduced
gradually until an effective maintenance level has been established.
As with all major tranquillisers clinical improvement may not be evident for
several weeks after starting treatment, and there may also be delay before
recurrence of symptoms after stopping treatment. Gradual withdrawal from
high-dosage treatment is advisable.
Children: Low dosage: For children aged 6-12 years, up to a maximum of 4
mg a day given in divided doses.
High dosage: For children aged under 12 years, the initial oral dosage should
not exceed 5mg a day, given in divided doses. Any subsequent increase
should be made with caution, at intervals of not less than three days, and
taking into account age, body weight and severity of symptoms.
Elderly: The starting dose for elderly or frail patients should be reduced by at least
half.
Administration:
Oral

4.3

Contraindications
Do not use ‘Stelazine’ in comatose patients, particularly is associated with
other central nervous system depressants. Do not use ‘Stelazine’ in those
patients with existing blood dyscrasias or known liver damage, or in those
hypersensitive to trifluoperazine, related compounds, or any of the excipients.
Patients with uncontrolled cardiac decompensation should not be given
‘Stelazine’.

4.4

Special warnings and precautions for use
‘Stelazine’ should be discontinued at the first sign of clinical symptoms of tardive
dyskinesia and Neuroleptic Malignant Syndrome.

Patients on long-term phenothiazine therapy require regular and careful surveillance
with particular attention to tardive dyskinesia and possible eye changes, blood
dyscrasias, liver dysfunction and myocardial conduction defects, particularly if other
concurrently administered drugs have potential effects in these systems.
Care should be taken when treating elderly patients, and the initial dosage should be
reduced. Such patients can be especially sensitive, particularly to extrapyramidal and
hypotensive effects. Patients with cardiovascular disease including arrhythmias
should also be treated with caution. Because ‘Stelazine’ may increase activity, care
should be taken in patients with angina pectoris. If an increase in pain is noted, the
drug should be discontinued. Patients who have demonstrated bone marrow
suppression or jaundice with a phenothiazine should not be re-exposed to ‘Stelazine
(or any trifluoperazine) unless in the judgement of the physician the potential benefits
of treatment outweigh the possible hazard.
In patients with Parkinson’s disease, symptoms may be worsened, and the effects of
levodopa reversed. Since phenothiazines may lower the convulsive threshold, patients
with epilepsy should be treated with caution, and metrizamide avoided. Although
‘Stelazine’ has minimal anticholinergic activity, this should be borne in mind when
treating patients with narrow angle glaucoma, myasthenia gravis or prostatic
hypertrophy.
Nausea and vomiting as a sign of organic disease may be masked by the antiemetic
action of ‘Stelazine’.
An approximately 3-fold increased risk of cerebrovascular adverse events have been
seen in randomised placebo controlled clinical trials in the dementia population with
some atypical antipsychotics. The mechanism for this increased risk is not known.
Stelazine should be used with caution in patients with risk factors for stroke
Caution should be used in patients with cardiovascular disease or family history of
QT prolongation. Concomitant use of neuroleptics should be avoided.
Cases of venous thromboembolism (VTE) have been reported with antipsychotic
drugs. Since patients treated with antipsychotics often present with acquired risk
factors for VTE, all possible risk factors for VTE should be identified before and
during treatment with Stelazine and preventive measures undertaken
Acute withdrawal symptoms including nausea, vomiting and insomnia have been
described after abrupt cessation of high doses of antipsychotic drugs. Recurrence of
psychotic symptoms may also occur, and the emergence of involuntary movement
disorders (such as akathisia, dystonia and dyskinesia) has been reported. Therefore, a
gradual withdrawal is advisable.
Phenothiazines should be used with care in extremes of temperature since they may
affect body temperature control.

Increased Mortality in Elderly people with Dementia
Data from two large observational studies showed that elderly people with dementia
who are treated with antipsychotics are at a small increased risk of death compared
with those who are not treated. There are insufficient data to give a firm estimate of
the precise magnitude of the risk and the cause of the increased risk is not known.
Stelazine is not licensed for the treatment of dementia-related behavioural
disturbances.

4.5

Interaction with other medicinal products and other forms of interaction
Potentiation may occur if antipsychotic drugs are combined with CNS depressants
such as alcohol, hypnotics, anaesthetics and strong analgesics, or with
antihypertensives or other drugs with hypotensive activity, anticholinergics or
antidepressants. Phenothiazines may antagonise the action of levodopa. Avoid drugs
that depress leucopoiesis.
Serum levels of phenothiazine can be reduced to non-therapeutic concentrations by
concurrent administration of lithium.
Desferrioxamine should not be used in combination with ‘Stelazine’, since prolonged
unconsciousness has occurred after combination with the related prochlorperazine.
Trifluoperazine may diminish the effect of oral anticoagulants.
Severe extrapyramidal side-effects or neurotoxicity have been observed in patients
concurrently treated with lithium and trifluoperazine. Sleep walking has been
described in some patients taking phenothiazines and lithium.
Antacids can reduce the absorption of phenothiazines.
Phenothiazines increase the risk of ventricular arrhythmias when given with drugs
which prolong the Q-T interval, drugs causing electrolyte imbalances.

4.6.

Pregnancy and lactation
‘Stelazine’ has been available since 1958. There are some animal studies that indicate
a teratogenic effect, but results are conflicting. There is no clinical evidence
(including follow-up surveys in over 800 women who had taken low-dosage
‘Stelazine’ during pregnancy) to indicate that trifluoperazine has a teratogenic effect
in man. Nevertheless, drug treatment should be avoided in pregnancy unless
essential, especially during the first trimester.
Neonates exposed to antipsychotics (including Trifluoperazine) during the third
trimester of pregnancy are at risk of adverse reactions including extrapyramidal
and/or withdrawal symptoms that may vary in severity and duration following
delivery. There have been reports of agitation, hypertonia, hypotonia, tremor,
somnolence, respiratory distress, or feeding disorder. Consequently, newborns should
be monitored carefully.

Trifluoperazine crosses the placenta and passes into the milk of lactating dogs; breast
feeding should only be allowed at the discretion of the physician.

4.7

Effects on ability to drive and use machines
Stelazine may cause side effects including drowsiness, dizziness and visual
disturbances which interfere with the ability to drive and operate machinery.
Do not drive or use machines when you first start to take this medicine until
you are certain that you are not getting these side effects

4.8.

Undesirable effects
Lassitude, drowsiness, dizziness, transient restlessness, insomnia, dry mouth, blurred
vision, muscular weakness, anorexia, mild postural hypotension, skin reactions
including photosensitivity reactions, weight gain, oedema and confusion may
occasionally occur. Tachycardia, constipation, urinary hesitancy and retention, and
hyperpyrexia have been reported very rarely. Adverse reactions tend to be doserelated and to disappear.
Hyperprolactinaemia may occur at higher dosages with associated effects such as
galactorrhoea, amenorrhoea or gynaecomastia; certain hormone-dependent breast
neoplasms may be affected. Phenothiazines can produce ECG changes with
prolongation of the QT interval and T-wave changes; ventricular arrhythmias(
VF,VT(rare)), sudden unexplained deaths; cardiac arrest and Torsades de pointes
have been reported. Such effects are rare with ‘Stelazine’.
In some patients, especially non-psychotic patients, ‘Stelazine’ even at low dosage
may cause unpleasant symptoms of being dulled or, paradoxically, of being agitated.
Extrapyramidal symptoms are rare at oral daily dosages of 6 mg or less; they are
considerably more common at higher dosage levels. These symptoms include
parkinsonism; akathisia, with motor restlessness and difficulty in sitting still; and
acute dystonia or dyskinesia, which may occur early in treatment and may present
with torticollis, facial grimacing, trismus, tongue protrusion and abnormal eye
movements including oculogyric crises. These effects are likely to be particularly
severe in children. Such reactions may often be controlled by reducing the dosage or
by stopping medication. In more severe dystonic reactions, an anticholinergic
antiparkinsonism drug should be given.
Tardive dyskinesia of the facial muscles, sometimes with involuntary movements of
the extremities, has occurred in some patients on long-term, high-dosage and, more
rarely, low-dosage phenothiazine therapy, including ‘Stelazine’. Symptoms may
appear for the first time either during or after a course of treatment; they may become
worse when treatment is stopped. The symptoms may persist for many months or
even years, and while they gradually disappear in some patients, they appear to be
permanent in others.

Patients have most commonly been elderly, female or with organic brain damage.
Particular caution should be observed in treating such patients.
Periodic gradual reduction of dosage to reveal persisting dyskinesia has been
suggested, so that treatment may be stopped if necessary.
Anticholinergic antiparkinsonism agents may aggravate the condition. Since the
occurrence of tardive dyskinesia may be related to length of treatment and dosage,
Trifluoperazine should be given for as short a time and at as low a dosage as possible
The neuroleptic malignant syndrome is a rare but occasionally fatal complication of
treatment with neuroleptic drugs, and is characterised by hyperpyrexia, muscle
rigidity, altered consciousness and autonomic instability. Intensive symptomatic
treatment, following discontinuation of ‘Stelazine’, should include cooling.
Intravenous dantrolene has been suggested for muscle rigidity.
Mild cholestatic jaundice and blood dyscrasias such as agranulocytosis, pancytopenia,
leucopenia and thrombocytopenia have been reported very rarely.
Signs of persistent infection should be investigated.
Very rare cases of skin pigmentation and lenticular opacities have been reported with
Stelazine’. Withdrawal reactions have been reported in association with antipyschotic
drugs(see 4.4)..
Cases of venous thromboembolism, including cases of pulmonary embolism and
cases of deep vein thrombosis have been reported with antipsychotic drugsFrequency unknown.

Pregnancy, puerperium and perinatal conditions-Drug withdrawal syndrome neonatal
(see 4.6) –Frequency not known.

4.9

Overdose
Signs and symptoms will be predominantly extrapyramidal; hypotension may
occur. Absorption of trifluoperazine from the ‘Spansule’ capsule is likely to
be prolonged and this should be borne in mind. Treatment consists of gastric
lavage together with supportive and symptomatic measures. Do not induce
vomiting. Extrapyramidal symptoms may be treated with an anticholinergic
antiparkinsonism drug. Treat hypotension with fluid replacement; if severe or
persistent, noradrenaline may be considered. Adrenaline is contra-indicated.

5

PHARMACOLOGICAL PROPERTIES

5.1

Pharmacodynamic properties
‘Stelazine’ is a Piperazine Phenothiazine tranquiliser with potent antipsychotic, anxiolytic and antiemetic activity, and a pharmacological profile of
moderate sedative and hypotensive properties, and fairly pronounced tendency
to cause extrapyramidal reactions.

5.2

Pharmacokinetic properties
Trifluoperazine is well absorbed but undergoes extensive first pass
metabolism. Distribution is wide and elimination occurs in the bile and urine.
Inactive ingredients in the tablets include sucrose.

5.3

Preclinical safety data
Not applicable.

6

PHARMACEUTICAL PARTICULARS

6.1

List of excipients
Calcium Sulphate
Icing sugar(Sucrose)
Maize Starch
Gelatin
Talc
Stearic acid
Coating
Opadry Blue OY -4492
Carnauba wax

Purified water

6.2

Incompatibilities
None known.

6.3

Shelf life
3 years.

6.4

Special precautions for storage
Do not store above 25°C. Protect from light and moisture.

6.5

Nature and contents of container
In opaque blister packs of 100 (4 x 25), 28, 56, 100, 112.
In securitainers of 28, 56, 100, 112, 1000, 5000.

6.6

Special precautions for disposal
Not applicable

7

MARKETING AUTHORISATION HOLDER

Mercury Pharmaceuticals Ltd
No. 1 Croydon,
12-16 Addiscombe Road,
Croydon CR0 0XT, UK

8

MARKETING AUTHORISATION NUMBER(S)
PL 12762/0030

9

DATE OF FIRST AUTHORISATION/RENEWAL OF THE
AUTHORISATION
01/08/1998 / 24/04/2003

10

DATE OF REVISION OF THE TEXT

27/07/2016

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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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