Consumer medicine information

NAUSETIL

Prochlorperazine maleate

BRAND INFORMATION

Brand name

Nausetil

Active ingredient

Prochlorperazine maleate

Schedule

SUMMARY CMI

NAUSETIL

Consumer Medicine Information (CMI) summary

The full CMI on the next page has more details. If you are worried about using this medicine, speak to your doctor or pharmacist.

1. Why am I using NAUSETIL?

NAUSETIL contains the active ingredient prochlorperazine maleate. NAUSETIL is used to treat nausea associated with migraine (severe headache).

For more information, see Section 1. Why am I using NAUSETIL? in the full CMI.

2. What should I know before I use NAUSETIL?

Do not use if you have ever had an allergic reaction to NAUSETIL or any of the ingredients listed at the end of the CMI.

Talk to your doctor if you have any other medical conditions, take any other medicines, or are pregnant or plan to become pregnant or are breastfeeding.

For more information, see Section 2. What should I know before I use NAUSETIL? in the full CMI.

3. What if I am taking other medicines?

Some medicines may interfere with NAUSETIL and affect how it works.

A list of these medicines is in Section 3. What if I am taking other medicines? in the full CMI.

4. How do I use NAUSETIL?

Your doctor or pharmacist will tell you how much NAUSETIL you will need to take each day.
For adults, the usual recommended dose is 1 or 2 tablets two to three times daily.

More instructions can be found in Section 4. How do I use NAUSETIL? in the full CMI.

5. What should I know while using NAUSETIL?

Things you should do	Remind any doctor, dentist or pharmacist you visit that you are using NAUSETIL. Tell your doctor if you notice any uncontrolled movements of the tongue, face, mouth or jaw, such as puffing of the cheeks, puckering of the mouth or chewing movements. If outdoors, wear protective clothing and use at least a SPF 15+ sunscreen.
Things you should not do	Do not give NAUSETIL to children and adolescents under 18 years of age.
Driving or using machines	Be careful driving or operating machinery until you know how NAUSETIL affects you. It may cause dizziness, light-headedness, tiredness and drowsiness especially in the first few days of treatment
Drinking alcohol	Be careful when drinking alcohol while taking NAUSETIL. If you drink alcohol, dizziness or lightheadedness may be worse.
Looking after your medicine	Keep your tablets in a cool dry place that is protected from light.

For more information, see Section 5. What should I know while using NAUSETIL? in the full CMI.

6. Are there any side effects?

Tell your doctor or pharmacist as soon as possible if you do not feel well while you are taking NAUSETIL. Some common side effects include constipation, dry mouth, drowsiness, trembling, rigid posture, twitching and blurry vision.

For more information, including what to do if you have any side effects, see Section 6. Are there any side effects? in the full CMI.

FULL CMI

NAUSETIL

Active ingredient(s): Prochlorperazine maleate

Consumer Medicine Information (CMI)

This leaflet provides important information about using NAUSETIL. You should also speak to your doctor or pharmacist if you would like further information or if you have any concerns or questions about using NAUETIL.

Where to find information in this leaflet:

1. Why am I using NAUSETIL?
2. What should I know before I use NAUSETIL?
3. What if I am taking other medicines?
4. How do I use NAUSETIL?
5. What should I know while using NAUSETIL?
6. Are there any side effects?
7. Product details

1. Why am I using NAUSETIL?

NAUSETIL contains the active ingredient prochlorperazine maleate. NAUSETIL is a phenothiazine, which helps to correct chemical imbalances in the brain allowing it to function correctly. These chemicals may also affect the parts of the brain which control nausea.

NAUSETIL is used to treat nausea associated with migraine (severe headache).

There is no evidence that it is addictive.

2. What should I know before I use NAUSETIL?

Warnings

Do not use NAUSETIL if:

you are taking other medicines that cause drowsiness
you have medical conditions such as:
- shock
- disease of the blood with a low number of blood cells
- being unconscious or in a coma
you are allergic to prochlorperazine, the group of medicines called phenothiazines, or any of the ingredients listed at the end of this leaflet.

Always check the ingredients to make sure you can use this medicine.

Symptoms of an allergic reaction may include asthma, wheezing, shortness of breath, swelling of the face, lips or tongue which may cause difficulty in swallowing or breathing, skin rash, itching or hives.

Check with your doctor if you:

Have any other medical conditions

phaechromocytoma, a rare tumour of the adrenal glands which sit near the kidneys
Parkinson's disease, a disease of the brain affecting movement which causes trembling, rigid posture, slow movement and a shuffling, unbalanced walk
myasthenia gravis, a disease of the muscles causing drooping eyelids, double vision, difficulty in speaking and swallowing and sometimes muscle weakness in the arms or legs
kidney problems
heart and blood vessel problems, low blood pressure, blood clots
liver disease
prostate problems
epilepsy, seizures or fits
low blood calcium levels
an underactive thyroid gland
glaucoma, a condition in which there is usually a build-up of fluid in the eye
neuroleptic malignant syndrome, a reaction to some medicines with a sudden increase in body temperature, extremely high blood pressure and severe convulsions
a reaction to some medicines with uncontrollable twitching or jerking movements of the arms and legs
dementia (especially in the elderly)
high blood sugar levels.
agranulocytosis, which affects blood count
schizophrenia, a mental illness.

Take any medicines for any other condition.

During treatment, you may be at risk of developing certain side effects. It is important you understand these risks and how to monitor for them. See additional information under Section 6. Are there any side effects?

Pregnancy and breastfeeding

Check with your doctor if you are pregnant or intend to become pregnant.

Like most phenothiazine medicines, NAUSETIL is not recommended for use during pregnancy. If there is a need to take this medicine during your pregnancy, your doctor will discuss with you the benefits and risks of taking it.

Talk to your doctor if you are breastfeeding or intend to breastfeed.

It is not recommended to take NAUSETIL while breastfeeding as it is not known whether it passes into breast milk.

Use in Elderly

NAUSETIL should be used with caution in the elderly particularly during very hot or very cold weather.

The elderly is more likely to experiencing dizziness and drowsiness.

Use in Children

NAUSETIL is not recommended for use in children and adolescents under 18 years of age.

3. What if I am taking other medicines?

Tell your doctor or pharmacist if you are taking any other medicines, including any medicines, vitamins or supplements that you buy without a prescription from your pharmacy, supermarket or health food shop.

Some medicines may interfere with NAUSETIL and affect how it works. These include:

some medicines used to control depression, mood swings or mental illness such as lithium
alcohol
desferrioxamine, a drug used in iron overdose
certain anticancer medicines such as procarbazine
some medicines used to control epilepsy
medicines used to treat Parkinson's disease
anticholinergic medicines which are used to relieve stomach cramps, spasms and travel sickness
atropine, a medicine which may be used in some eye drops or cough and cold preparations
medicines that prevent blood clotting
medicines used to treat high blood pressure and fluid build-up in your body such as guanethidine, clonidine
medicines that treat heart conditions
certain laxatives
some antibiotics
amfetamine, a stimulant drug
adrenaline, bepridil, cisapride, sultopride, thioridazine, methadone, erythromycin injection, vincamine injection, halofantrine, pentamidine, sparfloxacin, amphotericin B injection, glucocorticoids, tetracosactides (tetracosactrin).

Check with your doctor or pharmacist if you are not sure about what medicines, vitamins or supplements you are taking and if these affect NAUSETIL.

4. How do I use NAUSETIL?

How much to take

Your doctor or pharmacist will tell you how much NAUSETIL you will need to take each day. This depends on your condition and whether or not you are taking any other medicines.
For adults, the usual recommended dose is 1 or 2 tablets two to three times daily.
For acute treatment, 4 tablets at once followed if necessary, by 2 tablets two hours later, may be taken.
The elderly or patients who have a pre-existing liver condition may need to take fewer tablets.

When to take NAUSETIL

It does not matter if you take NAUSETIL before or after food.

How to take NAUSETIL

Swallow the tablet whole with a full glass of water.
Do not chew the tablet.

If you use too much NAUSETIL

If you think that you have used too much NAUSETIL, you may need urgent medical attention.

You should immediately:

phone the Poisons Information Centre
(by calling 13 11 26), or
contact your doctor, or
go to the Emergency Department at your nearest hospital.

You should do this even if there are no signs of discomfort or poisoning.

Symptoms of overdose may include tiredness, coma, restlessness, shaking, muscle twitching, muscle weakness, spasm, confusion, excitement or agitation, low blood pressure, fast heart beat, decrease body temperature, small pupils in the eye, difficulty in swallowing or breathing, or blue skin, difficulty speaking, or convulsions.

5. What should I know while using NAUSETIL?

Things you should do

If outdoors, wear protecting clothing and use at least a SPF 15+ sunscreen. NAUSETIL may cause your skin to be much more sensitive to sunlight than it is normally. Exposure to sunlight may cause a skin rash, itching, redness or severe sunburn.
Make sure you keep cool in hot weather and keep warm in cool weather. NAUSETIL may affect the way your body reacts to temperature changes.
If NAUSETIL makes you feel light-headed, dizzy or faint, get up slowly from a sitting or lying position.
If you plan to have surgery than needs a general anesthetic, tell your doctor or dentist that you are taking this medicine.
Tell your doctor or pharmacist immediately if you come pregnancy while taking NAUSETIL.

Call your doctor straight away if you:

Notice any uncontrolled movements of the tongue, face, mouth or jaw, such as puffing of the cheeks, puckering of the mouth or chewing movements.

These are symptoms of a very rare condition called tardive dyskinesia, which may develop in people taking phenothiazine medicines including NAUSETIL.

The condition is more likely to occur during long term treatment, especially in elderly women. In very rare cases, this may be permanent.

Notice an unexplained fever, ridged muscles or altered consciousness.

These are symptoms of a rare condition called neuroleptic malignant syndrome. Your doctor may tell you to stop taking NAUSETIL.

Remind any doctor, dentist or pharmacist you visit that you are using NAUSETIL.

Things you should not do

Do not give NAUSETIL to children or adolescents under 18 years of age.
Do not give NAUSETIL to anyone else, even if they have the same condition as you.
Do not take it to treat any other complaints unless your doctor or pharmacist tells you to.

Driving or using machines

Be careful before you drive or use any machines or tools until you know how NAUSETIL affects you.

NAUSETIL may cause dizziness, light-headedness, tiredness and drowsiness in some people, especially in the first few days of treatment.

Drinking alcohol

Tell your doctor if you drink alcohol.

If you drink alcohol, dizziness or light-headedness may be worse.

Your doctor or pharmacist may suggest you avoid alcohol while you are being treated with NAUSETIL.

Looking after your medicine

Keep your tablets in the blister pack until it is time to take them. If you take the tablets out of the blister they may not keep as well.

Follow the instructions in the carton on how to take care of your medicine properly.

Store it in a cool dry place away from moisture, heat or sunlight; for example, do not store it:

in the bathroom or near a sink, or
in the car or on window sills.

Keep it where young children cannot reach it.

Getting rid of any unwanted medicine

If you no longer need to use this medicine or it is out of date, take it to any pharmacy for safe disposal.

Do not use this medicine after the expiry date.

6. Are there any side effects?

All medicines can have side effects. If you do experience any side effects, most of them are minor and temporary. However, some side effects may need medical attention.

See the information below and, if you need to, ask your doctor or pharmacist if you have any further questions about side effects.

Less serious side effects

Less serious side effects	What to do
constipation dry mouth drowsiness restlessness trembling, rigid posture, mask-like face, slow movements and a shuffling unbalanced walk twitching blurred vision agitation	Speak to your doctor if you have any of these less serious side effects and they worry you.

Serious side effects

Serious side effects

What to do

dizziness, light-headedness
changes in heart beat
swelling of the hands, ankles or feet
swelling and redness along a vein which is extremely tender when touched, which may be a serious blood clot
for females: unusual secretion of breast milk, irregular periods
for males: breast enlargement, difficulty in ejaculating
severe pain in the stomach with bloating, gut cramps and vomiting
difficulty passing urine
yellowing of the skin and/or eyes
headache
insomnia
seizures
difficulty in breathing
frequent infections such as fever, severe chills, sore throat or mouth ulcers
bleeding or bruising more easily than normal
nasal stuffiness
excessive thirst
dry mouth and skin
eye problems such as changes in vision, changes in eye colour, uncontrolled eye movements or eye pain

If any of the following happen, go to Accident and Emergency at your nearest hospital:

unusual muscle tone or
unusual muscle tone or spasms causing distortion of the body in children
chest pain and shortness of breath

Call your doctor straight away, or go straight to the Emergency Department at your nearest hospital if you notice any of these serious side effects.

These are very serious side effects. Serious side effects are rare.

Tell your doctor or pharmacist if you notice anything else that may be making you feel unwell.

Other side effects not listed here may occur in some people.

Reporting side effects

After you have received medical advice for any side effects you experience, you can report side effects to the Therapeutic Goods Administration online at www.tga.gov.au/reporting-problems. By reporting side effects, you can help provide more information on the safety of this medicine.

Always make sure you speak to your doctor or pharmacist before you decide to stop taking any of your medicines.

7. Product details

This medicine is only available with a doctor's prescription.

What NAUSETIL contains

Active ingredient (main ingredient)	5 mg prochlorperazine maleate
Other ingredients (inactive ingredients)	wheat starch calcium hydrogen phosphate magnesium stearate sodium lauryl sulfate quinoline yellow
Potential allergens	gluten

Nausetil tablets do not contain sucrose or lactose.

Do not take this medicine if you are allergic to any of these ingredients.

What NAUSETIL looks like

NAUSETIL tablets are round, pale yellow tablets engraved with “M” on one side and plain on the other.

They are available in packs of 10 tablets.
(Aust R 159537)

Who distributes NAUSETIL

Aspen Pharmacare Australia Pty Ltd
34-36 Chandos St
St Leonards NSW 2065
Australia

This leaflet was prepared in December 2022

Published by MIMS April 2023

BRAND INFORMATION

Brand name

Nausetil

Active ingredient

Prochlorperazine maleate

Schedule

1 Name of Medicine

Prochlorperazine maleate.

2 Qualitative and Quantitative Composition

Each Nausetil tablet contains 5 mg of prochlorperazine maleate as the active ingredient.
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Nausetil 5 mg tablets are round, biconvex and pale yellow engraved with "M" on one side and plain on the other.

4 Clinical Particulars

4.1 Therapeutic Indications

For the treatment of nausea associated with migraine.

4.2 Dose and Method of Administration

Adults.

The recommended dosage is 5 or 10 mg two or three times daily.
For acute treatment, 20 mg at once, followed, if necessary, by 10 mg two hours later.

Children.

Do not use in children and adolescents under 18 years of age.

Geriatric.

In general, dosages in the lower range are sufficient for most elderly patients. Since they are especially susceptible to hypotension and extrapyramidal reactions, such patients should be observed closely. Dosage should be increased more gradually in elderly patients.

Impaired liver function.

Since prochlorperazine is extensively metabolised by the liver, dosage reduction may be necessary.

4.3 Contraindications

Circulatory collapse, central nervous system (CNS) depression (coma or drug intoxication), previous history of a hypersensitivity reaction (e.g. jaundice or blood dyscrasia) to phenothiazines, especially to prochlorperazine, bone marrow depression.

4.4 Special Warnings and Precautions for Use

Identified precautions.

Nausetil should be avoided in patients with renal dysfunction, Parkinson's disease, hypothyroidism, phaeochromocytoma, myasthenia gravis, prostatic hypertrophy. It should be avoided in patients with a history of narrow angle glaucoma or agranulocytosis.
As agranulocytosis has been reported, regular monitoring of the complete blood count is recommended. The occurrence of unexplained infections or fever may be evidence of blood dyscrasia and requires immediate haematological investigation.
Prochlorperazine can cause photosensitisation, therefore patients should be advised to avoid exposure to direct sunlight during treatment.
In schizophrenia, the response to prochlorperazine treatment may be delayed. If treatment is withdrawn, the reoccurrence of symptoms may not become apparent for some time. Avoid concomitant treatment with other neuroleptics.

Hypotension.

The autonomic side effects of the piperazine derivatives are less troublesome than those of other phenothiazines, however care should be taken if Nausetil is used in the elderly or in patients undergoing surgery with spinal anaesthesia.
Postural hypotension with tachycardia as well as local pain or nodule formation may occur after intramuscular administration of prochlorperazine.

Epileptics.

Close monitoring is required in patients with epilepsy or a history of seizures, as phenothiazines may lower the seizure threshold. The occurrence of convulsive seizures necessitates the discontinuation of treatment.
Piperazine derivatives are also less epileptogenic than other phenothiazines, but care should still be exercised in epileptic patients.

Anticholinergic effects.

Prochlorperazine can cause problems due to anticholinergic effects, especially in the elderly (urinary difficulties, constipation and precipitation of acute narrow angle glaucoma), but to a lesser extent than with other phenothiazines.

Hypocalcaemia.

It appears from a study of five hypocalcaemic patients with hypoparathyroidism that such patients are prone to acute dystonic reactions with prochlorperazine.

Sedative effect.

Prochlorperazine may impair mental and physical activity, especially during the first few days of therapy. Patients should be warned about activities requiring alertness.

Antiemetic effects.

The antiemetic effects of prochlorperazine may mask signs of overdosage of toxic drugs or obscure the diagnosis of conditions, e.g. intestinal obstruction and brain tumour.

Reye's syndrome.

The extrapyramidal symptoms which can occur secondary to prochlorperazine may be confused with the CNS signs of an undiagnosed primary disease responsible for the vomiting, e.g. Reye's syndrome or other encephalopathy. The use of prochlorperazine and other potential hepatotoxins should be avoided in children and adolescents whose signs and symptoms suggest Reye's syndrome.

Hypothermia.

Severe hypothermia may occur during swimming in cold water or in patients receiving antipyretic therapy.

Tardive dyskinesia.

Tardive dyskinesia may develop in patients on antipsychotic drugs. The disorder consists of repetitive involuntary movements of the tongue, face, mouth or jaw (e.g. protrusion of the tongue, puffing the cheeks, puckering of the mouth, chewing movements). The trunk and limbs are less frequently involved. It has been reported that fine vermicular movements of the tongue may be an early sign of the syndrome.
Both the risk of developing the syndrome and the likelihood that it will become irreversible are believed to increase as the duration of treatment and the total cumulative dose of the drug increases. Less commonly, the syndrome can develop after relatively brief treatment periods at low doses. The risk seems to be greater in elderly patients, especially females.
The syndrome may become clinically recognisable either during treatment, upon dosage reduction, or upon withdrawal of treatment. The dosage of antipsychotic drug should be reduced periodically (if clinically possible) and the patient observed for signs of the disorder, since the syndrome may be masked by a higher dose. In patients requiring long-term treatment, the smallest dose and the shortest duration of treatment producing a satisfactory clinical response should be sought.
There is no known effective treatment for tardive dyskinesia. Antiparkinsonian agents usually do not alleviate symptoms. It is suggested that antipsychotic agents be discontinued if symptoms of tardive dyskinesia appear.

Neuroleptic malignant syndrome.

A potentially fatal syndrome called neuroleptic malignant syndrome has been reported in association with antipsychotic drugs. The syndrome is characterised by muscular rigidity, fever, hyperthermia, altered consciousness and autonomic instability (e.g. tachycardia, labile blood pressure, profuse sweating, dyspnoea).
It is imperative that prochlorperazine treatment be discontinued in the event of unexplained fever, as this may be a sign of neuroleptic malignant syndrome (pallor, hyperthermia, autonomic dysfunction, altered consciousness, muscle rigidity).
Signs of autonomic dysfunction, such as sweating and arterial instability, may precede the onset of hyperthermia and serve as early warning signs.
The management of neuroleptic malignant syndrome should include immediate discontinuation of antipsychotic drugs, intensive monitoring and treatment of symptoms and treatment of any associated medical problems.

QT intervals.

Very rare cases of QT interval prolongation have been reported with prochlorperazine. Neuroleptic phenothiazines may potentiate QT interval prolongation which increases the risk of onset of serious ventricular arrhythmias of the torsades de pointes type, which is potentially fatal (sudden death). QT prolongation is exacerbated, in particular, in the presence of bradycardia, hypokalaemia and congenital or acquired (i.e. drug induced) QT prolongation. If the clinical situation permits, medical and laboratory evaluations should be performed to rule out possible risk factors before initiating treatment with a neuroleptic agent and as deemed necessary during treatment (see Section 4.8 Adverse Effects (Undesirable Effects)).

Cerebrovascular events.

An increased risk of cerebrovascular events has been reported in elderly patients with dementia treated with atypical antipsychotic drugs. An increase in the risk of cerebrovascular events with other antipsychotic drugs or other populations of patients cannot be excluded. Nausetil should, therefore, be used with caution in patients with stroke risk factors.

Thromboembolism.

Cases of venous thromboembolism, sometimes fatal, 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 Nausetil and preventative measures undertaken. Therefore, Nausetil should be used with caution in patients with risk factors for thromboembolism (see Section 4.8 Adverse Effects (Undesirable Effects)).

Hyperglycaemia.

Hyperglycaemia or intolerance to glucose has been reported in patients treated with Nausetil. Patients with an established diagnosis of diabetes mellitus or with risk factors for the development of diabetes who are started on Nausetil, should get appropriate glycaemic monitoring during treatment (see Section 4.8 Adverse Effects (Undesirable Effects)).

Hypersensitivity reactions.

Hypersensitivity reactions including anaphylaxis, urticaria and angioedema have been reported with prochlorperazine use. In case of allergic reactions, treatment with prochlorperazine must be discontinued and appropriate symptomatic treatment initiated (see Section 4.8 Adverse Effects (Undesirable Effects)).

Use in hepatic impairment.

Caution should be used in patients with existing liver disease, due to the extensive hepatic metabolism of prochlorperazine. A past history of jaundice resulting from phenothiazine therapy indicates a hypersensitivity reaction and there is a likelihood of cross sensitivity to other phenothiazines.

Use in renal impairment.

No data available.

Use in the elderly.

It should be used with caution in the elderly, particularly during very hot or very cold weather (risk of hyper-, hypothermia).
The elderly are particularly susceptible to postural hypotension, sedation and extrapyramidal side effects.
Nausetil should be used cautiously in the elderly owing to their susceptibility to drugs acting on the central nervous system and a lower initial dosage is recommended. There is an increased risk of drug-induced Parkinsonism in the elderly particularly after prolonged use. Care should also be taken not to confuse the adverse effects of Nausetil, e.g. orthostatic hypotension, with the effects due to the underlying disorder.

Elderly patients with dementia.

Elderly patients with dementia related psychosis treated with antipsychotic drugs are at an increased risk of death. Although the causes of death in clinical trials with atypical antipsychotics were varied, most of the deaths appeared to be either cardiovascular (e.g. heart failure, sudden death) or infectious (e.g. pneumonia) in nature. Observational studies suggest that, similar to atypical antipsychotic drugs, treatment with conventional antipsychotic drugs may increase mortality. The extent to which the findings of increased mortality in observational studies may be attributed to the antipsychotic drug as opposed to some characteristic(s) of the patients is not clear.
Prolonged administration of any phenothiazine may result in persistent or tardive dyskinesias, particularly in the elderly and children.

Paediatric use.

The medicine should not be given to children and adolescents under 18 years of age.

Effects on laboratory tests.

No data available.

4.5 Interactions with Other Medicines and Other Forms of Interactions

Adrenaline must not be used in patients overdosed with Nausetil.
Caution is required with the use of the following medicines due to the risk of QT prolongation (see Section 4.4 Special Warnings and Precautions for Use):
Class Ia antiarrhythmic agents such as quinidine and disopyramide.
Class III antiarrhythmic agents such as amiodarone and sotalol.
Other medications such as bepridil, cisapride, sultopride, thioridazine, methadone, intravenous erythromycin, intravenous vincamine, halofantrine, pentamidine, sparfloxacin.
Medicines which induce bradycardia, such as bradycardia-inducing calcium channel blockers (diltiazem, verapamil), beta-blockers, clonidine, guanfacine, digitalis.
Medicines which can cause hypokalaemia, such as diuretics, stimulant laxatives, intravenous amphotericin B, glucocorticoids, tetracosactides (tetracosactrin).
Other antipsychotics.
Prochlorperazine may enhance the CNS depressant effects of alcohol and other depressant drugs and potentiate the anticholinergic effects of atropinic agents and tricyclic antidepressants.
Respiratory depression may occur. Impaired vigilance may make it dangerous to drive or use machines. Avoid consumption of alcoholic beverages and medications containing alcohol.
The mild anticholinergic effect of prochlorperazine may be enhanced by other anticholinergic drugs, possibly leading to dry mouth, constipation, heat stroke, urinary retention and other adverse effects. Some drugs interfere with absorption of prochlorperazine:
Anti-Parkinson drugs.
Lithium.
Topical gastro-intestinal agents (magnesium, aluminium and calcium salts, oxides and hydroxides): reduced gastro-intestinal absorption of prochlorperazine. Antacids should not be taken at the same time as prochlorperazine.
High doses of prochlorperazine reduce the response to hypoglycaemic agents.
The hypotensive effect of most antihypertensive drugs especially alpha adrenoceptor blocking agents may be exaggerated by prochlorperazine.
The action of some drugs may be opposed by prochlorperazine; these include amfetamine, levodopa, clonidine, guanethidine, adrenaline.
Increases or decreases in the plasma concentrations of a number of drugs, e.g. propranolol, phenobarbital have been observed.
There is an increased risk of arrhythmias when prochlorperazine is used with concomitant QT prolonging drugs (including certain antiarrhythmics, antidepressants and other antipsychotics) and drugs causing electrolyte imbalance.
There is an increased risk of agranulocytosis when prochlorperazine is used concurrently with drugs with myelosuppressive potential, such as carbamazepine or certain antibiotics and cytotoxics.
In patients treated concurrently with prochlorperazine and lithium, there have been rare reports of neurotoxicity.
Phenothiazines are potent inhibitors of CYP2D6. Co-administration of phenothiazines with amitriptyline, a CYP2D6 substrate, may lead to an increase in the plasma levels of amitriptyline. Monitor patients for dose-dependent adverse reactions associated with amitriptyline.
Simultaneous administration of desferrioxamine and prochlorperazine has been observed to induce a transient metabolic encephalopathy characterised by loss of consciousness for 48 to 72 hours.
Procarbazine has been reported to potentiate the extrapyramidal side effects encountered with the use of prochlorperazine.
Phenothiazines have been reported both to impair and increase metabolism of phenytoin, with uncertain clinical significance.
Patients on levodopa should not be given phenothiazines because the two drugs are physiologically antagonistic.
Thiazide diuretics may accentuate the orthostatic hypotension that may occur with phenothiazines.
Antihypertensive effects of guanethidine and related compounds may be counteracted when phenothiazines are used concomitantly.
Phenothiazines can diminish the effect of oral anticoagulants.
Concomitant administration of propranolol and phenothiazines results in increased plasma levels of both drugs.
Phenothiazines may lower the convulsive threshold; dosage adjustments of anticonvulsants may be necessary.

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

No data available.
(Category C)
When given in high doses during late pregnancy, phenothiazines have caused jaundice, hyper-reflexia, hyporeflexia or prolonged extrapyramidal disturbances in the child. There is inadequate evidence of the safety of Nausetil in human pregnancy, but it has been widely used for many years without apparent ill consequence. There is evidence of harmful effects in animals. The following effects have been reported (in postmarketing surveillance) in neonates exposed to phenothiazines during the third trimester of pregnancy:
Various degrees of respiratory disorders ranging from tachypnoea to respiratory distress, bradycardia and hypotonia, most often when other drugs such as psychotropic or antimuscarinic drugs were coadministered.
Signs related to the atropinic properties of phenothiazines such as meconium ileus, delayed meconium passage, initial feeding difficulties, abdominal bloating, tachycardia.
Neurological disorders such as extrapyramidal symptoms including tremor and hypertonia, somnolence, agitation.
Appropriate monitoring and treatment of neonate born to mothers receiving prochlorperazine is recommended.
Like other drugs it should be avoided in pregnancy unless the doctor considers it essential.
Prochlorperazine may occasionally prolong labour, and at such a time should be withheld until the cervix is dilated 3 to 4 cm. Possible adverse effects on the foetus include lethargy or paradoxical hyperexcitability, tremor and a low Apgar score.
Trace amounts of another phenothiazine, chlorpromazine, have been detected in breast milk, but there is no information available for prochlorperazine. Consequently, it is not known whether it is excreted in breast milk nor whether it has a harmful effect on the newborn infant. Therefore, Nausetil is not recommended for breastfeeding mothers unless the expected benefits outweigh any potential risk.

4.7 Effects on Ability to Drive and Use Machines

Prochlorperazine may impair mental and physical activity, especially during the first few days of therapy. Patients should be warned about activities requiring alertness.

4.8 Adverse Effects (Undesirable Effects)

The following reactions have been reported for prochlorperazine or phenothiazines in general:

More common reactions.

Gastrointestinal.

Constipation, dry mouth.

Nervous system.

Drowsiness, akathisia, parkinsonism (with dyskinesia, tremor and rigidity).

Ocular.

Blurred vision.

Vascular.

Hypotension.

Less common reactions.

Biochemical abnormalities.

Elevated serum levels of bilirubin and hepatic enzymes may occur if the patient develops cholestatic jaundice.

Cardiovascular.

Peripheral oedema, cardiac arrhythmias, electrocardiographic (ECG) changes, QT interval prolongation, ST depression, U-Wave and T-Wave changes. Cardiac arrhythmias, including ventricular arrhythmias and atrial arrhythmias, a-v block, ventricular tachycardia, which may result in ventricular fibrillation or cardiac arrest have been reported during phenothiazine therapy.
Pre-existing cardiac disease, old age, hypokalaemia and concurrent tricyclic antidepressants may predispose patients to cardiac events. There have been isolated reports of sudden death, with possible causes of cardiac origin (see Section 4.4 Special Warnings and Precautions for Use), as well as cases of unexplained sudden death, in patients receiving neuroleptic phenothiazines.
Cases of venous thromboembolism, including cases of pulmonary embolism, sometimes fatal, and cases of deep vein thrombosis have been reported with antipsychotic drugs (see Section 4.4 Special Warnings and Precautions for Use).

Dermatological.

Dermatitis or contact dermatitis, maculopapular eruptions, erythema multiforme, urticaria, photosensitivity, abnormal pigmentation.

Endocrine.

Endocrine disturbances including elevated prolactin levels, hyperglycaemia, hypoglycaemia, menstrual irregularities, galactorrhoea, gynaecomastia.

Gastrointestinal.

Paralytic ileus.

Genitourinary.

Urinary retention, inhibition of ejaculation.

Haematological.

Agranulocytosis, atypical lymphocytes, thrombocytopenia, leucopenia, aplastic anaemia.

Hepatic.

Cholestatic jaundice, liver damage.

Nervous system.

Acute dystonia or dyskinesias including oculogyric crisis.
Tardive dyskinesia: It can even occur after treatment has been stopped.
Torticollis and opisthotonus and trismus, seizures, electroencephalographic (EEG) changes, headache, insomnia, catatonia, hyperpyrexia, agitation, dizziness.
Cases of convulsions have been reported.

Ocular.

Pigmentary retinopathy.
Brownish deposits in the anterior segment of the eye, due to accumulation of the product.

Psychiatric.

Activation of psychotic symptoms.

Respiratory.

Respiratory depression, nasal stuffiness.

Metabolism and nutrition disorders.

Hyponatraemia and inappropriate antidiuretic hormone secretion have also been reported.
In post-marketing surveillance cases of hyperglycaemia or intolerance to glucose have been reported with antipsychotic phenothiazines (see Section 4.4 Special Warnings and Precautions for Use).

Immune system disorders.

Hypersensitivity reactions such as angioedema and urticaria have been reported.
Anaphylactic reaction.

General disorders and administration site conditions.

Neuroleptic malignant syndrome (hyperthermia, rigidity, autonomic dysfunction and altered consciousness).

Pregnancy, puerperium and perinatal conditions.

Drug withdrawal syndrome neonatal (see Section 4.6 Fertility, Pregnancy and Lactation, Use in pregnancy).

Severe or life-threatening reactions.

Prochlorperazine can cause very serious acute dystonic reactions in children leading to cyanosis from laryngospasm, apnoea requiring artificial ventilation, life threatening tetanus-like syndromes, coma and even death. These reactions can occur with a single therapeutic dose. For treatment, see Section 4.9 Overdose.
Also, long-term phenothiazine therapy has been associated with ECG changes and life threatening cardiac arrhythmias.

Reporting suspected adverse effects.

Reporting suspected adverse reactions after registration 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 at www.tga.gov.au/reporting-problems.

4.9 Overdose

Symptoms.

Overdosage with phenothiazines may cause CNS depression progressing from drowsiness to coma with areflexia. Patients with early or mild intoxication may experience restlessness, confusion and excitement. Other symptoms include hypotension, tachycardia, hypothermia, pupillary constriction, restlessness, tremor, muscle twitching, spasm or rigidity, convulsions, muscular hypotonia, difficulty in swallowing or breathing, cyanosis and respiratory and/or vasomotor collapse, possibly with sudden apnoea. There is no information available regarding lethal dose in humans.
High doses cause depression of the central nervous system, presenting as lethargy, dysarthria, ataxia, stupor, reduction in consciousness into coma, convulsions; mydriasis; cardiovascular symptoms (related to risk of QT interval prolongation), such as hypotension, ventricular tachycardia and arrhythmia; respiratory depression; hypothermia. These effects may be potentiated by other medicines or by alcohol. Anticholinergic syndrome is of importance. Extremely serious parkinsonian syndrome may occur.

Treatment.

Acute dystonic reactions.

Intramuscular benztropine (or another antiparkinsonian agent) should be given immediately (adults: 1 to 2 mg intramuscularly; children: 0.2 mg intramuscularly initially, with increments if necessary).

Overdosage.

Emesis should not be induced, not only because the antiemetic action of prochlorperazine prevents the effect of the emetic agent, but also because the sedative and extrapyramidal side effects increase the risk of pulmonary aspiration should vomiting occur. Gastric lavage may be useful even several hours after the drug has been ingested since prochlorperazine reduces gastric motility. Management is generally supportive with particular attention to the possibility of obstructed ventilation, severe hypotension, hypothermia, cardiac arrhythmias, convulsions and prolonged deep sedation. Acute dystonic reactions usually occur early (if at all); treatment is with anticholinergic agents, as above.
Adrenaline must not be used as it may cause a paradoxical further lowering of blood pressure.
For information on the management of overdose, contact the Poisons Information Centre on 13 11 26 (Australia).

5 Pharmacological Properties

5.1 Pharmacodynamic Properties

Mechanism of action.

Prochlorperazine is a phenothiazine with a piperazine moiety in the side chain. It possesses strong antiemetic and antipsychotic activity with less sedative action than chlorpromazine.

Pharmacology.

As with other phenothiazines, prochlorperazine has actions on several neurotransmitter systems as follows:
Antidopamine action, which probably contributes to both the therapeutic effect and unwanted effects including extrapyramidal disorders and endocrine disturbances.
Alpha-adrenoreceptor antagonism, which contributes to cardiovascular side effects, e.g. orthostatic hypotension and reflex tachycardia.
Potentiation of noradrenaline by blocking its reuptake into nerve terminals.
Weak anticholinergic action.
Weak antihistamine action.
Weak serotonin antagonism.
Prochlorperazine also has an effect on temperature control and blocks conditioned avoidance responses.

Clinical trials.

No data available.

5.2 Pharmacokinetic Properties

There are few published data on prochlorperazine pharmacokinetics in the human. Most studies have been done in rats and dose levels do not correspond to those used clinically and metabolic pathways may differ. Similar overall pharmacokinetic patterns, however, would occur in the human.

Absorption.

Prochlorperazine is well absorbed from the gastrointestinal (GI) tract in rats, but absorption is slowed in repeatedly treated animals.

Distribution.

The drug is widely distributed to tissues including the brain, fat, kidney, heart and skin and is stored in reticuloendothelial tissues.

Metabolism.

Phenothiazines are metabolised primarily in the liver and are subject to enterohepatic circulation.

Excretion.

Excretion is mainly in the faeces. Only a very small amount (approximately 0.1%) of prochlorperazine and its metabolites is excreted in the first 24 hours in the urine and the drug may continue to be excreted in the urine for up to three weeks after cessation of long-term therapy. The elimination half-life is approximately 24 hours, presumably due to its enterohepatic circulation.

5.3 Preclinical Safety Data

Genotoxicity.

No data available.

Carcinogenicity.

No data available.

6 Pharmaceutical Particulars

6.1 List of Excipients

Excipients include wheat starch, magnesium stearate, sodium lauryl sulfate, calcium hydrogen phosphate anhydrous and quinoline yellow.

6.2 Incompatibilities

Incompatibilities were either not assessed or not identified as part of the registration of this medicine. Please see Section 4.5 Interactions with Other Medicines and Other Forms of Interactions.

6.3 Shelf Life

In Australia, information on the shelf life can be found on the public summary of the Australian Register of Therapeutic Goods (ARTG). The expiry date can be found on the packaging.

6.4 Special Precautions for Storage

Store below 30°C. Protect from light.

6.5 Nature and Contents of Container

PVC/Al Blister pack available in packs of 10 tablets.

6.6 Special Precautions for Disposal

In Australia, any unused medicine or waste material should be disposed of by taking to your local pharmacy.

6.7 Physicochemical Properties

Chemical structure.

CAS number.

84-02-6.
Chemical name: 2-chloro-10-[3-(4-methylpiperazin-1-yl) propyl]-10H-phenothiazine bis[hydrogen (Z)-butenedioate].
Chemical formula: C₂₀H₂₄ClN₃S, 2C₄H₄O₄.
Molecular weight: 606.2.
Prochlorperazine maleate is an odourless, nonhygroscopic, white or almost white, fine granular powder, which becomes coloured on exposure to light. It is very slightly soluble (about 0.1%) in water, ethanol or methanol and is insoluble in ether or chloroform.

7 Medicine Schedule (Poisons Standard)

S3 (Pharmacist Only Medicine).

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Prochlorperazine maleate

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