Consumer medicine information

APO-Prochlorperazine

Prochlorperazine maleate

BRAND INFORMATION

Brand name

APO-Prochlorperazine

Active ingredient

Prochlorperazine maleate

Schedule

What is in this leaflet

This leaflet answers some common questions about this medicine. It does not contain all the available information. It does not take the place of talking to your doctor or pharmacist.

All medicines have risks and benefits. Your doctor has weighed the risks of you taking this medicine against the benefits they expect it will have for you.

If you have any concerns about taking this medicine, ask your doctor or pharmacist.

Keep this leaflet with the medicine. You may need to read it again.

What this medicine is used for

The name of your medicine is APO-Prochlorperazine. It contains the active ingredient, prochlorperazine (as prochlorperazine maleate).

It is used to treat nausea, vomiting and dizziness due to various causes, including migraine (severe headache).

Prochlorperazine belongs to a group of medicines called phenothiazines. It 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 (feeling sick) and vomiting.

Ask your doctor if you have any questions about why this medicine has been prescribed for you. Your doctor may have prescribed this medicine for another reason.

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

Prochlorperazine is not recommended for use in children (under the age of 2 years or children under 10 kg in weight) because children may develop unusual face and body movements.

Do not use Prochlorperazine intramuscular injection in children.

Before you take prochlorperazine

When you must not take it

Do not take this medicine if you have an allergy to:

any medicine containing prochlorperazine
the group of medicines called phenothiazines
any of the ingredients listed at the end of this leaflet.
You have any of the following medical conditions:
- shock
- disease of the blood with a low number of blood cells
- yellowing of the skin and/or eye, also called jaundice.

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

Some of the symptoms of an allergic reaction may include:

shortness of breath
wheezing or difficulty breathing
swelling of the face, lips, tongue or other parts of the body
rash, itching or hives on the skin

Do not take this medicine if you have in the past experienced jaundice (yellow skin and/or eyes) or problems with your blood cells, after taking prochlorperazine or similar medicines called phenothiazines. This is called a hypersensitivity reaction.

Do not take this medicine if you suffer from bone marrow depression, a disease of the blood with a low number of blood cells.

Do not give this medicine to anyone who is in shock, unconscious or in a coma.

Do not take this medicine if you are pregnant. It may affect your developing baby if you take it during pregnancy.

Your doctor will discuss with you the benefits and risks of using it.

Do not breastfeed if you are taking this medicine. It is recommended that you do not breastfeed while taking prochlorperazine, as it is not known whether it passes into breast milk and there is a possibility that your baby may be affected.

Your doctor will discuss with you the benefits and risks of using it.

Do not take this medicine after the expiry date printed on the pack or if the packaging is torn or shows signs of tampering. If it has expired or is damaged, return it to your pharmacist for disposal.

If you are not sure whether you should start taking this medicine, talk to your doctor.

Before you start to take it

Tell your doctor if you have allergies to any other medicines, foods, preservatives or dyes.

Tell your doctor if you have or have had any of the following medical conditions:

phaeochromocytoma, 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 or problems urinating
constipation or bowel problems
heart and blood vessel problems, low blood pressure, blood clots,
liver disease
prostate problems
bowl problems
epilepsy, seizures or fits
low blood calcium levels associated with a condition called hypoparathyroidism
hypothyroidism (an underactive thyroid gland)
glaucoma, a condition in which there is 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,
tardive dyskinesia, a reaction to some medicines with uncontrollable twitching or jerking movements of the arms and legs
dementia
diabetes, or risk factors for diabetes (e.g. overweight)
you have lost lots of fluid due to vomiting, diarrhoea or sweating (which increases the chance of having low potassium levels)
a low number of white blood cells (agranulocytosis)
symptoms of Reye’s syndrome in children such as diarrhoea, rapid breathing vomiting and severe fatigue
chicken pox or measles in children
dehydration in children.
experience fever, sore throat or any other infection, they should inform physician and undergo a complete blood count. Treatment should be discontinued if any marked changes (hyperleukocytosis, granulocytopenia) are observed in the blood count.

Tell your doctor if you are planning to have surgery which requires a spinal and/or general anaesthetic.

Make sure to tell your doctor all of your symptoms, in case taking this medicine covers up any undiagnosed problem.

Taking other medicines

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

Some medicines may interact with prochlorperazine. These include:

some medicines used to control depression or mood swings or mental illness such as lithium
medicines metabolised by CYP2D6 enzymes such as amitriptyline
medicines used for the treatment of diabetes
any other medicines which make you drowsy
alcohol
desferrioxamine, used to treat excess iron in your blood
procarbazine, an anticancer drug
some medicines used to control epilepsy, e.g. phenytoin, phenobarbital or carbamazepine
antibiotics used to treat infections
medicines used to treat Parkinson's disease, e.g. levodopa
medicines used for the treatment of diabetes
anticholinergic medicines including those that can be 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
some oral medicines used to prevent your blood from clotting, e.g. warfarin
medicines used to treat high blood pressure
medicines used to treat heart problems, such as clonidine, guanethidine and propranolol
other medicines which can slow your heart rate down, such as diltiazem, verapamil, beta-blockers (e.g. propranolol), clonidine and guanfacine
medicines used to treat fluid build-up in your body
medicines used to treat a fast or irregular heart beat e.g. amiodarone, quinidine, disopyramide.
Medicines that can slow your heart e.g. diltiazem, verapamil
diuretic (fluid) tablets, for treating excess fluid and high blood pressure
medicines that can reduce potassium levels in the blood e.g. diuretics, laxatives.
Other medicines that can affect your heart rate e.g. methadone, pentamidine.
antacids containing magnesium, aluminium and calcium salts, oxides and hydroxides
adrenaline used for severe allergic reactions
amphetamines

These medicines may be affected by prochlorperazine or may affect how well it works. You may need different amounts of your medicines, or you may need to take different medicines. Your doctor will advise you.

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

Your doctor and pharmacist have more information on medicines to be careful with or avoid while taking this medicine.

How to take this medicine

Follow all directions given to you by your doctor or pharmacist carefully. They may differ from the information contained in this leaflet.

If you do not understand the directions, ask your doctor or pharmacist for help.

How much to take

The usual recommended dose for nausea and vomiting in adults is 1 or 2 tablets two to three times daily.

The usual recommended dose for dizziness in adults is 1 or 2 tablets three to four times daily. This may gradually be reduced to 1 or 2 tablets once a day.

Children are usually given lower doses which depend on their body weight.

If you have liver problems you may take a smaller dose.

How to take it

Swallow the tablets whole with a glass of water.

Do not chew the tablets.

When to take it

Take it at about the same time each day. Taking your medicine at the same time each day will have the best effect. It will also help you remember when to take it.

It does not matter if you take it before, with or after food.

How long to take it for

Continue taking your medicine for as long as your doctor tells you.

Make sure you have enough to last over weekends and holidays.

If you forget to take it

If it is almost time to take your next dose, skip the missed dose and take your next dose at the usual time.

Otherwise, take it as soon as you remember and then go back to taking your medicine as you would normally.

Do not take a double dose to make up for the dose that you missed. This may increase the chance of you getting an unwanted side effect.

If you have trouble remembering to take your medicine, ask your pharmacist for some hints to help you remember.

If you take too much (overdose)

Do not try to vomit.

If you think that you or anyone else may have taken too much of this medicine, immediately telephone your doctor or the Poisons Information Centre (Tel: 13 11 26 in Australia) for advice. Alternatively, go to the Accident and Emergency department at your nearest hospital.

Do this even if there are no signs of discomfort or poisoning. You may need urgent medical attention.

If you take too much prochlorperazine, you may get some or all of the following:

coma
restlessness, shaking, muscle twitching, muscle weakness, spasm
confusion
excitement or agitation
low blood pressure
fast heart beat
decrease in body temperature
small pupils in the eye
difficulty in swallowing or breathing
blue lips and/or skin

While you are taking this medicine

Things you must do

Tell your doctor immediately 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 prochlorperazine.

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

If you are about to be started on any new medicine, remind your doctor and pharmacist that you are taking this medicine.

Tell any other doctors, dentists, and pharmacists who treat you that you are taking this medicine.

If you are going to have surgery, tell the surgeon or anaesthetist that you are taking this medicine. It may affect other medicines used during surgery.

If you become pregnant or start to breastfeed while taking this medicine, tell your doctor immediately.

If you have diabetes or are at risk of developing diabetes be sure to monitor your blood glucose levels carefully. This medicine may affect blood glucose levels.

If you are about to have any blood tests, tell your doctor that you are taking this medicine.

Go to your doctor regularly for a check-up. Your doctor may occasionally do tests to make sure the medicine is working and to prevent side effects.

Things you must not do

Do not take this medicine to treat any other complaints unless your doctor or pharmacist tells you to.

Do not give your medicine to anyone else, even if they have the same condition as you.

Do not stop taking your medicine or lower the dosage, even if you are feeling better, without checking with your doctor.

Do not stop taking your medicine suddenly. If you do, your condition may worsen or your chance of getting an unwanted side effect may increase. To prevent this, your doctor may gradually reduce the amount of your medicine you take each day before stopping completely.

Do not take any medicines that cause drowsiness while you are taking this medicine.

Things to be careful of

Be careful while driving or operating machinery until you know how this medicine affects you. Prochlorperazine may cause dizziness, light-headedness, tiredness, blurred vision, drowsiness in some people.

Make sure you know how you react to prochlorperazine before you drive a car, operate machinery, or do anything else that could be dangerous if you are tired, drowsy, dizzy or light-headed. If this occurs do not drive. If you drink alcohol, drowsiness, dizziness or light-headedness may be worse.

If prochlorperazine makes you feel light-headed, dizzy or faint, be careful when getting up from a sitting or lying position. Getting up slowly may help.

Be careful when drinking alcohol while taking prochlorperazine. Combining this medicine and alcohol can make you more sleepy, dizzy or light-headed. Your doctor may suggest you avoid alcohol while you are being treated with prochlorperazine.

If outdoors, wear protective clothing and use at least a 15+ sunscreen. Prochlorperazine may cause your skin to be much more sensitive to sunlight than it is normally. It is advised to avoid exposure to direct sunlight during treatment. Exposure to sunlight may cause a skin rash, itching, redness, or even severe sunburn. If your skin does appear to be burning, tell your doctor.

Make sure you keep cool in hot weather and keep warm in cool weather. Prochlorperazine may affect the way your body reacts to temperature changes. For example if you swim in cold water your body may not be able to adjust your body temperature to keep you warm and you may get hypothermia.

Side effects

Tell your doctor or pharmacist as soon as possible if you do not feel well while you are taking this medicine.

All medicines can have side effects. This medicine helps most people with nausea, vomiting and dizziness, but it may have unwanted side effects in a few people. Sometimes they are serious but most of the time they are not.

If you are over 65 years of age you may have an increased chance of getting side effects.

Do not be alarmed by the following lists of side effects. You may not experience any of them.

Ask your doctor or pharmacist to answer any questions you may have.

Tell your doctor or pharmacist if you notice any of the following and they worry you:

constipation, dry mouth
ileus paralytic
drowsiness
headache
restlessness, uncontrolled twitching, jerking or writhing movements
trembling, rigid posture, mask-like face, slow movements and a shuffling unbalanced walk
blurred vision
low blood pressure
change in heart beats
swelling of the hands, ankles or feet
skin rash
for females; unusual secretion of breast milk, irregular or stopping of periods
for males: breast enlargement, difficulty in ejaculating, getting or maintaining an erection, or persistent painful erection
severe pain in the stomach with bloating, cramps and vomiting
difficulty passing urine
yellowing of the skin and/or eyes
headache
insomnia
seizures
agitation, confusional state, delirium, anxiety
dizziness
sedation
difficulty in breathing
brownish deposits in the eyes
stuffy nose

The above list includes the less common side effects of your medicine.

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

shortness of breath, wheezing or difficulty in breathing or swallowing
swelling of the face, lips, throat, tongue or other parts of the body
cold, clammy skin, palpitations, dizziness, weakness or fainting
rash, itching or hives on the skin
unusual muscle tone or spasms causing distortion of the body in children
General- hypersensitivity, fever, rash, facial swelling, swollen lymph nodes (which could be symptoms relating to raised levels of infection fighting cells (relating to eosinophilia)
neuroleptic malignant syndrome, a reaction to some medicines with a sudden increase in body temperature, extremely high blood pressure and severe convulsions
Nervous system related-high fever, muscle cramps or stiffness, dizziness, severe headache, fast heartbeat, confusion, agitation, hallucinations, or are sweating a lot (symptoms relating to Neuroleptic malignant syndrome).
Liver related- yellowing of the skin and/or eyes (jaundice) and urine becomes darker in color
Blood related: bleeding and bruising (thrombocytopenic purpura)

The above list includes very serious side effects. You may need urgent medical attention or hospitalisation. These side effects are very rare.

Storage and disposal

Storage

Keep your medicine in its original packaging until it is time to take it. If you take your medicine out of its original packaging it may not keep well.

Keep your medicine in a cool dry place where the temperature will stay below 25°C.

Do not store your medicine, or any other medicine, in the bathroom or near a sink. Do not leave it on a window sill or in the car. Heat and dampness can destroy some medicines.

Keep it where children cannot reach it. A locked cupboard at least one-and-a-half metres above the ground is a good place to store medicines.

Disposal

If your doctor tells you to stop taking this medicine or the expiry date has passed, ask your pharmacist what to do with any medicine that is left over.

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.

Product description

What APO-PROCHLORPERAZINE looks like

APO-Prochlorperazine 5 mg tablets

White/off white, round, uncoated tablets marked with "5" on one side. AUST R 158416.

Available in blister packs of 14, 25, 28, 56, 84, 100 and 250 tablets.

* Not all strengths, pack types and/or pack sizes may be available.

Ingredients

Each tablet contains 5 mg of prochlorperazine maleate as the active ingredient.

It also contains the following:

lactose monohydrate
maize starch
colloidal anhydrous silica
magnesium stearate

This medicine is gluten-free, sucrose-free, tartrazine-free and free of other azo dyes. This medicine contains sugars as lactose.

Sponsor

Arrotex Pharmaceutical Pty Ltd
15 – 17 Chapel Street
Cremorne VIC 3121
www.arrotex.com.au

This leaflet was last updated in January 2024.

Published by MIMS March 2024

BRAND INFORMATION

Brand name

APO-Prochlorperazine

Active ingredient

Prochlorperazine maleate

Schedule

1 Name of Medicine

Prochlorperazine maleate.

2 Qualitative and Quantitative Composition

Each tablet contains 5 mg prochlorperazine maleate as the active ingredient.

Excipients with known effect.

Contains sugars as lactose.
For the full list of excipients see Section 6.1 List of Excipients.

3 Pharmaceutical Form

APO-Prochlorperazine 5 mg tablets.

APO-Prochlorperazine 5 mg tablets are white to off-white, circular, uncoated tablets with '5' embossed on one side and are intended for oral administration.

4 Clinical Particulars

4.1 Therapeutic Indications

Nausea and vomiting due to various causes including migraine; vertigo due to Meniere's syndrome, labyrinthitis and other causes.

4.2 Dose and Method of Administration

Each tablet is intended for oral administration.

Dosage.

Nausea and vomiting.

Adults.

Dosage should be adjusted to suit the response of the individual, beginning with the lowest recommended dosage.
Oral: 5 or 10 mg two or three times daily.
Acute: 20 mg at once, followed, if necessary by 10 mg two hours later.

Children.

(See Section 4.3 Contraindications; Section 4.4 Special Warnings and Precautions for Use, Paediatric use).
If it is considered unavoidable to use prochlorperazine for a child, the dosage is 250 microgram/kg bodyweight two or three times a day.
Prochlorperazine has been associated with dystonic reactions particularly after a cumulative dosage of 500 microgram/kg. It should therefore be used cautiously in children.
Prochlorperazine is not recommended for children under 2 years of age or weighing less than 10 kg and should not be given to children by the intramuscular route.
When treating children, it is recommended that the 5 mg tablets are used.
Occasionally the patient may react to the drug with signs of restlessness and excitement; if this occurs, treatment should be discontinued.
Vertigo in Meniere's syndrome.

Adults.

Oral: 5 to 10 mg three or four times daily.
Dosage may be reduced gradually after several weeks to a maintenance dosage of 5 to 10 mg daily.

Children.

Oral: dose same as for nausea and vomiting.

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 depression (coma or drug intoxication with alcohol, barbiturates, narcotics etc).
Previous history of a hypersensitivity reaction (e.g. jaundice or blood dyscrasia) to phenothiazines, especially to prochlorperazine; bone marrow depression.
Hypersensitivity to prochlorperazine, other phenothiazines, or to any of the other ingredients of prochlorperazine listed, see Section 6.1.
In children, due to a possible association between use of phenothiazine-containing products and Sudden Infant Death Syndrome (SIDS).

4.4 Special Warnings and Precautions for Use

Hypersensitivity reactions including anaphylactic reaction, urticaria and angioedema have been reported with prochlorperazine use. In case of allergic reaction, treatment with prochlorperazine must be discontinued and appropriate symptomatic treatment initiated (see Section 4.8 Adverse Effects (Undesirable Effects)).
Prochlorperazine should be avoided in patients with liver or renal dysfunction, Parkinson's disease, hypothyroidism, cardiac failure, phaeochromocytoma, myasthenia gravis and prostate hypertrophy. It should be avoided in patients with a history of narrow angle glaucoma or agranulocytosis.
Acute withdrawal symptoms, including nausea, vomiting, headache, anxiety, agitation, dyskinesia, dystonia, disturbed temperature regulation, and insomnia, have very rarely been reported following the abrupt cessation of high doses of neuroleptics. Relapse may also occur, and the emergence of extrapyramidal reactions has been reported. Therefore, gradual withdrawal is advisable. Symptoms of withdrawal can occur following treatment at any dose. Withdrawal of treatment should occur under close medical supervision.
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.
All patients should be advised that, if they experience fever, sore throat or any other infection, they should inform their physician immediately and undergo a complete blood count. Treatment should be discontinued if any marked changes (hyperleucocytosis, granulocytopenia) are observed in the blood count.
As with all antipsychotic drugs, prochlorperazine should not be used alone where depression is predominant. However, it may be combined with antidepressant therapy to treat those conditions in which depression and psychosis coexist.
Prochlorperazine can cause photosensitisation, therefore patients should be advised to avoid exposure to direct sunlight during treatment.
To prevent skin sensitisation in those frequently handling preparations of phenothiazines, the greatest care must be taken to avoid contact of the drug with the skin (see Section 4.8 Adverse Effects (Undesirable Effects)).
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.
Phenothiazines may be additive with, or may potentiate the action of, other CNS depressants such as opiates or other analgesics, barbiturates or other sedatives, general anesthetics, or alcohol.

Stroke.

In randomised clinical trials versus placebo performed in a population with elderly patients with dementia and treated with certain atypical antipsychotic drugs, a 3-fold increase of the risk of cerebrovascular events has been observed. The mechanism of such risk increase is not known. An increase in the risk with other antipsychotic drugs or other populations of patients cannot be excluded. Prochlorperazine should be used with caution with stroke risk factors.

Hypotension.

The autonomic side effects of the piperazine derivatives are less troublesome than those of other phenothiazines, however care should be taken if prochlorperazine 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 5 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 such as intestinal obstruction, brain tumour.

Reye's syndrome.

The extrapyramidal symptoms which can occur secondary to prochlorperazine may be confused with the central nervous system 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. Although neuroleptic malignant syndrome may be idiosyncratic in origin, dehydration and organic brain disease are predisposing factors (see Section 4.8 Adverse Effects (Undesirable Effects)).
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 interval.

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 torsade 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. Prochlorperazine should therefore be used with caution in patients with stroke risk factors.

Thromboembolism.

Cases of venous thromboembolism (VTE), 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 prochlorperazine and preventative measures undertaken. Therefore, prochlorperazine 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 prochlorperazine. Patients with an established diagnosis of diabetes mellitus or with risk factors for the development of diabetes who are started on prochlorperazine, should get appropriate glycaemic monitoring during treatment (see Section 4.8 Adverse Effects (Undesirable Effects)).

Alcohol use.

Patients are strongly advised not to consume alcohol and alcohol-containing medicines while being treated with prochlorperazine.

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 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.
Prochlorperazine 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 prochlorperazine, 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.
Prochlorperazine is not licensed for the treatment of dementia-related behavioural disturbances.
Careful monitoring of treatment with prochlorperazine is required when administered in elderly patients exhibiting greater susceptibility to orthostatic hypotension, sedation, and extrapyramidal effects; chronic constipation (risk of ileus paralytic); possible prostatic hypertrophy.

Paediatric use.

(See Section 4.2 Dose and Method of Administration; Section 4.3 Contraindications.)
Prochlorperazine should not be used in children under 2 years unless potentially life-saving.
Prochlorperazine is not recommended for use in children under 10 kg in weight or under 2 years of age as acute extrapyramidal reactions are more likely to occur.
Prochlorperazine has been associated with dystonic reactions therefore, it should be used cautiously in children.
Prochlorperazine should not be given to children by the rectal or intramuscular route.
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 should be avoided in children and adolescents whose signs and symptoms suggest Reye's syndrome.
Children with an acute febrile illness (e.g. chickenpox, CNS infection, measles, gastroenteritis) or suffering from dehydration seem to be much more susceptible than adults to neuromuscular reactions, particularly dystonias. In such patients, the drug should be used under close supervision and at low doses.

Effects on laboratory tests.

No data available.

4.5 Interactions with Other Medicines and Other Forms of Interactions

Contraindicated combinations.

Dopaminergics, except in patients with Parkinson's disease. Mutual antagonism between dopaminergics and neuroleptics.
Where treatment for neuroleptic-induced extrapyramidal symptoms is required, anticholinergic antiparkinsonian agents should be used in preference to levodopa, since neuroleptics antagonise the antiparkinsonian action of dopaminergics.
Adrenaline must not be used in patients overdosed with prochlorperazine (see Section 4.9 Overdose).
Simultaneous administration of desferrioxamine and prochlorperazine has been observed to induce transient metabolic encephalopathy characterised by loss of consciousness for 48-72 hours.

Combinations not recommended or requiring precaution.

Dopaminergics in patients with Parkinson's disease.
Dopaminergics may cause or exacerbate psychotic disorders. If treatment with neuroleptics is required in patients with Parkinson's disease treated with a dopaminergic, the latter should be tapered off gradually (sudden discontinuation of dopaminergic agents exposes the patient to a risk of "neuroleptic malignant syndrome"). For parkinsonian patients who require treatment with both a neuroleptic and a dopaminergic agent, use the minimum effective doses of both medications.
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 (amphotericin), 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.
Anticholinergic agents may reduce the antipsychotic effect of neuroleptics. 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;
gastro-intestinal agents that are not absorbed (magnesium, aluminium and calcium salts, oxides and hydroxides): reduced gastro-intestinal absorption of phenothiazine neuroleptics may occur. Antacids should not be taken at the same time as prochlorperazine.
High doses of prochlorperazine reduce the response to hypoglycaemic agents, the dosage of which might have to be raised.
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.

Cytochrome P450 2D6 metabolism.

Some phenothiazines are moderate inhibitors of CYP2D6. There is a possible pharmacokinetic interaction between inhibitors of CYP2D6, such as phenothiazines, and CYP2D6 substrates. Co-administration of prochlorperazine 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.
Prochlorperazine should be avoided in patients taking monoamine oxidase inhibitors (MAOIs). If prochlorperazine use is required, MAOIs should be ceased at least 14 days prior to prochlorperazine commencement.
Because of convulsive risk, the combined use of medicinal products which lower the seizure threshold should be carefully assessed.
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 with 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)
The use of APO-Prochlorperazine is not recommended during pregnancy and in women of childbearing potential not using contraception, unless the potential benefits outweigh the potential risks.
Data from epidemiological studies cannot exclude the risk of congenital malformations in children exposed in utero to prochlorperazine.
Neuroleptics may occasionally prolong labour and at such time should be withheld until the cervix is dilated 3-4 cm.
When given in high doses during late pregnancy, phenothiazines have caused jaundice, hyperreflexia, hyporeflexia or prolonged extrapyramidal disturbances in the child. 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 physician considers it essential. Prochlorperazine may occasionally prolong labour and at such a time should be withheld until the cervix is dilated 3-4 cm. Possible adverse effects on the foetus include lethargy or paradoxical hyperexcitability, tremor and a low Apgar score.
Phenothiazines may be excreted in milk, therefore, breastfeeding is not recommended during treatment with APO-Prochlorperazine.
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 or whether it has a harmful effect on the newborn. Therefore, prochlorperazine is not recommended for nursing 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 drowsiness and advised not to drive or operate machinery, particularly during the early days of treatment, until they know how prochlorperazine affects them.

4.8 Adverse Effects (Undesirable Effects)

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

More common reactions.

Vascular.

More common: orthostatic hypotension. Elderly or volume depleted patients are particularly susceptible; it is more likely to occur after intramuscular injection.
Not known: 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).

Blood and lymphatic system disorders.

Not known: eosinophilia.
Less common: agranulocytosis, atypical lymphocytes, thrombocytopenia, leucopenia, aplastic anaemia.

Biochemical abnormalities.

Less common: elevated serum levels of bilirubin and hepatic enzymes may occur if the patient develops cholestatic jaundice.

Cardiac disorders.

Less common: peripheral oedema, cardiac arrhythmias, ECG changes, QT interval prolongation, ST depression, U-Wave and T-Wave changes. Cardiac arrhythmias, including ventricular arrhythmias and atrial arrhythmias, atrioventricular block, ventricular tachycardia, which may result in ventricular fibrillation or cardiac arrest have been reported during phenothiazine therapy possibly related to dosage.
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.
Not known: torsade de pointes.

Skin and subcutaneous tissue disorders.

Less common: dermatitis allergic or contact dermatitis, maculopapular eruptions, erythema multiforme, urticaria, photosensitivity, abnormal pigmentation.
Less common: contact skin sensitisation may occur rarely in those frequently handling preparations of certain phenothiazines (see Section 4.4 Special Warnings and Precautions for Use).

Endocrine disorders.

Less common: endocrine disturbances including elevated prolactin levels, hyperglycaemia, intolerance to glucose, hypoglycaemia, menstrual irregularities, galactorrhoea, gynaecomastia, amenorrhoea, impotence.
Not known: temperature regulation disorder.

Gastrointestinal.

More common: constipation, dry mouth.
Less common: paralytic ileus.

Renal and urinary disorders.

Less common: urinary retention, priapism, inhibition of ejaculation.

Hepatobiliary disorders.

Less common: jaundice cholestatic, liver damage.

Nervous system disorders.

More common: drowsiness, akathisia, parkinsonism, (with dyskinesia, tremor and rigidity).
Less common: dystonia or dyskinesias including oculogyric crisis usually transitory are commoner in children and young adults, and usually occur after dosage increases.
Less common: tardive dyskinesia: if this occurs it is usually, but not necessarily, after prolonged or high dosage. It can even occur after treatment has been stopped. Dosage should therefore be kept low whenever possible.
Less common: torticollis and opisthotonus and trismus, seizures, EEG changes, headache, insomnia, catatonia, hyperpyrexia, agitation, dizziness.
Less common: cases of convulsions have been reported.
Not known: anticholinergic effects such as ileus paralytic, risk of urinary retention, dry mouth, constipation, accommodation disorder.
Not known: extrapyramidal syndrome: akinesia with or without hypertonia, partially relieved by anticholinergic antiparkinsonian agents; hyperkinetic-hypertonic movements, motor excitation; and akathisia.
Not known: insomnia.
Not known: convulsions.
Not known: dizziness.
Not known: sedation or somnolence.
Not known: neuroleptic malignant syndrome (hyperthermia, rigidity, autonomic dysfunction and altered consciousness) may occur with any neuroleptic (see Section 4.4 Special Warnings and Precautions for Use).

Eye disorders.

More common: blurred vision.
Less common: pigmentary retinopathy.
Less common: corneal deposits (brownish deposits in the anterior segment of the eye, due to accumulation of the product and generally without effect on vision).
Not known: accommodation disorder.
Ocular changes and the development of metallic greyish-mauve coloration of exposed skin have been noted in some individuals mainly females, who have received chlorpromazine continuously for long periods (four to eight years). This could possibly happen with prochlorperazine.

Psychiatric disorders.

Less common: activation of psychotic symptoms.
Not known: agitation, confusional state, delirium, anxiety.

Respiratory thoracic and mediastinal disorders.

Less common: respiratory depression, nasal stuffiness.

Metabolism and nutrition disorders.

Less common: hyponatraemia and syndrome of inappropriate antidiuretic hormone secretion (SIADH) 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.

Less common: type 1 hypersensitivity reactions such as angioedema and urticaria have been reported.
Less common: anaphylactic reaction.

Reproductive system and breast disorders.

Less common: priapism, ejaculation disorder.

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).

Investigations.

Not known: weight increased, liver function test abnormal.

Serious 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 phenothiazines 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 (Australia).

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, possible with sudden apnoea. There is no information available regarding lethal dose in man.
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.

1. Acute dystonic reactions.

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

2. 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. 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 131126 (Australia).

5 Pharmacological Properties

5.1 Pharmacodynamic Properties

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.

Mechanism of action.

As with other phenothiazines, prochlorperazine has actions on several neurotransmitter systems:
1. Antidopamine action, which probably contributes to both the therapeutic effect and unwanted effects including extrapyramidal disorders and endocrine disturbances.
2. α-Adrenoreceptor antagonism, which contributes to cardiovascular side effects such as orthostatic hypotension and reflex tachycardia.
3. Potentiation of noradrenaline by blocking its reuptake into nerve terminals.
4. Weak anticholinergic action.
5. Weak antihistamine action.
6. 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 in clinically and metabolic pathways may differ. Similar overall pharmacokinetic patterns however would occur in the human.

Absorption.

Prochlorperazine is well absorbed from the 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 (approx. 0.1%) of prochlorperazine and its metabolites are excreted in the first 24 hours in the urine and the drug may continue to be excreted in the urine for up to 3 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

Lactose monohydrate, maize starch, purified water, colloidal anhydrous silica, magnesium stearate.

6.2 Incompatibilities

Incompatibilities were either not assessed or not identified as part of the registration of this medicine.

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 25°C and protect from light.

6.5 Nature and Contents of Container

APO-Prochlorperazine 5 mg tablets.

(PVC/PVDC/Aluminium foil) blister packs of 14*, 25, 28*, 56*, 84*, 100* and 250* tablets.
AUST R 158416.
(*non-marketed pack sizes).
Apotex Pty Ltd is the licensee of the registered trade mark APO from the registered proprietor, Apotex Inc.

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

Prochlorperazine maleate contains 62% of the active base. It is an odourless, nonhygroscopic white or almost white, fine granular powder, which becomes coloured on exposure to light. It is sparingly soluble (about 0.1%) in water, ethanol or methanol and is insoluble in ether or chloroform.

Chemical structure.

Chemical name: 2 chloro-10-(3-(4-methyl piperazinyl)-propyl) phenothiazine.
Molecular weight: 606.2.
Molecular formula: C₂₀H₂₄ClN₃S.2C₄H₄O₄.

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APO-Prochlorperazine 5 mg Tablets