Consumer medicine information

What is in this leaflet

This leaflet answers some of the common questions people ask about Pfizer Bupivacaine with adrenaline. It does not contain all the information that is known about Pfizer Bupivacaine with adrenaline.

It does not take the place of talking to your doctor or pharmacist.

All medicines have risks and benefits. Your doctor will have weighed the risks of you using Pfizer Bupivacaine with adrenaline against the benefits they expect it will have for you.

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

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

What Pfizer Bupivacaine with adrenaline is used for

Pfizer Bupivacaine with adrenaline is used to prevent or relieve pain, but it will not put you to sleep.

Pfizer Bupivacaine with adrenaline is also used after surgery to relieve pain. It can also be used to make childbirth less painful.

Pfizer Bupivacaine with adrenaline belongs to a group of medicines called local anaesthetics.

When injected, it makes the nerves nearby unable to pass messages to the brain and will therefore prevent or relieve pain.

Depending on the amount used, Pfizer Bupivacaine with adrenaline will either totally stop pain or will cause a partial loss of feeling.

Bupivacaine is combined with adrenaline (epinephrine) to make it last longer. Adrenaline (epinephrine) makes the blood vessels at the site of injection narrower, which keeps the Bupivacaine where it is needed for a longer time.

Your doctor will have explained why you are being treated with Pfizer Bupivacaine with adrenaline and told you what dose you will be given.

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

Your doctor may prescribe this medicine for uses other than those listed above. Ask your doctor if you want more information.

Pfizer Bupivacaine with adrenaline is not addictive

Before you are given Pfizer Bupivacaine with adrenaline

When you must not take it

Ask your doctor about the risks and benefits of being given Pfizer Bupivacaine with adrenaline while you are pregnant or breastfeeding. We do not know if it is safe for you to be given it while you are pregnant. It may affect your baby if you take it early in pregnancy or in the last weeks before your baby is due.

However, it can be used during childbirth.

Your baby can take in very small amounts of Pfizer Bupivacaine with adrenaline from breast milk if you are breastfeeding, but it is unlikely that the amount available to the baby will do any harm.

Pfizer Bupivacaine with adrenaline will only be used if the solution is clear, the package is undamaged and the use by (expiry) date marked on the pack has not been passed. It may have no effect at all, or worse, an entirely unexpected effect if you are given Pfizer Bupivacaine with adrenaline after the expiry date.

Before you are given it

You must tell your doctor if:

1. you have any allergies to

• any ingredients listed at the end of this leaflet
• other local anaesthetics e.g. lignocaine
• any other substances

If you have an allergic reaction, you may get a skin rash, hayfever, have difficulty breathing or feel faint.

2. you have any of these medical conditions

• problems with your blood pressure or circulation
• blood poisoning
• problems with the clotting of your blood
• acidosis, or too much acid in the blood.
• Epilepsy
• Nerve problems
• heart, liver or kidney problems
• disease of the brain or spine
• thyrotoxicosis
• diabetes
• muscle disease or weakness (e.g. myasthenia gravis)

It may not be safe for you to take Pfizer Bupivacaine with adrenaline if you have any of these conditions.

Taking other medicines

Tell your doctor if you are taking any other medicines, including

• medicines that control your heart beat
• medicines used to thin the blood, including aspirin
• low molecular weight heparin or other medicines used to prevent blood clots
• medicines for depression
• medicines that you buy at the chemist, supermarket or health food shop.

These medicines may affect the way Pfizer Bupivacaine with adrenaline works.

Your doctor or pharmacist can tell you what to do if you are taking any of these medicines.

If you have not told your doctor about any of these things, tell them before you are given any Pfizer Bupivacaine with adrenaline.

How Pfizer Bupivacaine with adrenaline is given

Pfizer Bupivacaine with adrenaline will be injected by your doctor into the skin, near a single nerve, or into an area which contains a large number of nerves. This will result in an area of numbness at the site of injection, near the site of injection or in an area that may seem unrelated to the site of injection. The last will be the case if you are given an EPIDURAL injection (an injection around the spinal cord) and will result in a feeling of numbness in your lower body.

If you are receiving an EPIDURAL INFUSION it will be injected by your doctor into the epidural space, near your spinal cord, through a space between vertebrae in your lower back. A thin tube will be inserted so a continuous dose can be given over a period of time.

Pfizer Bupivacaine with adrenaline should not be injected directly into the blood.

The dosage you will be given will depend on your body size, age and the type of pain relief required.

Your doctor will have had a lot of experience injecting Pfizer Bupivacaine with adrenaline or other local anaesthetics and will choose the best dose for you. They will be willing to discuss this decision with you.

Overdose

The doctor giving you Pfizer Bupivacaine with adrenaline will be experienced in the use of local anaesthetics, so it is unlikely that you will be given an overdose.

However, if you are particularly sensitive to Pfizer Bupivacaine with adrenaline, or the dose is accidentally injected directly into your blood, you may develop problems for a short time with your sight or hearing. You may get a numb feeling in or around the mouth, feel dizzy or stiff, or have twitchy muscles.

Whenever you are given Pfizer Bupivacaine with adrenaline, equipment will be available to revive you if an overdose happens.

While you are being given Pfizer Bupivacaine with adrenaline

Things to be careful of

Be careful driving or operating machinery after you have been given Pfizer Bupivacaine with adrenaline. You may be drowsy and your reflexes may be slow.

Do not drink alcohol while you are being given Pfizer Bupivacaine with adrenaline. If you drink alcohol while you are being given Pfizer Bupivacaine with adrenaline your blood pressure may drop, making you feel dizzy and faint.

Please talk to your doctor or pharmacist about these possibilities if you think they may bother you

Side effects

Tell your doctor or nurse as soon as possible if you do not feel well while you are being given Pfizer Bupivacaine with adrenaline.

Pfizer Bupivacaine with adrenaline will help relieve pain in most people, but it may have unwanted side-effects.

All medicines can have side effects. Sometimes they are serious, most of the time they are not. You may need medical treatment if you get some of the side effects.

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

Tell your doctor or nurse immediately if you notice any of the following:

• nervousness
• dizziness
• blurred vision
• a tingling feeling ("pins and needles")
• ringing in the ears
• numbness
• feeling strange (disoriented)
• nausea (feeling sick), vomiting

These are all mild side effects of Pfizer Bupivacaine with adrenaline.

After an epidural injection you may develop a headache or backache which is not always related to the medicine used. This can, on rare occasions, last for some months after the injection is given.

If Pfizer Bupivacaine with adrenaline is given wrongly, or you are very sensitive to it, it sometimes causes

• fits
• unconsciousness
• breathing problems
• low blood pressure
• slow heart beat
• collapse

These are all serious side effects. You may need urgent medical attention.

Serious side effects are rare.

Some people may get other side effects while being given Pfizer Bupivacaine with adrenaline.

Tell your doctor if you notice anything that is making you feel unwell.

After using Pfizer Bupivacaine with adrenaline

Storage

Pfizer Bupivacaine with adrenaline will be stored by your doctor or pharmacist under the recommended conditions.

Pfizer Bupivacaine with adrenaline should be kept in a cool dry place where the temperature stays below 25°C and should also be protected from light. Do not freeze.

Disposal

Any Pfizer Bupivacaine with adrenaline which is not used, and which is left in the container, will be disposed of in a safe manner by your doctor or pharmacist

Product description

Pfizer Bupivacaine with adrenaline solution is clear and colourless. It is practically free from visible particles.

Ingredients

Pfizer Bupivacaine with adrenaline solution contains Bupivacaine hydrochloride monohydrate and Adrenaline (epinephrine) acid tartrate as the active ingredients, plus Sodium chloride, Citric acid or sodium citrate pH.

• Sodium chloride
• Water for injections
• Sodium metabisulfate

This medicine does not contain lactose, sucrose, gluten, tartrazine or any other azo dyes (include any that are appropriate).

Pfizer Bupivacaine with adrenaline, Bupivacaine 0.25% with adrenaline (epinephrine) 1: 400,000

Bupivacaine hydrochloride monohydrate 2.5mg/mL

Adrenaline (epinephrine) acid tartrate 2.5 microgram/mL

Pack Size 5x 20mL

Pack type single dose vial

AUST R 292525

Pfizer Bupivacaine with adrenaline, Bupivacaine 0.5% with adrenaline (epinephrine) 1: 200,000

Bupivacaine hydrochloride monohydrate 5.0mg/mL

Adrenaline (epinephrine) acid tartrate 5.0 microgram/mL

Pack Size 5x 20mL

Pack type single dose vial

AUST R 292527

Not all presentation are marketed

Sponsor

Pfizer Bupivacaine with adrenaline is supplied in Australia by:

Pfizer Australia Pty Ltd
38-42 Wharf Road
West Ryde NSW 2114
Australia

This leaflet was prepared in September 2018

Published by MIMS June 2019

Boxed Warnings

Not for intravenous administration under any circumstances.

1 Name of Medicine

Bupivacaine hydrochloride (as monohydrate).
Adrenaline (epinephrine) acid tartrate.

2 Qualitative and Quantitative Composition

Pfizer Bupivacaine with Adrenaline, bupivacaine 0.25% w/v with adrenaline (epinephrine) 1:400,000 injection vial contains bupivacaine hydrochloride 2.5 mg/mL with adrenaline (epinephrine) 2.5 microgram/mL).
Pfizer Bupivacaine with Adrenaline, bupivacaine 0.5% w/v with adrenaline (epinephrine) 1:200,000 injection vial contains bupivacaine hydrochloride 5 mg/mL with adrenaline (epinephrine) 5 microgram/mL).
Bupivacaine hydrochloride is a white or almost white, crystalline powder or colourless crystal that is soluble in water and freely soluble in ethanol (96%). Bupivacaine has a pKa of 8.1 and is more lipid soluble than lignocaine.
Adrenaline (epinephrine) acid tartrate appears as a white or greyish-white, crystalline powder that is freely soluble in water and slightly soluble in ethanol (96%).
Pfizer Bupivacaine with Adrenaline solution for injection is a sterile, isotonic aqueous solution of bupivacaine hydrochloride, adrenaline (epinephrine) and sodium chloride in Water for Injections BP. The pH of the solution is adjusted with citric acid and sodium citrate to remain between 3.3 - 5.0. Pfizer Bupivacaine with Adrenaline contain sodium metabisulfite as an antioxidant.
Excipient(s) with known effect. Sodium metabisulfite.
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Pfizer Bupivacaine with Adrenaline is a sterile solution for injection. The solutions are practically free from visible particles.

4 Clinical Particulars

4.9 Overdose

Acute emergencies associated with the use of local anaesthetics are generally related to high plasma levels or to unintended subarachnoid injection of the local anaesthetic solution (see Section 4.8 Adverse Effects (Undesirable Effects); Section 4.4 Special Warnings and Precautions for Use).
With accidental intravascular injections of local anaesthetics, the toxic effects will be obvious within 1 - 3 minutes. With overdosage, peak plasma concentrations may not be reached for 20 - 30 minutes, depending on the site of injection and toxic signs will be delayed. Toxic reactions mainly involve the central nervous and cardiovascular systems.
Symptoms of acute toxicity. Central nervous system toxicity is a graded response with symptoms and signs of escalating severity. The first symptoms are circumoral paraesthesia, numbness of the tongue, lightheadedness, hyperacusis and tinnitus. Visual disturbances and muscular tremors are more serious and precede the onset of generalised convulsions. These signs must not be mistaken for neurotic behaviour.
Unconsciousness and grand mal convulsions may follow. These may last from a few seconds to several minutes. Hypoxia and hypercapnia occur rapidly following convulsions due to increased muscular activity, together with the interference with normal respiration and loss of the airway. In severe cases, apnoea may occur.
Acidosis, hyperkalaemia, hypocalcaemia and hypoxia increase and extend the toxic effects of local anaesthetics.
Recovery is due to redistribution of the local anaesthetic drug from the central nervous system and metabolism. Recovery may be rapid unless large amounts of the drug have been injected.
Signs of cardiovascular toxicity indicates a more severe situation. Hypotension, bradycardia, decreased cardiac output, heart block, arrhythmia and even ventricular arrhythmias, ventricular fibrillation and cardiac arrest may occur as a result of high systemic concentrations of local anaesthetics.
Overdosage with adrenaline (epinephrine) produces a rapid rise in blood pressure which may result in cerebrovascular haemorrhage, cardiac arrhythmia leading to ventricular fibrillation and death. Pulmonary oedema may also lead to death because of the peripheral constriction and cardiac stimulation produced.
Cardiovascular toxic effects are generally preceded by signs of toxicity in the central nervous system, unless the patient is receiving a general anaesthetic or is heavily sedated with drugs such as benzodiazepines or barbiturates.
Treatment of overdose. If signs of acute systemic toxicity appear, injection of the local anaesthetic should be immediately stopped.
If convulsions occur then immediate attention is required for the maintenance of patent airway and assisted or controlled ventilation with oxygen, via a positive airway pressure delivery system mask. Adequacy of the circulation should then be evaluated, bearing in mind that drugs used to treat convulsions depress the circulation when administered intravenously.
Should convulsions persist despite adequate respiratory support, and if the status of the circulation permits, appropriate anticonvulsant medication such as an ultra-short acting barbiturate (e.g. thiopentone) or a benzodiazepine (e.g. diazepam) may be administered IV. The clinician should be familiar with these anticonvulsant drugs prior to use of local anaesthetics.
Suxamethonium will stop the muscle convulsions rapidly but will require tracheal intubation and controlled ventilation, and should only be used by those familiar with these procedures.
If cardiovascular depression occurs (hypotension, bradycardia), appropriate treatment with intravenous fluids, vasopressor, inotropic agents and/or lipid emulsion should be considered. Children should be given doses commensurate with age and weight.
If ventricular fibrillation or cardiac arrest occurs, effective cardiovascular resuscitation treatment must be instituted and maintained for a prolonged period if necessary. Optimal oxygenation and ventilation, and circulatory support as well as treatment of acidosis are of vital importance.
To counteract the pressor effects of adrenaline (epinephrine), use rapidly acting vasodilators, for instance nitrates or α-blocking agents.
For information on the management of overdose, contact the Poisons Information Centre on 13 11 26 (Australia).

5 Pharmacological Properties

5.3 Preclinical Safety Data

Genotoxicity. Formal studies of mutagenic potential have not been carried out.
Carcinogenicity. Long-term studies in animals of most local anaesthetics, including bupivacaine, to evaluate the carcinogenic potential have not been conducted.

6 Pharmaceutical Particulars

6.7 Physicochemical Properties

The chemical name for bupivacaine hydrochloride (as monohydrate) is (2RS)-1-Butyl-N-(2,6-dimethylphenyl) piperidine-2-carboxamide hydrochloride monohydrate.
Bupivacaine hydrochloride (as monohydrate) has the chemical formula C₁₈H₂₉ClN₂O,H₂O and molecular weight value 342.9.
The chemical name for adrenaline (epinephrine) acid tartrate is (1R)-1-(3,4-Dihydroxyphenyl)-2-(methylamino)ethanol hydrogen (2R,3R)-2,3-dihydroxybutanedioate.
Adrenaline (epinephrine) acid tartrate has the chemical formula C₁₃H₁₉NO₉ and a molecular weight of 333.3.
Chemical structure. The chemical structure of bupivacaine hydrochloride (as monohydrate) is:
https://stagingapi.mims.com/au/public/v2/images/fullchemgif/CSBUPIHY.gif The chemical structure of adrenaline (epinephrine) acid tartrate is:
https://stagingapi.mims.com/au/public/v2/images/fullchemgif/CSDRENAT.gifCAS number. The CAS number for bupivacaine hydrochloride, (as monohydrate) is 73360-54-0.
The CAS number for bupivacaine HCl anhydrous is 18010-40-7.
The CAS number for adrenaline (epinephrine) is 51-43-4.
The CAS number for adrenaline acid tartrate is 51-42-3.

7 Medicine Schedule (Poisons Standard)

S4.