Consumer medicine information

What is in this leaflet

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

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 taking Xylocaine against the benefits they expect it will have for you.

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

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

What XYLOCAINE is for

Xylocaine is used to prevent or relieve pain, but it will not put you to sleep.

Xylocaine is also used after surgery to relieve pain. It can also be used to make childbirth less painful.

Xylocaine belongs to a group of medicines called local anaesthetics. It is injected into the body where it makes the nerves unable to pass messages to the brain.

Depending on the amount used, Xylocaine will either totally stop pain or will cause a partial loss of feeling.

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

Your doctor will have explained why you are being treated with Xylocaine 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 another use. Ask your doctor if you want more information.

Xylocaine is not addictive.

Before you are given XYLOCAINE

When you must not use it

If you are pregnant or breastfeeding do not use Xylocaine unless your doctor says so. Ask your doctor about the risks and benefits of using this medicine while you are pregnant or breastfeeding.

Xylocaine has been widely used during pregnancy and there have been no reports of any ill effects on the baby. It can be used during childbirth.

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

Xylocaine 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.

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 eg. bupivacaine
• other substances

If you have an allergic reaction, you may get a skin rash, hay fever or an asthma attack.

2. you have any of these medical conditions

• problems with your blood pressure or circulation
• blood poisoning
• problems with the clotting of your blood
• nerve problems, e.g. epilepsy
• heart, liver or kidney problems
• thyroid problems
• malignant hyperthermia
• diabetes
• skin infections

It may not be safe for you to take Xylocaine if you have any of these conditions.

Taking other medicines

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

• ones to control your heart beat
• ones for blood pressure (anti-hypertensives)
• ones for epilepsy or fits
• ones for depression
• cimetidine
• any medicines that you buy at the chemist, supermarket or health food shop.

These medicines may affect the way Xylocaine 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 Xylocaine.

How XYLOCAINE is given

Xylocaine 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).

Xylocaine 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 Xylocaine 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 Xylocaine 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 Xylocaine, 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 Xylocaine, equipment will be available to care for you if an overdose happens.

While you are being given it

Things to be careful of

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

Do not drink alcohol while you are being given Xylocaine. If you drink alcohol while you are being given Xylocaine 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 Xylocaine.

Xylocaine 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 if you notice any of the following and they worry you:

• tremors
• nervousness
• dizziness
• blurred vision
• drowsiness
• ringing in the ears
• numbness
• feeling strange (disoriented)
• nausea (feeling sick)
• vomiting

These are all mild side effects of Xylocaine.

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

If Xylocaine is given wrongly, or you are very sensitive to it, it sometimes causes

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

If you are sensitive to sodium metabisulphite (found in adrenaline (epinephrine) containing preparations), it may cause life-threatening reactions or less severe asthmatic episodes.

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

Some people may get other side effects while being given Xylocaine.

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

After using it

Storage

Xylocaine will be stored by your doctor or pharmacist under the recommended conditions.

2mL and 5mL Polyamp presentations, Xylocaine with adrenaline in glass ampoules and single dose vials should be kept in a cool dry place where the temperature stays below 25 °C.

20mL Polyamp presentations, Xylocaine in glass ampoules should be kept in a cool dry place where the temperature stays below 30 °C.

Disposal

Any Xylocaine from a single dose preparations which is not used, will be disposed of in a safe manner by your doctor or pharmacist.

Product description

Xylocaine and Xylocaine with Adrenaline containing solutions are clear and colourless.

Each Xylocaine solution contains lidocaine (lignocaine) hydrochloride as the active ingredient

plus

sodium chloride

sodium hydroxide +/- hydrochloric acid

water for Injections.

Each Xylocaine with Adrenaline solution contains lidocaine (lignocaine) hydrochloride and adrenaline (epinephrine) (as acid tartrate) as the active ingredients

plus

sodium chloride

sodium hydroxide

sodium metabisulfite (E223)

Water for Injections.

The exceptions are Xylocaine 1% with Adrenaline 1:100,000 and Xylocaine 2% with Adrenaline 1:80,000 5mL ampoules which may also use hydrochloric acid for pH adjustment.

For a full list of Xylocaine products see next page.

What is in Xylocaine®

XYLOCAINE 0.5% with Adrenaline 1:200,000
Contains lidocaine (lignocaine) hydrochloride 5 mg/mL and adrenaline (epinephrine) 5 microgram/mL (as acid tartrate)

in 20 mL* single dose vials

AUST R 12008

XYLOCAINE 1%
contains lidocaine (lignocaine) hydrochloride 10 mg/mL

in

50 X 2 mL polyethylene ampoules Polyamp®

AUST R 12013

50 x 5 mL polyethylene ampoules Polyamp®

AUST R 48357

5 x 20 mL polyethylene ampoules Polyamp®

AUST R 48361

XYLOCAINE 1% with Adrenaline 1:100,000
contains lidocaine (lignocaine) hydrochloride 10 mg/mL and adrenaline (epinephrine) 10 microgram/mL as acid tartrate

in

10 x 5 mL* glass ampoules

AUST R 12017

XYLOCAINE 1% with Adrenaline 1:200,000
contains lidocaine (lignocaine) hydrochloride 10 mg/mL and adrenaline (epinephrine) 5 microgram/mL (as acid tartrate)

in

5 x 20 mL* single dose vials

AUST R 12015

XYLOCAINE 2%
contains lidocaine (lignocaine) hydrochloride 20 mg/mL

in

50 x 2 mL polyethylene ampoules Polyamp®

AUST R 12020

50 x 5mL polyethylene ampoules Polyamp®

AUST R 48362

5 x 20 mL polyethylene ampoules Polyamp®

AUST R 48364

XYLOCAINE 2% with Adrenaline 1:80,000
contains lidocaine (lignocaine) hydrochloride 20 mg/mL and adrenaline (epinephrine) 12.5 microgram/mL (as acid tartrate)

in

10 x 5 mL* glass ampoules

AUST R 54520

XYLOCAINE 2% with Adrenaline 1:200,000
contains lidocaine (lignocaine) 20 mg/mL and adrenaline (epinephrine) 5 microgram/mL (as acid tartrate)

in

5 x 20 mL* single dose vials

AUST R 12021

* contains sodium metabisulfite

Sponsor

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

This leaflet was revised in June 2017.

®Trade Marks herein are the property of the AstraZeneca group

Published by MIMS October 2017

1 Name of Medicine

Xylocaine: lidocaine (lignocaine) hydrochloride.
Xylocaine with Adrenaline: lidocaine (lignocaine) hydrochloride and adrenaline (epinephrine) acid tartrate.

2 Qualitative and Quantitative Composition

Plain aqueous solutions are sterile, isotonic and contain lidocaine (lignocaine) hydrochloride, sodium chloride, sodium hydroxide and/or hydrochloric acid for pH adjustment and water for injections.
Lidocaine (lignocaine) hydrochloride with adrenaline (epinephrine) acid tartrate solutions are also sterile and isotonic, and in addition contain adrenaline (epinephrine) acid tartrate and sodium metabisulfite.
Excipients with known effect. Xylocaine with Adrenaline contains sulphites.
Xylocaine solutions contain no antimicrobial agent and should be used only once and any residue discarded.
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Clear, colourless solution for injection.

4 Clinical Particulars

4.9 Overdose

Symptoms. 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, the toxic effect will be obvious within 1 - 3 min. With overdosage, peak plasma concentrations may not be reached for 20 - 30 min depending on the site of injection, and toxic signs will be delayed. Toxic reactions mainly involve the central nervous and cardiovascular systems.
In children, early signs of local anaesthetic toxicity may be difficult to detect in cases where the block is given during general anaesthesia.
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 disturbance 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 hypercarbia occur rapidly following convulsions due to the increased muscular activity, together with the interference with normal respiration and loss of the airway. In severe cases, apnoea may occur. Acidosis increases 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.
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 huge systemic concentrations of local anaesthetics.
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 a benzodiazepine or a barbiturate. In rare cases, cardiac arrest has occurred without prodromal CNS effects.
Treatment of overdosage. If signs of acute systemic toxicity appear, injection of the local anaesthetic should be stopped immediately. If convulsions occur then immediate attention is required for the maintenance of a 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 ultrashort 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 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.
If cardiovascular depression occurs (hypotension, bradycardia), appropriate treatment with intravenous fluids, vasopressor, chronotropic and/or inotropic agents should be considered. Children should be given doses commensurate with age and weight.
Dialysis is of negligible value in the treatment of acute overdosage with lidocaine (lignocaine).
To counteract the pressor effects of adrenaline (epinephrine) acid tartrate, use rapidly acting vasodilators, for instance nitrates or α-blocking agents.
For treatment of reactions caused by adrenaline (epinephrine) acid tartrate, consult standard textbooks.
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. The genotoxic potential of 2,6-xylidine has been studied with mixed results. Positive results were reported in assays for gene mutations (weakly positive in the Ames test with metabolic activation and in the mouse lymphoma assay) and chromosomal damage (chromosomal aberrations in Chinese hamster ovary cells at concentrations at which the drug precipitated from solution). No evidence of genotoxicity was found in in vivo assays for chromosomal damage (micronucleus assay) and DNA damage (unscheduled DNA synthesis). Covalent binding studies of DNA from liver and ethmoid turbinates in rats indicate that 2,6-xylidine may be genotoxic under certain conditions in vivo.
Carcinogenicity. A two year oral toxicity study of 2,6-xylidine, a metabolite of lidocaine (lignocaine), has shown that in both male and female rats 2,6-xylidine in daily doses of 900 mg/m² (150 mg/kg) resulted in carcinomas and adenomas of the nasal cavity. No nasal tumours were observed in the low dose (15 mg/kg) or control animals. In addition, the compound also caused subcutaneous fibromas and/or fibrosarcomas in male and female rats (significant at 150 mg/kg).

6 Pharmaceutical Particulars

6.7 Physicochemical Properties

The chemical name for lidocaine (lignocaine) hydrochloride is 2-Diethylaminoaceto-2'6'- xylidide hydrochloride. The Australian Approved Name is lidocaine (lignocaine) hydrochloride.
The chemical name for adrenaline (epinephrine) acid tartrate is (R)-1-(3,4-Dihydroxyphenyl)- 2-methylaminoethanol. The Australian Approved Name is adrenaline (epinephrine).
Lidocaine (lignocaine) is classed as a membrane stabilising agent and is a local anaesthetic of the amide type. It is extremely stable and plain solutions can be sterilised by autoclaving, repeated a maximum of two times if necessary. Xylocaine solutions are available with or without adrenaline (epinephrine) acid tartrate.
Plain aqueous solutions of lidocaine (lignocaine) hydrochloride have a pH of 5.0 - 7.0 (approx.); lidocaine (lignocaine) hydrochloride with adrenaline (epinephrine) acid tartrate solutions have a pH of 3.3 - 5.5 (approx.). Lidocaine (lignocaine) base has a pKa of 7.85 (25°C), an oil/water coefficient of 2.9 and a molecular weight of 234.3.
Chemical structure. The chemical structure of lidocaine (lignocaine) hydrochloride is:
https://stagingapi.mims.com/au/public/v2/images/fullchemgif/CSLIGNOC.gif The chemical structure of adrenaline (epinephrine) acid tartrate is:
https://stagingapi.mims.com/au/public/v2/images/fullchemgif/CSADRENA.gif CAS number. The CAS number for lidocaine (lignocaine) hydrochloride monohydrate (AAN) is 6108-05-0 and lidocaine (lignocaine) hydrochloride is 73-78-9.
The CAS number for adrenaline (epinephrine) acid tartrate is 51-43-4.

7 Medicine Schedule (Poisons Standard)

S4 (Prescription only medicine).

Summary Table of Changes

https://stagingapi.mims.com/au/public/v2/images/fulltablegif/XYLOCIST.gif