Consumer medicine information

XYLOCAINE OINTMENT

Lidocaine (lignocaine)

BRAND INFORMATION

Brand name

Xylocaine 5% Ointment

Active ingredient

Lidocaine (lignocaine)

Schedule

S2

 

Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using XYLOCAINE OINTMENT.

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, pharmacist or dentist.

All medicines have risks and benefits.

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

Keep this leaflet with the medicine.

You may need to read it again.

What Xylocaine is for

Xylocaine 5% Ointment is used:

  • to provide temporary relief of pain and/or itching due to minor burns, non-blistered sunburn, insect bites and sore nipples;
  • to help prevent pain and discomfort and to act as a lubricant during certain medical procedures and tests performed by a doctor;
  • to help relieve pain of some conditions of the back passage such as haemorrhoids (piles) or fissures;
  • in dentistry to help prevent pain during scaling or injection and when fitting dentures.

Xylocaine belongs to a group of medicines called local anaesthetics. It works by making the pain nerves unable to pass messages to the brain.

Your doctor, pharmacist or dentist will have explained what Xylocaine 5% Ointment is used for and told you what dose you should use.

Follow all directions given to you by your doctor, pharmacist or dentist carefully.

They may differ from the information contained in this leaflet.

A health professional may recommend this medicine for another use. Ask them if you want more information.

Xylocaine 5% Ointment is not addictive.

Before you use Xylocaine

When you must not use it

Do not use Xylocaine 5% Ointment if you an allergy to:

  • the active ingredient lignocaine
  • other local anaesthetics of the same type
  • any of the ingredients listed at the end of this leaflet

Some of the symptoms of an allergic reaction may include:

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

Do not use Xylocaine 5% Ointment in children under 2 years of age.

Do not use 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 be using this medicine, talk to your doctor, pharmacist or dentist.

Before you start to use it

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

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

  • epilepsy
  • heart problems
  • liver problems
  • kidney problems
  • open wounds or infection where the ointment will be used
  • malignant hyperthermia or if you have a family history of malignant hyperthermia (Malignant hyperthermia is a condition characterised by dangerously high body temperature where a rapid rise in body temperature to a dangerously high level is brought on by general anaesthesia)

It may not be safe for you to use Xylocaine 5% Ointment if you have any of these conditions.

Tell your doctor or pharmacist if you are pregnant or plan to be pregnant or are breastfeeding.

Your doctor can discuss with you the risks and benefits involved.

Taking other medicines

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

Some medicines and Xylocaine 5% Ointment may interfere with each other. These include:

  • medicines to treat irregular heart beat such as amiodarone and mexiletine
  • antihypertensive medicines to help lower blood pressure such as betablockers
  • medicines used to treat epilepsy or fits such as phenytoin, phenobarbitone, primidone or carbamazepine
  • cimetidine, a medicine used to treat reflux and ulcers

If you have not told your doctor, pharmacist or dentist about any of these things, tell them before you use any Xylocaine 5% Ointment.

Using Xylocaine

How to use it

Your doctor, pharmacist or dentist will tell you how much ointment you should use. The dose depends on the size of the area and the procedure involved.

Apply a thin layer of the ointment to the affected area for adequate control of symptoms.

A sterile gauze pad covering to the affected area is recommended.

Do not apply to large areas of the body, except on the advice of a doctor or pharmacist.

Do not apply to broken skin.

Do not exceed the recommended dose or use of Xylocaine 5% Ointment for prolonged periods except on the advice of your doctor.

For tender or sore nipples, apply a small amount of the ointment on a piece of gauze. Wash all the ointment away before breastfeeding.

ADULTS:
Apply a thin layer of ointment to the affected area no more than 3 to 4 times a day when necessary.

The maximum single dose is 5g of ointment. This is roughly equivalent to squeezing a 15 cm length of ointment from the tube. Do not use more than 17 - 20g of ointment in any 24 hours.

CHILDREN (2 - 12 YEARS):
For children 2 to 12 years old, apply a thin layer to the affected area no more than 3 times a day, when necessary.

Do not use more than 0.1g ointment/kg bodyweight as a single dose.

Do not apply more than 3 doses during any 24 hours. Do not use in children under 2 years of age.

Ask your doctor, pharmacist or dentist if you are unsure about the amount of Xylocaine 5% Ointment to use.

Overdose

Immediately telephone your doctor or the Poisons Information Centre (telephone 13 11 26) for advice or go to Accident and Emergency at your nearest hospital immediately if you think that you or anyone else may have used too much Xylocaine 5% Ointment or accidentally swallowed Xylocaine 5% Ointment. Do this even if there are no signs of discomfort or poisoning. The first signs that too much Xylocaine 5% Ointment has been used are drowsiness, light headedness, dizziness and sometimes blurred vision. In the event of a serious overdosage, trembling, seizures or unconsciousness may occur.

While you are using it

Things you must not do

Do not eat or drink anything for at least 1 hour after using Xylocaine 5% Ointment in the mouth or throat area.

You may swallow your food down the wrong way, or burn or bite your mouth.

Do not use Xylocaine 5% Ointment on open wounds or infected areas.

Do not get Xylocaine 5% Ointment in your eyes.

If any of the ointment does go in your eye, rinse immediately with lots of water for at least 15 minutes and call your doctor.

Things you must do

Discontinue use if skin irritation occurs and seek advice from your doctor or pharmacist.

Discontinue use if the condition persists or worsens and seek advice from your doctor or pharmacist.

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

Side effects

Tell your doctor, pharmacist or dentist as soon as possible if you do not feel well while you are using Xylocaine 5% Ointment.

Xylocaine 5% Ointment will help to relieve pain and discomfort in most people, but it may have unwanted side effects in a few people.

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.

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

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

Stop using Xylocaine 5% Ointment and tell your doctor or pharmacist as soon as possible if you notice the following:

  • Skin rash or irritation

Tell your doctor immediately or go to Accident and Emergency at your nearest hospital if you notice any of the following:

  • Drowsiness
  • Confusion
  • Dizziness
  • Lightheadedness
  • Blurred vision
  • Ringing in the ears
  • Tremors
  • Fits
  • Unconsciousness
  • Low blood pressure
  • Slow heartbeat
  • Collapse
  • Wheezing or difficulty breathing
  • Chest pain
  • Severe rash or itching
  • Increased sweating

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

Tell your doctor if you notice anything else that is making you feel unwell. Other side effects not listed above may also occur is some people.

Storage

Keep your Xylocaine 5% Ointment in a cool place where the temperature stays below 25°C.

Do not store it or any other medicine in the bathroom or near a sink.

Heat and dampness can destroy some medicines.

Keep it where young children cannot reach it.

A locked cupboard at least one-and-a-half metres above the ground is a good place to store medicines.

Do not leave it in the car on hot days.

Disposal

Ask your pharmacist what to do with any ointment you have left over if your doctor tells you to stop using it, or you find that the expiry date has passed.

Product description

Xylocaine 5% Ointment is a white to greyish white ointment. Each gram of ointment contains 50mg lignocaine base,

plus

Propylene Glycol
Macrogols (300, 1500 and 3350)

Xylocaine 5% Ointment is available in pack sizes of 15g and 35g aluminium tube.

Lignocaine is known as lidocaine in the U.S.A.

BRAND INFORMATION

Brand name

Xylocaine 5% Ointment

Active ingredient

Lidocaine (lignocaine)

Schedule

S2

 

Name of the medicine

Lignocaine.

Excipients.

Propylene glycol, macrogols 300, 1500 and 3350.

Description

Molecular formula: C14H22N2O. MW: 234.3. CAS: 137-58-6. Xylocaine 5% Ointment is a water soluble topical anaesthetic.

Pharmacology

Lignocaine, the active ingredient of Xylocaine 5% Ointment, stabilises the neuronal membrane and prevents the initiation and conduction of nerve impulses, thereby effecting local anaesthetic action.
The onset of action of Xylocaine 5% Ointment occurs within 3-5 minutes on mucous membranes and the effect lasts for approximately 15-20 minutes. It is ineffective when applied to intact skin.
Lignocaine may be absorbed following topical administration to mucous membranes; its rate of absorption and the amount of dose absorbed depend upon the concentration and total dose administered, the specific site of application and the duration of exposure. In general, absorption occurs most rapidly after intratracheal administration. Lignocaine is well absorbed from the gastrointestinal tract but little intact drug appears in the circulation because of biotransformation in the liver.
Lignocaine is metabolised rapidly by the liver, and metabolites and unchanged drug are excreted by the kidney.
Excessive blood levels may cause changes in cardiac output, total peripheral resistance and mean arterial pressure. These changes may be attributable to a direct depressant effect of the anaesthetic agent on various components of the cardiovascular system.
Biotransformation includes oxidative N-dealkylation, ring hydroxylation, cleavage of the amide linkage and conjugation. The pharmacological/ toxicological actions of the metabolites are similar to, but not less potent than, those of lignocaine. Approximately 90% of lignocaine is excreted in the form of various metabolites, and less than 10% is excreted unchanged. The primary metabolite in urine is a conjugate of 4-hydroxy-2,6-dimethylaniline.
The plasma binding of lignocaine is dependent on drug concentration, and the fraction bound decreases with increasing concentration. At concentrations of 1 to 4 microgram of free base/mL, 60 to 80% of lignocaine is protein bound. Binding is also dependent on the plasma concentrations of the alpha-1-acid glycoprotein.
Lignocaine crosses the blood brain and placental barriers, presumably by passive diffusion.
Studies of lignocaine metabolism following iv bolus injection have shown that the elimination half-life is usually 1.5 to 2 hours. The half-life may be prolonged 2-fold or more in patients with liver dysfunction. Renal dysfunction does not affect lignocaine kinetics, but may increase the accumulation of metabolites.
Factors such as acidosis and the use of CNS stimulants and depressants affect the CNS levels of lignocaine required to produce overt systemic effects. Objective adverse manifestations become increasingly apparent with increasing venous plasma levels above 6.0 microgram free base/mL. In the rhesus monkey, arterial blood levels of 18 to 21 microgram/mL have been shown to be the threshold for convulsive activity.

Indications

Temporary relief of pain and/or itching associated with minor burns, nonblistered sunburn, insect bites, sore nipples.
Anaesthesia of mucous membranes, e.g. various anal conditions such as haemorrhoids and fissures.
Anaesthetic lubricant during examination and instrumentation, e.g. proctoscopy, sigmoidoscopy.
Surface anaesthesia of the gums prior to injection, before deep scaling and in conjunction with the fitting of new dentures.

Contraindications

Known hypersensitivity to lignocaine or other local anaesthetics of the amide type or to other components of the ointment.

Precautions

Warning.

Excessive dosage, or short intervals between doses, can result in high levels of lignocaine or its metabolites and serious adverse effects. Patients should be instructed to strictly adhere to the recommended dosage and administration guidelines. The management of serious adverse reactions may require the use of resuscitative equipment, oxygen and other resuscitative drugs.
Patients should not exceed the recommended dose or use Xylocaine 5% Ointment for prolonged periods except on the advice of their physician. If the condition persists or worsens, discontinue use and seek medical advice.
The lowest dose that results in effective anaesthesia should be used to avoid high plasma levels and serious adverse effects. Tolerance to elevated blood levels varies with the status of the patient.

Dosage reduction.

Debilitated, elderly and/or acutely ill patients, patients with sepsis, severe liver disease or cardiac failure and children should be given reduced doses commensurate with their age and physical status.

Excessive absorption.

Absorption from wound surfaces and mucous membranes is relatively high, especially in the bronchial tree. This should be taken into consideration when the ointment is used in children for treatment of large areas. Because of the possibility of significant systemic absorption, Xylocaine 5% Ointment should be used with caution in patients with traumatised mucosa and/or sepsis in the region of the proposed application.
If the dose or site of administration is likely to result in high blood levels, lignocaine, in common with other local anaesthetics, should be used with caution in patients with epilepsy, impaired cardiac conduction, bradycardia, impaired hepatic function and in severe shock.

Antiarrhythmic drugs class III.

Patients treated with antiarrhythmic drugs class III (e.g. amiodarone) should be kept under close surveillance and ECG monitoring considered, since cardiac effects may be additive.

Eating and drinking.

The use of topical anaesthetic agents in the oral cavity may interfere with swallowing and thus enhance the danger of aspiration of food or drink. For this reason, food or drink should not be ingested within 60 minutes of using local anaesthetics in the mouth or throat area. Numbness of the tongue or buccal mucosa may increase the danger of biting or heat trauma. Food, chewing gum or hot drinks should not be taken while the mouth or throat area is anaesthetised.

Malignant hyperthermia.

Many drugs used during the conduct of anaesthesia are considered potential triggering agents for familial malignant hyperthermia. It has been shown that the use of amide local anaesthetics in malignant hypothermia patients is generally safe, but cases of malignant hyperthermia have occasionally been documented after use.

Endotracheal tube lubrication.

When used for endotracheal tube lubrication, the ointment may dry on the inner surface leaving residue which tends to clump with flexion, narrowing the lumen. Xylocaine 5% Ointment is, therefore, not recommended to be used for endotracheal tube lubrication.

Sterile instruments.

Xylocaine 5% Ointment is not intended for use with sterile instruments.

Carcinogenic and mutagenic potential.

Genotoxicity tests with lignocaine are inconclusive. In genotoxicity studies, a metabolite of lignocaine, 2,6-xylidine, showed evidence of activity in some tests but not in other tests. This metabolite has been shown to have carcinogenic potential (nasal and subcutaneous tumours) in preclinical toxicological studies evaluating chronic exposure.

Use in pregnancy.

(Category A)
Lignocaine crosses the placental barrier and may be taken up by foetal tissues. When used for surface anaesthesia, lignocaine blood levels after normal doses are low so little drug is available for placental transfer.
There are, however, no adequate and well controlled studies in pregnant women. Reproduction studies have been performed in rats at doses of 500 mg/kg/day and have revealed no evidence of harm to the foetus caused by lignocaine.
It is reasonable to assume that a large number of pregnant women and women of childbearing age have used lignocaine. No specific disturbances to the reproductive process have so far been reported.

Labour and delivery.

Lignocaine is not contraindicated in labour and delivery.

Use in lactation.

Lignocaine enters breast milk, but in such small quantities that there is generally no risk of affecting the child at therapeutic dose levels.

Use in children.

Xylocaine 5% Ointment is not recommended for use in children under 2 years of age.

Effects on ability to drive and operate machines.

Depending on the dose, local anaesthetics may have a very mild effect on mental function and coordination even in the absence of overt CNS toxicity and may temporarily impair locomotion and alertness. With the recommended doses of lignocaine ointment, adverse effects on the CNS are unlikely.

Contact with eyes.

Xylocaine 5% Ointment is not intended for ophthalmological use. If it inadvertently comes into contact with eyes, rinse immediately with copious amounts of water for at least 15 minutes and seek medical advice.

Interactions

Antiarrhythmic drugs.

Lignocaine should be used with caution in patients receiving other local anaesthetics or agents structurally related to local anaesthetics, e.g. antiarrhythmic drugs such as mexiletine, since the toxic effects are additive.
Specific interaction studies with lidocaine and antiarrhythmic drugs class III (e.g. amiodarone) have not been performed, but caution is advised.

Enzyme inducing drugs.

Phenytoin and other antiepileptic drugs, such as phenobarbitone, primidone and carbamazepine, appear to enhance the metabolism of lignocaine but the significance of this effect is not known. Phenytoin and lignocaine have additive cardiac depressant effects.

Clearance reducing drugs.

Cimetidine or beta blockers have been shown to cause potentially toxic plasma concentrations when lignocaine is given in repeated high doses over a longer period of time. Therefore, caution should be taken if lignocaine was administered at higher than the recommended doses over extended period of time.

Adverse Effects

Systemic adverse reactions are rare and may result from high plasma levels caused by excessive dosage or rapid absorption, or may result from a hypersensitivity, idiosyncrasy or reduced tolerance on the part of the patient. Such reactions are systemic in nature and involve the central nervous system and/or the cardiovascular system.

Central nervous system.

CNS reactions are excitatory and/or depressant and may be characterised by lightheadedness, nervousness, apprehension, euphoria, confusion, dizziness, drowsiness, tinnitus, blurred vision, vomiting, sensations of heat, cold or numbness, twitching, tremors, convulsions, unconsciousness and possibly respiratory arrest. The excitatory reactions may be brief or may not occur at all, in which case the first manifestations of toxicity may be drowsiness, progressing to unconsciousness and respiratory arrest.
Drowsiness following administration of lignocaine is usually an early sign of a high blood level of the drug and may occur as a result of rapid absorption.

Cardiovascular.

Cardiovascular reactions are usually depressant and may be characterised by hypotension, myocardial depression, bradycardia and possibly cardiac arrest.

Allergic reactions.

Allergic reactions may occur as a result of sensitivity either to the local anaesthetic agent or to other ingredients in the formulation. Allergic reactions as a result of sensitivity to lignocaine are rare (< 0.1%). The detection of sensitivity by skin testing is of doubtful value.
The extremely rare cases of allergy to local anaesthetic preparations have included bronchospasm, chest pain, dyspnoea, pruritus, rash, rhinitis, increased sweating, urticaria, sleepiness, dizziness, paraesthesia, oedema and, in the most severe instances, anaphylactic shock. Several cases of contact dermatitis have been reported with the use of lignocaine.

Endotracheal tube occlusions.

There have been rare reports of endotracheal tube occlusions associated with the presence of dried ointment residue in the inner lumen of the tube (see Precautions).
Local skin irritation has been reported with topical products which contain propylene glycol.

Dosage and Administration

As with any local anaesthetic, reactions and complications are best averted by employing the minimal effective dosage. Debilitated, acutely ill or elderly patients and children should be given doses commensurate with their age and physical condition.
The dose of topical lignocaine should be taken into consideration in estimating the total dose of lignocaine if parenteral lignocaine is to be administered concomitantly.
The ointment should be applied in a thin layer for adequate control of symptoms. A sterile gauze pad covering to the affected area is recommended.
The ointment should not be applied to large areas of the body, except on the advice of a doctor. It should not be applied on broken skin.
In dentistry, apply to previously dried oral mucosa and allow at least 3-5 minutes for anaesthesia to become effective. When inserting new dentures, apply to all denture surfaces contacting mucosa.
For tender nipples, apply on a small piece of gauze; the ointment must be washed away before the next feeding.

Adults.

The ointment should be applied to the affected area no more than 3 to 4 times a day, when necessary. The maximum single recommended dose of Xylocaine 5% Ointment is 5 g, containing 250 mg of lignocaine base (approximately equivalent to 300 mg lignocaine hydrochloride). This is roughly equivalent to squeezing a 15 cm length of ointment from the tube. Not more than 17-20 g of the ointment should be administered in any 24 hour period.

Children.

In children 2-12 years of age, the ointment should be applied to the affected area no more than 3 times a day, when necessary. A single dose should not exceed 0.1 g ointment/kg bodyweight (corresponding to 5 mg lignocaine/kg bodyweight). Not more than three doses should be administered during 24 hours.

Overdosage

In the event of an overdose, contact the Poisons Information Centre on 131 126.

Management of local anaesthetic emergencies.

The first consideration is prevention, best accomplished by careful and constant monitoring of cardiovascular and respiratory vital signs and the patient's state of consciousness after each local anaesthetic administration. At the first sign of change, oxygen should be administered.

Treatment.

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. thiopental) or a benzodiazepine (e.g. diazepam) may be administered intravenously. The clinician should be familiar with these anticonvulsant drugs prior to use of local anaesthetics.
Dialysis is of negligible value in the treatment of acute overdosage with lignocaine.

Presentation

Ointment (white-greyish white, water soluble), 5% (50 mg/g lignocaine base): 15 g, 35 g (aluminium tube).

Storage

Store below 25°C.

Poison Schedule

S2.