Xylocaine

Italy
Brand name Xylocaine
Form solution for injection
Active substance / Dosage
LIDOCAINE HYDROCHLORIDE
Prescription type Prescription only – non-repeatable
ATC code
N01BB02
Registration number 004535
Manufacturer ASPEN PHARMA TRADING LIMITED

Table of Contents

Package leaflet: Information for the patient

XYLOCAIN 20 mg/ml injection solution

lidocaine hydrochloride
Please read this leaflet carefully before you are given this medicine because it contains important information for you.

  • Keep this leaflet. You may need to read it again.
  • If you have any questions, ask your doctor or nurse.
  • This medicine has been prescribed for you only. Do not give it to other people, even if they have the same symptoms as you, because it could be harmful.
  • If you experience any side effects, including those not listed in this leaflet, contact your doctor or pharmacist. See section 4.

Contents of this leaflet:

  1. What Xylocain is and what it is used for
  2. What you need to know before you are given Xylocain
  3. How Xylocain will be administered to you
  4. Possible side effects
  5. How to store Xylocain
  6. Contents of the pack and other information

1. What Xylocaine is and what it is used for

Xylocaine contains lidocaine hydrochloride, a medicine belonging to the group of local anaesthetic medicines.
Xylocaine is used to numb (anaesthetize) parts of the body in adults and adolescents aged 12 years and older.
Xylocaine is used for local anaesthesia, that is, to eliminate pain in a specific area of the body without loss of consciousness.

2. What you should know before Xylocaine is administered to you

Xylocaine will not be administered to you if:

  • you are allergic to lidocaine hydrochloride or to any of the other ingredients of this medicine (listed in section 6).
  • you are allergic to other local anesthetics and/or similar substances.
  • you are allergic to the preservative methyl parahydroxybenzoate (methyl paraben), ester-type local anesthetics, or to the metabolite para-aminobenzoic acid (PABA).
  • administration is intended for the eye, brain, spinal cord, or via other routes allowing contact of the medicine with the fluid in the central nervous system (cerebrospinal fluid) (e.g. intracisternal, epidural, intrathecal routes).
  • you require administration in amounts exceeding the recommended maximum dose.

Warnings and precautions
Speak to your doctor or nurse before Xylocaine is administered to you.
Inform your doctor, who will monitor you closely:

  • if the area of the body selected for injection shows signs of infection or inflammation;
  • if you have nerve disorders;
  • if you suffer from high blood pressure (hypertension);
  • if you have advanced liver disease or severe kidney disease;
  • if you have heart disease (partial or complete heart block);
  • if you are elderly or in poor general health;
  • if you are taking class III antiarrhythmic drugs (e.g. amiodarone) for irregular heartbeat (see section “Other medicines and Xylocaine”). Your doctor may perform ECG monitoring (electrocardiogram, a test to assess heart function);
  • if you are taking MAO inhibitors (monoamine oxidase inhibitors) or tricyclic antidepressants used to treat depression (see section “Other medicines and Xylocaine”);
  • if you suffer from porphyria, an inherited disorder affecting the production of certain blood cells, red blood cells;
  • if you are pregnant (see section “Pregnancy and breastfeeding”).

Children and adolescents
The use of Xylocaine is not recommended:

  • for numbing body parts during surgery (local anesthesia) in children under 12 years of age. In pediatric patients aged 1 to 12 years, a less concentrated solution is recommended.

Other medicines and Xylocaine
Inform your doctor or nurse if you are taking, have recently taken, or might take any other medicines.
In particular, inform your doctor if you are taking:

  • other local anesthetics or similar substances;
  • medicines such as mexiletine and tocainide, or class III antiarrhythmics (e.g. amiodarone), used to treat heart rhythm disorders;
  • drugs such as cimetidine, used to treat certain stomach disorders, or beta-blockers, used to treat certain heart conditions;
  • MAO inhibitors (monoamine oxidase inhibitors) or tricyclic antidepressants, used to treat depression.

Pregnancy and breastfeeding
If you are pregnant, suspect you may be pregnant, planning to become pregnant, or are breastfeeding, consult your doctor before this medicine is administered to you.
Pregnancy
Xylocaine will be administered to you during pregnancy only if necessary and under direct medical supervision.
Breastfeeding
If you are breastfeeding, consult your doctor before this medicine is administered to you.
Like other local anesthetics, lidocaine may be excreted in breast milk.

Driving and using machines
Lidocaine may impair your ability to drive vehicles or operate machinery.
Local anesthetics may have a slight effect on mental function and coordination, and may temporarily impair motor ability and level of alertness.

Xylocaine contains sodium
This medicine contains approximately 1 mmol (24 mg) of sodium per maximum dose.
This should be taken into account in patients with impaired renal function or those on a low-sodium diet.

Xylocaine contains methyl parahydroxybenzoate
May cause allergic reactions (including delayed reactions) and, rarely, bronchospasm.

3. How Xylocaine will be administered to you

The dose will be determined by your doctor based on your weight and your overall health condition.
Xylocaine will be administered by a doctor specialised in the use of this type of medicine, in appropriately equipped facilities, into the affected area of your body.
If a large area of your body needs to be anaesthetised or if you are to be given a high dose of the medicine, your doctor will insert a small tube into a vein (catheter) before administering Xylocaine.
Use in children and adolescents
The dosage depends on the patient's age, physical condition and weight, and will be determined by the anaesthetist.
In paediatric patients aged 1 to 12 years, a less concentrated solution is recommended.
If you are given more Xylocaine than you should
It is highly unlikely that you will be given more solution than required, as your doctor will monitor you during treatment.
Accidental injection of local anaesthetics into a blood vessel may cause immediate generalised adverse effects (occurring within seconds to a few minutes). In cases of excessive dosing, adverse effects appear later (15–60 minutes after injection) (see section 4).
Your doctor will determine which resuscitation techniques or medications may be necessary should you be given more solution than required.
If you stop treatment with Xylocaine
If you have any doubts about the use of this medicine, consult your doctor or nurse.

4. Possible side effects

Like all medicines, this medicine can cause side effects, although not everyone will experience them.
Immediate access to appropriate equipment, medications, and trained personnel for emergency treatment is required, as severe, sometimes fatal, allergic reactions have been reported following the use of local anaesthetics, even in the absence of known allergy.

The possible side effects are listed below according to the following frequency:
Common (may affect up to 1 in 10 people)

  • lowering of blood pressure (hypotension);
  • increase in blood pressure (hypertension);
  • nausea, vomiting;
  • numbness (paraesthesia), dizziness;
  • decreased heart rate (bradycardia).

Uncommon (may affect up to 1 in 100 people)

  • uncontrolled body movements (convulsions);
  • numbness around the mouth (circumoral paraesthesia);
  • tongue numbness;
  • increased sensitivity to sounds (hyperacusis);
  • visual disturbances;
  • tremor;
  • ringing in the ears (tinnitus);
  • difficulty speaking (dysarthria);
  • reduced activity of the central nervous system (CNS depression).

Rare (may affect up to 1 in 1,000 people)

  • cardiac arrest;
  • heart rhythm disorders (cardiac arrhythmias);
  • allergic reactions, anaphylactic shock (severe allergic reaction);
  • respiratory depression;
  • nerve disease (neuropathy);
  • nerve injury;
  • inflammation of a meningeal membrane covering the brain (arachnoiditis);
  • double vision (diplopia).

Other reported side effects include:
Allergic reactions

  • swelling and pain (oedema);
  • urticaria;
  • itching.

Effects on the nervous system

  • excitation (which may present initially as drowsiness);
  • depression;
  • anxiety;
  • tremors followed by changes in consciousness;
  • respiratory arrest.

Effects on the heart and circulation

  • reduced heart activity (myocardial depression).

Reporting of side effects
If you experience any side effect, including those not listed in this leaflet, consult your doctor. You may also report side effects directly via the national reporting system at www.agenziafarmaco.gov.it/it/responsabili. By reporting side effects, you can help provide more information on the safety of this medicine.

5. How to store Xylocaine

Do not store above 25°C. Do not freeze.
Re-sterilization of Xylocaine is not recommended.
Keep this medicine out of the sight and reach of children.
Do not use this medicine after the expiry date stated on the carton after "Exp." The expiry date refers to the last day of that month.
Do not dispose of medicines via wastewater or household waste. Ask your pharmacist how to dispose of medicines no longer required. This will help protect the environment.

6. Package Contents and Other Information

What Xylocaine Contains

  • The active substance is lidocaine hydrochloride 20 mg.
    The other components are sodium chloride, methyl parahydroxybenzoate (see section 2 “Xylocaine contains sodium” and “Xylocaine contains methyl parahydroxybenzoate”), sodium hydroxide (pH regulator), hydrochloric acid (pH regulator), water for injections.

Description of the Appearance of Xylocaine and Contents of the Pack
Xylocaine is a clear, colourless injectable solution.
Xylocaine 20 mg/ml solution for injection is available in packs containing
1 vial of 50 ml.
Marketing Authorisation Holder
Aspen Pharma Trading Limited
3016 Lake Drive
Citywest Business Campus
Dublin 24
Ireland
Manufacturer
Astrea Monts, 18 Rue De Montbazon, Monts, 37260, France

The following information is intended exclusively for physicians or healthcare professionals:
Precautions for Use
Regional anaesthetic techniques must always be performed in adequately equipped areas by trained personnel. Immediate availability of equipment and medications necessary for monitoring and emergency resuscitation is essential.
In patients receiving high doses of the drug, an intravenous catheter should be inserted prior to administration of the local anaesthetic. The physician must have received full and appropriate training in the technique to be used and must be experienced in the diagnosis and treatment of adverse reactions, systemic toxicity, or other complications (see Adverse Reactions and Overdose).
The safety of lidocaine depends on appropriate dosing, correct technique, and adoption of precautionary measures. Therefore, the product should be used at the lowest effective dose, which must be determined considering the patient's age, physical condition, and weight, particularly in elderly and acutely ill patients.
Use with extreme caution in patients with cardiovascular disorders, especially in cases of shock or atrioventricular conduction disturbances.
The solution must be injected slowly and with frequent aspirations; repeated injections of lidocaine may lead to significant increases in plasma levels due to accumulation of the substance or its metabolites. Drowsiness represents the first sign of elevated plasma levels, which may also occur with excessively rapid absorption or accidental intravenous injection.
Loco-regional anaesthetic techniques must be performed cautiously when the tissue or injection site shows signs of infection or inflammation. Specific precautions must be taken depending on the regions involved.

Special Warnings
Some local anaesthetic techniques may be associated with severe adverse reactions, regardless of the local anaesthetic used, such as:

  • Accidental intra-arterial injections may cause severe symptoms even at low doses;
  • Continuous intra-articular infusion is not an approved indication for Xylocaine. However, post-marketing cases of chondrolysis have been reported exclusively in North America in patients who received continuous post-operative intra-articular infusion of local anaesthetics. Most reported cases of chondrolysis involved the shoulder joint. A causal relationship has not been established.

Dosage, Method, and Timing of Administration
The recommended maximum dose is 10 ml. This dose should be appropriately reduced in adolescents and patients in poor health. In adolescents with high body weight, a gradual dose reduction is often necessary and should be based on ideal body weight. The total dose must not exceed 5 mg/kg of lidocaine based on ideal body weight. The correct dose and concentration will be determined by the physician.
Reference texts should be consulted regarding factors influencing specific nerve block techniques and individual patient requirements.
The dose to be administered must be calculated based on the physician’s experience and knowledge of the patient’s clinical status. The lowest possible dose that provides adequate anaesthesia should be used (see Precautions for Use). Individual variations in onset time and duration may occur.
The volume of drug used influences the extent and speed of anaesthesia.
To prevent intravascular injection, aspiration must be performed before and during administration of the main dose, which should be injected slowly or in incremental doses. During the procedure, monitor the patient’s vital functions carefully and maintain verbal contact.
Accidental intravascular injection may be recognized by a transient increase in heart rate; accidental intrathecal injection may be recognized by signs of spinal block. At the first sign of toxicity, administration must be stopped immediately.
The use of multidose vials carries a higher risk of microbial contamination compared to single-dose vials. Therefore, single-dose vials are preferred whenever possible. Multidose vials contain a preservative (see section 2 “What you need to know before Xylocaine is administered to you”).
If a multidose vial is used, specific procedures must be followed to prevent contamination. These procedures include:

  • Use of sterile, single-use equipment for local anaesthetic injection;
  • Use of sterile syringes and needles each time a dose is withdrawn from the vial;
  • Avoid introducing contaminated materials or fluids into the multidose vial.
    Re-sterilization of Xylocaine is not recommended. The solubility of lidocaine at pH above 6.5 is limited. This should be considered when adding alkaline solutions such as carbonates, which may cause precipitation of the solution. The solution should not be stored in contact with metals, for example metal cannulas or syringes. Metallic ions may leach out, potentially causing swelling at the injection site.

Paediatric Population
In paediatric patients aged 1 to 12 years, a less concentrated solution is recommended.

Additional Information on Potential Adverse Effects
The adverse reaction profile of Xylocaine is similar to that of other amide-type local anaesthetics. Drug-related adverse reactions are difficult to distinguish from the physiological effects resulting from nerve conduction block (such as decreased arterial pressure, bradycardia) and from events directly caused by injection (e.g., nerve fibre trauma) or indirectly.
Side effects from lidocaine include hypersensitivity reactions or elevated plasma levels due to excessive dosing, rapid absorption, or accidental intravascular injection. Hypersensitivity reactions include oedema, urticaria, pruritus, and anaphylactic reactions, which should be treated with conventional methods. High plasma level reactions primarily affect the central nervous system (CNS) and the cardiovascular system. CNS involvement may manifest as excitation or depression, with dizziness, visual disturbances, anxiety, tremors, followed by altered consciousness, seizures, and respiratory arrest. Excitatory signs preceding the depressive phase may be brief or completely absent, and drowsiness may be the first manifestation. Cardiovascular involvement is characterized by bradycardia, hypotension, myocardial depression, and potentially cardiac arrest.

Acute Systemic Toxicity
Toxic systemic reactions primarily involve the central nervous system (CNS) and the cardiovascular system (CVS). These reactions are caused by high blood concentrations of local anaesthetic, which may result from accidental intravascular injection, overdose, or exceptionally rapid absorption from a highly vascularized area (see Overdose). CNS reactions are similar for all amide-type local anaesthetics, whereas cardiac reactions are more drug-dependent, both quantitatively and qualitatively. Signs of CNS toxicity generally precede cardiovascular toxic effects, except in patients under general anaesthesia or deeply sedated with drugs such as benzodiazepines or barbiturates.

Central Nervous System Toxicity manifests gradually, with symptoms and signs of increasing severity. Initial symptoms include circumoral paraesthesia, tongue numbness, a feeling of emptiness in the head, hyperacusis, tinnitus, and visual disturbances. Dysarthria, muscle twitching, and tremors are more severe manifestations and precede generalized seizures. These signs should not be mistaken for hysterical behaviour. Unconsciousness and convulsive seizures may follow, lasting from several seconds to several minutes. After seizures, due to increased muscular activity, interference with normal respiration, and airway obstruction, hypoxia and hypercapnia develop rapidly. In severe cases, apnoea may occur. Hyperkalaemic acidosis, hypocalcaemia, and hypoxia increase and prolong the toxic effects of local anaesthetics.
Recovery of the patient to baseline clinical condition follows redistribution of the local anaesthetic from the CNS and its metabolism and excretion. Recovery may be rapid if large quantities of the drug have not been administered.

In severe cases, cardiovascular system toxic effects may occur, usually preceded by signs of central nervous system toxicity.
In patients under general anaesthesia or deeply sedated, prodromal CNS symptoms may be absent. As a result of high systemic concentrations of local anaesthetics, hypotension, bradycardia, arrhythmias, and even cardiac arrest may occur. Cardiac arrest, in rare cases, may occur without preceding CNS prodromal symptoms.

Treatment of Acute Toxicity
Administration of the local anaesthetic must be stopped immediately if signs of acute systemic toxicity appear. Symptoms of central nervous system toxicity (seizures, CNS depression) must be promptly treated with appropriate ventilatory/respiratory support and administration of anticonvulsants.
If circulatory arrest occurs, immediate cardiopulmonary resuscitation must be initiated. Ensuring optimal oxygenation, ventilation, circulatory support, and treatment of acidosis is vital.
In case of cardiovascular depression (hypotension, bradycardia), treatment with intravenous fluids, vasoconstrictors, chronotropic, and/or inotropic agents should be considered.