4.1. Therapeutic indications

General

This product is non-sterile and therefore not recommended for use prior to procedures that require aseptic techniques.

For the prevention of pain associated with the following procedures:

Otorhinolaryngology

Anaesthesia prior to minor non-invasive procedures in the nasal cavity, pharynx and epipharynx including rhinoscopy and laryngoscopy.

Obstetrics

As supplementary pain control for procedures not requiring aseptic technique.

Insertion of instruments and catheters into the respiratory and digestive tract

Provides surface anaesthesia for the oropharyngeal and tracheal areas to reduce reflex activity, attenuate haemodynamic response and to facilitate insertion of the catheter or the passage of instruments during endotracheal intubation, laryngoscopy, bronchoscopy, oesophagoscopy and gastroscopy.

Dental practice

Before minor dental procedures where local anaesthesia is desired.

4.2. Posology and method of administration

As with any local anaesthetic, reactions and complications are best averted by employing the minimal effective dosage. Debilitated or elderly patients and children should be given doses commensurate with their age and physical condition.

Xylocaine Spray should not be used on cuffs of endotracheal tubes (ETT) made of plastic (see also section 4.4).

Each activation of the metered dose valve delivers 10 mg lidocaine base. It is unnecessary to dry the site prior to application. No more than 20 spray applications should be used in any adult to produce the desired anaesthetic effect.

The number of sprays depend on the extent of the area to be anaesthetised.

– Dental practice

1–5 applications to the mucous membranes.

– Obstetrics

Up to 20 applications (200 mg lidocaine base).

– Insertion of instruments and catheters into the respiratory and digestive tract

Up to 20 applications (200 mg lidocaine base) for procedures in pharynx, larynx, and trachea.

Method of administration

Xylocaine spray is administered using the supplied nozzle. Nozzles are supplied in the finished product packaging and also available separately in boxes of 50. Nozzles are non-sterile single patient single use only. Appropriate measures should be undertaken to avoid cross contamination (see Section 6.6).

4.3. Contraindications

Hypersensitivity to the active substance, to any of the excipients listed in section 6.1 or to local anaesthetics of the amide-type.

4.4. Special warnings and precautions for use

Excessive dosage, or short intervals between doses, may result in high plasma levels and serious adverse effects. Absorption from mucous membranes is variable but is especially high from the bronchial tree. Such applications may therefore result in rapidly rising or excessive plasma concentrations, with an increased risk of toxic symptoms, such as convulsions. Xylocaine Spray should be used with caution in patients with wounds or traumatised mucosa in the region of the proposed application. A damaged mucosa will permit increased systemic absorption. The management of serious adverse reactions may require the use of resuscitative equipment, oxygen and other resuscitative drugs (see section 4.9).

In paralysed patients under general anaesthesia, higher blood concentrations may occur than in spontaneously breathing patients. Unparalysed patients are more likely to swallow a large proportion of the dose, which then undergoes considerable first-pass hepatic metabolism following absorption from the gut.

The oropharyngeal use of topical anaesthetic agents may interfere with swallowing and thus enhance the danger of aspiration. This is particularly important in children because of their frequency of eating. Numbness of the tongue or buccal mucosa may increase the danger of biting trauma.

If the dose or site of administration is likely to result in high blood levels, lidocaine, in common with other local anaesthetics, should be used with caution in the following patients who will require special attention to prevent potentially dangerous side effects:

• Patients with epilepsy.

• Patients with cardiovascular disease and heart failure.

• Patients with impaired cardiac conduction or bradycardia.

• Patients with severe renal dysfunction.

• Patients with impaired hepatic function.

• Patients in severe shock.

• The elderly and patients in poor general health.

Avoid contact with the eyes.

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

Xylocaine Spray should not be used on cuffs of endotracheal tubes (ETT) made of plastic. Lidocaine base in contact with both PVC and non-PVC cuffs of endotracheal tubes may cause damage of the cuff. This damage is described as pinholes, which may cause leakage that could lead to pressure loss in the cuff.

Xylocaine Spray is probably porphyrinogenic and should only be prescribed to patients with acute porphyria on strong or urgent indications. Appropriate precautions should be taken for all porphyric patients.

4.5. Interaction with other medicinal products and other forms of interaction

Lidocaine should be used with caution in patients receiving other local anaesthetics or agents structurally related to amide-type 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 (see section 4.4).

Drugs that reduce the clearance of lidocaine (e.g. cimetidine or beta-blockers) may cause potentially toxic plasma concentrations when lidocaine is given in repeated high doses over a long time period. Such interactions should therefore be of no clinical importance following short-term treatment with lidocaine (e.g. Xylocaine Spray) at recommended doses.

4.6. Fertility, pregnancy and lactation

Pregnancy

There is no, or inadequate evidence of safety of the drug in human pregnancy but it has been in wide use for many years without apparent ill consequence, and animal studies have shown no hazard. If drug therapy is needed in pregnancy, this drug can be used if there is no safer alternative.

Breastfeeding

Lidocaine enters the mother's milk, but in such small quantities that there is generally no risk of the child being affected at therapeutic dose levels.

4.7. Effects on ability to drive and use machines

Xylocaine Spray has minor influence on the ability to drive and use machines. Depending on the dose, local anaesthetics may have a very mild effect on mental function and may temporarily impair locomotion and co-ordination.

4.8. Undesirable effects

In extremely rare cases amide-type local anaesthetic preparations have been associated with allergic reactions (in the most severe instances anaphylactic shock).

Local irritation at the application site has been described. Following application to laryngeal mucosa before endotracheal intubation, reversible symptoms such as “sore throat”, “hoarseness” and “loss of voice” have been reported. The use of Xylocaine pump spray provides surface anaesthesia during an endotracheal procedure but does not prevent post-intubation soreness.

Systemic adverse reactions are rare and may result from high plasma levels due to excessive dosage or rapid absorption (e.g. following application to areas below the vocal chords) or from hypersensitivity, idiosyncrasy or reduced tolerance on the part of the patient. Such reactions involve the central nervous system and/or the cardiovascular system.

CNS reactions are excitatory and/or depressant and may be characterised by nervousness, dizziness, convulsions, unconsciousness and possibly respiratory arrest. The excitatory reactions may be very brief or may not occur at all, in which case the first manifestations of toxicity may be drowsiness, merging into unconsciousness and respiratory arrest.

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

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation 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 via the Yellow Card Scheme.

Website: www.mhra.gov.uk/yellowcard or search for MHRA Yellow Card in the Google Play or Apple App Store

4.9. Overdose

Acute systemic toxicity

Toxic reactions originate mainly in the central nervous and the cardiovascular systems.

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, light-headedness, hyperacusis and tinnitus. Visual disturbance and muscular tremors are more serious and precede the onset of generalized convulsions. Unconsciousness and grand mal convulsions may follow, which 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. In severe cases, apnoea may occur. Acidosis increases the toxic effects of local anaesthetics.

Cardiovascular effects are only seen in cases with high systemic concentrations. Severe hypotension, bradycardia, arrhythmia and cardiovascular collapse may be the result in such cases.

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 barbiturate.

Recovery is due to redistribution and metabolism of the local anaesthetic drug from the central nervous system. Recovery may be rapid unless large amounts of the drug have been administered.

Treatment of acute toxicity

Treatment of acute toxicity should be instituted at the latest when twitches occur. The necessary drugs and equipment should be immediately available. The objectives of treatment are to maintain oxygenation, stop the convulsions and support the circulation. Oxygen must be given and, if necessary, assisted ventilation (mask and bag).

An anticonvulsant should be given i.v. if the convulsions do not stop spontaneously in 15–30 sec. Thiopentone sodium 1–3 mg/kg i.v. will abort the convulsions rapidly. Alternatively, diazepam 0.1 mg/kg body-weight i.v. may be used, although its action will be slow. Prolonged convulsions may jeopardise the patient's ventilation and oxygenation. If so, injection of a muscle relaxant (e.g. succinylcholine 1 mg/kg body-weight) will facilitate ventilation, and oxygenation can be controlled. Early endotracheal intubation must be considered in such situations.

If cardiovascular depression is evident (hypotension, bradycardia), ephedrine 5–10 mg i.v. should be given and repeated, if necessary, after 2–3 minutes.

Should circulatory arrest occur, immediate cardiopulmonary resuscitation should be instituted. Optimal oxygenation and ventilation and circulatory support as well as treatment of acidosis are of vital importance, since hypoxia and acidosis will increase the systemic toxicity of local anaesthetics.

Children should be given doses commensurate with their age and weight.