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LIDOCAINE 10%W.W LOCAL ANAESTHETIC SPRAY

Active substance(s): LIDOCAINE BASE / LIDOCAINE BASE / LIDOCAINE BASE

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SUMMARY OF PRODUCT CHARACTERISTICS

1

NAME OF THE MEDICINAL PRODUCT
Lidocaine 10%w/w local anaesthetic spray

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QUALITATIVE AND QUANTITATIVE COMPOSITION
Active Ingredient Lidocaine Base %w/w 10.0

Each actuation delivers 0.1ml spray, containing 10mg lidocaine. For full list of excipients see section 6.1

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PHARMACEUTICAL FORM
Local anasthetic spray Lidocaine Spray is a clear, colourless liquid contained within a clear glass bottle fitted with a silver metering pump.

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4.1

CLINICAL PARTICULARS
Therapeutic indications
For the prevention of pain associated with the following procedures: Otorhinolaryngology: Puncture of the maxillary sinus and minor surgical procedures in the nasal cavity, pharynx and epipharynx. Paracentesis. Obstetrics: During the final stages of delivery and before episiotomy and perineal suturing as supplementary pain control.

Introduction of instruments and catheters into the respiratory and digestive tract: Provides surface anaesthesia for the otopharyngeal and tracheal areas to reduce reflex activity, attenuate haemodynamic response and to facilitate insertion of the tube or the passage of instruments during endotracheal intubation, laryngoscopy, bronchoscopy and oesophagoscopy. Dental Practice: Before injection, dental impressions, X-ray photography, removal of calculus, seating or adjustment of dentures.

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. Each activation of the metered dose valve delivers 10mg lidocaine base. It is necessary 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 is dependent on the extent of the area to be anaesthetised. Otorhinolaryngology: 3 applications for puncture of the maxillary sinus. During delivery: Up to 20 applications (200mg lidocaine base)

Introduction of instruments and catheters into the respiratory and digestive tract: Up to 20 applications (200mg lidocaine base) for procedures in the pharynx, larynx and trachea. Dental Practice: 1-5 applications to the mucous membrane.

4.3

Contraindications
Contraindicated in known hypersensitivity to local anaesthetics of the amide type or to other components of the spray solution.

4.4

Special warnings and precautions for use
Avoid contact with the eyes. Absorption from wound surfaces and mucous membranes is relatively high, especially in the bronchial tree. Lidocaine Spray 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, lidocaine 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. 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.

4.5

Interaction with other medicinal products and other forms of interaction
Lidocaine should be used with caution in patients receiving anti-arrhythmic drugs such as tocainide, since the toxic effects are additive. Significant increases in plasma lidocaine concentrations have occurred during concomitant therapy with beta-blockers, such as propanolol, metoprolol or nalodol, owing to a reduction in the clearance of lidocaine from plasma and possibly a direct inhibition of hepatic metabolism. Cimetidine appears to reduce the hepatic metabolism of lidocaine although it may also reduce its clearance by decreasing hepatic blood flow.

4.6

Pregnancy and lactation
There is no or inadequate evidence of safety of lidocaine in human pregnancy but it has been in wide use for many years without apparent ill consequence; animal studies having shown no hazard. If drug therapy is needed in pregnancy, this drug can be used if there is no safer alternative. Lidocaine enters the breast milk, but in such small quantities that there is generally no risk of the breast milk being affected at therapeutic dose levels.

4.7

Effects on ability to drive and use machines
In multiple or higher doses, local anaesthetics may have an effect on mental function and temporarily impair locomotion and co-ordination.

4.8

Undesirable effects
In rare cases local anaesthetic preparations have been associated with allergic reactions (in most severe instances anaphylactic shock). Systemic adverse reactions are rare and may result from high plasma levels due to excessive dosage or rapid absorption or from hypersensitivity, idiosyncrasy or reduced tolerance on the part of the patient. Such reactions involve the central nervous system and / or 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.

4.9

Overdose
The treatment of a patient with toxic manifestations consists of ensuring adequate ventilation and arresting convulsions. Ventilation should be maintained with oxygen by assisted or controlled respiration as required. If convulsions occur, they should be treated rapidly by the intravenous administration of succinylcholine 50-100mg and / or 5-15mg diazepam. As succinylcholine will arrest respiration, it should only be used if the clinician has the ability to perform endotracheal intubation and to manage a totally paralysed patient. Thiopentone may also be used to abort convulsions in the dosage 100-200mg. If ventricular fibrillation or cardiac arrest occurs, effective cardiovascular resuscitation must be instituted. Adrenaline in repeated doses and sodium bicarbonate should be given as rapidly as possible.

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5.1

PHARMACOLOGICAL PROPERTIES
Pharmacodynamic properties
ATC Code: C05 AD01 Lidocaine is a potent local anaesthetic of the amide type. Like other local anaesthetics, it prevents both the generation and conduction of nerve impulses by slowing depolarisation. This results from blocking of the large transient increase in permeability of the cell membrane to sodium ions that follows initial depolarisation of the membrane. Its mechanism of action is a reversible blockade of impulse propagation by prevention of sodium flux. Lidocaine may have similar effects on the brain and myocardium and symptoms and signs of toxicity may appear as a results of the drug reaching the systemic circulation, and thus the brain and heart. Lidocaine also acts as an anti-arrhythmic agent.

5.2

Pharmacokinetic properties
Lidocaine is readily absorbed from mucous membranes, the respiratory tract, the gastrointestinal tract and through damaged skin. Only about 30-35% of lidocaine is systemically bioavailable after oral administration because of pre-systemic metabolism. Uptake of lidocaine from tissues into the blood is influenced by the site of application or injection and its vascularity. Absorption may be particularly high from the tracheobronchial tree. Application of 10mg lidocaine from a 10% spray during laryngoscopy has produced mean maximum plasma concentrations of 1.03 (+/- 0.25) mcg/ml within about 20 minutes. Application of 50, 100 and 200mg lidocaine during upper endoscopy has resulted in maximum plasma levels of 0.49, 0.77 and 1.0 mcg/ml respectively 20 minutes after application by means of a 10% spray. Mean maximum plasma levels of 0.657 3.63 mcg/ml have been reported following application of doses of 118 572 mg lidocaine (as 2 of 4% nebulisers) during bronchoscopy. Following absorption, there is rapid distribution to all body tissues; the volume of distribution being approximately 100 litres. Plasma protein binding is variable but approximately 65% is bound to plasma protein including alpha-1-acid glycoprotein. Lidocaine crosses the blood-brain barrier. It is excreted in breast milk.

Lidocaine has an elimination half-life of 1.6 hours. About 80% of lidocaine is metabolised in the liver with only about 3% being found unchanged in the urine. Lidocaine is N-de-ethylated to monoethylglycinexylidide (MEGX) and glycinexylidide. Hydrolysis of glycinexylidide results in 2,6-xylidine, the main excretion product in the urine being 4-hydroxy-2,6-xylidine. 5-hydroxylation of the benzene ring of both lidocaine and MEGX results in the formation of 5-hydroxy MEGX and 5-hydroxylidocaine. Both de-ethylation metabolites have anti-arrhythmic activity, MEGX being 33-83% as active lidocaine and glycinexylidide being 10-42% as active. Only MEGX has convulsive activity, being approximately 88% that of lidocaine. As lidocaine is largely metabolised in the liver, any alteration in liver function or hepatic blood flow may have a significant effect on its metabolism. Reduced clearance of lidocaine has been found in patients with heart failure, alcoholic liver disease or chronic or viral hepatitis. Concomitant therapy with agents that alter hepatic blood flow or induce drugmetabolising microsomal enzymes can also effect the clearance of lidocaine. Signs of toxicity are observed with plasma levels greater than 5mcg/ml.

5.3

Preclinical safety data
No relevant data

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6.1

PHARMACEUTICAL PARTICULARS
List of excipients
Propylene Glycol Sodium Saccharin Absolute Ethanol Purified Water Banana Flavour P473-1N1

6.2

Incompatibilities
No relevant incompatibilities

6.3

Shelf life
3 Years

6.4

Special precautions for storage
Do not store above 30 C

6.5

Nature and contents of container
A clear Type I glass bottle of 60ml capacity with a metered pump and a polyethylene / polypropylene dip tube, which is crimped onto the neck of the bottle. The pump assembly is protected by a white polypropylene overcap. The polypropylene nozzle actuator (for directing the spray to the target surface area) is supplied separately inside the carton and replaces the overcap prior to use. The bottle contains 50ml lidocaine spray. Each actuation delivers 0.1ml spray, containing 10mg lidocaine.

6.6

Special precautions for disposal
No special requirements.

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MARKETING AUTHORISATION HOLDER
Ayrton Saunders Limited Ayrton House Parliament Business Park,Commerce Way Liverpool L8 7BA

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MARKETING AUTHORISATION NUMBER(S)
PL 16431/0125

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DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION
06/03/2007

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DATE OF REVISION OF THE TEXT
22/02/2008

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Source: Medicines and Healthcare Products Regulatory Agency

Disclaimer: Every effort has been made to ensure that the information provided here is accurate, up-to-date and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. This information has been compiled for use by healthcare practitioners and consumers in the United States. The absence of a warning for a given drug or combination thereof in no way should be construed to indicate that the drug or combination is safe, effective or appropriate for any given patient. If you have questions about the substances you are taking, check with your doctor, nurse or pharmacist.

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