Lidocaine Hydrochloride Injection BP Minijet 2% (International Medication Systems)

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1. Name Of The Medicinal Product

Lidocaine Hydrochloride Injection BP Minijet 2% w/v.

2. Qualitative And Quantitative Composition

Lidocaine Hydrochloride BP 20 mg per ml

3. Pharmaceutical Form

Sterile aqueous solution for infiltration injection or intravenous administration.

4. Clinical Particulars 4.1 Therapeutic Indications

For local anaesthesia by infiltration, intravenous regional anaesthesia and nerve blocks.

By intravenous injection for the emergency management of ventricular arrhythmias, particularly after myocardial infarction and cardiac surgery.

4.2 Posology And Method Of Administration

For local anaesthesia:

The dosage varies depending upon the area to be anaesthetised, vascularity of the tissues, number of neuronal segments to be blocked, individual tolerance and the anaesthetic technique. The lowest dosage needed to provide anaesthesia should be administered.

Adults: the usual dose should not exceed 200 mg.

Children: the usual dose should not exceed 3 mg/kg.

For epidurals, a test dose should be administered at least 5 minutes before total dose to prevent inadvertent intravascular or subarachnoid injection.

For continuous epidural, caudal or paracervical anaesthesia, the maximal dose should not be repeated at intervals under 90 minutes.

For IV regional anaesthesia (Bier's block), the tourniquet should not be released until at least 20 minutes after administration.

For intravenous use in cardiac arrhythmias:

Adults: the usual dose is 50 to 100 mg administered intravenously under ECG monitoring. This dose may be injected at a rate of approximately 25 to 50 mg (2.5 to 5.0 ml 1% solution or 1.25 to 2.5 ml 2% solution) per minute. A sufficient period of time should be allowed to enable a slow circulation to carry the drug to the site of action. If the initial dose of 50 to 100 mg does not produce the desired response, a second dose may be given after 5 minutes. No more than 200 to 300 mg of lidocaine should be administered during a one hour period.

Following a single injection in those patients in whom arrhythmia tends to recur and who are incapable of receiving oral antiarrhythmic therapy, intravenous infusions of lidocaine may be administered at the rate of 1 to 4 mg/minute (20 to 50 mcg/kg/minute). IV infusions must be given under ECG monitoring to avoid potential overdosage and toxicity. The infusion should be terminated as soon as the patient's basic cardiac rhythm appears to be stable or at the earliest signs of toxicity. It should rarely be necessary to continue the infusion beyond 24 hours. As soon as possible, patients should be changed to an oral antiarrhythmic agent for maintenance therapy.

Children: experience with lidocaine is limited. A suggested paediatric dose is a loading dose of 0.8 to 1 mg/kg repeated if necessary up to 3-5 mg/kg, followed by continuous infusion of 10 to 50 mcg/kg/minute.

Elderly: doses may need to be reduced depending on age and physical state.

4.3 Contraindications

Lidocaine is contraindicated in patients with known hypersensitivity to local anaesthetics of the amide type and in patients with porphyria.

4.4 Special Warnings And Precautions For Use

Constant ECG monitoring is necessary during IV administration. Resuscitative equipment and drugs should be immediately available for the management of severe adverse cardiovascular, respiratory or central nervous system effects. If severe reactions occur, lidocaine should be discontinued.

Use with caution in patients with epilepsy, liver disease, congestive heart failure, severe renal disease, marked hypoxia, severe respiratory depression, hypovolaemia or shock and in patients with any form of heart block or sinus bradycardia. Hypokalaemia, hypoxia and disorders of acid-base balance should be corrected before treatment with lidocaine begins.

4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction

Propranolol and cimetidine may reduce the renal and hepatic clearance of lidocaine, thus increasing toxicity. The cardiac depressant effects of lidocaine are additive to those of other antiarrhythmic agents. Lidocaine prolongs the action of suxamethonium.

4.6 Pregnancy And Lactation

The safe use of lidocaine has not been established with respect to possible adverse effects upon foetal development. Lidocaine is excreted in breast milk and so should be used with caution in nursing women.

4.7 Effects On Ability To Drive And Use Machines

Not applicable; this preparation is intended for use only in emergencies.

4.8 Undesirable Effects

Adverse effects are usually due to inadvertent intravenous administration or overdosage. Allergic reactions (including anaphylaxis) have been reported rarely.

The following systemic reactions have been reported in association with lidocaine:

Central nervous system: light-headedness, drowsiness, dizziness, apprehension, nervousness, euphoria, tinnitus, blurred or double vision, nystagmus, vomiting, sensations of heat, cold or numbness, twitching, tremors, paraesthesia, convulsions, unconsciousness, respiratory depression and arrest.

Cardiovascular system: hypotension, cardiovascular collapse and bradycardia which may lead to cardiac arrest.

4.9 Overdose

Symptoms: reactions due to overdose with lidocaine (high plasma levels) are systemic and involve the central nervous and cardiovascular systems. Effects include medullary depression, tonic and clonic convulsions and cardiovascular collapse.

Treatment: institute emergency resuscitative procedures and administer the drugs necessary to manage the severe reaction. For severe convulsions, small increments of diazepam or an ultra-short acting barbiturate (thiopentone), or if not available, a short-acting barbiturate (pentobarbitone or quinalbarbitone), or if the patient is under anaesthesia, a short-acting muscle relaxant (suxamethonium) may be given intravenously. Patency of the airway and adequacy of ventilation must be assured.

Should circulatory depression occur vasopressors such as metaraminol may be used.

5. Pharmacological Properties 5.1 Pharmacodynamic Properties

Lidocaine stabilises the neuronal membrane and prevents the initiation and transmission of nerve impulses, thereby effecting local anaesthetic action. The onset of action is rapid and the blockade may last up to 2 hours.

In the heart, lidocaine reduces automaticity by decreasing the rate of diastolic (phase 4) depolarisation. Lidocaine is considered as a class 1b (membrane stabilising) antiarrhythmic agent. The duration of the action potential is decreased due to blockade of the sodium channel and the refractory period is shortened.

5.2 Pharmacokinetic Properties

Lidocaine is rapidly distributed to all body tissues. About 65% is plasma bound. Lidocaine crosses the placenta and the blood brain barrier. The plasma half life is 1.6 hours. About 80% of the dose is metabolised in the liver; less than 10% is found unchanged in the urine.

5.3 Preclinical Safety Data

Not applicable since lidocaine has been used in clinical practice for many years and its effects in man are well known.

6. Pharmaceutical Particulars 6.1 List Of Excipients

Hydrochloric Acid BP

Sodium Chloride BP

Sodium Hydroxide BP

Water for Injection USP

6.2 Incompatibilities

None known.

6.3 Shelf Life

3 years.

6.4 Special Precautions For Storage

Store below 25°C.

6.5 Nature And Contents Of Container

The solution is contained in a USP type I glass vial with an elastomeric closure which meets all the relevant USP specifications. The product is available as a 2% solution in a 5ml vial.

6.6 Special Precautions For Disposal And Other Handling

The container is specially designed for use with the IMS Minijet injector.

7. Marketing Authorisation Holder

International Medication Systems (UK) Ltd

208 Bath Road

Slough

Berkshire

SL1 3WE

UK

8. Marketing Authorisation Number(S)

PL 03265/0006R

9. Date Of First Authorisation/Renewal Of The Authorisation

Date first granted: 28 February 1991

Date renewed: 29 November 1996

10. Date Of Revision Of The Text

June 2004

11. Legal category

POM

Lidocaine Hydrochloride Injection BP Minijet 2 International Medication Systems

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