2%W/V LIDOCAINE

Posology Local and regional anaesthesia As a matter of principle the smallest possible dose that produces adequate anaesthesia should be administered. The dosage should be adjusted individually according to the particulars of each case.

5 mg/kg body weight (BW) (or 300 mg). If combined with a vasoconstrictor, 7 mg/kg BW (or 500 mg) of lidocaine hydrochloride monohydrate per single dose should not be exceeded. g. epinephrine. Addition of epinephrine at a concentration of 1:100 000 to 1:200 000 has proven useful.

Paediatric population For children, the doses are calculated individually according to the patient’s age, body weight and the nature of the procedure. Up to 5 mg/kg BW may be administered. With the addition of epinephrine, up to 7 mg/kg can be used.

In children with a high body weight a gradual reduction of the dosage is often necessary and should be based on the ideal body weight. Standard textbooks should be consulted for factors affecting specific block techniques and for individual patient requirements.

5% w/v) of the local anaesthetic should be used. To achieve a complete motor block, a higher strength (1% w/v) may be required. Lidocaine should be used with caution in children younger than two years of age as there are limited data to support the safety and efficacy of this product in this patient population at this time.

Elderly patients For elderly patients, the doses must be calculated individually according to the patient’s age and body weight. 2). g. from renal insufficiency, liver insufficiency, cancer, pregnancy). 2). • Patients with liver diseases show reduced tolerance towards amide-type local anaesthetics.

This may be due to reduced hepatic metabolism and decreased protein synthesis resulting in a lower protein binding rate of the local anaesthetic. Dose reduction is advisable in such cases. • The dose should be reduced in patients showing clinical signs of cardiac insufficiency.

Nevertheless, local or regional nerve blockage can be the anaesthetic method of choice in such patients. • During pregnancy, the dose may need to be reduced depending on the type of anaesthesia. Regional anaesthetic blocks in which usually large doses are required should be avoided during the first trimester.

For use in anaesthetic blocks in which smaller doses are administered the dosage may need to be reduced because of the altered anatomical and physiological characteristics in late pregnancy. Antiarrhythmic therapy Adults The dosage must be adjusted according to individual requirements and the therapeutic effect.

Braun 20 mg/ml. 5 ml/min of 2 % w/v Lidocaine Injection BP. If the therapeutic effect of the first dose is insufficient within the first 5 - 10 minutes, the initial dose may be repeated once or twice up to a maximum dose of 200 - 300 mg in 1 hour.

0025 ml/kg BW/min. Infusions can be prepared by adding 1000 mg of lidocaine hydrochloride monohydrate, corresponding to 50 ml of 2% w/v Lidocaine Injection BP, to 500 ml of glucose solution or physiological saline. 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. Paediatric patients The safety and the efficacy of the use of lidocaine in children have not yet been definitely established.

The dose should be adapted according to the clinical situation and the nature of the procedure. 5 - 1 mg/kg BW. This dose may be repeated according to the response of the patient, but the total dose should not exceed 3-5 mg/kg BW. If required, a maintenance IV infusion of 10 – 50 μg/kg BW/min may be given via an infusion pump.

e. bolus) of 1 mg/kg BW up to […]

8. Antiarrhythmic therapy In acidosis, the plasma protein binding of lidocaine is reduced and therefore the concentration of free lidocaine is increased. Hence the effect of lidocaine may be intensified in acidosis. Hypokalaemia, hypoxia and disorders of acid-base balance need to be corrected prior lidocaine is used in patients who require large doses of antiarrhythmic agents.

During prolonged parenteral therapy with lidocaine, fluid balance, serum electrolytes and acid-base balance should be monitored regularly. Administration of lidocaine should be accompanied by continuous monitoring of ECG, blood pressure, state of consciousness and respiration.

Especially adjustment of the dose of the anti-arrhythmic drug requires careful cardiological monitoring. Cardiological emergency equipment must be available. If one or more parameters indicate worsening of cardiac function, revision of therapy, which may include discontinuation of lidocaine, is necessary.

Note:

In narcotised patients central nervous disorders may remain unrecognised and cardiac adverse effects may suddenly occur without other previous warning symptoms.

Special warnings/ precautions regarding excipients 2 ml, 5 ml and 10 ml ampoule:

This medicinal product contains less than 1 mmol (23 mg) per ampoule, that is to say essentially ‘sodium free’. 2% of the WHO recommended maximum daily intake of 2 g sodium for an adult. g. epinephrine. If lidocaine is given as antiarrhythmic agent, additional medication with epinephrine or norepinephrine may lead to potentiation of the cardiac side effects.

● Sedatives, hypnotics Lidocaine should be administered with due caution to patients receiving medication with sedatives that also affect the function of the CNS and therefore may alter the toxicity of lidocaine. There may be an additive effect between the local anaesthetic effect and sedatives or hypnotics.

● Muscle relaxants The effect of muscle relaxants is prolonged by lidocaine. ● Combination with other local anaesthetics Combination of different local anaesthetics may lead to additive effects on the cardiovascular and the central nervous system.

● Volatile anaesthetics If lidocaine and volatile anaesthetics are given simultaneously, the depressive effects of both may be intensified. ● Class I antiarrhythmic agents Simultaneous administration of lidocaine and other class I antiarrhythmic agents should be avoided because of the risk that serious cardiac adverse effects occur.

● Other anti-arrhythmic agents If lidocaine is combined with other anti-arrhythmic agents such as beta receptor blockers or calcium channel blockers, the inhibitory effect on atrioventricular and intraventricular conduction and on contractility may be enhanced.

g. tramadol or bupropion) may increase the risk of seizures. Pharmacokinetic interactions ● Medicinal products that alter the hepatic blood flow, cardiac output or peripheral distribution of lidocaine may influence plasma levels of lidocaine.

g. propranolol, metoprolol, see also below), cimetidine (see also below) and vasoconstrictors like norepinephrine reduce cardiac output and/or hepatic blood flow and therefore reduce the plasma clearance of lidocaine prolonging its elimination half life.

Therefore, due account should be taken of the possibility of accumulation of lidocaine. ● As lidocaine is mainly metabolized via the cytochrome P450 isoenzymes CYP3A4 and CYP1A2 concurrently administered drug substances that are substrates, inhibitors or inducers of hepatic enzymes, isoenzyme CYP3A4 and CYP1A2, may have an influence on the pharmacokinetics of lidocaine and thus also on its effect.

Inhibitors of CYP3A4 and/or CYP1A2 Concurrent administration of lidocaine with inhibitors of CYP3A4 and/or CYP1A2 may lead to accelerated plasma concentrations of lidocaine. g. erythromycine, fluvoxamine, amiodarone, cimetidine, protease inhibitors.

g. barbiturates (mainly phenobarbital), carbamazepine, phenytoin or primidone, accelerate the plasmatic clearance of lidocaine and thus reduce the efficacy of lidocaine. Substrates of CYP 3A4 and/or CYP1A2 Co-administration with other substrates of CYP3A4 and/or CYP1A2 may lead to increased plasma levels of the drugs.

6 Fertility, pregnancy and lactation Pregnancy There are no or a limited amount of data from the use of lidocaine in pregnant women. 3). However, lidocaine rapidly crosses the placenta. Therefore high plasma concentrations of lidocaine in the mother`s plasma may cause central nervous depression, alteration of the peripheral vascular tone and cardiac function in the foetus/neonate.

Lidocaine should only be used in pregnancy if there is an imperative indication . Then doses should be as low as possible. g. bradycardia, hypotonia or respiratory depression). An accidental subcutaneous injection of lidocaine in the foetus during paracervical or perineal block may cause apnoea, hypotension and convulsive fits and may thus put the newborn at vital risk.

In general lidocaine in strengths of 10 mg/ml should be preferred […]

General In the case of known allergy towards other amide-type local anaesthetics, group allergy towards lidocaine should be considered. 3), cardiac insufficiency, bradycardia, impaired respiratory function and severe shock. 2. In general, prior to injection of lidocaine, it must be made sure that all equipment for resuscitation and emergency medication for the treatment of toxic reactions are instantly available.

Patients with epilepsy should be carefully monitored for the occurrence of central nervous symptoms. An increased tendency to convulsions should be considered even with doses below maximum. Local and regional anaesthesia Sudden arterial hypotension may occur as a complication of spinal and epidural anaesthesia, in particular in elderly patients.

Particular caution should also be exercised if the local anaesthetic is to be injected into inflamed (infected) tissue because of increased systemic absorption due to higher blood flow and decreased effect due to the lower pH of infected tissue.

A risk of post-spinal headache is associated with spinal anaesthesia mainly in adolescents and in adults up to the age of 30 years. This risk of post-spinal headache can be markedly reduced by choosing sufficiently thin injection cannulae.

After removing the tourniquet after intravenous regional anaesthesia there is an increased risk of adverse effects. Therefore the local anaesthetic should be drained off in several portions. During anaesthetic procedures in the neck and head region patients are at increased risk of central nervous toxic effects of the drug.

8. Antiarrhythmic therapy In acidosis, the plasma protein binding of lidocaine is reduced and therefore the concentration of free lidocaine is increased. Hence the effect of lidocaine may be intensified in acidosis. Hypokalaemia, hypoxia and disorders of acid-base balance need to be corrected prior lidocaine is used in patients who require large doses of antiarrhythmic agents.

During prolonged parenteral therapy with lidocaine, fluid balance, serum electrolytes and acid-base balance should be monitored regularly. Administration of lidocaine should be accompanied by continuous monitoring of ECG, blood pressure, state of consciousness and respiration.

Especially adjustment of the dose of the anti-arrhythmic drug requires careful cardiological monitoring. Cardiological emergency equipment must be available. If one or more parameters indicate worsening of cardiac function, revision of therapy, which may include discontinuation of lidocaine, is necessary.

Note:

In narcotised patients central nervous disorders may remain unrecognised and cardiac adverse effects may suddenly occur without other previous warning symptoms.

Special warnings/ precautions regarding excipients 2 ml, 5 ml and 10 ml ampoule:

This medicinal product contains less than 1 mmol (23 mg) per ampoule, that is to say essentially ‘sodium free’. 2% of the WHO recommended maximum daily intake of 2 g sodium for an adult.

1. Local and regional anaesthesia The special contraindications for spinal and epidural anaesthesia must also be observed: ● uncorrected hypovolaemia ● coagulopathy (acquired, induced, genetic) ● increased intracranial pressure ● intracranial or intraspinal haemorrhage.

Antiarrhythmic therapy ● Severe conduction disorders ● Myocardial infarction within the preceding 3 months or markedly decreased cardiac output unless there is life threatening ventricular cardiac arrhythmia.