Lidocaine is a local anaesthetic of the amide group. Lidocaine solution for
injection is indicated for use in infiltration anaesthesia, intravenous regional
anaesthesia and nerve blocks.

For local anesthesia:
The method of administration of Lidocaine varies according to the procedure
(infiltration anaesthesia, intravenous regional anaesthesia or nerve block).

The dosage should be adjusted according to the response of the patient and the
site of administration. The lowest concentration and smallest dose producing the
required effect should be given. The dosage varies depending on 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.
Unnecessarily high doses of local anaesthetics are to be avoided. In general,
surgical anaesthesia (e.g. epidural administration) requires the use of higher
concentrations and doses.
When blocking smaller nerves, or when a less intense block is required, the use of
a lower concentration is indicated. The volume of drug used will affect the extent
and spread of anaesthesia. The maximum dose for healthy adults should not
exceed 200 mg.
Care should be taken to prevent acute toxic reactions by avoiding intravascular
injection.
Careful aspiration before and during the injection is recommended. When a large
dose is to be injected, e.g. in epidural block, a test dose of 3 – 5 ml of Lidocaine
containing adrenaline (epinephrine) is recommended. An accidental intravascular
injection may be recognised by a temporary increase in heart rate. The main dose
should be injected slowly while keeping in constant verbal contact with the
patient. If toxic symptoms occur, the injection should be stopped immediately.
Children: The dosage should be calculated on a weight basis and should not
exceed 5 mg/kg.
Standard textbooks should be consulted for factors affecting specific block
techniques and for individual patient requirements.

As with other local anaesthetics, Lidocaine should be used with caution in
patients with epilepsy, impaired cardiac conduction, congestive cardiac failure,
bradycardia or impaired respiratory function, if the dose or site of administration
is likely to produce high blood levels.

Lidocaine is metabolized in the liver and it should be used with caution in patients
with impaired hepatic function.
Facilities for resuscitation should be available when administering local
anaesthetics.
The effect of local anaesthetics may be reduced if the injection is made into an
inflamed or infected area.
Solutions containing adrenaline should be used with caution in patients with
hypertension, cardiac disease, cerebrovascular insufficiency, thyrotoxicosis, in
patients taking tricyclic antidepressants, MAOI's or receiving potent anaesthetic
agents.
Certain local anaesthetic procedures may be associated with serious adverse
reactions, regardless of the local anaesthetic drug used, e.g.:
- Central nerve blocks may cause cardiovascular depression, especially in the
presence of hypovolaemia, and therefore epidural anaesthesia should be used with
caution in patients with impaired cardiovascular function.
- Retrobulbar injections may rarely reach the cranial subarachnoid space, causing
serious / severe reactions, including cardiovascular collapse, apnoea, convulsions
and temporary blindness.
- Retro- and peribulbar injections of local anaesthetics carry a low risk of
persistent ocular muscle dysfunction. The primary causes include trauma and/or
local toxic effects on muscles and/or nerves.
The severity of such tissue reactions is related to the degree of trauma, the
concentration of the local anaesthetic and the duration of exposure of the tissue to
the local anaesthetic. For this reason, as with all local anaesthetics, the lowest
effective concentration and dose of local anaesthetic should be used.
- Injections in the head and neck regions may be made inadvertently into an
artery, causing cerebral symptoms even at low doses.
- Paracervical block can sometimes cause foetal bradycardia/tachycardia, and
careful monitoring of the foetal heart rate is necessary.
Epidural anaesthesia may lead to hypotension and bradycardia. This risk can be
reduced by preloading the circulation with crystalloidal or colloidal solutions.
Hypotension should be treated promptly with e.g. ephedrine 5-10 mg
intravenously and repeated as necessary.

The speed of onset and duration of action of Lidocaine are increased by the
addition of a vasoconstrictor such as adrenaline and absorption from the site of
injection is reduced

Dopamine and 5-hydroxytryptamine depletion both reduce the convulsant
threshold of Lidocaine, and the concomitant use of pethidine increases the
incidence of Lidocaine-induced convulsions in animals.
Cimetidine and propranolol depress microsomal enzyme activity, thus enhancing
Lidocaine toxicity during anti-arrhythmic infusions if concomitantly administered
with these drugs. Opioid-antiemetic combination sometimes used for sedation in
children could reduce the convulsant threshold to lignocaine and increase the
CNS depressant effect.
While adrenaline (epinephrine) when used in conjunction with Lidocaine might
decrease vascular absorption, it greatly increases the danger of ventricular
tachycardia and fibrillation if accidentally injected intravenously.
Cardiovascular collapse has been reported following the use of bupivacaine in
patients on treatment with verapamil and timolol; Lidocaine is closely related to
bupivacaine.

Lidocaine given by epidural or paracervical block, especially in large doses, or by
local perineal infiltration prior to delivery crosses rapidly into the foetal
circulation.
Elevated Lidocaine levels may persist in the newborn for at least 48 hours after
delivery.
Foetal bradycardia or neonatal bradycardia, hypotonia or respiratory depression
may occur.
Although animal studies have revealed no evidence of harm to the foetus,
Lidocaine should not be administered during early pregnancy unless the benefits
are considered to outweigh the risks.
Small amounts of Lidocaine are secreted into breast milk and the possibility of an
allergic reaction in the infant, albeit remote, should be borne in mind when using
Lidocaine in nursing mothers.

Where outpatient anaesthesia affects areas of the body involved in driving or
operating machinery, patients should be advised to avoid these activities until
normal function is fully restored

In common with other local anaesthetics, adverse reactions to Lidocaine are rare
and are usually the result of raised plasma concentrations due to accidental
intravascular injection, excessive dosage or rapid absorption from highly vascular
areas, or may result from a hypersensitivity, idiosyncrasy or diminished tolerance

system and/or the cardiovascular system.
CNS reactions may be excitatory and/or depressant and may manifest as
nervousness, tremor, blurred vision, nausea and vomiting, followed by
drowsiness, coma and possibly respiratory arrest. The excitatory reactions may be
brief or may not occur at all, so that the first signs of toxicity may be drowsiness,
followed by coma and respiratory failure. Cardiovascular reactions are depressant
and may manifest as hypotension, bradycardia, myocardial depression and
possibly cardiac arrest.
Allergic reactions are rare. They may be characterised by cutaneous lesions,
urticaria, oedema or anaphylactoid reactions. Skin testing for allergy to Lidocaine
is not considered to be reliable.
Localised nerve damage at the site of injection (very rare).
Prolonged neural blockade following epidural may be due to delayed spread.
Permanent neural blockade may be more likely associated with hypotension and
cord ischaemia.
Following regional blockade as when Lidocaine is injected intrathecally or
extradurally, hypotension, hypoventilation, Horners Syndrome and
hypoglycaemia may be seen. The degree of these effects will depend on the dose
and the height of the block. Urinary retention may occur following sacral or
lumbar epidural block. It should not outlast the duration of the block. Apnoea and
coma followed by aphasia and hemiparesis may occur following stellate ganglion
block. The probable cause is a direct injection of Lidocaine into the vertebral or
carotid arteries.
Profound lethargy and death have been reported following the injection of only 10
– 32 mg of Lidocaine for dental blocks. Diplopia and temporary blindness has
been reported following Lidocaine for maxillary block, also respiratory arrest
following retrobulbar block.
The major adverse effects on the CNS and CVS are primarily due to the
absorption of Lidocaine into the systemic circulation. Lidocaine may also produce
methaemoglobinaemia.

The initial CNS toxic effects are demonstrated by a gradual onset of drowsiness
or inebriation similar to alcoholic intoxication. Balance is disturbed, circumoral
pins and needles, numb tongue, roaring in the ears, visual disturbances,
restlessness and twitching may occur. Severe intoxication of rapid onset may
immediately lead to convulsions followed by circulatory depression. Major
overdosage may depress all systems simultaneously. Psychotic reactions have
been reported following infusion for the control of arrhythmia.

sympathetic block from spinal or epidural block, intercostal nerve block
administration or supine hypotension in pregnancy.
Ventricular fibrillation occurs less frequently than that seen with bupivacaine

The effects of over dosage involve the CNS, where reactions may be excitatory
and/or depressant, and the CVS where the effects are depressant. In the event of
an overdose, immediate steps should be taken to maintain the circulation and
respiration and to control convulsions.
A patent airway should be established and oxygen should be administered,
together with assisted ventilation if necessary. The circulation should be
maintained with infusions of plasma or intravenous fluids. Where further
supportive treatment of circulatory depression is required, use of a vasopressor
agent may be considered although this involves a risk of CNS excitation.
Convulsions may be controlled by the intravenous administration of diazepam or
thiopentone sodium, bearing in mind those anti-convulsant drugs may also
depress respiration and the circulation. If cardiac arrest should occur, standard
cardiopulmonary resuscitation procedures should be instituted.
Dialysis is of negligible value in the treatment of acute over dosage with
Lidocaine.

ATC Code:N01BB02
Lidocaine is a local anaesthetic of the amide type. It is used to provide local
anaesthesia at various sites in the body and it acts by inhibiting the ionic refluxes
required for the initiation and conduction of impulses, thereby stabilizing the
neuronal membrane. In addition to blocking conduction in nerve axons in the
peripheral nervous system, Lidocaine has important effects on the central nervous
system and cardiovascular system. After absorption, Lidocaine may cause
stimulation of the CNS followed by depression and in the cardiovascular system;
it acts primarily on the myocardium where it may produce decreases in electrical
excitability, conduction rate and force of contraction.

Lidocaine is absorbed from injection sites including muscle and its rate of
absorption is determined by factors such as the site of administration and the
tissue vascularity. Except for intravascular administration, the highest blood
levels occur following intercostal nerve block and the lowest after subcutaneous
administration. Lidocaine is bound to plasma proteins, including alpha-1-acid-
Page 6 of 9

glycoprotein. The drug crosses the blood-brain and placental barriers. Lidocaine is
metabolised in the liver and about 90% of a given dose undergoes N-dealkylation
to form monoethylglycinexylidide and glycinexylidide, both of which may
contribute to the therapeutic and toxic effects of Lidocaine. Further metabolism
occurs and metabolites are excreted in the urine with less than 10% as unchanged
Lidocaine.
The elimination half-life of Lidocaine following an intravenous bolus injection is
one to two hours, but this may be prolonged in patients with hepatic dysfunction

No further relevant information other than that which is included in other sections
of the Summary of Product Characteristics.

Sodium Chloride (Isotonic)
Methyl 4-hydroxybenzoate –paraben- (Antimicrobial Preservative)
Water for Injections (Diluent)

Lidocaine solution for injection should not be mixed with other preparations
unless compatibility is known.

Do not store above 25°C.

Before administration, the product should be visually inspected for any particulate matter and
discoloration.
For multiple use.

Unused portion after 7 days from opening :
Multiple dose with preservative (Methyl Paraben) used for l.M., S.C. as local
anesthesia.
Based on our review of the available information in the safety and potency of
multi-dose vials “MDV” and on our internal experimental data, can be used for
subsequent treatment session for upto a maximum of one week provided that all
of the following parameters are met.
• The expiry date has not passed.
• Dating and initialing the vial once opened.
• The vial is stored in the same recommended storage conditions
mentioned on product label i.e. at room temperature not exceeding 25°C
or refrigerated.
• Sterile device has been used each time a “MDV” is accessed.
• Aseptic technique has been used to withdraw all doses.
• All measures have been considered to prevent alteration of drug potency.
Conclusion:
Any change or non compliance to the recommended condition of use render, the
proposed validity is invalid.