ESRACAIN INJECTION 1%

ESRACAIN

INTRAVENOUS INJECTION FOR CARDIAC ARRHYTHMIAS

Composition

Each ampoule of 10ml contains:

Lidocaine hydrochloride 1% or2% (Lignocaine hydrochloride)

in an isotonic sodiumchloride solution without preservatives.

Action

Lidocaine controls ventricular arrhythmias by suppressing automaticityin the His-Purkinje system

and by suppressing spontaneous depolarization of the ventriclesduring diastole. These effects

occur at lidocaine concentrations (therapeuticdosage) that do not suppress automaticity of the

sinoatrial (SA) node. At therapeutic plasmaconcentrations, lidocainehas little effect on

atrioventricular (AV) node conduction and His-Purkinje conduction inthe normal heart. The

specialized conducting tissues of theatria are less sensitive to the effects of lidocaine than those of

ventricular tissues. Lidocaine hasa variable effect on the effective refractory period (ERP) of the

AV node; the drug shortens the ERP and the action potential duration of the His-Purkinje system.

Lidocaine does not appear to affectexcitability ofnormal cardiac tissue.

Lidocaine ismetabolizedin the liver and excreted via the kidneys.

Lidocaine plasmaconcentrations of approximately 1.5-6mcg base/ml are required to suppress

ventricular arrhythmias. Plasmalevels above 6 mcg/mlresult in increased toxicity.

Indications

Acute management of ventricular arrhythmias occurring during cardiac manipulation, such as in

cardiac surgery and in life-threatening arrhythmias which are ventricular in origin, i.e. as occur

during acute myocardial infarction.

Contraindications

Lidocaine hydrochloride is contraindicated in patients with a known historyof hypersensitivity to

local anesthetics of the amide type. It should not be used in patients with Stokes-Adams syndrome,

Wolf-Parkinson-White syndrome, orin severedegrees of sinoatrial,atrioventricular or

intraventricular block in the absence ofan artificial pacemaker.

Warnings

This preparation is intended for use as a bolus injection by the intravenous route only. Prior dilution

is required when using this preparation for intravenous infusion (see Dosage and Administration).

In order to manage possible adverse reactions, resuscitative equipment and drugs, including

oxygen, should be immediately available when lidocaine hydrochloride injections are used. CNS

depression (sedation) or irritability (twitching) may progress tofrank convulsions accompanied by

respiratory depression and/or arrest.

Should convulsions persist despite ventilatorytherapy with oxygen, small increments of

anticonvulsant drugs may be administered intravenously. Such agents include diazepam, thiopental,

thiamylal or pentobarbital. Ifthe patient is under anesthesia,a short-acting relaxant (e.g.

succinylcholine) may be used. Longer-actingdrugs should be used only when recurrent

convulsions are evidenced. Shouldcirculatory depression occur,vasopressors may be used.

Constant electrocardiographic monitoring is essential to the proper administration of lidocaine

hydrochloride bolus injection. Signsof excessive depression of cardiacelectrical activity such as

sinus node dysfunction, prolongation of the P-R interval and QRS complex or the appearance or

aggravation of arrhythmias, should be followedby flow adjustment and if necessary, prompt

cessation of the intravenous infusionof this agent. Occasionally, acceleration of ventricular rate

may occur when lidocaine bolus injection is administered to patients with atrial flutter or

fibrillation.

Survival

Prophylactic single dose lidocaine administered in a monitored environment does not appear to

affect mortality in the earliest phase ofacute MI,and may harmsomepatients who are later shown

not to have suffered an acute MI.

Use in Pregnancy

Safe use has not been established. Lidocaine hydrochloride should not be used in women of

childbearing potential, particularlyduring early pregnancy, unless, inthe opinion of the clinician,

the potential benefits outweigh the unknown hazards.

Use in Labor and Delivery

The effects on the mother and the fetus in the management of cardiac arrhythmias during labor and

delivery are not known. Lidocaine hydrochloride readily crosses the placental barrier.

Use in Breastfeeding

It is not known whether this drug is excretedin human milk. However, because many drugs are

excreted in human milk, it is recommended thatnursing be discontinued when lidocaine is

indicated.

Use in Pediatrics

Safety of use of this drug inchildren has not been established.

Malignant Hyperthermia

Amide local anesthetic administration has beenassociated with acute onset of fulminant

hypermetabolismof skeletal muscle known as malignanthyperthermic crisis. Recognition of early

unexplained signs of tachycardia, tachypnea, labile blood pressure and metabolic acidosis may

precede temperature elevation. Successfuloutcomedepends on early diagnosis, prompt

discontinuance of the triggering agent and institution of treatment, including oxygen, supportive

measures and IV dantrolene sodium(see individual monograph).

The safety ofamide local anestheticsin patients with genetic predisposition of malignant

hyperthermia has not been fully assessed; use lidocaine with caution insuch patients. In hospitals

where triggering agents for malignant hyperthermia are administered, a standard protocol for

managementshould be available.

Constant ECG monitoring

Constant ECG monitoring is essential for the properadministration of IV lidocaine hydrochloride.

Signs of excessive depression of cardiac conductivity, such as prolongationof the PR and the QRS

complex and the appearance of arrhythmias, shouldlead to the prompt cessation of the IV infusion.

Emergency resuscitive equipment

It is mandatory to have emergency resuscitive equipment and drugs immediately available to

manage possible adverse reactionsinvolving the cardiovascular, respiratory or central nervous

systems.

Adverse Reactions

Adverse reaction may result fromhigh plasmalevels caused by excessive dosage, or from

hypersensitivity, idiosyncrasy or diminished tolerance on the partof the patient. Serious adverse

experiences are generally systemic in nature. The following types are those commonly reported.

The CNS and cardiovascular adverse experiences are listed, in general, in aprogression frommild

to severe.

Serious adverse reactions to lidocaine are uncommon. Adverse effects of the drug mainly involve

the CNS. They are usually ofshort duration and are dose related.

Central Nervous System

Manifested by drowsiness, dizziness, disorientation, confusion, lightheadedness, tremulousness,

psychosis, nervousness, apprehension, agitation, euphoria, tinnitus, visual disturbances including

blurred ordouble vision, nausea, vomiting, paresthesia, sensations of heat, cold ornumbness,

difficulty in swallowing, dyspnea and slurred speech. Muscle twitching or tremors, seizures,

unconsciousness, comaand respiratory depression and arrest may also occur.

Cardiovascular

Although usual doses of lidocainegenerally have no adverse cardiovascular effects, patients with

high plasmaconcentrations of the drug orwith myocardial conduction defects may develop

hypotension, arrhythmias, heart block, cardiovascular collapse andbradycardia which may lead to

cardiac arrest.

Allergic

Hypersensitivity to lidocaine israre and may be characterized by skin lesions, urticaria, edema and

anaphylactoid reactions. No cross-sensitivtyhas been reported between lidocaine and

procainamide or quinidine.

Precautions

Caution should be taken with the repeated use oflidocaine hydrochloride in patients with severe

liver or kidney disease, in patients with hypovolemia, shock, or any formof heart block. In patients

with sinus bradycardia or incomplete heart block,the administration of lidocaine hydrochloride I.V.

or the elimination of ventricular ectopic beatswithout prior acceleration in heart rate (e.g. by,

atropine, isoproterenole or by electric pacing) may produce more frequent and serious ventricular

arrhythmias or complete heart block.

Lactation: In a single case report,lidocaine was excreted into breast milk at concentrations 40% of

serumlevels. At this level, an infant might ingest up to 1.5 mg, a very small amount that would not

be expected to lead to significant accumulation. However, exercise caution when administering to

a nursing woman.

Children:Safety and efficacy have not been established;reduce dosage. The IM autoinjector

device is not recommended in children < 50 kg (110 lbs).

Care should be observed in patients suffering from epilepsy.

Drug Interactions

Lidocaine/Anticonvulsants/or benzodiazepines/or barbiturates: May lower plasmalevels of

lidocaine when used concomitantly.

Lidocaine/Beta-adrenoreceptor blocking agents: Co-administration ofbeta-blockers may reduce

the plasmaclearance of lidocaine;possibly enhancing its toxicity.

Lidocaine/Cimetidine:Combined use results in increased plasmaconcentrations of lidocaine and,

thus, enhanced toxicity.

Lidocaine/Disopyramide: Very high doses of lidocaine and disopyramide were reported, in one

case to prolong the Q-T interval and to produce atrioventricular block andventricular fibrillation.

Lidocaine/Muscle relaxants: The neuro-blocking effect of succinylcholine is increased by high

I.V. doses of lidocaine.

Lidocaine/Phenytoin: Concurrent use yields a high incidence of CNS toxicity. Sino-atrial arrest

occurred in one case with heart block when both drugs were given intravenously.

Lidocaine/Procainamide/Quinidine: Concurrent use is synergistic.

Lidocaine/Sympathomimetic Agents

Isoprenaline increases total bodyclearance of lidocaine. Noradrenaline has the opposite effect.

Diagnostic Interference

Because IM injection of lidocainemay increase serumcreatinine phosphokinase (CPK)

concentrations, isoenzyme separation is necessary when CPK determinations are usedin the

diagnosis of acute myocardial infarction in patients receiving the drug IM.

Dosage and Administration

Single Intravenous Injection (Bolus Injection)

The usual dose is 50-100mg administered INTRAVENOUSLY , under ECG monitoring, at a rate of

approximately 20-50mg/min.

Sufficient timeshould be allowed toenable a slow circulation to carry the drug to itssite of action.

If the above initial injectionof 50-100mgdoes not produce a desired response, a second dose may

be repeated after 5 minutes.

NOTE: No more than 200-300mg oflidocaine hydrochloride shouldbe administered during a one-

hour period.

Continuous Intravenus Infusion

The I.V. bolus is only used to establish rapid therapeutic levels. A I.V. continuous infusion is used

to maintain therapeutic levels. An infusion solution should be prepared using 5% dextrose in

water. This solution is stable for a minimum of 24 hours at roomtemperature.

Overdosage

Manifestations

Reactions due to overdosage are systemic and involve the central nervous and cardiovascular

systems. Nervousness, dizziness, blurred visionor tremors may occur followed by drowsiness,

convulsions, unconsciousness andpossibly respiratory arrest.

Reactions involving the cardiovascular systeminclude depression of the myocardium, hypotension,

bradycardia and even cardiac arrest.

Treatment

In the treatment of CNS and cardiovascular reactions, generalphysiological supportive measures,

such as maintenance of an adequate airway,oxygen uptake and carbon dioxide removal should be

instituted immediately.

Administration of oxygen and assistedrespiration may be sufficientto control anoxia in patients

with convulsions, and avoids thehazards associated with the administration of CNS depressant

drugs. For control of severe convulsions, slow I.V.infusion of diazepam or an ultra-short or short-

acting barbiturate has been recommended. If these are not available, a short-acting muscle relaxant

(succinylcholine) together withoxygen may be used. If circulatory depression occurs, administer

vasopressors and, if necessary, institute CPR.

Pharmaceutical Precautions

Lidocaine hydrochloride injections orsolutionsshould be stored at roomtemperature; freezing

should be avoided.

Presentation

Esracain Injection 1%: 50 ampoules of 10ml.

Esracain Injection 2%: 50 ampoules of 10ml.

The formatandcontent ofthisdocument have beenapprovedbythe MinistryofHealthinNovember 2006.

Rafa Laboratories, POB 405, Jerusalem91003, tel: 02-5893939, fax: 02-5870282

ESRACAIN

AMPOULES FOR LOCAL ANESTHESIA

Composition

1% or 2% Lidocaine Hydrochloride (Lignocaine HCl) in an isotonic sodium chloride

solution. Contains no antibacterial preservatives.

Action

Lidocaine hydrochloride stabilizes the neuronal membrane and prevents the initiation

and conduction of nerve impulses thereby effecting local anesthetic action. Lidocaine

hydrochloride is metabolized mainly in the liver and excreted via the kidneys, mainly

in the form of various metabolites.

Indications

Lidocaine hydrochloride solutions are indicated for the production of local or regional

anesthesia by infiltration techniques, including percutaneous and intravenous regional

anesthesia; by peripheral nerve block techniques, such as brachial plexus and

intercostal blocks; and by central neural techniques, including epidural and caudal

blocks.

Contraindications

Lidocaine hydrochloride is contraindicated in patients with a known history of

hypersensitivity to local anesthetics of the amide type.

“Local anesthetics” are contraindicated in patients with myasthenia gravis, severe

shock or impaired cardiac conduction. Lidocaine hydrochloride is also

contraindicated by any route when the area or site of injection is infected or inflamed

and it should be used with extreme caution in patients with skin infections anywhere

on the body.

Contraindications to epidural (including caudal) anesthesia include serious diseases of

the CNS or of the spinal cord such as meningitis, spinal fluid block, cranial or spinal

hemorrhage, tumors, poliomyelitis, syphilis and tuberculosis.

Other contraindications include: spinal deformities, arteriosclerosis, occlusive arterial

disease, pernicious anemia with spinal cord involvement, severe anemia, cachexia or

moribund condition, septicemia, bowel obstruction, chronic backache, preoperative

headaches of long duration or history of migraine, high or low blood pressure and

emotional instability, hysteria or nervous tension.

Warnings

Use in Pregnancy

Safe use in pregnancy has not been established. Lidocaine hydrochloride should not

be used during early pregnancy unless, in the opinion of the clinician, the potential

benefits outweigh the unknown hazards. This does not exclude the use of this drug at

term for obstetrical analgesia.

Use in Labor and Delivery

Local anesthetics rapidly cross the placenta and when used for epidural, paracervical,

pudendal or caudal block anesthesia, they can cause varying degrees of maternal, fetal

and neonatal toxicity. The potential for toxicity depends upon the procedure

performed, the type and amount of drug used, and the technique of drug

administration. Adverse reactions in the parturient, fetus and neonate involve

alterations of the central nervous system, peripheral vascular tone and cardiac

function.

Material hypotension has resulted from regional anesthesia. Local anesthetics

produce vasodilation by blocking sympathetic nerves. Elevating the patient’s legs and

positioning her on her left side will help prevent decreases in blood pressure.

Fetal bradycardia frequently follows paracervical block and may be associated with

fetal acidosis.

The fetal heart rate also should be monitored continuously, and electronic fetal

monitoring is highly advisable.

Epidural, spinal, paracervical or pudendal anesthesia may alter the forces of

parturition through changes in uterine contractility or maternal expulsive efforts. In

one study, paracervical block anesthesia was associated with a decrease in the mean

duration of first stage labor and facilitation of cervical dilation. However, spinal and

epidural anesthesia have also been reported to prolong the second stage of labor by

removing the parturient’s reflex urge to bear down or by interfering with motor

function. The use of obstetrical anesthesia may increase the need for forceps

assistance.

The use of some local anesthetic drug products during labor and delivery may be

followed by diminished muscle strength and tone for the first day or two of life. The

long-term significance of these observations is unknown. Fetal bradycardia may

occur in 20 to 30 percent of patients receiving paracervical nerve block anesthesia

with the amide type local anesthetics and may be associated with fetal acidosis. Fetal

heart rate should always be monitoried during paracervical anesthesia. The physician

should weigh the possible advantages against risks when considering a paracervical

block in prematurity, toxemia of pregnancy, and fetal distress. Careful adherence to

recommended dosage is of the utmost importance in obstetrical paracervical block.

Failure to achieve adequate analgesia with recommended doses should arouse

suspicion of intravascular or fetal intracranial injection. Cases compatible with

unintended fetal intracranial injection of local anesthetic solution have been reported

following intended paracervical or pudendal block or both. Babies so affected present

with unexplained neonatal depression at birth, which correlates with high local

anesthetic serum levels, and often manifest seizures within six hours. Prompt use of

supportive measures combined with forced urinary excretion of the local anesthetic

has been used successfully to manage this complication.

Case reports of maternal convulsions and cardiovascular collapse following use of

some local anesthetics for paracervical block in early pregnancy (as anesthesia for

elective abortion) suggest that systemic absorption under these circumstances may be

rapid. The recommended maximum dose of each drug should not be exceeded.

Injection should be made slowly and with frequent aspiration. Allow a 5-minute

interval between sides.

Use in Breastfeeding

It is not known whether this drug is excreted in human milk. Because many drugs are

excreted in human milk, caution should be exercised when lidocaine is administered

to a nursing woman.

Lidocaine injection for infiltration and nerve block should be employed only by

clinicians who are well versed in diagnosis and management of dose-related toxicity

and other acute emergencies that might arise from the block to be employed and then

only after ensuring the IMMEDIATE availability of oxygen, other resuscitative drugs,

cardiopulmonary equipment and the personnel needed for proper management of

toxic reactions and related emergencies (see also Adverse Reactions and Precautions).

Delay in proper management of dose-related toxicity, underventilation from any cause

and/or altered sensitivity may lead to the development of acidosis, cardiac arrest and,

possibly, death.

To avoid intravascular injection, aspiration should be performed before the local

anesthetic solution is injected. The needle must be repositioned until no return of

blood can be elicited by aspiration. Note, however, that the absence of blood in the

syringe does not guarantee that intravascular injection has been avoided

.

The safety and effectiveness of lidocaine depend on proper dosage, correct technique,

adequate precautions, and readiness for emergencies. Standard textbooks should be

consulted for specific techniques and precautions for various regional anesthetic

procedures.

Use in Pediatrics

Dosage in children should be reduced in accordance with age, body weight and

physical conditions.

Adverse Reactions

Adverse experiences following the administration of lidocaine are similar in nature to

those observed with other amide local anesthetic agents. These adverse experiences

are, in general, dose-related and may result from high plasma levels caused by

excessive dosage, rapid absorption or inadvertent intravascular injection, or may

result from a hypersensitivity, idiosyncrasy or diminished tolerance on the part of the

patient. Serious adverse experiences are generally systemic in nature. The following

types are those most commonly reported:

Central Nervous System

CNS manifestations are excitatory and/or depressant, and may be characterized by

lightheadedness, nervousness, apprehension, euphoria, confusion, dizziness,

drowsiness, tinnitus, blurred or double vision, vomiting, sensations of heat, cold or

numbness, twitching, tremors, convulsions, unconsciousness, respiratory depression

and arrest. The excitatory manifestations may be very brief or may not occur at all, in

which case the first manifestation of toxicity may be drowsiness, merging into

unconsciousness and respiratory arrest.

Drowsiness following the administration of lidocaine is usually an early sign of a high

blood level of the drug and may occur as a consequence of rapid absorption

.

Cardiovascular System

Cardiovascular manifestations are usually depressant and are characterized by

bradycardia, hypotension, and cardiovascular collapse, which may lead to cardiac

arrest.

Allergic

Allergic reactions are characterized by cutaneous lesions, urticaria, edema or

anaphylactoid reactions. Allergic reactions may occur as a result of sensitivity either

to local anesthetic agents or to the methylparaben used as a preservative in the

multiple dose vials. Allergic reactions as a result of sensitivity to lidocaine are

extremely rare and, if they occur, should be managed by conventional means. The

detection of sensitivity by skin testing is of doubtful value.

Neurologic

The incidences of adverse reactions associated with the use of local anesthetics may

be related to the total dose of local anesthetic administered and are also dependent

upon the particular drug used, the route of administration and the physical status of

the patient. In a prospective review of 10,440 patients who received lidocaine for

spinal anesthesia, the incidences of adverse reactions were reported to be about 3

percent each for positional headaches, hypotension and backache; 3 percent for

shivering; and less than 1 percent each for peripheral nerve symptoms, nausea,

respiratory

inadequacy and double vision. Many of these observations may be related

to local anesthetic techniques, with or without a contribution from the local anesthetic.

In the practice of caudal or lumbar epidural block, occasional unintentional

penetration of the subarachnoid space by the catheter may occur. Subsequent adverse

effects may depend partially on the amount of drug administered subdurally. These

may include spinal block of varying magnitude (including total spinal block),

hypotension secondary to spinal block, loss of bladder and bowel control, and loss of

perineal sensation and sexual function. Persistent motor, sensory and/or autonomic

(sphincter control) deficit of some lower spinal segments with slow recovery (several

months) or incomplete recovery have been reported in rare instances when caudal or

lumbar epidural block have been attempted. Backache and headache have also been

noted following use of these anesthetic procedures.

There have been reported cases of permanent injury to extraocular muscles requiring

surgical repair following retrobulbar administration.

Precautions

The lowest dosage that results in effective anesthesia should be used. Syringe

aspirations should also be performed before and during each supplemental injection

when using indwelling catheter techniques. During the administration of epidural

anesthesia, it is recommended that a test dose be administered initially and that the

patient be monitored for central nervous system toxicity and cardiovascular toxicity,

as well as for signs of unintended intrathecal administration before proceeding.

An intravascular injection is still possible even if aspirations for blood are negative.

Repeated doses of lidocaine may cause significant increases in blood levels with each

repeated dose because of slow accumulation of the drug or its metabolites. Tolerance

to elevated blood levels varies with the status of the patient.

Careful and constant monitoring of cardiovascular and respiratory (adequacy of

ventilation) vital signs and the patient’s state of consciousness should be

accomplished after each local anesthetic injection. It should be kept in mind at such

times that restlessness, anxiety, tinnitus, dizziness, blurred vision, tremors, depression

or drowsiness may be early warning signs of central nervous

system toxicity.

Lidocaine solutions should be used with caution in patients with digitalis toxicity

accompanied by atrioventricular block.

Debilitated, elderly patients, acutely ill patients and children should be given reduced

doses, in accordance with their age and physical status.

Lidocaine hydrochloride should be used with caution in patients with severe shock or

impaired cardiac conduction.

Epidural anesthesia and caudal anesthesia should be used with extreme caution in

conditions such as those existing in neurological disease, spinal deformities,

septicemia, severe hypertension and in the extremely young.

Lidocaine hydrochloride should be used with caution in patients with known drug

sensitivity. Caution is recommended when local amide-anesthetics are used in patients

with malignant hyperthermia. Many drugs used during the conduct of anesthesia are

considered potential triggering agents for familial malignant hyperthermia. Since it is

not known whether amide-type local anesthetics may trigger this reaction and since

the need for supplemental general anesthesia cannot be predicted in advance, it is

suggested that a standard protocol for the management of malignant hyperthermia

should be available. Early unexplained signs of tachycardia, tachypnea, labile blood

pressure and metabolic acidosis may precede temperature elevation. Successful

outcome is dependent on early diagnosis, prompt discontinuance of the suspect

triggering agent(s) and institution of treatment, including oxygen therapy, indicated

supportive measures and dantrolene (consult dantrolene sodium intravenous package

insert before using).

Since amide-type local anesthetics are metabolized by the liver, lidocaine should be

used with caution in patients with hepatic disease. Patients with severe hepatic

disease, because of their inability to metabolize local anesthetics normally, are at

greater risk of developing toxic plasma concentrations.

Local anesthetic procedures should be used with caution when there is inflammation

and/or sepsis in the region of the proposed injection. Patients with cardiac disease,

hyperthyroidism, or other endocrine diseases may be particularly susceptible to the

toxic effects of “local anesthetics”.

Use in the Head and Neck Area: Small doses of local anesthetics injected into the

head and neck area, including retrobulbar, dental and stellate ganglion blocks, may

produce adverse reactions similar to systemic toxicity seen with unintentional

intravascular injections of larger doses. Confusion, convulsions, respiratory

depression and/or respiratory arrest, and cardiovascular stimulation or depression

have been reported. These reactions may be due to intra-arterial injection of the local

anesthetic with retrograde flow to the cerebral circulation. Patients receiving these

blocks should have their circulation and respiration monitored and be constantly

observed. Dosage recommendations should not be exceeded. (See Dosage and

Administration)

Drug Interactions

Vasopressor agents (administered for the treatment of hypotension related to caudal or

other epidural blocks) should be used with caution in the presence of oxytocic drugs,

as a severe persistent hypertension and even rupture of cerebral blood vessels may

occur.

Lidocaine HCl/Cimetidine:

Both the pharmacologic and toxic effects of Lidocaine hydrochloride may be

increased (e.g. dysphoric sensations, circumoral and digital paresthesias, lethargy,

confusion).

Lidocaine HCl/Procainamide:

The CNS toxicity (delirium) of both drugs may be increased.

Lidocaine HCl/Succinylcholine:

The neuromuscular blocking effects of succinylcholine may be increased. Prolonged

respiratory depression with extended periods of apnea may occur. The effects of this

interaction are dependent upon the dose of Lidocaine HCl.

Lidocaine/Beta-adrenoreceptor blocking agents

: Co-administration of

beta-blokers

may reduce the plasma clearence of lidocaine; possibly enhancing its toxicity.

Lidocaine/Sympathomimetic Agents

Isoprenaline increases total body clearance of lidocaine. Noradrenaline has the

opposite effect.

In one study serum creatinine phosphokinase was sevenfold elevated following IM

lidocaine administration in healthy subjects.

Dosage and Administration

Proper technique is inherent to the safe use of lidocaine hydrochloride. It should be

injected slowly and with frequent aspiration to guard against intravascular injection.

The injection should be terminated if toxic effects appear.

The following table summarizes the recommended volumes and concentrations of

lidocaine hydrochloride solutions for various types of anesthetic procedures.

The dosages suggested in this table are for normal, healthy adults and refer to

epinephrine free solutions. These recommended dosages serve only as a guide to the

amount of anesthetic required for most routine procedures.

The actual volume and concentrations to be used depend on a number of factors, such

as the type and extent of the surgical procedure, degree of muscular relaxation

required, duration of anesthesia required and the physical state of the patient. The

lowest concentration and smallest dose that will produce the desired result should be

given.

Note:

The onset and duration of anesthesia and the degree of muscular relaxation (and

appearance of adverse reactions) are proportional to the volume and concentration of

local anesthetic injection used.

LIDOCAINE HCL (without epinephrine and bacteriostatic agents)

PROCEDURE

conc.(%)

vol. (ml)

Total Dose

(mg)

Infiltration:

Percutaneous

0.5 or 1.0

1-60

5-300

IV Regional

10-60

50-300

Peripheral Nerve Blocks

Brachial

15-20

225-300

Dental

1- 5

20-100

Intercostal

Paravertebral

3- 5

30- 50

Pudental (each side)

Paracervical

Obstetrical analgesia (each side)

Sympathetic Nerve Block

Cervical (stillate ganglion)

Lumbar

5-10

50-100

Central Nerve Blocks

Epidural:*

Thoracic

5-10

50-100

Lumbar:

Analgesia

25-30

250-300

Anesthesia

10-15

200-300

Caudal:

Obstetrical analgesia

20-30

200-300

Surgical anesthesia

15-20

225-300

*

dose determined by number of dermatomes to be anesthetized (2-3 mg/dermatome)

Note: a test dose of 2 ml should be administered at least 5 minutes prior to injecting

the total required volume for central neural blocks (epidural or caudal anesthesia).

Maximum Recommended Dose for Normal Healthy Adults

The individual dose of a Lidocaine hydrochloride solution, when used without

epinephrine, should be such that it is kept below 300 mg and, in any case, should not

exceed 4.5 mg/kg body weight.

For continuous epidural or caudal anesthesia, the maximum recommended dosage

should not be administered at intervals of less than 90 minutes.

For paracervical block for obstetrical analgesia (including abortion), the maximum

recommended dosage (200mg) should not be administered at intervals of less than 90

minutes.

For I.V. regional anesthesia in adults (using 0.5% lidocaine hydrochloride solution

without epinephrine), the dose should not exceed 4mg/kg of body weight.

Maximum Recommended Dose for Children

The maximum dose for children varies as a function of age and weight.

The amount of lidocaine hydrochloride solution should not exceed 4.5mg/kg of body

weight. The use of 0.5% or 1.0% solutions is recommended for most anesthetic

procedures. More dilute injections of 0.25-0.5% and total dosages not exceeding

3mg/kg are recommended for the induction of I.V. regional anesthesia in children.

Overdosage

Manifestations

Toxic cardiovascular reactions to local anesthetics are usually depressant in nature,

and are characterized by peripheral vasodilation, hypotension, myocardial depression,

bradycardia and possible cardiac arrest.

Treatment

Treatment consists in assuring and maintaining a patent airway, supporting ventilation

with oxygen, and assisting or controlling respiration.

Should a convulsion persist, small increments of anticonvulsive agents may be

administered intravenously, (e.g. diazepam), ultra short-acting barbiturates (e.g.

thiopental or thiamylal) or a short acting barbiturate (e.g. pentobarbital or

secobarbital).

Cardiovascular depression may require circulatory assistance (unit IV fluids and/or

vasopressors (e.g. ephedrine), as dictated by the clinical situation).

Pharmaceutical Precautions

Lidocaine hydrochloride injections or solutions should be stored at room temperature.

Do not freeze.

Presentation

Esracain Injection 1%: 50 ampoules of 10 ml or 5 ml.

Esracain Injection 2%: 50 ampoules of 10 ml or 5 ml.

Reg. no.

Esracain Injection 1%:

019 20 21029 00

Reg. no.

Esracain Injection 2%:

020 82 21028 00

Rafa Laboratories, POB 405, Jerusalem 91003,

The format and content of this document have been approved by the Ministry of Health in Junuary 2007.

032004