Lidocaine 2%

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• Consult your doctor or pharmacist if you need advice or further information.
• This medicine has been prescribed for a specific individual and should not be passed on to others, as it may harm them even if their symptoms are the same.

LIGNOCAIN 2%
injection solution
COMPOSITION:
1 ml of solution contains:
lidocaine hydrochloride (monohydrate) 20 mg
Excipients:
sodium chloride: 5.30 mg
sodium hydroxide (0.1 M solution) 0.04 ml
water for injections to 1.00 ml
*)

Marketing Authorisation Holder
Manufacturer
B. Braun Melsungen AG
Carl-Braun-Strasse 1
D-34212 Melsungen
Germany
B. Braun Melsungen AG
Mistelweg 2
D-12357 Berlin
Germany

Package Leaflet Contents

1. What Lignocain 2% is and what it is used for
2. Before you use Lignocain 2%
3. How to use Lignocain 2%
4. Possible side effects
5. How to store Lignocain 2%
6. Further information

1. What Lignocain 2% is and what it is used for

Pharmaceutical form
Injection solution

Contents of the pack
Lignocain 2% is supplied in the following pack sizes:

• Glass ampoules of 5 ml volume – packed 10 units per cardboard box
• Plastic containers of 5, 10, 20 ml volume – packed 20 units per cardboard box

Therapeutic group
Local and conduction anaesthetic
(2% solution is not suitable for intravenous regional anaesthesia)

• For local anaesthesia: infiltration, perineural (epidural), and topical (superficial) anaesthesia;
• For nerve and ganglion block anaesthesia (perineural);
• For dental nerve anaesthesia.

As an antiarrhythmic agent

• In life-threatening ventricular arrhythmias: ventricular tachycardia or ventricular fibrillation, and for prevention of their occurrence in myocardial infarction, after invasive cardiological procedures and cardiac surgery;
• For prevention of recurrence of ventricular fibrillation and ventricular tachycardia after defibrillation or cardioversion.

2. Before using Lignocain 2%

• Main contraindications Administration of Lignocain 2% solution is contraindicated in the following conditions:

  • hypersensitivity to amide-type local anaesthetics; occasional use may be allowed after determining a safe dose by gradual dose escalation, under full safety precautions;
  • second- or third-degree atrioventricular block, bundle branch block;
  • cardiac pacemaker failure.

• Contraindications related to use as a local anaesthetic Intramuscular injections should be avoided. The 2% lidocaine solution should not be used for pain relief in obstetrics. Special contraindications for spinal (intrathecal) and epidural anaesthesia should also be considered, e.g.:

  • uncorrected hypovolemia;
  • coagulation disorders;
  • increased intracranial pressure.

Spinal (intrathecal) anaesthesia should not be performed in adolescents and adults under 30 years of age due to the frequent occurrence of post-spinal headache in this age group.
Safety instructions for epidural (extradural) and spinal anaesthesia under thromboprophylactic conditions are described in the section "Precautions for use in local anaesthesia".

• Contraindications related to use as an antiarrhythmic agent Lignocain 2% should not be used in the following cases:
  • second- and third-degree atrioventricular block, bundle branch block;
  • cardiac pacemaker failure;
  • acute heart failure (left ventricular ejection fraction less than 35%), unless ventricular arrhythmia is life-threatening;
  • hypersensitivity to amide-type local anaesthetics;
  • renal or hepatic failure.

Warnings and precautions
In patients treated with anticoagulant drugs (e.g. heparins), nonsteroidal anti-inflammatory drugs (NSAIDs), or plasma substitutes, there is an increased risk of bleeding following injection of a local anaesthetic. Therefore, coagulation status should be assessed prior to administration in such patients (see also below).
In acidosis, protein binding of lidocaine is reduced, resulting in increased levels of unbound (free) lidocaine. In such cases, the effects of lidocaine may be enhanced.

• Precautions for use in local anaesthesia Before initiating any local anaesthesia procedure, adequate intravascular volume replacement should be ensured and, if necessary, hypovolemia corrected. During anaesthesia of areas in the head and neck region, patients are at higher risk of central nervous system toxicity from the drug. Circulation in patients receiving the drug must be carefully monitored. All instruments and medications necessary for life support, including artificial ventilation, anticonvulsants, and resuscitation equipment, must be readily available. Similarly, prior to epidural anaesthesia, full resuscitation equipment, such as intubation devices, oxygen supply, and emergency drugs for toxic reactions, must be accessible. To avoid adverse effects, the following recommendations should be observed:
  • Establish intravenous access in high-risk patients when doses exceeding 25% of the maximum recommended dose are used.
  • Use the lowest possible doses.
  • Do not routinely use vasoconstrictor agents in combination with local anaesthetics.
  • Ensure proper patient positioning.
  • Perform dual-direction aspiration (rotate the needle!).
  • Avoid injections into inflamed areas whenever possible, due to the risk of increased systemic absorption and reduced efficacy.
  • Inject the local anaesthetic slowly!
  • Monitor blood pressure, pulse, and pupil size.
  • Observe all general and specific contraindications and drug interactions. In patients treated with anticoagulants (e.g. heparins), nonsteroidal anti-inflammatory drugs, or plasma substitutes, accidental puncture of a blood vessel during anaesthesia may lead to serious bleeding complications; in such patients, increased general bleeding risk during local anaesthetic injection should also be considered. If necessary, partial thromboplastin time (PTT) or kaolin-kephalin clotting time (aPTT), Quick's index (INR), and platelet count should be measured in these patients. The same tests should be performed in patients undergoing spinal or epidural anaesthesia while receiving low-dose heparin thromboprophylaxis. Local anaesthesia should be performed with particular caution in patients receiving low-molecular-weight heparins (LMWH) for prevention of thromboembolic events.

Bleeding time assessment is essential in patients who have taken nonsteroidal anti-inflammatory drugs within five days prior to spinal or epidural anaesthesia.

• Precautions for use in antiarrhythmic treatment During prolonged parenteral administration of lidocaine, water balance, serum electrolyte concentrations, and acid-base balance should be monitored regularly.

Use with food and drink
Food intake does not affect the drug's efficacy.
Pregnancy or breastfeeding
There are insufficient data to definitively assess the safety of lidocaine use during pregnancy.
Regarding use in antiarrhythmic treatment, lidocaine should be administered to pregnant women only in highly significant indications and at the lowest possible doses.
Regarding use in local nerve block during pregnancy, although this technique is associated with the lowest risk among various medical interventions, lidocaine should only be administered after careful evaluation of potential benefits and risks, and only if no safer alternatives are available.
Epidural anaesthesia is contraindicated in obstetric applications when significant bleeding is expected or when the placenta is deeply implanted.
In rare cases during childbirth with local anaesthesia using lidocaine, newborns may exhibit signs of toxicity: bradycardia, atrioventricular block, and ventricular tachycardia.
It is unknown whether lidocaine passes into breast milk. Therefore, lidocaine use during breastfeeding requires caution.
Driving and operating machinery
After lidocaine administration in surgical, dental, or other procedures involving large body surface areas, the physician must assess whether the patient is fit to drive or operate mechanical equipment.
Concomitant use with other medicines
Caution is required when administering lidocaine to patients taking sedatives or drugs affecting the central nervous system. An antagonistic effect exists between local anaesthetics and sedatives or hypnotics (e.g. diazepam). The latter increase the seizure threshold in the central nervous system. This should be considered when monitoring patients for signs of lidocaine toxicity.
Caution is also advised in patients treated with propranolol, diltiazem, verapamil, and norepinephrine. These drugs reduce lidocaine clearance and increase its plasma concentration, thereby prolonging lidocaine's half-life. Therefore, lidocaine accumulation should be considered.
Lidocaine should be administered with particular caution to patients concurrently taking cimetidine. Due to reduced hepatic perfusion and inhibition of hepatic microsomal enzymes, toxic plasma concentrations of lidocaine may occur even with normal doses used in intercostal nerve blocks.
Concomitant administration of lidocaine and aprindine may lead to additive adverse effects. Due to similar chemical structure, the adverse effects of aprindine and lidocaine are comparable.
Synergism between local anaesthetics and centrally acting analgesics, chloroform, ether, and thiopental has been reported regarding central nervous system depressant effects.
Cardiac glycosides reduce the toxicity of lidocaine.
Lidocaine prolongs the action of non-depolarizing muscle relaxants, especially succinylcholine chloride.
Drugs that enhance hepatic drug metabolism by induction of microsomal enzymes, such as barbiturates (mainly phenobarbital) or phenytoin, increase lidocaine clearance from plasma, thereby reducing its efficacy.
When lidocaine is administered concomitantly with inhaled general anaesthetics, depressant effects may be intensified.

• Other interactions relevant during use in local anaesthesia The local anaesthetic effect is prolonged when administered with a vasoconstrictor. Concurrent administration of ergot alkaloids (e.g. ergotamine) with epinephrine, which may be present in the local anaesthetic mixture, may cause severe hypertension. Combining different local anaesthetics may lead to additive effects on the cardiovascular and central nervous systems. The local anaesthetic effect of lidocaine may be prolonged by adding small amounts of atropine, presumably due to reduced tissue permeability caused by atropine. Low doses of physostigmine may protect against toxic effects of lidocaine.
• Other interactions relevant during use in antiarrhythmic treatment If lidocaine is administered simultaneously with other antiarrhythmic drugs, such as beta-receptor blockers or calcium channel blockers, the inhibitory effect on atrioventricular and intraventricular conduction may be intensified. Additional administration of epinephrine or norepinephrine may lead to significant exacerbation of cardiac adverse effects.

3. How to use Lignocain 2%

Dosage and method of administration
Dosage

• Local anaesthesia Generally, the smallest possible dose providing adequate anaesthesia should be administered. The dose must be individually adjusted according to the patient's age, body weight, and the circumstances of each individual case. When injecting into tissues characterized by significant systemic absorption, without simultaneous administration of a vasoconstrictor, a single dose of lidocaine should not exceed 300 mg. If used in combination with a vasoconstrictor, the single dose should not exceed 500 mg. In elderly patients and children, dosage must be individually adjusted. In the clinical applications listed below, the following single doses of the injection solution and active substance are recommended for adult and adolescent patients over 15 years of age:

To prolong anesthesia, lidocaine may be used in combination with a vasoconstrictor agent, e.g. epinephrine. It has been demonstrated that adding epinephrine at a concentration of 1:100,000 to 1:200,000 is beneficial. In dentistry, in particular, local anesthesia combined with a vasoconstrictor may be necessary. However, lidocaine with epinephrine should be used exclusively for anesthesia in the facial area (teeth, oral cavity, jaws).

In children, lower concentrations of the local anesthetic should be used. Doses must be calculated individually, taking into account the patient's age and body weight.

Lower doses should be used in patients with poor general health status and in those with reduced protein-binding capacity (e.g. due to renal failure, hepatic failure, malignancies, or pregnancy).

In patients with renal failure, a shorter duration of local anesthesia has been observed. This effect may be attributed to accelerated systemic absorption due to acidosis or increased cardiac output.

Patients with liver disease show reduced tolerance to amide-type local anesthetics due to decreased hepatic metabolism and limited protein synthesis, resulting in reduced binding of the anesthetic agent to plasma proteins. In such cases, dose reduction is recommended.

A lower dose should also be used in patients exhibiting clinical signs of heart failure or impaired impulse generation and conduction. In such patients, cardiac function should be monitored, including after the local anesthetic effect has subsided. Regardless, local nerve block may be the preferred method of anesthesia in these patients.

In peripartum applications, the dose should be reduced by approximately one-third due to altered anatomical characteristics in late pregnancy.

• Treatment of acute ventricular tachycardia or tachyarrhythmia
  Adults
  Initially, 70 to 100 mg (1 to 1.5 mg/kg body weight) of lidocaine hydrochloride monohydrate, corresponding to 3.5 to 5 ml (0.05 to 0.075 ml/kg body weight) of Lignocain 2% preparation, administered slowly intravenously.

The administration rate should not exceed 25 mg/minute, equivalent to 1.25 ml of Lignocain 2% preparation per minute.

If the therapeutic effect of the initial dose is insufficient, a second dose equal to one-third to one-half of the initial dose may be administered after 10–15 minutes.

Within one hour, no more than 200 to 300 mg of lidocaine hydrochloride monohydrate should be administered, corresponding to 10 to 15 ml of Lignocain 2% preparation.

To maintain a therapeutic plasma concentration of lidocaine (1.5–5 mg/L), lidocaine hydrochloride monohydrate should be administered as a continuous intravenous infusion at a rate of 20 to 50 micrograms/kg body weight/minute, equivalent to 0.001 to 0.0025 ml of Lignocain 2%/kg body weight/minute.

The infusion may be prepared by adding 1000 mg of lidocaine hydrochloride monohydrate (corresponding to 50 ml of Lignocain 2% preparation) to 500 ml of glucose solution or physiological saline.

A 70 kg patient should receive 1 to 2 ml of this solution per minute, corresponding to 2 to 4 mg of lidocaine hydrochloride monohydrate per minute.

The dose should be adjusted according to individual requirements and therapeutic response.

After prolonged lidocaine infusion (over 12 hours), accumulation should be expected due to the prolonged biological half-life of lidocaine, and the dose should be appropriately reduced.

The dose should also be reduced in patients with heart failure or liver disease, in patients taking drugs that potentiate the effects of lidocaine (see section 4.5 Interactions), during pregnancy, and in patients over 60 years of age.

Renal failure does not generally require specific dose adjustment; however, patients in this group should be monitored for toxic effects due to accumulation of active metabolites.

Dose adjustment of antiarrhythmic drugs requires careful cardiac monitoring. Access to resuscitation equipment and continuous ECG monitoring should be ensured. During therapy, cardiac function should be monitored at regular intervals, e.g. standard ECG once a month or long-term ECG every three months. If necessary, exercise electrocardiography should also be performed. If one or more parameters indicate worsening cardiac function, e.g. QRS or QT interval prolongation exceeding 25%, PQ interval prolongation exceeding 50%, QT interval exceeding 500 ms, or increased frequency and/or severity of cardiac arrhythmia episodes, treatment modification is required.

Children
The safety and efficacy of lidocaine in children have not been definitively established. The American Heart Association in its "Standards and Guidelines for Cardiopulmonary Resuscitation and Emergency Cardiovascular Care" (1992) recommends an initial dose of 1 mg/kg body weight, followed, if necessary, by an intravenous infusion of 20 to 50 micrograms/kg body weight/minute. To ensure an adequately high plasma lidocaine concentration, a second dose of 1 mg/kg body weight may be administered prior to the infusion.

Special dosage recommendations
In critical cases and during prolonged treatment, monitoring of plasma lidocaine concentration is recommended, maintaining levels at 3 (1.5–5) mg/L. Precise dosing should be individually determined for each patient.

Duration of treatment
Infusion should be discontinued immediately after stabilization of cardiac rhythm or upon observation of the first signs of overdose.

Administration method

• Local anesthesia
  Depending on the anesthetic procedure, the solution is administered via intradermal, subcutaneous, or epidural injection, injected into a limited tissue space (infiltration anesthesia), or applied locally by puncture appropriate to the anatomical situation.

All anesthesia procedures should be performed by personnel adequately qualified in the respective anesthetic technique.

Generally, lower concentrations are recommended for continuous anesthesia.

• Treatment of acute ventricular tachyarrhythmia
  Slow intravenous injection or intravenous infusion after dilution in an appropriate diluent.

Lidocaine administration should be accompanied by continuous monitoring of ECG, blood pressure, and respiration. If prolongation of the P-Q interval, widening of the QRS complex, or further widening of a previously widened QRS complex is observed during lidocaine administration (which may be the first sign of overdose), or if cardiac arrhythmia worsens, lidocaine administration should be discontinued. In critical situations, if bradycardia is excluded, lidocaine may be administered with continuous monitoring of heart rate.

Due to the relatively short duration of action of lidocaine, a continuous infusion should follow the initial bolus injection, preferably using an infusion pump, if possible.

When using lidocaine-containing preparations, it should be noted that treatment with Class I antiarrhythmic drugs has not been proven to improve survival.

Note:
In patients under general anesthesia, central nervous system disturbances may not manifest clinically, and sudden cardiovascular adverse effects may occur.

In case of overdose

Low toxic doses of lidocaine cause central nervous system excitation. Large overdoses leading to high toxic plasma concentrations cause central depression.

Two phases of lidocaine toxicity can be distinguished:

a) Excitation phase
Central nervous system:
Unpleasant oral sensation, tongue paresthesia, anxiety, delirium, seizures
Cardiovascular system:
Tachycardia, hypertension, hot flushes

b) Depression phase
Central nervous system:
Coma, respiratory arrest
Cardiovascular system:
Impalpable pulse, pallor, cardiac arrest

In the initial phase of local anesthetic toxicity, patients mainly exhibit excitatory symptoms: anxiety, dizziness, auditory and visual disturbances, tingling (mainly in the tongue and mouth), dysarthria. Tremor or muscle twitching may be a sign of impending seizure. Plasma lidocaine concentrations not causing seizures may still induce drowsiness or sedation. As central nervous system toxicity progresses, after the seizure phase, increasing brainstem dysfunction occurs, manifesting as respiratory depression and coma, potentially leading to death.

Sudden hypotension is often the first sign of lidocaine cardiotoxicity. Hypotension is primarily caused by the negative inotropic effect of lidocaine and reduced cardiac output. However, these toxic effects are less dangerous than neurologic adverse effects.

The appearance of neurologic or cardiologic symptoms requires immediate intervention

• Discontinue administration of the anesthetic agent.
• Ensure airway patency. Provide oxygen ventilation (100% O₂) – assisted or controlled – initially via face mask, and if necessary, followed by intubation. Oxygenation must be continued until all vital functions return to normal.
• Carefully monitor blood pressure, pulse, and pupil size. These measures should also be applied in cases of accidental spinal anesthesia, initially presenting with anxiety, muffled speech, and drowsiness, which may progress to loss of consciousness and respiratory arrest. Additionally, the following therapeutic measures are recommended:
• In case of severe hypotension, immediately lower the patient's head position and administer an alpha-sympathomimetic drug as a slow intravenous injection (e.g. 10–20 drops of a solution containing 1 mg isoprenaline in 200 ml glucose solution). Additionally, administer fluids (e.g. electrolyte solution).
• In case of increased vagal tone (bradycardia), administer 0.5–1 mg atropine intravenously.
• In case of seizures, administer small intravenous doses of an ultra-short-acting barbiturate, e.g. thiopental (50–100 mg), or diazepam (5–10 mg), until seizure control is achieved. If seizures persist, administer thiopental (250 mg) and a short-acting muscle relaxant, perform intubation, and ensure mechanical ventilation with 100% oxygen. It should be noted that oxygen ventilation alone may be sufficient treatment after the first signs of seizures appear.
• It is assumed that standard procedures for cardiac arrest are known. In severe cases, consultation with an anesthesiology and intensive care specialist is recommended. The use of central nervous system analeptic agents is contraindicated! There is no specific antidote. Lidocaine is not removed during dialysis.

4. Possible adverse reactions

Possible adverse reactions of lidocaine are largely similar to those of other amide-type local anesthetics. Systemic adverse reactions, expected at plasma concentrations exceeding 5–10 mg/L, are related to the specific injection technique used or to disturbances in pharmacokinetics or pharmacodynamics. These reactions manifest with both neurological and cardiovascular symptoms.
Blood pressure usually increases only slightly at standard clinical plasma concentrations of lidocaine, due to its positive inotropic and chronotropic effects. Sudden hypotension, as a sign of cardiotoxicity, may be the first indication of relative drug overdose.
As with other local anesthetics, malignant hyperthermia cannot be entirely ruled out when using lidocaine. In principle, the use of lidocaine is considered safe in patients with a personal or family history of predisposition to or malignant hyperthermia, although this complication has been reported in one patient who received epidural anesthesia with lidocaine.
After spinal anesthesia, transient pain in the lower limbs and lower back commonly occurs. This pain may persist for up to 5 days and resolves spontaneously.
Neurological complications following central nerve blocks—mainly after subarachnoid anesthesia—are rare, but may include persistent paresthesia, paralysis of the lower limbs, or urinary incontinence (e.g. cauda equina syndrome).
In very rare cases, allergy to amide-type local anesthetics may present as urticaria, angioedema, bronchospasm, or respiratory and circulatory disturbances.
Proarrhythmic effects, evident as new-onset or worsening of pre-existing arrhythmias, may lead to severe cardiac dysfunction, potentially resulting in cardiac arrest.
Thrombophlebitis may occur as a result of prolonged infusion.

Reporting suspected adverse reactions
Following marketing authorization of the medicinal product, it is important to report suspected adverse reactions. This enables continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are required to report any suspected adverse reactions through the Department of Monitoring Adverse Drug Reactions at the Office for Registration of Medicinal Products, Medical Devices and Biocidal Products:
Al. Jerozolimskie 181C, 02-222 Warsaw
Tel.: +48 22 49 21 301
Fax: +48 22 49 21 309
Website: https://smz.ezdrowie.gov.pl
Reporting adverse reactions will help gather additional information on the safety of this medicinal product.

5. Storage of the medicinal product Lignocain 2%

Store below 25°C.
Expiry date
Do not use after the expiry date stated on the packaging.

6. Other information

For more detailed information, please contact the marketing authorization holder:
Poland
Aesculap Chifa Sp. z o.o.
Tysiąclecia 14
64-300 Nowy Tomyśl
tel. (0-61) 44 20 100
Date of leaflet preparation: 2023-04-17