Lignocaine (Lidocaine) Injection - Uses, Dose, Side effects

Lidocaine is a common local anesthetic and antiarrhythmic medication. It works by blocking nerve signals in the body and numbing the area where it is applied. This makes it useful for various medical procedures, such as dental work, minor surgeries, and certain diagnostic procedures.

Lignocaine (Lidocaine) Injection is a local anesthetic and a Class Ib anti-arrhythmic medication. It is used for life-threatening arrhythmias, local anesthesia, and spinal anesthesia.

Indications of Lidocaine (Lignocaine):

  • It is used to treat ventricular arrhythmias brought on by myocardial infarction or to manipulate the heart.
  • It is utilized for local and regional anesthesia via infiltration, nerve block, epidural, or spinal procedures (eg, cardiac surgery).

Note:

  • It is used to treat ventricular arrhythmias brought on by myocardial infarction or to manipulate the heart. It is utilized for local and regional anesthesia via infiltration, nerve block, epidural, or spinal procedures (eg, cardiac surgery).
  • Off-Label Use of Lidocaine in Adults:
    • Interstitial cystitis (syndrome of bladder discomfort) (alkalinized lidocaine)
    • recommendations for ACLS monomorphic VT brought on by drugs
    • Monomorphic ventricular tachycardia (VT) with hemodynamic stability (preserved ventricular function)
    • VT polymorphic (preserved ventricular function)
    • a substitute for amiodarone in the treatment of ventricular fibrillation (VF) or pulseless VT (unresponsive to CPR, defibrillation, and vasopressor therapy)

Lidocaine (Lidocaine) dose in adults:

Lignocaine dose in the treatment of Arrhythmic (off-label):

Initial Dose:

  • If someone has these heart rhythm problems, after trying defibrillation (shocking the heart), CPR, and using epinephrine, lidocaine is given directly into the vein (IV) or bone (IO) as a quick injection.
  • The first dose is 1 to 1.5 milligrams per kilogram (mg/kg) of the person's weight. If the heart rhythm doesn't improve, more doses of 0.5 to 0.75 mg/kg can be given every 5 to 10 minutes, up to a maximum total dose of 3 mg/kg.

Continuous Infusion:

  • After the heart's normal rhythm is restored, lidocaine can be given continuously through a drip into the vein at a rate of 1 to 4 milligrams per minute.

If the Rhythm Comes Back:

  • If the abnormal rhythm comes back while the person is getting a continuous infusion, another quick dose of 0.5 mg/kg can be given, and the infusion might need to be changed.

Endotracheal Route:

  • If it's difficult to give lidocaine through a vein, it can be given directly into the windpipe (endotracheal tube) in a larger dose, which is 2 to 3.75 mg/kg. However, this method is not as effective as giving it through a vein.

Stable Monomorphic VT:

  • For people with a certain type of stable abnormal heart rhythm called monomorphic ventricular tachycardia, lidocaine can be given in a similar way to the initial dose, but it may need to be repeated every 5 to 10 minutes if needed, up to a maximum total dose of 3 mg/kg. Then, a continuous infusion is started.

Adjustment for Certain Conditions:

  • For people with heart failure, shock, or liver problems, the dose of continuous infusion might need to be adjusted and started at a lower rate.

Lignocaine Dose as a local injectable anesthetic:

In anesthesia for local injection, the dose of lidocaine can vary based on several factors:

  • Type of Procedure: The amount of lidocaine used depends on the specific medical procedure being performed.
  • Level of Anesthesia Needed: The dose also depends on how much anesthesia is required for the procedure.
  • Tissue Vascularity: The level of blood flow in the tissue being treated affects the dose.
  • Duration of Anesthesia: The length of time the anesthesia needs to last influences the dose.
  • Patient's Physical Condition: The overall health and condition of the patient help determine the appropriate dose.

For cutaneous infiltration (injecting lidocaine under the skin),

  • The maximum dose is 4.5 milligrams per kilogram (mg/kg) per dose, not exceeding 300 mg in total. Repeat doses should not be given within 2 hours.

For pain relief through an intraosseous line (a needle inserted into the bone),

  • The initial dose is 40 mg given over 1 to 2 minutes. The usual adult dose range is 20 to 50 mg per dose. After allowing the lidocaine to dwell for up to 1 minute, it's followed by a flush with normal saline (NS).
  • Some centers then administer a second, lower dose (50% dose reduction) over 30 to 60 seconds. If discomfort reoccurs, doses may be repeated, with a maximum frequency of every 45 minutes during intraosseous access. The maximum total dose is not established.

It's important to follow specific instructions and consult product information for accurate dosing, especially regarding intraosseous access devices, which have specific weight and age requirements for use.

Lignocaine dose in the therapy of Interstitial cystitis (bladder pain syndrome) (off-label): Intravesical:

In the treatment of interstitial cystitis, also known as bladder pain syndrome, lidocaine is sometimes used intravesically, meaning it's instilled directly into the bladder.

Single Instillation:

  • A single dose involves instilling a mixture of lidocaine (200 mg), heparin (50,000 units), and sodium bicarbonate (420 mg) in 15 mL of sterile water into the bladder via catheter. It's left in the bladder for 30 minutes before draining.

Weekly Instillation:

  • This involves weekly instillations for 12 consecutive weeks. The mixture used includes lidocaine 4% (5 mL), heparin (20,000 units), and sodium bicarbonate 7% (25 mL). It's instilled into an empty bladder via catheter and left to dwell for 30 minutes before drainage.

Daily Instillation:

  • Daily bladder instillations for 5 days with a mixture of lidocaine (200 mg) and sodium bicarbonate 8.4% solution to a final volume of 10 mL. It's instilled into an empty bladder and left to dwell for 1 hour before drainage.

It's important to note that proper alkalinization of lidocaine is necessary to prevent precipitation. The stability and pH of the mixture should be determined before administration. These dosing regimens are considered off-label, meaning they are not specifically approved by regulatory authorities for this indication, but they are used based on clinical experience and evidence.


Lidocaine (Lignocaine) dose in children:

When treating shock-refractory ventricular fibrillation or pulseless ventricular tachycardia, lignocaine dosage:

In the treatment of ventricular fibrillation (VF) or pulseless ventricular tachycardia (VT) that doesn't respond to shock, the dosing of lidocaine for infants, children, and adolescents is as follows:

  • Loading Dose:
    • For infants, children, and adolescents, the initial loading dose is 1 milligram per kilogram (mg/kg) of body weight.
    • If there's a delay of more than 15 minutes between the initial bolus and starting the continuous infusion, a second bolus may be administered.
  • Continuous IV Infusion:
    • After the loading dose, lidocaine is given as a continuous intravenous infusion at a rate of 20 to 50 micrograms per kilogram per minute (mcg/kg/minute).
    • However, in patients with certain conditions like shock, hepatic disease, cardiac arrest, or congestive heart failure (CHF), the manufacturer recommends not exceeding 20 mcg/kg/minute.
  • Endotracheal Route:
    • If it's not possible to give lidocaine through an intravenous or intraosseous route, it can be given directly into the windpipe (endotracheal tube).
    • The loading dose for this route is higher, at 2 to 3 mg/kg.
    • After administering the dose, the tube should be flushed with 5 milliliters (mL) of normal saline (NS), followed by 5 assisted manual ventilations.

These dosages are based on recommendations from pediatric advanced life support (PALS) guidelines.

Lignocaine Dose in the Anesthesia as a local anesthetic:

In local anesthesia, the dose of lidocaine varies depending on several factors:

  • Type of Procedure: The amount of lidocaine used depends on the specific medical procedure being performed.
  • Level of Anesthesia Needed: The dose is adjusted based on how much anesthesia is required for the procedure.
  • Tissue Vascularity: The level of blood flow in the tissue being treated influences the dose.
  • Duration of Anesthesia: The length of time the anesthesia needs to last affects the dose.
  • Patient's Age and Weight:
    • Children and Adolescents for Cutaneous Infiltration: Typically, lidocaine solutions with concentrations less than 2% should be used. The maximum dose is 5 milligrams per kilogram (mg/kg) per dose, not exceeding the recommended maximum adult dose of 300 mg per dose. Repeat doses should not be given within 2 hours.
    • Infants, Children, and Adolescents for Intraosseous Line or Infusion Pain: The initial dose is 0.5 mg/kg given over 1 to 2 minutes. The usual adult dose range and maximum dose are 20 to 50 mg per dose. A second lower dose (50% reduction) may be administered over 30 to 60 seconds if needed. Repeat doses may be given at a maximum frequency of every 45 minutes during intraosseous access. The maximum total dose is not established, but some centers suggest that it should not exceed 3 mg/kg within 24 hours.

It's important to follow specific instructions and consult product information, especially regarding intraosseous access devices, which have specific weight and age requirements for use. These dosing guidelines are based on considerations for children, adolescents, and infants to ensure safe and effective anesthesia.


Lignocaine Pregnancy Risk Category: B

  • Lidocaine, when given to pregnant women for anesthesia before delivery, can cross the placenta and reach the baby's bloodstream.
  • This might lead to adverse effects on the baby's central nervous system, heart, or blood vessels.
  • It's recommended to monitor the baby's heart during the procedure.
  • Lidocaine injections are approved for pain relief during childbirth, like before epidural or spinal anesthesia, and for local pain relief during procedures like episiotomy and obstetric laceration repair.
  • However, it's important to note that using lidocaine in the perineal area may lead to more absorption than when used epidurally.
  • Doctors consider the total amount of lidocaine exposure from all sources.
  • If a pregnant woman needs surgery, it's recommended not to delay it if it's medically necessary, but elective procedures should be postponed until after delivery.
  • In cases of cardiac arrest during pregnancy, medications used for treatment are the same as for non-pregnant women, following current guidelines, and concerns about harming the baby should not prevent the use of appropriate medications.

Lidocaine use during breastfeeding:

  • Lidocaine can be found in breast milk, with a relative infant dose (RID) of 4.9%, calculated from the highest concentration of lidocaine found in breast milk compared to the mother's dose for epidural anesthesia.
  • Generally, breastfeeding is considered safe when the RID is less than 10%.
  • The estimated daily dose of lidocaine for a breastfeeding infant via breast milk is 129 micrograms per kilogram per day, based on a mean milk concentration of 0.86 micrograms per milliliter sampled 2 hours after maternal administration during cesarean delivery.
  • Lidocaine concentrations in breast milk decrease over time.
  • Metabolites of lidocaine have also been detected in breast milk, but lower concentrations are observed after dental procedures, infusion for arrhythmias, and liposuction.
  • Oral absorption by the breastfeeding infant is expected to be minimal.
  • Guidelines generally consider lidocaine compatible with breastfeeding when used as an antiarrhythmic or local anesthetic, but cumulative exposure from all sources should be considered.

Lignocaine Dose adjustment in renal disease:

  • The manufacturer's labeling for lidocaine does not provide dosage adjustments.
  • However, it's important to note that the accumulation of lidocaine metabolites may increase in individuals with renal dysfunction.
  • Lidocaine is not significantly removed by hemodialysis or peritoneal dialysis, with only 0% to 5% removed through these methods.
  • Therefore, supplemental doses of lidocaine are not necessary during dialysis.

Lignocaine Dose adjustment in liver disease:

  • When using lidocaine in patients with certain conditions or risk factors, caution is advised.
  • In such cases, it's recommended to reduce the maintenance infusion rate.
  • The initial infusion rate should be set at 0.75 milligrams per minute or 10 micrograms per kilogram per minute.
  • The maximum allowable dose is 1.5 milligrams per minute or 20 micrograms per kilogram per minute.
  • It's essential to closely monitor lidocaine concentrations in the bloodstream and adjust the infusion rate as needed.

The administration route has an impact on the effects. Numerous effects are dose-dependent.

Side Effects of Lidocaine (Lignocaine):

  • Central nervous system:
    • Shivering
    • Radiculopathy
    • Headache

Uncommon Side effects of Lignocaine (Lidocaine):

  • Neuromuscular & Skeletal:
    • Tremor
    • Weakness
  • Gastrointestinal:
    • Nausea (Including Following Spinal Anesthesia)
    • Vomiting
  • Cardiovascular:
    • Circulatory Shock
    • Cardiac Arrhythmia
    • Bradycardia
    • Coronary Artery Vasospasm
    • Hypotension (Including Following Spinal Anesthesia)
    • Heart Block
    • Edema
    • Local Thrombophlebitis
    • Flushing
    • Vascular Insufficiency (Periarticular Injections)
  • Central Nervous System:
    • Disorientation
    • Cauda Equina Syndrome (Following Spinal Anesthesia)
    • Coma
    • Dizziness
    • Agitation
    • Anxiety
    • Hallucination
    • Hyperesthesia
    • Apprehension
    • Confusion
    • Drowsiness
    • Euphoria
    • Hypoesthesia
    • Paresthesia
    • Peripheral Neuropathy (Following Spinal Anesthesia)
    • Intolerance To Temperature
    • Lethargy
    • Nervousness
    • Seizure
    • Loss Of Consciousness
    • Metallic Taste
    • Slurred Speech
    • Twitching
    • Psychosis
  • Otic:
    • Tinnitus
  • Hypersensitivity:
    • Anaphylactoid Reaction
    • Hypersensitivity Reaction
    • Anaphylaxis
  • Respiratory:
    • Respiratory Depression
    • Dyspnea
    • Respiratory Insufficiency (Following Spinal Anesthesia)
    • Bronchospasm

Contraindications to Lidocaine (Lignocaine):

  • Lidocaine is contraindicated in individuals who have a hypersensitivity to lidocaine itself or to any component of the formulation, as well as those who are hypersensitive to other local anesthetics of the amide type.
  • Additionally, it is contraindicated in individuals with Adam-Stokes syndrome, Wolff-Parkinson-White syndrome, severe degrees of sinoatrial (SA), atrioventricular (AV), or intraventricular heart block (except in patients with a functioning artificial pacemaker).
  • Premixed lidocaine injections may contain corn-derived dextrose, making their use contraindicated in patients with allergies to corn or corn-related products.
  • In Canadian labeling, additional contraindications include hypersensitivity to ester local anesthetics (for paraben-containing solutions only).
  • Antimicrobial preservative-containing solutions should not be used intra- or retro-ocularly, for epidural or spinal anesthesia, or in any route that would introduce the solution into the cerebrospinal fluid, or in doses greater than or equal to 15 mL for other types of blockades.

Warnings and precautions

Infusion-related intra-articular chondrolysis

  • Continuous intra-articular infusion of local anesthetics after arthroscopic or other surgical procedures is not an approved use due to the risk of chondrolysis, particularly in the shoulder joint.
  • Chondrolysis is the destruction of cartilage, which can lead to severe joint pain and dysfunction.
  • Some cases of chondrolysis have been reported following intra-articular infusion, necessitating arthroplasty or shoulder replacement surgeries.
  • Therefore, caution should be exercised, and alternative pain management strategies should be considered to minimize this risk.

Methemoglobinemia:

  • Methemoglobinemia, a condition where the blood carries an abnormal amount of methemoglobin, has been reported with the use of local anesthetics.
  • Clinically significant methemoglobinemia requires immediate treatment, and the use of the anesthetic and other oxidizing agents should be stopped.
  • Symptoms of methemoglobinemia, such as cyanosis (bluish discoloration of the skin), headache, rapid pulse, shortness of breath, lightheadedness, and fatigue, may occur immediately or several hours after exposure to the anesthetic.
  • Patients with certain conditions, including glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary issues, exposure to oxidizing agents, or infants under six months old, are at higher risk and should be closely monitored for signs and symptoms of methemoglobinemia.

Hepatic dysfunction

  • In patients with severe hepatic dysfunction, extreme caution should be exercised when using lidocaine, as they may have an increased risk of lidocaine toxicity.
  • Hepatic dysfunction can affect the metabolism and clearance of lidocaine from the body, potentially leading to higher concentrations of the drug in the bloodstream and an increased risk of adverse effects.
  • Therefore, careful monitoring of liver function and lidocaine levels is essential in these patients to ensure safe and effective use of the medication.

Pseudocholinesterase deficiency:

  • In patients with pseudocholinesterase deficiency, caution should be exercised when using lidocaine, as they may have an increased risk of lidocaine toxicity.
  • Pseudocholinesterase is an enzyme involved in the breakdown of certain medications, including lidocaine.
  • Deficiency of this enzyme can result in slower metabolism and clearance of lidocaine from the body, potentially leading to higher concentrations of the drug in the bloodstream and an increased risk of adverse effects.
  • Therefore, careful monitoring of lidocaine levels and clinical response is important in these patients to prevent toxicity.

Lidocaine (systemic): Drug Interaction

Risk Factor C (Monitor therapy)

Amiodarone

might increase the blood level of lidocaine (Systemic).

Aprepitant

may increase the blood level of CYP3A4 substrates (High risk with Inhibitors).

Beta-Blockers

might increase the blood level of lidocaine (Systemic).

Bosentan

may decline the level of CYP3A4 substrates in the blood (High risk with Inducers).

Broccoli

may decline the level of CYP3A4 substrates in the blood (High risk with Inducers).

Cannabis

may decline the level of CYP3A4 substrates in the blood (High risk with Inducers).

Clofazimine

may raise the serum level of CYP3A4 substrates (High risk with Inhibitors).

CYP1A2 Inducers (Moderate)

Could lower the serum level of lidocaine (Systemic).

CYP1A2 Inhibitors (Strong)

Lidocaine serum concentration can rise (Systemic).

CYP3A4 Inducers (Moderate)

may lower the serum level of CYP3A4 substrates (High risk with Inducers).

CYP3A4 Inhibitors (Moderate)

may slow down CYP3A4 substrate metabolism (High risk with Inhibitors).

Dapsone (Topical)

may intensify the harmful/toxic effects of agents associated with methemoglobinemia.

Deferasirox

could reduce the serum concentration of CYP3A4 substrates (High risk with Inducers).

Disopyramide

may increase the effects of lidocaine on heart rhythm (Systemic). Disopyramide may cause the serum levels of lidocaine to increase (Systemic). especially the amount of lidocaine that is free and unbound

Duvelisib

may increase CYP3A4 substrates' serum concentration (High risk with Inhibitors).

Erdafitinib

may decline the blood level of CYP3A4 substrates (High risk with Inducers).

Erdafitinib

May raise the blood concentration of CYP3A4 Substrates (High risk with Inhibitors).

Etravirine

May decline the blood concentration of Lidocaine (Systemic).

Fosaprepitant

May raise the blood concentration of CYP3A4 Substrates (High risk with Inhibitors).

Fosnetupitant

May raise the blood concentration of CYP3A4 Substrates (High risk with Inhibitors).

Hyaluronidase

May enhance the adverse/toxic effect of Local Anesthetics.

Ivosidenib

may lower the serum level of CYP3A4 substrates (High risk with Inducers).

Lacosamide

Lidocaine (Systemic) may intensify Lacosamide's negative or hazardous effects. Particularly, there may be an increased risk for bradycardia, ventricular tachyarrhythmias, or a longer PR interval.

Larotrectinib

may increase CYP3A4 substrates' serum concentration (High risk with Inhibitors).

Local Anesthetics

The harmful or toxic effects of local anesthetics may be increased by methemoglobinemia-associated agents. In particular, there may be an elevated risk for methemoglobinemia.

Methemoglobinemia Associated Agents

might make local anesthetics more harmful or poisonous. In particular, there may be an elevated risk for methemoglobinemia.

Netupitant

may increase CYP3A4 substrates' serum concentration (High risk with Inhibitors).
may increase CYP3A4 substrates' serum concentration (High risk with Inhibitors).

Neuromuscular-Blocking Agents

The neuromuscular-blocking action of neuromuscular-blocking agents may be strengthened by local anesthetics.

Nitric Oxide

may intensify the harmful/toxic effects of agents associated with methemoglobinemia. Combinations of these medications may make substantial methemoglobinemia more likely.

Palbociclib

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Prilocaine

The harmful or toxic effects of Prilocaine may be increased by methemoglobinemia-associated agents. Combinations of these medications may make substantial methemoglobinemia more likely. Monitoring patients for methemoglobinemia symptoms (such as hypoxia and cyanosis) is necessary when prilocaine is used with other medications that might cause methemoglobinemia in patients. When giving these medicines to newborns, avoid using lidocaine or prilocaine.

Sarilumab

could reduce the blood concentration of CYP3A4 substrates (High risk with Inducers).

Siltuximab

could reduce the blood concentration of CYP3A4 substrates (High risk with Inducers).

Simeprevir

may elevate blood levels of CYP3A4 substrates (High risk with Inhibitors).

Sodium Nitrite

Sodium nitrite may be made more dangerous or detrimental by methemoglobinemia-associated agents. Combining these drugs may increase the likelihood of significant methemoglobinemia.

Technetium Tc 99m Tilmanocept

Technetium Tc 99m Tilmanocept's diagnostic utility may be reduced by local anesthetics. Management: Prevent co-injecting local anesthetics and technetium Tc 99m tilmanocept at the same time. Other applications of these agents in combination do not appear to be affected by this interaction.

Tobacco (Smoked)

may lower the level of lidocaine in the serum (Systemic).

Tocilizumab

may lower the serum level of CYP3A4 substrates (High risk with Inducers).

Risk Factor D (Consider therapy modification)

Bupivacaine (Liposomal)

Bupivacaine's harmful or toxic effects might be exacerbated by systemic lidocaine (Liposomal). Treatment: Topical lidocaine and liposomal bupivacaine should not be used. It is possible to provide liposomal bupivacaine 20 minutes or longer after giving lidocaine.

CYP3A4 Inducers (Strong)

may speed up CYP3A4 substrate metabolism (High risk with Inducers). Management: Take into account a substitute for one of the interfering medications. Specific contraindications may apply to some combinations. the relevant manufacturer's label.

CYP3A4 Inhibitors (Strong)

may slow down CYP3A4 substrate metabolism (High risk with Inhibitors).

Dabrafenib

may lower the serum level of CYP3A4 substrates (High risk with Inducers). Management: When feasible, look for substitutes for the CYP3A4 substrate. If concurrent therapy cannot be avoided, pay special attention to the substrate's clinical consequences (particularly therapeutic effects).

Enzalutamide

may lower the serum level of CYP3A4 substrates (High risk with Inducers). Treatment: Enzalutamide should not be used concurrently with CYP3A4 substrates that have a limited therapeutic index. Enzalutamide use, like with the use of any other CYP3A4 substrate, should be done cautiously and under close observation.

Lorlatinib

may lower the serum level of CYP3A4 substrates (High risk with Inducers). Management: Avoid using lorlatinib at the same time as any CYP3A4 substrates for which even a small drop in blood levels of the substrate might result in therapeutic failure and negative clinical outcomes.

MiFEPRIStone

may increase CYP3A4 substrates' serum concentration (High risk with Inhibitors). Management: During and two weeks after mifepristone treatment, reduce dosages of CYP3A4 substrates and keep an eye out for elevated amounts or toxicity. Fentanyl, pimozide, quinidine, sirolimus, and tacrolimus should all be avoided. Cyclosporine should also be avoided.

Mitotane

may lower the serum level of CYP3A4 substrates (High risk with Inducers). Treatment: When administered in individuals receiving mitotane, doses of CYP3A4 substrates may need to be significantly modified.

Stiripentol

may lower the serum level of CYP3A4 substrates (High risk with Inducers). Treatment: When administered in individuals receiving mitotane, doses of CYP3A4 substrates may need to be significantly modified.

Risk Factor X (Avoid combination)

Conivaptan

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Fusidic Acid (Systemic)

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Idelalisib

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Saquinavir

May intensify Lidocaine's arrhythmogenic effects (Systemic). Saquinavir may elevate Lidocaine's serum levels (Systemic).

Monitoring parameters:

Liver Function Tests:

  • Patients with liver problems should have their liver function monitored closely.
  • Liver dysfunction can affect how lidocaine is processed in the body.

Lidocaine Concentrations:

  • Regular monitoring of lidocaine levels in the blood is important.
  • This helps ensure that the drug is at safe and effective levels.

ECG Monitoring:

  • Electrocardiogram (ECG) monitoring may be necessary during lidocaine therapy.
  • This helps detect any changes in heart rhythm that may indicate lidocaine toxicity.

Blood Level Monitoring for Long-Term Use:

  • For patients requiring lidocaine treatment for more than 24 hours, blood level monitoring is recommended.
  • This ensures that lidocaine levels stay within a safe range over time.

How to administer Lidocaine?

Intravenous (IV) Administration:

Bolus:

  • The manufacturer recommends administering lidocaine at a rate of 25 to 50 mg per minute. In cardiac arrest situations, such as ventricular fibrillation or pulseless ventricular tachycardia, lidocaine may be infused rapidly into a peripheral vein.

Continuous Infusion:

  • After the initial bolus dose, lidocaine can be given as a continuous infusion. Specific infusion rates depend on the indication and should be followed per dosing guidelines. Continuous infusion may be initiated in cardiac arrest cases once spontaneous circulation returns after lidocaine administration, but ongoing infusion solely for preventing recurrence lacks evidence support.

Endotracheal Administration (Off-label):

  • Lidocaine can be diluted in normal saline (NS) or sterile water for administration through an endotracheal tube. Absorption is better with sterile water, causing less impairment of oxygen levels. Stop chest compressions, quickly spray the drug down the tube, flush with 5 mL of NS, followed by quick insufflations, and resume chest compressions.

Intraosseous (IO) Administration (Off-label):

  • Intraosseous administration is an alternative when rapid IV access isn't feasible, especially in emergency situations.

Intravesical Administration (Off-label):

  • Various regimens of alkalinized lidocaine, sometimes with heparin, have been used by instilling them into the bladder for certain medical conditions.

On-Q® Infusion Pump:

  • This pump is used for slow administration of local anesthetics like lidocaine around surgical wounds or nerves for pre- or postoperative regional anesthesia. However, direct infusion into the shoulder joint has led to chondrolysis (cartilage destruction). It's crucial never to place On-Q® pumps directly into any joint to avoid this risk.

Mechanism of action of Lidocaine (Lignocaine):

  • Lidocaine is classified as a Class Ib antiarrhythmic medication.
  • It works by suppressing the automaticity of conduction tissue in the heart.
  • This is achieved by increasing the electrical stimulation threshold of the ventricles and the His-Purkinje system.
  • Additionally, lidocaine inhibits the spontaneous depolarization of the ventricles during diastole through a direct action on the heart tissues.
  • It blocks both the initiation and conduction of nerve impulses by reducing the permeability of the neuronal membrane to sodium ions.
  • This inhibition of depolarization results in the blockade of electrical conduction in the heart.

Onset of Action:

  • A single bolus dose typically takes 45 to 90 seconds to start working.

Duration:

  • The effects of lidocaine usually last for 10 to 20 minutes.

Distribution:

  • Lidocaine has a distribution volume of approximately 1.5 ± 0.6 liters per kilogram (L/kg).
  • This volume can vary based on individual patient factors.
  • Lidocaine can cross the blood-brain barrier, affecting the central nervous system.

Protein Binding:

  • Approximately 60% to 80% of lidocaine binds to alpha-1 acid glycoprotein in the blood.

Metabolism:

  • About 90% of lidocaine is metabolized in the liver.
  • Active metabolites, including monoethylglycinexylidide (MEGX) and glycinexylidide (GX), can accumulate in the body and may cause central nervous system (CNS) toxicity.

Half-life Elimination:

  • Lidocaine has a biphasic elimination half-life.
  • The half-life is prolonged in conditions such as congestive heart failure, liver disease, shock, and severe renal disease.
  • Initial half-life ranges from 7 to 30 minutes.
  • Terminal half-life is shorter in adults (1.5 to 2 hours) compared to infants and premature infants (3.2 hours).

Excretion:

  • Lidocaine is primarily excreted in urine.
  • Less than 10% of the drug is eliminated unchanged, while approximately 90% is excreted as metabolites.

International Brands of Lidocaine:

  • P-Care X
  • ReadySharp Lidocaine
  • Xylocaine
  • Xylocaine (Cardiac)
  • Xylocaine-MPF
  • Xylocaine Plain
  • Xylocard
  • Anocaine
  • Chalocaine
  • Dequaspray
  • Dolocaine
  • Ecocain
  • Esracain
  • Ke Ze Pu
  • Lidocard
  • Lignotox
  • Lignox
  • Locaine
  • Locana
  • Lox
  • Lydocan
  • Peterkaien
  • Procomil
  • Rapidocain
  • Roxicaina
  • Sensinal
  • Sensinil
  • Themicain
  • Xilonest
  • Xylo-Efa 10% Cardiologica
  • Xylobex
  • Xylocaine
  • Xylocaine IV
  • Xylocard
  • Xylone

Lignocaine Brands in Pakistan:

Lignocaine Injection 2 % w/w

Lignocain

Shifa Laboratories.(Pvt) Ltd.

Lignocaine Injection 10 Mg/Ml

Epocain

Epoch Pharmaceutical

Lacain

Pulse Pharmaceuticals

Lidex

Caraway Pharmaceuticals

Lidocaine

Amson Vaccines & Pharma (Pvt) Ltd.

Lignosel

Hansel Pharmacueutical Pvt (Ltd)

Locain

Saydon Pharmaceutical Industries (Pvt) Ltd.

Zecaine

Asian Agencies

Zylo

Crest Pharmaceuticals

Lignocaine Injection 20 Mg/Ml

Anacaine

Akson Pharmaceuticals (Pvt) Ltd.

Fist

Shaigan Pharmaceuticals (Pvt) Ltd

Km Lidocaine

Hoffman Health Pakistan Ltd.

Lacain

Pulse Pharmaceuticals

Licain

Epoch Pharmaceutical

Lidoject

Surge Laboratories (Pvt) Ltd.

Ligno Ans

Ipram International

Lignocain

Orient Laboratories

Lignocain

Orient Laboratories

Lignocaine

Elite Pharma

Lignocaine

Elite Pharma

Lignocaine

Elko Organization (Pvt) Ltd.

Lignol

Mass Pharma (Private) Limited

Ligocane

Global Pharmaceuticals

Ligocane

Global Pharmaceuticals

Mb-Cain

Multinational Buisness Link

Neusthetic

Neutro Pharma (Pvt) Ltd.

Xylex

Venus Pharma

Xylex

Venus Pharma

Xylocaine

Barrett Hodgson Pakistan (Pvt) Ltd.

Xylodos

Dosaco Laboratories

Lignocaine Solution 2 % W/V

Elkocaine

Elko Organization (Pvt) Ltd.

Lignocaine Solution 4 % W/V

Primadent Solution

Prime Labs. (Pvt) Ltd.

Xylocaine

Barrett Hodgson Pakistan (Pvt) Ltd.

Lignocaine Liquid 0.6 % W/V

Tripol

Davis Pharmaceutical Laboratories

Lignocaine Oint 5 % W/W

Xylocaine

Barrett Hodgson Pakistan (Pvt) Ltd.

Lignocaine Gel 2 % W/W

Anscon

Ophth-Pharma (Pvt) Ltd.

Grenocin

Gray`S Pharmaceuticals

Lignocaine

Lahore Chemical & Pharmaceutical Works (Pvt) Ltd

Lignopar

Nimrall Laboratories

Lignozin

Trigon Pharmaceuticals Pakistan (Pvt) Ltd.

Logel

Elite Pharma

Primacaine

Prime Labs. (Pvt) Ltd.

Sylogel

Sapient Pharma

Xylocaine

Barrett Hodgson Pakistan (Pvt) Ltd.

Xylogel

Harmann Pharmaceutical Laboratories (Pvt) Ltd.

Zyocain

Pharmawise Labs. (Pvt) Ltd.

Lignocaine Gel 5 % W/W

Taufel

Lexicon Pharmaceuticals (Pvt) Ltd.

Lignocaine Gel 20 Mg/Ml

Lignocain

Safina Pharma (Pvt) Ltd