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Lidocaine 2% Inj, 50ml

Manufacturer HOSPIRA Active Ingredient Lidocaine Injection Solution (Anesthetic)(LYE doe kane) Pronunciation LYE doe kane
It is used to numb an area before a procedure.It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Local Anesthetic, Antiarrhythmic (Class IB)
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Pharmacologic Class
Voltage-gated sodium channel blocker
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Pregnancy Category
Category B
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FDA Approved
Jan 1948
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Lidocaine is a medication used to numb a specific area of your body to prevent pain during medical procedures, or to treat certain heart rhythm problems. It works by temporarily blocking nerve signals in the area where it's applied or injected.
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How to Use This Medicine

To use this medication correctly, follow your doctor's instructions and carefully read all accompanying information. Take this medication exactly as directed, and follow all instructions provided. This drug is administered via injection.

If you need to store this medication at home, consult with your doctor, nurse, or pharmacist to determine the proper storage method.

If you miss a dose, contact your doctor immediately to receive guidance on the appropriate course of action.
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Lifestyle & Tips

  • Inform your healthcare provider about all medications, supplements, and herbal products you are taking.
  • Report any unusual symptoms or discomfort during or after the procedure.
  • Avoid eating or drinking until sensation returns if the mouth or throat area is numbed, to prevent choking or biting your tongue/cheek.
  • Avoid activities requiring fine motor skills or full sensation until the anesthetic effect wears off, especially after nerve blocks.
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Available Forms & Alternatives

Available Strengths:

Dosing & Administration

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Adult Dosing

Standard Dose: Varies significantly by procedure and site of administration. For infiltration: 0.5% to 1% solution. For nerve block: 1% to 2% solution. Max single dose: 4.5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine), not to exceed 300 mg (without epinephrine) or 500 mg (with epinephrine).
Dose Range: 0.5 - 7 mg

Condition-Specific Dosing:

infiltration: 0.5% to 1% solution, up to 4.5 mg/kg (max 300 mg)
peripheralNerveBlock: 1% to 2% solution, up to 4.5 mg/kg (max 300 mg)
epidural: 1% to 2% solution, up to 4.5 mg/kg (max 300 mg)
spinal: 0.5% to 5% solution (hyperbaric), dose varies by level of anesthesia required
antiarrhythmic_IV: Initial bolus 1-1.5 mg/kg, then 1-4 mg/min continuous infusion
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Pediatric Dosing

Neonatal: Not established for routine use; extreme caution if used. Max 2-4 mg/kg.
Infant: Max 3-5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine), not to exceed 300 mg. Use lowest effective concentration.
Child: Max 3-5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine), not to exceed 300 mg. Use lowest effective concentration.
Adolescent: Max 3-5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine), not to exceed 300 mg. Use lowest effective concentration.
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment for local anesthesia. For IV antiarrhythmic use, monitor for toxicity.
Moderate: No specific adjustment for local anesthesia. For IV antiarrhythmic use, monitor for toxicity.
Severe: No specific adjustment for local anesthesia. For IV antiarrhythmic use, consider dose reduction (e.g., 50%) and monitor for toxicity due to accumulation of metabolites.
Dialysis: Lidocaine is not significantly removed by hemodialysis. For IV antiarrhythmic use, consider dose reduction and monitor for toxicity.

Hepatic Impairment:

Mild: Consider dose reduction (e.g., 30-50%) for IV antiarrhythmic use. For local anesthesia, use lowest effective dose.
Moderate: Significant dose reduction (e.g., 50-75%) for IV antiarrhythmic use. For local anesthesia, use lowest effective dose and monitor closely for toxicity.
Severe: Contraindicated or extreme caution with significant dose reduction (e.g., 75% or more) for IV antiarrhythmic use. For local anesthesia, use with extreme caution and significantly reduced doses.

Pharmacology

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Mechanism of Action

Lidocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action. It blocks voltage-gated sodium channels in the neuronal cell membrane, preventing depolarization and propagation of action potentials. As an antiarrhythmic, it suppresses automaticity and shortens the effective refractory period and action potential duration in the His-Purkinje system and ventricles.
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Pharmacokinetics

Absorption:

Bioavailability: Varies widely depending on site of administration (e.g., 3% after oral, 50-100% after IM, variable after local/regional).
Tmax: Varies (e.g., 5-15 minutes for infiltration, 60-90 minutes for epidural, 10-20 minutes for IM).
FoodEffect: Not applicable for injectable forms.

Distribution:

Vd: 1.1 L/kg (adults), 1.5-2.5 L/kg (neonates).
ProteinBinding: 60-80% (primarily to alpha-1-acid glycoprotein and albumin).
CnssPenetration: Yes

Elimination:

HalfLife: 1.5-2 hours (adults); prolonged in neonates, elderly, and patients with hepatic impairment.
Clearance: Approximately 10 mL/min/kg.
ExcretionRoute: Renal (primarily as metabolites).
Unchanged: Less than 10% (adults).
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Pharmacodynamics

OnsetOfAction: Rapid (2-5 minutes for infiltration, 5-15 minutes for nerve block).
PeakEffect: Varies with onset, typically within 10-30 minutes.
DurationOfAction: 1-3 hours (without epinephrine); 2-6 hours (with epinephrine).

Safety & Warnings

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BLACK BOX WARNING

Fatalities have been reported in children who have accidentally ingested or been exposed to excessive amounts of lidocaine topical preparations. Lidocaine injection is intended for administration by trained healthcare professionals. Accidental intravascular injection or systemic absorption of large doses can lead to serious adverse reactions, including cardiovascular collapse and central nervous system toxicity (e.g., seizures, respiratory arrest). Resuscitative equipment and drugs should be immediately available.
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Side Effects

Urgent Side Effects: Seek Medical Help Right Away

Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical attention immediately:

Signs of an allergic reaction:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
 Signs of methemoglobinemia (a rare but potentially life-threatening condition):
+ Blue or gray color of the lips, nails, or skin
+ Abnormal heartbeat
+ Seizures
+ Severe dizziness or fainting
+ Severe headache
+ Excessive sleepiness
+ Feeling tired or weak
+ Shortness of breath
Signs of too much acid in the blood (acidosis):
+ Confusion
+ Rapid breathing
+ Rapid heartbeat
+ Abnormal heartbeat
+ Severe stomach pain, nausea, or vomiting
+ Excessive sleepiness
+ Shortness of breath
+ Feeling tired or weak
 Other severe side effects:
+ Trouble breathing, slow breathing, or shallow breathing
+ Feeling lightheaded, sleepy, confused, or having blurred vision
+ Slow heartbeat
+ Feeling nervous and excitable
+ Trouble speaking
+ Burning, numbness, or tingling sensation
+ Restlessness
+ Anxiety
+ Changes in vision
+ Ringing in the ears
+ Dizziness or fainting
+ Severe headache
+ Twitching
+ Shakiness
+ Seizures
+ Feeling hot or cold
+ Metallic taste
+ Chest pain
+ Mood changes

Additional Side Effects of Spinal Injection

If you receive this medication via spinal injection, you may also experience:

Erectile dysfunction
 Loss of motor function
Loss of bowel or bladder control
 Difficulty urinating

Other Possible Side Effects

Like all medications, this drug can cause side effects, although not everyone will experience them. If you have any side effects that bother you or do not go away, contact your doctor for advice. Some common side effects may include:

Mild allergic reactions
 Gastrointestinal symptoms
Fatigue
 Dizziness
* Headache

Reporting Side Effects

If you experience any side effects, you can report them to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch. You can also contact your doctor for guidance on managing side effects.
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Seek Immediate Medical Attention If You Experience:

  • Dizziness or lightheadedness
  • Ringing in the ears (tinnitus)
  • Numbness or tingling around the mouth (perioral numbness)
  • Metallic taste in the mouth
  • Slurred speech
  • Confusion or drowsiness
  • Muscle twitching or tremors
  • Seizures
  • Slow heartbeat or feeling faint
  • Difficulty breathing
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

To ensure safe treatment, inform your doctor of the following:

Any allergies you have to this medication, its components, or other substances, including foods and drugs. Describe the allergic reactions you experienced.
 If you are scheduled to receive this medication via spinal injection, tell your doctor if you have:
+ Heart block
+ Severe bleeding
+ Severe infection
+ An infection at the injection site

It is crucial to disclose all your health conditions and medications to your doctor and pharmacist, including:
Prescription and over-the-counter (OTC) medications
 Natural products
* Vitamins

This will help determine if it is safe to take this medication with your existing treatments and health conditions. Never start, stop, or adjust the dosage of any medication without consulting your doctor first.
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Precautions & Cautions

Important Warnings and Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.

Risk of Methemoglobinemia
A severe blood disorder called methemoglobinemia has been associated with drugs like this one. Your risk may be increased if you have:
Glucose-6-phosphate dehydrogenase (G6PD) deficiency
 Heart problems
Lung problems
 Are taking certain other medications
* Are an infant younger than 6 months of age
If you have a history of methemoglobinemia, notify your doctor.

Sulfite Allergy
If you are allergic to sulfites, consult your doctor, as some products may contain sulfites.

Post-Treatment Precautions
Avoid driving and engaging in activities that require alertness until the effects of this medication have worn off and you feel fully awake. If you are discharged before the numbness has resolved, protect the treated area from injury until sensation returns.

Special Considerations
If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects. Similarly, if the patient is a child, use this medication with caution, as the risk of certain side effects may be higher in children.

Pregnancy and Breastfeeding
If you are pregnant, plan to become pregnant, or are breastfeeding, discuss the benefits and risks of this medication with your doctor.

Spinal Injection
If this medication is administered into the spine, you may experience temporary loss of feeling and motor function in the lower half of your body. Do not attempt to get out of bed or perform other activities until normal sensation and motor function have returned.

Mouth and Dental Procedures
Do not eat while your mouth feels numb, as you may accidentally bite your tongue.
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Overdose Information

Overdose Symptoms:

  • Severe dizziness or lightheadedness
  • Profound drowsiness or loss of consciousness
  • Seizures
  • Respiratory arrest (stopping breathing)
  • Severe low blood pressure
  • Slow heart rate (bradycardia)
  • Cardiac arrest

What to Do:

Seek immediate medical attention. Call 911 or your local emergency number. For non-emergencies, call Poison Control at 1-800-222-1222.

Drug Interactions

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Major Interactions

  • Class I Antiarrhythmics (e.g., procainamide, quinidine, disopyramide): Increased risk of cardiac depression and arrhythmias.
  • Class III Antiarrhythmics (e.g., amiodarone, sotalol): Increased risk of cardiac depression and arrhythmias.
  • Beta-blockers (e.g., propranolol, metoprolol): May decrease hepatic clearance of lidocaine, leading to increased lidocaine levels and toxicity.
  • Cimetidine: May decrease hepatic clearance of lidocaine, leading to increased lidocaine levels and toxicity.
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Moderate Interactions

  • Phenytoin: May alter lidocaine metabolism.
  • Succinylcholine: May prolong neuromuscular blockade.
  • MAOIs, TCAs, Phenothiazines (if lidocaine contains epinephrine): Risk of severe hypertension and arrhythmias.
  • Other local anesthetics: Additive systemic toxicity.
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Minor Interactions

  • Digoxin: Possible additive bradycardia.

Monitoring

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Baseline Monitoring

Allergy history

Rationale: To identify hypersensitivity reactions.

Timing: Prior to administration

Vital signs (HR, BP, RR)

Rationale: To establish baseline and detect early signs of systemic toxicity.

Timing: Prior to administration

Cardiac rhythm (ECG)

Rationale: Essential for IV antiarrhythmic use; useful for high-dose local/regional blocks to detect cardiac toxicity.

Timing: Prior to administration (if indicated)

Renal and Hepatic function tests

Rationale: To assess organ function, especially in patients receiving IV infusions or with pre-existing impairment, as metabolism and excretion are affected.

Timing: Prior to administration (if indicated)

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Routine Monitoring

Vital signs (HR, BP, RR)

Frequency: Every 5-15 minutes during and immediately after administration, then as clinically indicated.

Target: Within patient's normal limits.

Action Threshold: Significant deviations (e.g., bradycardia, hypotension, respiratory depression) require immediate intervention.

Level of consciousness/CNS status

Frequency: Continuously during and after administration.

Target: Alert and oriented.

Action Threshold: Signs of CNS toxicity (e.g., dizziness, tinnitus, perioral numbness, confusion, seizures) require immediate intervention.

Cardiac rhythm (ECG)

Frequency: Continuous monitoring for IV antiarrhythmic use; intermittent for high-dose local/regional blocks.

Target: Normal sinus rhythm or controlled arrhythmia.

Action Threshold: Arrhythmias, QRS widening, PR prolongation, or other conduction disturbances.

Injection site

Frequency: Visually inspect during and after administration.

Target: No signs of hematoma, infection, or excessive swelling.

Action Threshold: Signs of complications (e.g., hematoma, infection, nerve damage symptoms).

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Symptom Monitoring

  • Lightheadedness
  • Dizziness
  • Tinnitus
  • Perioral numbness
  • Metallic taste
  • Slurred speech
  • Drowsiness
  • Confusion
  • Muscle twitching
  • Tremors
  • Seizures
  • Bradycardia
  • Hypotension
  • Cardiac arrest
  • Respiratory depression

Special Patient Groups

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Pregnancy

Lidocaine is classified as Pregnancy Category B. Studies in animals have not shown harm to the fetus, and there are no adequate and well-controlled studies in pregnant women. It is generally considered safe for use as a local anesthetic during pregnancy when administered appropriately and at the lowest effective dose. It crosses the placenta.

Trimester-Specific Risks:

First Trimester: Generally considered low risk; use only if clearly needed.
Second Trimester: Generally considered safe for local anesthesia.
Third Trimester: Generally considered safe for local anesthesia, commonly used in labor and delivery (e.g., epidural, pudendal block). Monitor for fetal bradycardia.
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Lactation

Lidocaine is excreted into breast milk in small amounts. The amount ingested by the infant is typically very low and unlikely to cause adverse effects. It is considered compatible with breastfeeding (Lactation Risk Category L2).

Infant Risk: Low risk of adverse effects to the breastfed infant. Monitor for drowsiness or feeding difficulties, though unlikely.
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Pediatric Use

Children, especially infants and neonates, are more susceptible to systemic toxicity due to differences in metabolism, distribution, and a higher ratio of surface area to weight. Dosing must be carefully calculated based on weight, and the lowest effective concentration and volume should be used. Close monitoring for signs of CNS and cardiovascular toxicity is crucial.

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Geriatric Use

Elderly patients may have reduced hepatic blood flow, decreased plasma protein binding, and impaired renal function, leading to decreased clearance and increased plasma concentrations of lidocaine and its metabolites. This increases the risk of systemic toxicity. Lower doses and slower administration rates may be necessary. Monitor closely for CNS and cardiovascular adverse effects.

Clinical Information

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Clinical Pearls

  • Always aspirate prior to injection to avoid inadvertent intravascular administration, which can lead to rapid systemic toxicity.
  • Use the lowest effective concentration and volume of lidocaine to achieve the desired anesthetic effect.
  • The addition of epinephrine prolongs the duration of action and reduces systemic absorption, but should not be used in areas with end-arterial circulation (e.g., fingers, toes, nose, penis, ears) due to risk of ischemia.
  • Be vigilant for early signs of CNS toxicity (e.g., perioral numbness, tinnitus, metallic taste, dizziness) as these often precede more severe symptoms like seizures.
  • Lipid emulsion therapy (Intralipid) is the antidote for severe local anesthetic systemic toxicity (LAST) and should be readily available in settings where large volumes or high concentrations of local anesthetics are used.
  • For antiarrhythmic use, monitor ECG continuously and adjust infusion rate based on patient response and plasma levels if available.
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Alternative Therapies

  • Other local anesthetics (e.g., Bupivacaine, Ropivacaine, Mepivacaine, Prilocaine, Chloroprocaine)
  • General anesthesia (for procedures requiring complete unconsciousness)
  • Non-pharmacological pain management techniques (e.g., distraction, cognitive behavioral therapy)
  • Other antiarrhythmics (e.g., procainamide, amiodarone, sotalol for ventricular arrhythmias)
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Cost & Coverage

Average Cost: Low to moderate per 50ml vial
Generic Available: Yes
Insurance Coverage: Tier 1 (Generic)
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General Drug Facts

If your symptoms or health problems persist or worsen, it is essential to contact your doctor for further guidance. To ensure safe use, never share your medication with others, and do not take medication prescribed for someone else. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion. Dispose of unused or expired medications properly. Unless instructed to do so by a healthcare professional, do not flush medications down the toilet or pour them down the drain. If you are unsure about the proper disposal method, consult your pharmacist, who can also inform you about potential drug take-back programs in your area. Some medications may come with an additional patient information leaflet, which your pharmacist can provide. If you have any questions or concerns about your medication, discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately contact your local poison control center or seek emergency medical attention. Be prepared to provide information about the medication taken, the amount, and the time of ingestion.