Lidocaine 1% Inj, 5ml

Manufacturer HOSPIRA Active Ingredient Lidocaine IV Solution(LYE doe kane) Pronunciation LYE doe kane
It is used to treat certain types of abnormal heartbeats.It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Antiarrhythmic, Local Anesthetic
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Pharmacologic Class
Class IB Antiarrhythmic; Voltage-gated Sodium Channel Blocker
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Pregnancy Category
Category B
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FDA Approved
Jun 1948
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Lidocaine is a medication given by injection, often into a vein, to help control certain types of irregular heartbeats (arrhythmias). It works by calming overactive electrical signals in the heart. It can also be used to numb areas of the body for pain relief, but this specific formulation is for IV use.
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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 adhere to all guidelines provided. This drug is administered intravenously over a specified period.

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

In the event that you miss a dose, contact your doctor promptly to receive guidance on the appropriate course of action.
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Lifestyle & Tips

  • Report any unusual symptoms immediately to your healthcare provider.
  • Avoid alcohol and other CNS depressants if possible, as they may worsen side effects.
  • Follow all instructions from your healthcare provider regarding activity and diet.

Dosing & Administration

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Adult Dosing

Standard Dose: Ventricular Arrhythmias: Initial bolus 1-1.5 mg/kg IV, followed by continuous infusion 1-4 mg/min.
Dose Range: 1 - 4 mg

Condition-Specific Dosing:

Ventricular Arrhythmias (Loading Dose): 1-1.5 mg/kg IV bolus, may repeat 0.5-0.75 mg/kg every 5-10 minutes up to a total of 3 mg/kg.
Ventricular Arrhythmias (Maintenance Infusion): 1-4 mg/min (20-50 mcg/kg/min) IV continuous infusion.
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Pediatric Dosing

Neonatal: Ventricular Arrhythmias: Loading dose 1 mg/kg IV bolus, then 20-50 mcg/kg/min IV continuous infusion. Use with caution.
Infant: Ventricular Arrhythmias: Loading dose 1 mg/kg IV bolus, then 20-50 mcg/kg/min IV continuous infusion.
Child: Ventricular Arrhythmias: Loading dose 1 mg/kg IV bolus, then 20-50 mcg/kg/min IV continuous infusion.
Adolescent: Ventricular Arrhythmias: Loading dose 1 mg/kg IV bolus, then 20-50 mcg/kg/min IV continuous infusion.
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment required, monitor for toxicity.
Moderate: No specific adjustment required, monitor for toxicity.
Severe: No specific adjustment required, monitor for toxicity, especially with prolonged infusions due to accumulation of active metabolites.
Dialysis: Lidocaine is not significantly removed by hemodialysis. Monitor for toxicity.

Hepatic Impairment:

Mild: Consider 25-50% dose reduction for maintenance infusion.
Moderate: Consider 50% dose reduction for maintenance infusion.
Severe: Consider 50% or greater dose reduction for maintenance infusion. Avoid bolus doses if possible. Monitor plasma concentrations.

Pharmacology

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Mechanism of Action

Lidocaine is a Class IB antiarrhythmic that acts by blocking voltage-gated sodium channels in the cardiac cell membrane. This action decreases the rate of phase 0 depolarization, reduces automaticity, and shortens the effective refractory period and action potential duration in the His-Purkinje system and ventricular muscle. It also raises the ventricular fibrillation threshold. As a local anesthetic, it stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action.
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Pharmacokinetics

Absorption:

Bioavailability: 100% (IV)
Tmax: Immediate (IV)
FoodEffect: Not applicable (IV)

Distribution:

Vd: 0.7-2.7 L/kg (increases in CHF, liver disease)
ProteinBinding: 60-80% (primarily to alpha-1-acid glycoprotein)
CnssPenetration: Yes

Elimination:

HalfLife: 1.5-2 hours (prolonged in CHF, liver disease)
Clearance: 10-20 mL/min/kg
ExcretionRoute: Renal (primarily as metabolites)
Unchanged: Less than 10%
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Pharmacodynamics

OnsetOfAction: Within 1-2 minutes (IV)
PeakEffect: Within 5-10 minutes (IV)
DurationOfAction: 10-20 minutes (after bolus, due to rapid redistribution); sustained with continuous infusion

Safety & Warnings

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Side Effects

Urgent Side Effects: Seek Medical Help Right Away

While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:

Signs of an allergic reaction, such as:
+ 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 deadly condition, including:
+ Blue or gray discoloration 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 acidosis (too much acid in the blood), such as:
+ 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, including:
+ Trouble breathing, slow breathing, or shallow breathing
+ Feeling lightheaded, sleepy, confused, or experiencing blurred vision
+ Slow heartbeat
+ Feeling nervous or excitable
+ Difficulty speaking
+ Burning, numbness, or tingling sensations
+ 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

Other Possible Side Effects

Like all medications, this drug can cause side effects. However, many people may not experience any side effects or may only have mild ones. If you notice any side effects that bother you or do not go away, contact your doctor or seek medical attention. This is not an exhaustive list of possible side effects. If you have questions or concerns, talk to your doctor.

Reporting Side Effects

You can report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch. Your doctor can also provide guidance on managing side effects and offer medical advice.
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Seek Immediate Medical Attention If You Experience:

  • Dizziness or lightheadedness
  • Numbness or tingling sensations (especially around the mouth)
  • Tremors or muscle twitching
  • Slurred speech
  • Confusion or unusual drowsiness
  • Blurred vision or ringing in the ears (tinnitus)
  • Seizures
  • Slow or irregular heartbeat
  • Difficulty breathing
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Before Using This Medicine

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

It is essential to inform your doctor about the following:

Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
Certain heart conditions, including heart block, Stokes-Adams syndrome, or Wolff-Parkinson-White syndrome.

This list is not exhaustive, and it is crucial to discuss all your health problems and medications with your doctor.

To ensure your safety, provide your doctor and pharmacist with a comprehensive list of:

All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
* Your health problems, including any medical conditions or allergies

Before making any changes to your medication regimen, including starting, stopping, or adjusting the dose of any medication, consult with your doctor to confirm it is safe to do so.
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Precautions & Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. As directed by your doctor, regularly have your blood work checked and an electrocardiogram (ECG) performed to monitor your heart rhythm.

There is a risk of developing a severe blood disorder called methemoglobinemia associated with this type of medication. Certain factors may increase this risk, including having glucose-6-phosphate dehydrogenase (G6PD) deficiency, pre-existing heart or lung problems, taking specific other medications, or being an infant under 6 months of age. If you have a history of methemoglobinemia, notify your doctor.

If you are 65 years or older, exercise caution when using this medication, as you may be more susceptible to experiencing side effects. Similarly, when administering this drug to children, use it with caution, as they may have a higher risk of developing certain side effects.

Before taking this medication, inform your doctor if you are pregnant, planning to become pregnant, or are breastfeeding. It is crucial to discuss the potential benefits and risks of this medication to both you and your baby.
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Overdose Information

Overdose Symptoms:

  • Severe dizziness or fainting
  • Seizures
  • Respiratory depression or arrest
  • Profound hypotension
  • Bradycardia
  • Asystole or ventricular fibrillation
  • Coma

What to Do:

Seek immediate medical attention. Call 911 or Poison Control (1-800-222-1222). Treatment involves supportive care, maintaining airway, breathing, and circulation, managing seizures (e.g., with benzodiazepines), and treating arrhythmias/hypotension. Lipid emulsion therapy may be considered for severe systemic toxicity.

Drug Interactions

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Major Interactions

  • Amiodarone (increased lidocaine levels, increased risk of CNS/cardiac toxicity)
  • Beta-blockers (e.g., Propranolol, Metoprolol - decreased lidocaine clearance, increased toxicity)
  • Cimetidine (decreased lidocaine clearance, increased toxicity)
  • Class I Antiarrhythmics (additive cardiac effects, increased risk of arrhythmias)
  • Phenytoin (increased lidocaine clearance, decreased lidocaine effect; also increased phenytoin levels)
  • Procainamide (additive cardiac effects, increased risk of arrhythmias)
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Moderate Interactions

  • Anticonvulsants (e.g., Carbamazepine, Phenobarbital - may increase lidocaine clearance)
  • Diltiazem, Verapamil (may decrease lidocaine clearance)
  • Erythromycin (may increase lidocaine levels)
  • Rifampin (may decrease lidocaine levels)
  • Succinylcholine (prolonged neuromuscular blockade)
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Minor Interactions

  • Not available

Monitoring

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Baseline Monitoring

ECG (12-lead)

Rationale: To assess baseline cardiac rhythm and conduction, identify pre-existing abnormalities.

Timing: Prior to initiation of therapy

Blood Pressure, Heart Rate

Rationale: To establish baseline hemodynamic status.

Timing: Prior to initiation of therapy

Liver Function Tests (LFTs)

Rationale: Lidocaine is primarily metabolized by the liver; impaired function can lead to accumulation.

Timing: Prior to initiation, especially in patients with suspected hepatic impairment

Renal Function Tests (RFTs)

Rationale: Metabolites are renally excreted; severe impairment can lead to metabolite accumulation.

Timing: Prior to initiation, especially in patients with suspected renal impairment

Electrolytes (Potassium, Magnesium)

Rationale: Imbalances can affect lidocaine efficacy and arrhythmogenic potential.

Timing: Prior to initiation

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Routine Monitoring

ECG (continuous monitoring)

Frequency: Continuously during infusion

Target: Normal sinus rhythm or controlled arrhythmia

Action Threshold: Worsening of arrhythmia, new arrhythmias, QRS widening (>25% of baseline), PR prolongation, or QT prolongation. Bradycardia or AV block.

Blood Pressure, Heart Rate

Frequency: Every 5-15 minutes during bolus/initiation, then hourly or as clinically indicated during infusion

Target: Within patient's normal range

Action Threshold: Significant hypotension, bradycardia, or tachycardia.

Neurological Status (mental status, seizures)

Frequency: Continuously, especially during initiation and dose changes

Target: Alert and oriented, no seizures

Action Threshold: Drowsiness, confusion, paresthesias, tremors, slurred speech, seizures.

Lidocaine Plasma Levels (therapeutic range: 1.5-5 mcg/mL)

Frequency: As clinically indicated, especially in patients with hepatic/renal impairment, CHF, or suspected toxicity/inefficacy.

Target: 1.5-5 mcg/mL

Action Threshold: Levels > 5 mcg/mL (increased risk of CNS toxicity); levels > 9 mcg/mL (increased risk of cardiovascular toxicity).

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Symptom Monitoring

  • Dizziness
  • Lightheadedness
  • Paresthesias (numbness, tingling)
  • Tremors
  • Slurred speech
  • Confusion
  • Drowsiness
  • Seizures
  • Blurred vision
  • Tinnitus
  • Bradycardia
  • Hypotension
  • Cardiac arrest

Special Patient Groups

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Pregnancy

Category B. Studies in animals have not shown harm to the fetus, but there are no adequate and well-controlled studies in pregnant women. Use only if clearly needed.

Trimester-Specific Risks:

First Trimester: Generally considered low risk, but use only if benefits outweigh risks.
Second Trimester: Generally considered low risk, but use only if benefits outweigh risks.
Third Trimester: Generally considered low risk, but use only if benefits outweigh risks. May cross the placenta and cause fetal bradycardia or CNS depression in the neonate if used in high doses near term.
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Lactation

Lidocaine is excreted into breast milk in small amounts. The amount ingested by the infant is generally considered too small to cause adverse effects. L2 (Safer). Monitor infant for drowsiness or feeding difficulties.

Infant Risk: Low risk of adverse effects in breastfed infants.
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Pediatric Use

Use with caution. Pediatric patients, especially neonates and infants, may be more susceptible to systemic toxicity due to differences in metabolism and distribution. Dosing must be carefully calculated based on weight. Close monitoring for CNS and cardiovascular effects is crucial.

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Geriatric Use

Elderly patients may have reduced hepatic blood flow and metabolism, leading to increased plasma concentrations and increased risk of toxicity. Lower doses and slower infusion rates may be necessary. Monitor closely for CNS and cardiovascular adverse effects.

Clinical Information

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Clinical Pearls

  • Lidocaine is primarily used for acute management of ventricular arrhythmias, especially post-MI or during cardiac procedures.
  • Always administer IV bolus slowly (over 2-3 minutes) to minimize adverse effects.
  • Monitor ECG continuously for signs of toxicity (e.g., QRS widening, PR prolongation, bradycardia, AV block).
  • CNS toxicity (e.g., tremors, seizures) often precedes cardiovascular toxicity (e.g., hypotension, bradycardia), serving as an early warning sign.
  • Dose adjustments are critical in patients with heart failure, liver disease, or advanced age due to altered pharmacokinetics.
  • Ensure adequate oxygenation and ventilation, as hypoxia and acidosis can worsen lidocaine toxicity.
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Alternative Therapies

  • Amiodarone (for ventricular arrhythmias)
  • Procainamide (for ventricular arrhythmias)
  • Magnesium sulfate (for Torsades de Pointes)
  • Beta-blockers (e.g., Esmolol, Metoprolol for rate control or certain arrhythmias)
  • Other Class I antiarrhythmics (e.g., Mexiletine, Flecainide, Propafenone - generally not first-line for acute IV use like lidocaine)
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Cost & Coverage

Average Cost: Varies widely based on concentration, volume, and supplier per 5ml vial
Generic Available: Yes
Insurance Coverage: Generally covered by most insurance plans as a generic medication, often Tier 1 or 2.
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General Drug Facts

If your symptoms or health problems persist or worsen, it is essential to contact your doctor promptly. 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; do not flush them down the toilet or pour them down the drain unless instructed to do so by a healthcare professional. If you are unsure about the correct 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 to ensure prompt and effective treatment.