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Lidocaine 1% 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, preventing you from feeling pain during medical procedures. It works by temporarily blocking nerve signals in that area.
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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 medication 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 procedure.

In the event that 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 you are taking, including over-the-counter drugs, supplements, and herbal products.
  • Report any unusual symptoms or discomfort during or after the procedure, such as dizziness, ringing in the ears, numbness, or tingling.
  • Avoid eating or drinking until sensation returns to the treated area, especially if the mouth or throat was numbed, to prevent choking or biting your tongue/cheek.
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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 injection. For local infiltration: 0.5% to 1% solution. Max single dose: 4.5 mg/kg (not to exceed 300 mg) without epinephrine; 7 mg/kg (not to exceed 500 mg) with epinephrine.
Dose Range: 0.5 - 7 mg

Condition-Specific Dosing:

local_infiltration: Up to 4.5 mg/kg (300 mg total) without epinephrine; up to 7 mg/kg (500 mg total) with epinephrine.
peripheral_nerve_block: Varies by nerve, typically 1-2% solution, up to max dose.
epidural_anesthesia: Varies by segment, typically 1-2% solution, up to max dose.
intravenous_antiarrhythmic: Initial bolus 1-1.5 mg/kg, then infusion 1-4 mg/min (different formulation/concentration).
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Pediatric Dosing

Neonatal: Not established for routine use; use with extreme caution. Max 4.5 mg/kg.
Infant: Max single dose: 4.5 mg/kg (not to exceed 300 mg). Use lowest effective dose.
Child: Max single dose: 4.5 mg/kg (not to exceed 300 mg). Use lowest effective dose.
Adolescent: Max single dose: 4.5 mg/kg (not to exceed 300 mg). May follow adult dosing guidelines if weight appropriate.
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment needed.
Moderate: No specific adjustment needed.
Severe: No specific adjustment needed, but monitor for signs of toxicity due to potential accumulation of active metabolites.
Dialysis: Lidocaine is not significantly removed by hemodialysis. Monitor for toxicity.

Hepatic Impairment:

Mild: Consider dose reduction, monitor for toxicity.
Moderate: Reduce dose by 50% or more; monitor plasma levels if possible. Increased risk of toxicity.
Severe: Significant dose reduction required (e.g., 50-75%); avoid if possible. Increased risk of toxicity due to impaired metabolism.

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 exerting a local anesthetic action. It specifically blocks voltage-gated sodium channels, preventing the propagation of action potentials.
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Pharmacokinetics

Absorption:

Bioavailability: Highly variable depending on administration site (e.g., 35% oral, nearly 100% IV, variable for local infiltration based on vascularity and presence of vasoconstrictor).
Tmax: Varies by route: IV (minutes), local infiltration (5-15 minutes), epidural (10-20 minutes).
FoodEffect: Not applicable for injectable formulation.

Distribution:

Vd: 0.7-2.7 L/kg (average 1.1 L/kg). Rapidly distributes into highly perfused organs (brain, heart, kidneys, lungs) and then into skeletal muscle and adipose tissue.
ProteinBinding: 60-80% (primarily to alpha-1-acid glycoprotein and albumin). Binding is concentration-dependent and can be reduced in renal/hepatic impairment.
CnssPenetration: Yes, readily crosses the blood-brain barrier and placenta.

Elimination:

HalfLife: 1.5-2 hours (prolonged in patients with heart failure, liver disease, or renal impairment due to metabolite accumulation).
Clearance: Approximately 10 mL/min/kg.
ExcretionRoute: Renal (less than 10% as unchanged drug; metabolites excreted renally).
Unchanged: Less than 10%
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Pharmacodynamics

OnsetOfAction: Rapid, typically within 2-5 minutes for local infiltration.
PeakEffect: 5-15 minutes for local infiltration.
DurationOfAction: 0.5-3 hours, depending on dose, site of injection, and presence of vasoconstrictor (e.g., epinephrine prolongs duration).

Safety & Warnings

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Side Effects

Urgent Side Effects: Seek Medical Help Right Away

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

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, or swelling of the mouth, face, lips, tongue, or throat.
 Methemoglobinemia: A blue or gray color of the lips, nails, or skin, irregular heartbeat, seizures, severe dizziness or fainting, severe headache, excessive sleepiness, feeling tired or weak, or shortness of breath. This rare condition can be life-threatening if left untreated.
Acidosis (Too Much Acid in the Blood): Confusion, rapid breathing, rapid heartbeat, irregular heartbeat, severe stomach pain, nausea, vomiting, excessive sleepiness, shortness of breath, or feeling extremely tired or weak.
 Respiratory Problems: Trouble breathing, slow breathing, or shallow breathing.
Neurological Symptoms: Feeling lightheaded, sleepy, confused, or experiencing blurred vision.
 Cardiovascular Issues: Slow heartbeat.
Nervous System Symptoms: Feeling nervous and excitable, trouble speaking, burning, numbness, or tingling sensations, restlessness, anxiety, changes in vision, ringing in the ears, dizziness, or fainting.
 Severe Headache, Twitching, Shakiness, or Seizures.
Other Symptoms: Feeling extremely hot or cold, metallic taste, chest pain, or mood changes.

Additional Side Effects of Spinal Injection:

 Sexual Dysfunction: Difficulty getting or maintaining an erection.
Motor Function: Loss of movement or control over bowel or bladder function.
 Urinary Problems: Trouble urinating.

Other Possible Side Effects

As with any medication, you may experience side effects. While many people have no side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any side effects that bother you or persist, contact your doctor for guidance.

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 advice on managing side effects.
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Seek Immediate Medical Attention If You Experience:

  • Dizziness or lightheadedness
  • Numbness or tingling around the mouth
  • Ringing in the ears (tinnitus)
  • Blurred or double vision
  • Muscle twitching or tremors
  • Feeling unusually sleepy or confused
  • Difficulty breathing
  • Slow or irregular heartbeat
  • Seizures
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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 about the following:

Any allergies you have to this medication, its components, or other substances, including foods and drugs. Describe the allergic reaction you experienced, including any symptoms.
 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 essential 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 health conditions and other medications. 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.

Caution with Daily Activities
Avoid driving and engaging in activities that require alertness until the effects of this medication have worn off and you feel fully awake.

Post-Treatment Precautions
If you are discharged before the numbness has resolved, take precautions to protect the treated area from injury until you have regained sensation.

Special Considerations
- If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects.
- 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.

Injection into the Spine
This medication may cause 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 until the numbness in your mouth has resolved, as you may inadvertently bite your tongue.
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Overdose Information

Overdose Symptoms:

  • Severe CNS depression (drowsiness, confusion, coma)
  • Seizures
  • Respiratory depression or arrest
  • Profound hypotension
  • Bradycardia
  • Cardiac arrest
  • Metabolic acidosis

What to Do:

Immediate medical attention is required. Call 911 or your local emergency number. Management includes maintaining airway, breathing, and circulation; administering oxygen; managing seizures (e.g., with benzodiazepines); treating hypotension (e.g., with vasopressors); and managing arrhythmias. Lipid emulsion therapy may be considered for severe systemic toxicity.

Drug Interactions

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Major Interactions

  • Antiarrhythmics (Class I, III): Additive cardiac effects, increased risk of arrhythmias or conduction disturbances (e.g., amiodarone, procainamide, quinidine, flecainide).
  • Beta-blockers (e.g., propranolol, metoprolol): May decrease hepatic blood flow, reducing lidocaine clearance and increasing plasma levels, leading to toxicity.
  • Cimetidine: Inhibits lidocaine metabolism, increasing plasma levels and risk of toxicity.
  • Succinylcholine: Lidocaine may potentiate or prolong the neuromuscular blockade of succinylcholine.
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Moderate Interactions

  • Phenytoin: May increase lidocaine metabolism (CYP3A4 inducer), potentially reducing efficacy. Conversely, phenytoin can also increase lidocaine levels by displacing it from protein binding.
  • Other local anesthetics: Additive systemic toxicity.
  • MAOIs, TCAs (if lidocaine contains epinephrine): Risk of severe hypertension and arrhythmias.
  • Dopamine, Norepinephrine (if lidocaine contains epinephrine): Increased pressor effects.
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Minor Interactions

  • Alcohol: May alter hepatic metabolism.
  • Smoking: May induce CYP1A2, potentially increasing lidocaine clearance.

Monitoring

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Baseline Monitoring

Patient history (allergies, cardiac/hepatic/renal disease, current medications)

Rationale: To identify contraindications, risk factors for toxicity, and potential drug interactions.

Timing: Prior to administration

Vital signs (heart rate, blood pressure, respiratory rate)

Rationale: To establish baseline and monitor for systemic effects or adverse reactions.

Timing: Prior to administration

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Routine Monitoring

Signs and symptoms of systemic toxicity (CNS and cardiovascular)

Frequency: Continuously during and immediately after administration, then periodically as clinically indicated.

Target: Absence of symptoms (e.g., perioral numbness, dizziness, tinnitus, blurred vision, muscle twitching, seizures, bradycardia, hypotension).

Action Threshold: Any signs of toxicity warrant immediate cessation of administration and supportive care.

Vital signs (heart rate, blood pressure, respiratory rate)

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

Target: Within patient's normal range; stable.

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

ECG monitoring (if large doses or IV administration)

Frequency: Continuous during administration.

Target: Normal sinus rhythm, absence of conduction abnormalities.

Action Threshold: Arrhythmias, conduction blocks, or QRS widening.

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Symptom Monitoring

  • Lightheadedness
  • Dizziness
  • Tinnitus (ringing in ears)
  • Perioral numbness or tingling
  • Metallic taste
  • Blurred vision
  • Tremors or muscle twitching
  • Nausea/vomiting
  • Slurred speech
  • Drowsiness
  • Confusion
  • Seizures (severe toxicity)
  • Bradycardia
  • Hypotension
  • Cardiac arrest (severe toxicity)
  • Respiratory depression/arrest (severe toxicity)

Special Patient Groups

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Pregnancy

Category B. Studies in animals have not shown a risk to the fetus, but there are no adequate and well-controlled studies in pregnant women. Generally considered safe for use during pregnancy when clinically indicated and used at appropriate doses.

Trimester-Specific Risks:

First Trimester: Low risk, but use only if clearly needed.
Second Trimester: Low risk.
Third Trimester: Low risk; commonly used for epidural anesthesia during labor. 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 generally considered too small to cause adverse effects. L2 (Safer) rating by Hale's Lactation Risk Category.

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

Use with caution. Dosing must be carefully calculated based on weight (mg/kg) to avoid systemic toxicity. Children, especially younger ones, may be more susceptible to the toxic effects of lidocaine due to differences in metabolism and distribution. Avoid large volumes or high concentrations.

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Geriatric Use

Elderly patients may be more susceptible to the systemic toxic effects of lidocaine due to decreased hepatic function, reduced plasma protein binding, and altered body composition. Lower doses and slower administration rates may be necessary. Monitor closely for signs of toxicity.

Clinical Information

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Clinical Pearls

  • Always aspirate prior to injection to ensure the needle is not in a blood vessel, which can lead to rapid systemic absorption and toxicity.
  • Use the lowest effective dose and concentration to achieve the desired anesthetic effect.
  • The addition of epinephrine (vasoconstrictor) prolongs the duration of action and reduces systemic absorption, but should be avoided in areas with end-arterial circulation (e.g., fingers, toes, nose, penis, ears) due to risk of ischemia.
  • Monitor patients closely for signs of systemic toxicity, especially CNS (e.g., perioral numbness, dizziness, tinnitus, seizures) and cardiovascular (e.g., bradycardia, hypotension) effects.
  • Be aware of the maximum recommended doses for lidocaine, both with and without epinephrine, and do not exceed them.
  • In cases of severe systemic toxicity, particularly cardiovascular collapse, lipid emulsion therapy should be considered as an antidote.
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Alternative Therapies

  • Bupivacaine (longer duration of action, higher potency)
  • Ropivacaine (similar to bupivacaine, less cardiotoxic)
  • Mepivacaine (intermediate duration)
  • Prilocaine (intermediate duration, lower CNS toxicity, but risk of methemoglobinemia with high doses)
  • Chloroprocaine (short duration, ester-type local anesthetic)
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Cost & Coverage

Average Cost: Highly variable, typically low 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 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. Unless instructed otherwise, do not flush medications down the toilet or drain. 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 quantity, and the time of ingestion.