Lidocaine 1% Inj, 10ml

Manufacturer FRESENIUS KABI 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 medicine used to numb a specific area of your body. It works by temporarily blocking nerve signals, so you don't feel pain during medical procedures like stitches, minor surgery, or dental work.
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How to Use This Medicine

To use this medication correctly, follow your doctor's instructions and read all the information provided. It is essential to follow the dosage instructions carefully. 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 next steps to take.
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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.
  • Inform your healthcare provider about any allergies, especially to local anesthetics.
  • Avoid eating or drinking until the numbness wears off if the injection was in or around the mouth/throat, to prevent choking or biting your tongue/cheek.
  • Follow post-procedure instructions carefully, as the numbed area may be more prone to injury.

Dosing & Administration

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Adult Dosing

Standard Dose: Varies significantly based on procedure, site, and patient factors. Max single dose for infiltration/nerve block without epinephrine: 4.5 mg/kg (not to exceed 300 mg). With epinephrine: 7 mg/kg (not to exceed 500 mg).

Condition-Specific Dosing:

infiltration: 0.5% to 1% solution, 2-50 mL (max 300 mg without epi, 500 mg with epi)
peripheralNerveBlock: 1% to 2% solution, 5-60 mL (max 300 mg without epi, 500 mg with epi)
epidural: 1% to 2% solution, 10-20 mL (max 300 mg without epi, 500 mg with epi)
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Pediatric Dosing

Neonatal: Not established for routine use; use with extreme caution. Max single dose: 2-4 mg/kg.
Infant: Max single dose: 2-4 mg/kg (not to exceed 4.5 mg/kg).
Child: Max single dose: 2-4 mg/kg (not to exceed 4.5 mg/kg).
Adolescent: Max single dose: 2-4 mg/kg (not to exceed 4.5 mg/kg).
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Dose Adjustments

Renal Impairment:

Mild: No specific dose adjustment typically required, but monitor for toxicity.
Moderate: No specific dose adjustment typically required, but monitor for toxicity.
Severe: No specific dose adjustment typically required, but monitor for toxicity.
Dialysis: Lidocaine is not significantly removed by hemodialysis. Monitor for toxicity.

Hepatic Impairment:

Mild: Consider dose reduction and monitor for toxicity.
Moderate: Reduce dose by 50% or more; monitor plasma concentrations if possible.
Severe: Reduce dose significantly (e.g., 75% or more); monitor plasma concentrations if possible.

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 blocking nerve impulse conduction. It primarily acts by blocking voltage-gated sodium channels in the neuronal cell membrane.
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Pharmacokinetics

Absorption:

Bioavailability: Varies significantly based on site of administration (e.g., highly vascularized areas lead to faster absorption), presence of vasoconstrictor (e.g., epinephrine), and dose.
Tmax: Varies (e.g., 5-15 minutes for intercostal block, 60-90 minutes for brachial plexus block).
FoodEffect: Not applicable for injectable formulation.

Distribution:

Vd: 0.7-2.7 L/kg (average 1.1 L/kg)
ProteinBinding: 60-80% (primarily to alpha-1-acid glycoprotein and albumin)
CnssPenetration: Yes

Elimination:

HalfLife: 1.5-2 hours (prolonged in hepatic impairment, heart failure, and in neonates)
Clearance: Approximately 10 mL/min/kg
ExcretionRoute: Renal (less than 10% as unchanged drug)
Unchanged: Less than 10%
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Pharmacodynamics

OnsetOfAction: 2-5 minutes (infiltration, nerve block)
PeakEffect: Varies with site and dose, typically within 5-15 minutes for local anesthesia.
DurationOfAction: 30-60 minutes (without epinephrine); 60-120 minutes (with epinephrine)

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; an 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.
Central Nervous System Effects: Feeling lightheaded, sleepy, confused, or experiencing blurred vision.
Cardiovascular Effects: Slow heartbeat.
Neurological Effects: 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, seizures, feeling hot or cold, metallic taste, chest pain, or mood changes.

Additional Side Effects of Spinal Injection: If this medication is administered into the spine, you may experience:
Erectile dysfunction
Loss of motor function
Loss of bowel or bladder control
Urinary retention

Other Side Effects

As with any medication, you may experience side effects. While many people do not experience any side effects or only minor ones, it is essential to contact your doctor or seek medical help if you notice any side effects that bother you or persist.

Reporting Side Effects

If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Dizziness or lightheadedness
  • Ringing in your ears (tinnitus)
  • Numbness or tingling around your mouth
  • Unusual anxiety or restlessness
  • Blurred or double vision
  • Tremors or muscle twitching
  • Feeling unusually sleepy or confused
  • Slow or irregular heartbeat
  • Difficulty breathing
  • 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 of the following:

Any allergies you have to this medication, its components, or other substances, including foods and drugs. Describe the allergic reaction you experienced, such as symptoms and signs.
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 health conditions and other drugs. Never start, stop, or adjust the dose of any medication without consulting your doctor first.
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Precautions & Cautions

Important Warnings and Cautions

Before taking this medication, inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are using this drug.

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 before using this medication, as some products may contain sulfites.

Caution with Daily Activities
Avoid driving and other 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, 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.
- If you are pregnant, plan to become pregnant, or are breastfeeding, discuss the benefits and risks with your doctor.

Spinal Injection
If this medication is administered into the spine, it 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 while your mouth is numb, as you may accidentally bite your tongue.
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Overdose Information

Overdose Symptoms:

  • Severe dizziness or lightheadedness
  • Profound drowsiness or unconsciousness
  • Seizures
  • Difficulty breathing or respiratory arrest
  • Severe low blood pressure (hypotension)
  • Slow heart rate (bradycardia)
  • Irregular heartbeats (arrhythmias)
  • Cardiac arrest

What to Do:

If you experience any of these severe symptoms, 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

  • Antiarrhythmics (e.g., Class I antiarrhythmics like mexiletine, procainamide): Increased risk of cardiac depression and CNS effects.
  • 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.
  • Amiodarone: Increased risk of cardiac depression and CNS effects.
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Moderate Interactions

  • Succinylcholine: Lidocaine may prolong the neuromuscular blockade.
  • Phenytoin: May increase lidocaine metabolism, but also increased risk of cardiac depression.
  • CYP1A2 inhibitors (e.g., fluvoxamine, ciprofloxacin): May increase lidocaine levels.
  • CYP3A4 inhibitors (e.g., ketoconazole, erythromycin): May increase lidocaine levels.
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Minor Interactions

  • Not available

Monitoring

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Baseline Monitoring

Allergy history

Rationale: To identify hypersensitivity reactions.

Timing: Prior to administration

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

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

Timing: Prior to administration

Site of injection assessment

Rationale: To ensure appropriate site and technique, and identify potential contraindications (e.g., infection).

Timing: Prior to administration

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Routine Monitoring

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

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

Target: Within patient's normal range; significant deviations may indicate systemic toxicity.

Action Threshold: Bradycardia, hypotension, respiratory depression, or significant changes from baseline.

Neurological status (CNS toxicity)

Frequency: Continuously during and immediately after administration.

Target: Normal mental status, no signs of CNS excitation or depression.

Action Threshold: Dizziness, tinnitus, perioral numbness, metallic taste, blurred vision, tremors, muscle twitching, anxiety, drowsiness, seizures.

Cardiac rhythm (ECG)

Frequency: Continuous monitoring during high-risk procedures or with large doses.

Target: Normal sinus rhythm; no arrhythmias.

Action Threshold: Bradycardia, heart block, ventricular arrhythmias, cardiac arrest.

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Symptom Monitoring

  • Lightheadedness
  • Dizziness
  • Tinnitus (ringing in ears)
  • Perioral numbness (numbness around the mouth)
  • Metallic taste
  • Blurred vision
  • Tremors
  • Muscle twitching
  • Anxiety
  • Restlessness
  • Drowsiness
  • Slurred speech
  • Nausea/vomiting
  • Bradycardia
  • Hypotension
  • Seizures
  • Respiratory depression or arrest
  • Cardiac arrest

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 clinically indicated and used at the lowest effective dose.

Trimester-Specific Risks:

First Trimester: Generally considered low risk; use only if clearly needed.
Second Trimester: Generally considered low risk; use only if clearly needed.
Third Trimester: Generally considered low risk; use only if clearly needed. Can cross the placenta and may cause fetal bradycardia or CNS depression if high maternal levels occur.
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Lactation

Lidocaine is excreted into breast milk in small amounts. The amount transferred to the infant is generally considered too small to cause adverse effects. It is rated L2 (Likely Compatible) by LactMed. Breastfeeding can usually continue after local anesthetic use.

Infant Risk: Low risk of adverse effects to the breastfed infant.
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Pediatric Use

Pediatric patients, especially infants and young children, are more susceptible to systemic toxicity due to differences in metabolism, distribution, and higher relative doses per body weight. Dosing must be carefully calculated based on weight, and the lowest effective dose should be used. Close monitoring for signs of systemic toxicity is crucial.

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Geriatric Use

Elderly patients may have reduced hepatic blood flow and metabolic capacity, leading to decreased clearance and increased plasma concentrations of lidocaine. Lower doses may be required, and careful monitoring for systemic toxicity is recommended.

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 to achieve the desired anesthetic effect.
  • The addition of epinephrine (vasoconstrictor) prolongs the duration of action and reduces systemic absorption, thereby decreasing the risk of systemic toxicity, but should not be used in areas with end-arterial supply (e.g., fingers, toes, nose, penis, earlobe) due to risk of ischemia.
  • Monitor patients closely for signs of CNS and cardiovascular toxicity, especially after large doses or in patients with underlying cardiac or hepatic conditions.
  • Be aware of the potential for methemoglobinemia, especially with high doses or prolonged exposure, though this is more commonly associated with topical lidocaine or other local anesthetics like prilocaine.
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Alternative Therapies

  • Bupivacaine (longer acting local anesthetic)
  • Mepivacaine (similar onset and duration to lidocaine)
  • Ropivacaine (similar to bupivacaine, less cardiotoxic)
  • Procaine (ester-type local anesthetic, shorter duration)
  • Chloroprocaine (ester-type local anesthetic, very short duration)
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Cost & Coverage

Average Cost: Varies widely by manufacturer, quantity, and specific formulation (e.g., with/without epinephrine). per 10ml vial
Generic Available: Yes
Insurance Coverage: Generally covered by most insurance plans as a generic medication, typically 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 for further evaluation and 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 drain. If you are unsure about the correct disposal method, consult your pharmacist for guidance. Many communities have drug take-back programs, which your pharmacist can help you locate. Some medications may come with an additional patient information leaflet; check with your pharmacist to see if this applies to your prescription. 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 call your local poison control center or seek emergency medical attention. Be prepared to provide information about the medication taken, the amount, and the time it was taken, as this will aid in providing appropriate treatment.