Lidocaine 1% Inj, 20ml

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
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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 to prevent pain during medical procedures, or to relieve pain from certain conditions. It works by temporarily blocking nerve signals in the area where it's 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 be sure to follow all instructions 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 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 you are taking, including over-the-counter drugs, supplements, and herbal products.
  • Report any unusual symptoms or discomfort during or after the procedure.
  • Avoid touching or putting pressure on the numb area until sensation returns to prevent injury.

Dosing & Administration

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Adult Dosing

Standard Dose: Varies significantly based on procedure and site of injection. For infiltration anesthesia: 0.5% to 1% solution, max single dose 4.5 mg/kg (not to exceed 300 mg). For peripheral nerve block: 1% to 2% solution, max single dose 4.5 mg/kg (not to exceed 300 mg).
Dose Range: 0.5 - 4.5 mg

Condition-Specific Dosing:

infiltration_anesthesia: 0.5% to 1% solution, max 4.5 mg/kg (300 mg total)
peripheral_nerve_block: 1% to 2% solution, max 4.5 mg/kg (300 mg total)
epidural_anesthesia: 1% to 2% solution, max 300 mg total
caudal_anesthesia: 1% solution, max 300 mg total
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Pediatric Dosing

Neonatal: Not established for routine use; extreme caution if used. Max 2-3 mg/kg.
Infant: Max 3-5 mg/kg (without epinephrine).
Child: Max 3-5 mg/kg (without epinephrine).
Adolescent: Max 3-5 mg/kg (without epinephrine), or adult dose if weight allows.
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Dose Adjustments

Renal Impairment:

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

Hepatic Impairment:

Mild: Consider dose reduction in patients with severe hepatic impairment.
Moderate: Reduce dose by 50% or more in patients with moderate to severe hepatic impairment. Monitor plasma levels if possible.
Severe: Reduce dose by 50% or more in patients with moderate to severe hepatic impairment. Monitor plasma levels 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 exerting a local anesthetic action. It blocks voltage-gated sodium channels in the neuronal cell membrane, preventing the influx of sodium ions and thus inhibiting depolarization and propagation of action potentials.
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Pharmacokinetics

Absorption:

Bioavailability: Varies greatly depending on site of administration, presence of vasoconstrictor (e.g., epinephrine), and vascularity of the tissue. Systemic absorption occurs from all sites of administration.
Tmax: Variable, typically 5-15 minutes for local infiltration, longer for nerve blocks.
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 (readily crosses blood-brain barrier and placenta)

Elimination:

HalfLife: 1.5-2 hours (prolonged in hepatic dysfunction, 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 (for local infiltration)
PeakEffect: 5-15 minutes
DurationOfAction: 30-60 minutes (without epinephrine); 60-120 minutes (with epinephrine)
Confidence: High

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 when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:

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, such as:
+ Blue or gray discoloration of the lips, nails, or skin
+ Abnormal heartbeat
+ Seizures
+ Severe dizziness or fainting
+ Severe headache
+ Excessive sleepiness
+ Fatigue or weakness
+ 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
+ Fatigue or weakness
Other severe side effects, including:
+ Breathing difficulties, slow breathing, or shallow breathing
+ Lightheadedness, drowsiness, confusion, or blurred vision
+ Slow heartbeat
+ Nervousness or excitability
+ Speech difficulties
+ Abnormal sensations, such as burning, numbness, or tingling
+ Restlessness
+ Anxiety
+ Changes in vision
+ Ringing in the ears
+ Dizziness or fainting
+ Severe headache
+ Twitching
+ Shakiness
+ Seizures
+ Feeling excessively hot or cold
+ Metallic taste
+ Chest pain
+ Mood changes

Additional Side Effects

As with any medication, some people may experience side effects. If you notice any of the following symptoms, contact your doctor:

* Injection site reactions (if given into the spine), such as:
+ Erectile dysfunction
+ Loss of mobility
+ Loss of bladder or bowel control
+ Urination difficulties

Reporting Side Effects

If you experience any side effects that bother you or do not go away, 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 the ears (tinnitus)
  • Numbness or tingling around the mouth
  • Blurred 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 reactions you experienced.
If you are scheduled to receive this medication via spinal injection, alert your doctor to any of the following health issues:
+ Heart block
+ Severe bleeding
+ Severe infection
+ Presence of an infection at the injection site

It is crucial to disclose all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, as well as any health problems you are experiencing. This information will help your doctor and pharmacist assess potential interactions and ensure the safe use of this medication. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
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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 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. 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 sensation and motor function have returned to normal.

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

Overdose Symptoms:

  • Severe CNS depression (drowsiness, unconsciousness)
  • Seizures
  • Respiratory arrest
  • Severe hypotension
  • Bradycardia
  • Cardiac arrest

What to Do:

Seek immediate medical attention. Call 911 or poison control. Management includes maintaining airway, breathing, and circulation, administering anticonvulsants for seizures, and vasopressors for hypotension. Lipid emulsion therapy may be considered for severe systemic toxicity.

Drug Interactions

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Major Interactions

  • Antiarrhythmics (Class I, e.g., mexiletine, tocainide): Increased risk of cardiac depression and CNS toxicity.
  • Beta-blockers (e.g., propranolol, metoprolol): May decrease hepatic metabolism of lidocaine, leading to increased lidocaine levels and toxicity.
  • Cimetidine: Inhibits hepatic metabolism of lidocaine, increasing lidocaine levels and toxicity.
  • Amiodarone: Increased risk of cardiac depression and CNS toxicity.
  • Phenytoin (IV): Increased risk of cardiac depression.
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Moderate Interactions

  • Other local anesthetics: Additive systemic toxicity.
  • Skeletal muscle relaxants (e.g., succinylcholine): May prolong neuromuscular blockade.
  • CYP1A2 inhibitors (e.g., fluvoxamine, ciprofloxacin): May increase lidocaine levels.
  • CYP3A4 inhibitors (e.g., macrolide antibiotics, azole antifungals, protease inhibitors): May increase lidocaine levels.
  • Dopamine: May increase risk of ventricular arrhythmias.
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Minor Interactions

  • Not available

Monitoring

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Baseline Monitoring

Patient history (allergies, cardiac, hepatic, renal disease)

Rationale: To identify contraindications, precautions, and potential for altered pharmacokinetics.

Timing: Prior to administration

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

Rationale: To establish baseline and monitor for cardiovascular or respiratory depression.

Timing: Prior to administration

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Routine Monitoring

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

Frequency: During and immediately after administration, then as clinically indicated.

Target: Within patient's normal range

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

Neurological status (level of consciousness, signs of CNS toxicity)

Frequency: During and immediately after administration, then as clinically indicated.

Target: Alert and oriented, no signs of toxicity

Action Threshold: Drowsiness, dizziness, tinnitus, perioral numbness, muscle twitching, seizures require immediate intervention.

ECG monitoring (for large doses or IV administration)

Frequency: Continuous during and after administration for high-risk patients or large doses.

Target: Normal sinus rhythm, no arrhythmias

Action Threshold: Arrhythmias (e.g., bradycardia, heart block, ventricular arrhythmias) require immediate intervention.

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Symptom Monitoring

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

Special Patient Groups

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Pregnancy

Lidocaine is 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 during pregnancy when clinically indicated, especially for local anesthesia.

Trimester-Specific Risks:

First Trimester: Low risk, but use with caution and only if clearly needed.
Second Trimester: Generally considered safe for local anesthesia.
Third Trimester: Generally considered safe for local anesthesia, commonly used in obstetrics (e.g., epidural anesthesia).
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Lactation

Lidocaine is considered L2 (Safer) by LactMed. It is excreted into breast milk in small amounts. The amount ingested by the infant is typically very low and unlikely to cause adverse effects.

Infant Risk: Low risk. Monitor infant for drowsiness or feeding difficulties, though unlikely with typical local anesthetic doses.
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Pediatric Use

Use with caution. Dosing must be carefully calculated based on weight (mg/kg) to avoid toxicity. Neonates and infants may have reduced protein binding and hepatic metabolism, increasing susceptibility to toxicity. Avoid formulations with preservatives (e.g., methylparaben) in neonates.

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Geriatric Use

Elderly patients may be more susceptible to systemic toxicity due to decreased hepatic blood flow, reduced protein binding, and altered body composition. Lower doses and careful monitoring are recommended.

Clinical Information

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Clinical Pearls

  • Always aspirate prior to injection to avoid inadvertent intravascular administration, which can lead to systemic toxicity.
  • The addition of epinephrine prolongs the duration of action and reduces systemic absorption, but should be avoided in areas with end-arterial supply (e.g., fingers, toes, nose, penis, ears) due to risk of ischemia.
  • Monitor for early signs of CNS toxicity (e.g., perioral numbness, metallic taste, tinnitus) as these often precede more severe symptoms like seizures.
  • Lidocaine is also used as an antiarrhythmic (Class IB) for ventricular arrhythmias, but this typically involves IV administration of higher concentrations and different dosing protocols.
  • Ensure proper storage conditions (room temperature, protect from light) and check for particulate matter or discoloration before use.
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Alternative Therapies

  • Bupivacaine (longer-acting local anesthetic)
  • Ropivacaine (longer-acting local anesthetic, less cardiotoxic than bupivacaine)
  • Mepivacaine (intermediate-acting local anesthetic)
  • Procaine (short-acting local anesthetic)
  • Chloroprocaine (short-acting local anesthetic)
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Cost & Coverage

Average Cost: Highly variable, typically low cost for generic injectable solutions. per 20ml 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 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 have additional patient information leaflets; check with your pharmacist for more information. 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 medical attention. Be prepared to provide information about the medication taken, the quantity, and the time of the incident.