Lidocaine 2% Inj, 2ml

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
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Pharmacologic Class
Amide-type local anesthetic; Voltage-gated sodium channel blocker
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Pregnancy Category
B
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FDA Approved
Jan 1970
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Lidocaine is a numbing medicine that works by temporarily blocking nerve signals in a specific area of your body. It's used to prevent pain during minor medical procedures or to relieve pain from certain conditions.
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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 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.

If you miss a dose, contact your doctor 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 injection.
  • Avoid touching or putting pressure on the numbed area until sensation returns to prevent injury.

Dosing & Administration

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Adult Dosing

Standard Dose: Varies significantly by procedure and site of injection. For infiltration, typically 20-200 mg (1-10 mL of 2% solution).

Condition-Specific Dosing:

Local Infiltration (without epinephrine): Max single dose: 4.5 mg/kg (not to exceed 300 mg)
Local Infiltration (with epinephrine): Max single dose: 7 mg/kg (not to exceed 500 mg)
Peripheral Nerve Block: Varies by nerve, e.g., Brachial Plexus: 225-300 mg (11.25-15 mL of 2%)
Epidural Anesthesia: Varies by segment, e.g., Lumbar: 250-300 mg (12.5-15 mL of 2%)
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Pediatric Dosing

Neonatal: Not established for routine use; extreme caution and reduced doses if used.
Infant: Max single dose: 3-5 mg/kg (not to exceed 4.5 mg/kg or 300 mg total, whichever is less).
Child: Max single dose: 3-5 mg/kg (not to exceed 4.5 mg/kg or 300 mg total, whichever is less).
Adolescent: Max single dose: 3-5 mg/kg (not to exceed 4.5 mg/kg or 300 mg total, whichever is less).
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment typically required.
Moderate: No specific adjustment typically required, but monitor for signs of toxicity.
Severe: No specific adjustment typically required, 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 lower doses and monitor for toxicity.
Moderate: Reduce dose by 50% or more; monitor plasma levels if possible and observe for toxicity.
Severe: Reduce dose significantly (e.g., 50-75%); monitor plasma levels if possible and observe for toxicity.

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 the influx of sodium ions and thus inhibiting depolarization and nerve impulse propagation.
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Pharmacokinetics

Absorption:

Bioavailability: 100% (IV); Variable (local infiltration, depends on site, vascularity, and presence of vasoconstrictor)
Tmax: Variable (minutes to hours depending on route and site of administration)
FoodEffect: Not applicable for injectable forms.

Distribution:

Vd: 0.7-2.7 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 (primarily as metabolites)
Unchanged: Less than 10% (as unchanged drug)
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Pharmacodynamics

OnsetOfAction: Rapid (within 2-5 minutes for infiltration)
PeakEffect: Varies by route and site of administration
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 symptoms, contact your doctor or seek immediate medical attention:

Signs of an allergic reaction, including:
+ 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
+ Fatigue or weakness
+ Shortness of breath
Signs of acidosis (too much acid in the blood), including:
+ 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 administered into the spine), including:
+ Erectile dysfunction
+ Loss of mobility
+ Loss of bowel or bladder 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:

  • Feeling lightheaded or dizzy
  • Ringing in your ears (tinnitus)
  • Numbness or tingling around your mouth
  • Unusual anxiety or restlessness
  • Muscle twitching or tremors
  • Blurred vision
  • 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

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, disclose any history of:
+ Heart block
+ Severe bleeding
+ Severe infection
* If the injection site is infected, inform your doctor.

It is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. This includes any health problems you are experiencing. Your doctor will assess potential interactions and determine the safety of taking this medication with your other treatments.

Do not initiate, stop, or adjust the dosage of any medication without first consulting your doctor to confirm it is safe to do so.
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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 with 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.

Protecting the Treated Area
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.
If you are pregnant, plan to become pregnant, or are breastfeeding, discuss the benefits and risks with your doctor.

Injection (Spinal Administration)
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 sensation and motor function have returned to normal.

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
  • Seizures (convulsions)
  • Loss of consciousness
  • Severe drowsiness
  • Slow or irregular heartbeat
  • Low blood pressure
  • Respiratory depression or arrest

What to Do:

Seek immediate medical attention. Call 911 or your local emergency number. In the US, you can also call Poison Control at 1-800-222-1222.

Drug Interactions

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Contraindicated Interactions

  • Not typically contraindicated for local anesthetic use unless severe hypersensitivity or specific cardiac conditions (e.g., severe heart block without pacemaker) are present.
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Major Interactions

  • Antiarrhythmics (Class I, III): Additive cardiac effects, increased risk of toxicity.
  • Beta-blockers (e.g., Propranolol): May decrease hepatic blood flow, reducing lidocaine clearance and increasing plasma levels.
  • Cimetidine: Inhibits lidocaine metabolism, increasing plasma levels and risk of toxicity.
  • Succinylcholine: May prolong neuromuscular blockade.
  • Other local anesthetics: Additive systemic toxicity.
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Moderate Interactions

  • CYP1A2 inhibitors (e.g., Fluvoxamine, Ciprofloxacin): May increase lidocaine levels.
  • CYP3A4 inhibitors (e.g., Macrolide antibiotics, Azole antifungals, Protease inhibitors): May increase lidocaine levels.
  • Phenytoin: May increase lidocaine metabolism (inducer) or increase risk of cardiac depression (additive effect).
  • Dopamine: May increase risk of ventricular arrhythmias.
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Minor Interactions

  • Not well-defined for minor interactions with local anesthetic use.

Monitoring

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Baseline Monitoring

Allergy history

Rationale: To identify potential 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

Cardiac status (ECG if indicated)

Rationale: To assess for pre-existing cardiac conditions that may increase risk of toxicity.

Timing: Prior to administration, especially for larger doses or high-risk patients

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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 physiological range.

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

Signs and symptoms of systemic toxicity (CNS and cardiovascular)

Frequency: Continuously during and for at least 30 minutes after administration.

Target: Absence of symptoms.

Action Threshold: Presence of lightheadedness, dizziness, tinnitus, perioral numbness, muscle twitching, anxiety, seizures, bradycardia, hypotension, or arrhythmias.

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Symptom Monitoring

  • Lightheadedness
  • Dizziness
  • Tinnitus (ringing in ears)
  • Perioral numbness or tingling
  • Metallic taste
  • Blurred vision
  • Tremors or muscle twitching
  • Anxiety or restlessness
  • Drowsiness or sedation
  • Slurred speech
  • Nausea/vomiting
  • Bradycardia
  • Hypotension
  • Arrhythmias
  • Seizures
  • Respiratory depression or 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 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.
Third Trimester: Generally considered low risk; caution with epidural/spinal use near term due to potential for fetal bradycardia or effects on uterine contractility.
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Lactation

Lidocaine is rated L2 (likely safe) 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.
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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 body surface area to weight ratio. Dosing must be carefully calculated based on weight (mg/kg) and the lowest effective dose should be used. Close monitoring for signs of toxicity is crucial.

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Geriatric Use

Geriatric patients may have reduced hepatic function, decreased protein binding, and altered body composition, which can lead to higher plasma concentrations and increased 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 ensure the needle is not in a blood vessel, which can lead to rapid systemic absorption and toxicity.
  • Use the lowest effective dose 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., lightheadedness, tinnitus, perioral numbness, seizures) and cardiovascular (e.g., bradycardia, hypotension) effects.
  • Lidocaine is ineffective in infected or inflamed tissues due to the acidic environment reducing its ability to penetrate nerve membranes.
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Alternative Therapies

  • Other amide-type local anesthetics (e.g., Bupivacaine, Mepivacaine, Ropivacaine, Prilocaine)
  • Ester-type local anesthetics (e.g., Procaine, Tetracaine, Chloroprocaine - less common due to higher allergenicity)
  • Topical anesthetics (e.g., Lidocaine cream, patch, spray)
  • Non-pharmacologic pain management techniques (e.g., ice, distraction)
  • Systemic analgesics (e.g., NSAIDs, opioids) for pain not amenable to local anesthesia.
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Cost & Coverage

Average Cost: Inexpensive per 2ml vial
Generic Available: Yes
Insurance Coverage: Generally covered by most insurance plans as a generic medication.
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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 the 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 it was taken to ensure prompt and effective treatment.