Lidocaine 1% Inj, 2ml
It is used to numb an area before a procedure.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Local Anesthetic, Antiarrhythmic (Class IB)
Pharmacologic Class
Voltage-gated sodium channel blocker
Pregnancy Category
Category B
FDA Approved
Jan 1948
DEA Schedule
Not Controlled
Overview
What is this medicine?
Lidocaine is a medicine used to numb a specific area of your body. It works by temporarily blocking nerve signals in that area, so you don't feel pain during minor procedures or injuries. It's often used by doctors or dentists.
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 method.
If you miss a dose, contact your doctor to receive guidance on the appropriate course of action.
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 to receive guidance on the appropriate course of action.
Lifestyle & Tips
- Avoid touching or disturbing the numb area until sensation returns to prevent accidental injury.
- Follow post-procedure instructions carefully, especially regarding eating or drinking if the mouth/throat is numbed.
Available Forms & Alternatives
Available Strengths:
- Lidocaine 4% Top Soln 50ml
- Lidocaine 2% Visc Oral Solution
- Lidocaine 1% Inj, 10ml
- Lidocaine 2% Inj, 2ml
- Lidocaine 4% Injection, 5ml
- Lidocaine 1% Inj, 5ml
- Lidocaine 1% Inj, 20ml
- Lidocaine 2% Inj, 20ml
- Lidocaine 1% Inj, 2ml
- Lidocaine 1% Inj, 50ml
- Lidocaine 2% Inj, 5ml
- Lidocaine 2% Inj, 10ml
- Lidocaine 1% Inj, 30ml
- Lidocaine 2% Inj, 50ml
- Lidocaine 2% Inj, 5ml
- Lidocaine 10mg/ml Inj, 5ml
- Lidocaine 3% Cream 28.35gm
- Lidocaine 3% Cream 85gm
- Lidocaine 2% Topical Jelly 5ml
- Lidocaine 2% Topical Jelly 10ml
- Lidocaine 2% Topical Jelly 20ml
- Lidocaine 20mg/ml Inj, 5ml
- Lidocaine 2% Jelly Gel (uro-Jet)5ml
- Lidocaine 0.5% Inj, 50ml
- Lidocaine 5% Patch
- Lidocaine 5% Topical Ointment 30gm
- Lidocaine 5% Topical Oint 35.44gm
- Lidocaine 5% Topical Ointment 50gm
- Lidocaine 1.5% Inj, 1 Ampule
- Lidocaine 5% Top/oral Oint 50gm
- Lidocaine 4% Cream 15gm
- Lidocaine 4% Cream 30gm
- Lidocaine 4% Cream 5gm
- Lidocaine 3% Cream 85gm
- Lidocaine Pain Relief 4% Patch
- Lidocaine 5% Top/oral Oint (sprmt)
- Lidocaine 5% Anorectal Cream
- Lidocaine 4% Cream 15gm
- Lidocaine 5% Topical Ointment 30gm
- Lidocaine 5% Anorectal Cream 15gm
- Lidocaine Pain Relief 4% Patch
- Lidocaine 5% Cream 30gm
- Lidocaine 2% Inj 25ml
- Lidocaine 5% Ointment 50gm
- Lidocaine 4% Cream 15gm
- Lidocaine 4% Topical Pain Patch
- Lidocaine 3%/hc 0.5% Cream 28.3gm
- Lidocaine 2% Topical Jelly 30ml
Dosing & Administration
Adult Dosing
Standard Dose:
Varies significantly by procedure and site of injection. For infiltration: 0.5% to 1% solution, up to 4.5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine). Max single dose 300 mg (without epi) or 500 mg (with epi).
Dose Range:
0.5 - 7 mg
Condition-Specific Dosing:
localInfiltration:
Up to 4.5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine), not to exceed 300 mg (without epi) or 500 mg (with epi) total dose.
peripheralNerveBlock:
50-300 mg (e.g., 1-2% solution)
epiduralAnesthesia:
200-300 mg (e.g., 1-2% solution)
intravenousAntiarrhythmic:
Initial bolus 1-1.5 mg/kg, followed by infusion 1-4 mg/min (for IV formulation, not typically 1% injection for local use)
Pediatric Dosing
Neonatal:
Not established for routine use as local anesthetic; extreme caution if used. Max 2-4 mg/kg.
Infant:
Max 4.5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine), not to exceed 300 mg total dose.
Child:
Max 4.5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine), not to exceed 300 mg total dose.
Adolescent:
Max 4.5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine), not to exceed 300 mg total dose.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment typically required, but use with caution.
Moderate:
No specific adjustment typically required, but use with caution.
Severe:
Use with caution; accumulation of metabolites may occur. Monitor for toxicity.
Dialysis:
Lidocaine is not significantly removed by hemodialysis. Use with caution, monitor for toxicity.
Hepatic Impairment:
Mild:
No specific adjustment typically required.
Moderate:
Consider dose reduction (e.g., 50%) due to decreased clearance. Monitor for toxicity.
Severe:
Significant dose reduction (e.g., 50-75%) is required due to impaired metabolism. Monitor plasma levels if possible.
Pharmacology
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 specifically blocks voltage-gated sodium channels, preventing the propagation of action potentials.
Pharmacokinetics
Absorption:
Bioavailability:
Varies significantly by route of administration and presence of vasoconstrictors. For local injection, systemic absorption depends on vascularity of injection site. Rapidly absorbed from GI tract but undergoes extensive first-pass metabolism.
Tmax:
Varies by route and site of administration (e.g., 5-15 minutes for infiltration, longer for nerve blocks).
FoodEffect:
Not applicable for injectable formulation.
Distribution:
Vd:
0.8-1.3 L/kg (adults)
ProteinBinding:
60-80% (primarily to alpha-1-acid glycoprotein)
CnssPenetration:
Yes, readily crosses the blood-brain barrier and placenta.
Elimination:
HalfLife:
1.5-2 hours (prolonged in patients with heart failure or liver disease)
Clearance:
Approximately 10-20 mL/min/kg
ExcretionRoute:
Renal (primarily as metabolites)
Unchanged:
<10% (in urine)
Pharmacodynamics
OnsetOfAction:
Rapid (e.g., 2-5 minutes for infiltration)
PeakEffect:
Varies by route and site; generally within 5-15 minutes for local anesthesia.
DurationOfAction:
0.5-3 hours (depending on dose, site, and presence of vasoconstrictor like epinephrine)
Confidence:
High
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an 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
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of methemoglobinemia (a rare but potentially deadly condition):
+ Blue or gray color 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 too much acid in the blood (acidosis):
+ 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:
+ Trouble breathing, slow breathing, or shallow breathing
+ Feeling lightheaded, sleepy, confused, or having blurred vision
+ Slow heartbeat
+ Feeling nervous and excitable
+ Trouble speaking
+ Burning, numbness, or tingling sensation
+ 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
Additional Side Effects of Spinal Injection
If you receive this medication via spinal injection, you may also experience:
Erectile dysfunction
Loss of movement
Loss of bladder or bowel control
Trouble urinating
Other Possible Side Effects
Like all medications, this drug can cause side effects, although many people may not experience any or may only have mild side effects. If you have any side effects that bother you or do not go away, contact your doctor or seek medical attention.
Reporting Side Effects
If you have questions about side effects or want to report any, you can:
Call your doctor for medical advice
Report side effects to the FDA at 1-800-332-1088
* Visit the FDA's MedWatch website at https://www.fda.gov/medwatch
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an 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
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of methemoglobinemia (a rare but potentially deadly condition):
+ Blue or gray color 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 too much acid in the blood (acidosis):
+ 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:
+ Trouble breathing, slow breathing, or shallow breathing
+ Feeling lightheaded, sleepy, confused, or having blurred vision
+ Slow heartbeat
+ Feeling nervous and excitable
+ Trouble speaking
+ Burning, numbness, or tingling sensation
+ 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
Additional Side Effects of Spinal Injection
If you receive this medication via spinal injection, you may also experience:
Erectile dysfunction
Loss of movement
Loss of bladder or bowel control
Trouble urinating
Other Possible Side Effects
Like all medications, this drug can cause side effects, although many people may not experience any or may only have mild side effects. If you have any side effects that bother you or do not go away, contact your doctor or seek medical attention.
Reporting Side Effects
If you have questions about side effects or want to report any, you can:
Call your doctor for medical advice
Report side effects to the FDA at 1-800-332-1088
* Visit the FDA's MedWatch website at https://www.fda.gov/medwatch
Seek Immediate Medical Attention If You Experience:
- Feeling lightheaded or dizzy
- Ringing in your ears (tinnitus)
- Numbness or tingling around your mouth
- Metallic taste in your mouth
- Blurred vision
- Tremors or muscle twitching
- Feeling unusually sleepy or confused
- Difficulty breathing
- Slow heartbeat
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, including any symptoms.
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, as this may affect the administration of the medication.
It is essential to provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
Your complete medical history, including any health problems
This information will help your doctor determine if it is safe to take this medication with your other treatments and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting 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, including any symptoms.
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, as this may affect the administration of the medication.
It is essential to provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
Your complete medical history, including any health problems
This information will help your doctor determine if it is safe to take this medication with your other treatments and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
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, 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.
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, 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.
Overdose Information
Overdose Symptoms:
- Severe dizziness or lightheadedness
- Seizures
- Unconsciousness
- Slow or irregular heartbeat
- Difficulty breathing or stopping breathing
- Cardiac 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
Major Interactions
- Class I Antiarrhythmics (e.g., procainamide, quinidine, disopyramide): Increased risk of cardiac adverse effects.
- Class III Antiarrhythmics (e.g., amiodarone, sotalol): Increased risk of cardiac adverse effects (e.g., QT prolongation, bradycardia).
Moderate Interactions
- Beta-blockers (e.g., propranolol, metoprolol): May decrease hepatic blood flow, reducing lidocaine clearance and increasing plasma levels.
- Cimetidine: Inhibits CYP450 enzymes, potentially increasing lidocaine plasma levels.
- Phenytoin: May increase lidocaine metabolism (CYP3A4 inducer) or have additive cardiac effects.
- Succinylcholine: Lidocaine may prolong the neuromuscular blockade of succinylcholine.
- Other local anesthetics: Additive systemic toxicity.
Minor Interactions
- CYP3A4 inhibitors (e.g., macrolide antibiotics, azole antifungals): May slightly increase lidocaine levels.
- CYP3A4 inducers (e.g., rifampin, carbamazepine): May slightly decrease lidocaine levels.
Monitoring
Baseline Monitoring
Patient history (allergies, cardiac/hepatic/renal disease)
Rationale: To identify contraindications, risk factors for toxicity, and guide dosing.
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
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; significant deviations warrant investigation.
Action Threshold: Bradycardia, hypotension, respiratory depression, or significant changes from baseline.
Signs of CNS toxicity (drowsiness, dizziness, tinnitus, perioral numbness, tremors, seizures)
Frequency: Continuously during and after administration, especially with higher doses or systemic absorption.
Target: Absence of symptoms.
Action Threshold: Any new or worsening CNS symptoms.
ECG monitoring (if large doses or IV administration)
Frequency: Continuous during and after administration.
Target: Normal sinus rhythm, absence of arrhythmias.
Action Threshold: Bradycardia, heart block, QRS widening, ventricular arrhythmias.
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
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.
Trimester-Specific Risks:
First Trimester:
Low risk; no evidence of increased congenital anomalies.
Second Trimester:
Low risk.
Third Trimester:
Low risk; commonly used during labor and delivery (e.g., epidural anesthesia).
Lactation
Lidocaine is excreted into breast milk in small amounts. The amount ingested by the infant is typically very low and unlikely to cause adverse effects. It is considered compatible with breastfeeding (Lactation Risk L2).
Infant Risk:
Low risk; monitor for drowsiness or feeding difficulties, though unlikely.
Pediatric Use
Dosing must be carefully calculated based on weight (mg/kg) to avoid systemic toxicity. Children, especially younger ones, may be more susceptible to systemic toxicity. Use the lowest effective dose.
Geriatric Use
Elderly patients may have reduced hepatic function, leading to decreased lidocaine clearance and increased risk of systemic toxicity. A reduced dose may be necessary. Monitor closely for adverse effects.
Clinical Information
Clinical Pearls
- Always aspirate before injecting to ensure the needle is not in a blood vessel, which can lead to rapid systemic absorption and toxicity.
- The addition of epinephrine prolongs the duration of action and reduces systemic absorption by causing vasoconstriction at the injection site. However, epinephrine should be used with caution or avoided in areas with end-arterial blood supply (e.g., fingers, toes, nose, penis, ears) due to risk of ischemia.
- Systemic toxicity typically manifests as CNS effects (e.g., perioral numbness, tinnitus, seizures) followed by cardiovascular effects (e.g., bradycardia, hypotension, cardiac arrest).
- Lipid emulsion therapy (Intralipid) is an antidote for severe local anesthetic systemic toxicity (LAST).
- Lidocaine 1% contains 10 mg/mL of lidocaine.
Alternative Therapies
- Bupivacaine (longer acting local anesthetic)
- Ropivacaine (similar to bupivacaine, less cardiotoxic)
- Mepivacaine (intermediate acting local anesthetic)
- Procaine (short acting local anesthetic)
- Chloroprocaine (very short acting local anesthetic)
Cost & Coverage
Average Cost:
Typically low cost per 2ml vial
Generic Available:
Yes
Insurance Coverage:
Tier 1 (Generic)
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 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, 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.