Lidocaine 4% Injection, 5ml
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
Pharmacologic Class
Voltage-gated sodium channel blocker
Pregnancy Category
B
FDA Approved
Jan 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
Lidocaine is a medicine used to numb a specific area of your body, preventing you from feeling pain during minor medical procedures or to relieve pain from certain conditions. It works by temporarily blocking nerve signals in the area where it's injected.
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.
If you miss a dose, contact your doctor immediately 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 procedure.
If you miss a dose, contact your doctor immediately to receive guidance on the appropriate course of action.
Lifestyle & Tips
- Avoid touching or putting pressure on the numb area until sensation returns to prevent injury.
- Follow post-procedure instructions carefully, especially regarding eating or drinking if the mouth/throat was 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:
Highly variable based on procedure, site, and patient factors. Max single dose for local infiltration/nerve block: 4.5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine), not to exceed 300 mg (without epinephrine) or 500 mg (with epinephrine). For 4% solution (40 mg/ml), this means careful volume calculation.
Condition-Specific Dosing:
local_infiltration:
Max 4.5 mg/kg (without epinephrine), 7 mg/kg (with epinephrine). Total dose not to exceed 300 mg (without epinephrine) or 500 mg (with epinephrine).
nerve_block:
Max 4.5 mg/kg (without epinephrine), 7 mg/kg (with epinephrine). Total dose not to exceed 300 mg (without epinephrine) or 500 mg (with epinephrine).
epidural_anesthesia:
Not typically used as 4% for epidural; lower concentrations (1-2%) are common. Max 300 mg (without epinephrine) or 500 mg (with epinephrine).
Pediatric Dosing
Neonatal:
Not established for routine use; extreme caution. Max 2-3 mg/kg.
Infant:
Max 4.5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine). Total dose not to exceed 300 mg. Careful calculation is critical.
Child:
Max 4.5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine). Total dose not to exceed 300 mg. Careful calculation is critical.
Adolescent:
Max 4.5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine). Total dose not to exceed 300 mg. Careful calculation is critical.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment for single doses. Caution with repeated doses.
Moderate:
No specific adjustment for single doses. Caution with repeated doses.
Severe:
No specific adjustment for single doses. Caution with repeated doses.
Dialysis:
Lidocaine is not significantly removed by hemodialysis. Caution with repeated doses due to potential accumulation of metabolites.
Hepatic Impairment:
Mild:
Consider dose reduction (e.g., 50%) in patients with severe hepatic impairment.
Moderate:
Consider dose reduction (e.g., 50%) in patients with severe hepatic impairment.
Severe:
Significant dose reduction (e.g., 50%) recommended due to impaired metabolism and increased half-life. Monitor for toxicity.
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 blocks voltage-gated sodium channels in the neuronal cell membrane, preventing depolarization and propagation of action potentials.
Pharmacokinetics
Absorption:
Bioavailability:
Highly variable depending on site of administration (e.g., intercostal block > caudal > epidural > brachial plexus > subcutaneous). Systemic absorption is rapid from highly vascularized areas.
Tmax:
Varies significantly with site of injection and presence of vasoconstrictor (e.g., 5-15 minutes for epidural, longer for subcutaneous).
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 (primarily as metabolites)
Unchanged:
Less than 10% (typically 3% unchanged in urine)
Pharmacodynamics
OnsetOfAction:
2-5 minutes (depending on concentration, site, and presence of epinephrine)
PeakEffect:
5-15 minutes
DurationOfAction:
30-60 minutes (without epinephrine); 60-120 minutes (with epinephrine), depending on dose and site.
Safety & Warnings
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:
+ 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 life-threatening condition):
+ Blue or gray discoloration 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 acidosis (too much acid in the blood):
+ 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:
+ Breathing difficulties, slow breathing, or shallow breathing
+ Feeling lightheaded, sleepy, confused, or experiencing blurred vision
+ Slow heartbeat
+ Feeling nervous or excitable
+ Speech difficulties
+ Abnormal 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
+ Mood changes
Additional Side Effects (Injection into the Spine)
If you receive this medication via injection into the spine, you may experience:
Erectile dysfunction
Loss of mobility
Loss of bladder or bowel control
Urination difficulties
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to contact your doctor if you notice any symptoms that bother you or persist. Not all possible side effects are listed here. If you have questions or concerns about side effects, consult your doctor.
Reporting Side Effects
You can report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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:
+ 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 life-threatening condition):
+ Blue or gray discoloration 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 acidosis (too much acid in the blood):
+ 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:
+ Breathing difficulties, slow breathing, or shallow breathing
+ Feeling lightheaded, sleepy, confused, or experiencing blurred vision
+ Slow heartbeat
+ Feeling nervous or excitable
+ Speech difficulties
+ Abnormal 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
+ Mood changes
Additional Side Effects (Injection into the Spine)
If you receive this medication via injection into the spine, you may experience:
Erectile dysfunction
Loss of mobility
Loss of bladder or bowel control
Urination difficulties
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to contact your doctor if you notice any symptoms that bother you or persist. Not all possible side effects are listed here. If you have questions or concerns about side effects, consult your doctor.
Reporting Side Effects
You can report side effects to the FDA at 1-800-332-1088 or online 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
- Shaking or tremors
- Confusion or unusual drowsiness
- Difficulty breathing
- Slow or irregular 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 or drugs. Be prepared to describe the allergic reaction 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 existing health problems. This will enable your doctor to assess potential interactions and ensure safe use of this medication. Do not initiate, terminate, or modify the dosage of any medication without first consulting your doctor to confirm it is safe to do so.
To ensure safe treatment, inform your doctor of the following:
Any allergies you have to this medication, its components, or other substances, including foods or drugs. Be prepared to describe the allergic reaction 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 existing health problems. This will enable your doctor to assess potential interactions and ensure safe use of this medication. Do not initiate, terminate, or modify the dosage of any medication without first consulting your doctor to confirm it is safe to do so.
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, 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 engage in 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.
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, 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 engage in 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.
Overdose Information
Overdose Symptoms:
- Severe dizziness or lightheadedness
- Seizures
- Unconsciousness
- Slow or irregular heartbeat
- Very low blood pressure
- Difficulty breathing or stopping breathing
- Cardiac arrest
What to Do:
Seek immediate emergency medical attention. Call 911 or your local emergency number. For poison control, call 1-800-222-1222.
Drug Interactions
Major Interactions
- Antiarrhythmics (Class I, e.g., mexiletine, procainamide): Increased risk of cardiac depression and toxicity.
- Beta-blockers (e.g., propranolol, metoprolol): May decrease lidocaine clearance, increasing risk of toxicity.
- Cimetidine: May inhibit lidocaine metabolism, increasing plasma levels and toxicity risk.
- Amiodarone: Increased risk of cardiac adverse effects.
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.
- Skeletal muscle relaxants (e.g., succinylcholine): Prolongation of neuromuscular blockade.
- Other local anesthetics: Additive systemic toxicity.
Minor Interactions
- Phenytoin: May alter lidocaine metabolism.
- Phenobarbital: May induce lidocaine metabolism.
Monitoring
Baseline Monitoring
Allergy history
Rationale: To identify contraindications to lidocaine or related amide anesthetics.
Timing: Prior to administration
Medical history (cardiac, hepatic, renal disease, seizure disorder)
Rationale: To assess 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: Every 5-15 minutes during and immediately after injection, then as clinically indicated.
Target: Within patient's normal limits, or as per clinical protocol.
Action Threshold: Significant deviations (e.g., bradycardia, hypotension, respiratory depression) warrant immediate intervention.
Neurological status (CNS effects)
Frequency: Continuously during and immediately after injection.
Target: No signs of CNS excitation or depression.
Action Threshold: Signs like dizziness, tinnitus, perioral numbness, confusion, tremors, seizures, or drowsiness indicate potential systemic toxicity.
ECG monitoring (if large doses or systemic absorption is expected)
Frequency: Continuous during and immediately after injection.
Target: Normal sinus rhythm, no significant conduction abnormalities.
Action Threshold: Arrhythmias, widened QRS, prolonged PR interval, or bradycardia indicate potential cardiac toxicity.
Symptom Monitoring
- Lightheadedness
- Dizziness
- Tinnitus (ringing in ears)
- Perioral numbness
- Metallic taste
- Blurred vision
- Tremors
- Muscle twitching
- Confusion
- Drowsiness
- Seizures
- Bradycardia
- Hypotension
- Cardiac arrest
- Respiratory depression
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 during pregnancy when clinically indicated and used at appropriate doses.
Trimester-Specific Risks:
First Trimester:
Generally considered low risk; use when clearly needed.
Second Trimester:
Generally considered low risk; use when clearly needed.
Third Trimester:
Generally considered low risk; use when clearly needed. Can cross the placenta, but adverse effects on the neonate are rare with appropriate dosing.
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 Category L2).
Infant Risk:
Low risk of adverse effects to the breastfed infant. Monitor infant for drowsiness or feeding difficulties, though unlikely.
Pediatric Use
Dosing must be carefully calculated based on the child's weight to avoid systemic toxicity. Children, especially younger ones, may be more susceptible to systemic toxicity. Monitor closely for CNS and cardiovascular effects. The 4% concentration requires very precise volume measurement to avoid overdose.
Geriatric Use
Elderly patients may have reduced hepatic blood flow and metabolic capacity, leading to decreased clearance and increased plasma concentrations of lidocaine. A reduced dose may be necessary, and careful monitoring for systemic toxicity is recommended.
Clinical Information
Clinical Pearls
- Always aspirate prior to injection to ensure the needle is not in a blood vessel, especially with higher concentrations like 4%.
- The 4% concentration is potent; careful calculation of total milligrams and volume is crucial to avoid exceeding maximum safe doses, particularly in smaller patients.
- Epinephrine can be added to lidocaine to prolong its duration of action and reduce systemic absorption, but it should not be used in areas with end-arterial circulation (e.g., fingers, toes, nose, penis, ears) due to risk of ischemia.
- Monitor for signs of CNS toxicity (e.g., lightheadedness, tinnitus, perioral numbness, tremors, seizures) and cardiovascular toxicity (e.g., bradycardia, hypotension, arrhythmias).
- Lipid emulsion therapy (Intralipid) is the antidote for severe local anesthetic systemic toxicity (LAST).
Alternative Therapies
- Bupivacaine (longer duration)
- Ropivacaine (less cardiotoxic than bupivacaine)
- Mepivacaine (intermediate duration)
- Prilocaine (intermediate duration, risk of methemoglobinemia)
- Chloroprocaine (short duration, ester-type)
Cost & Coverage
Average Cost:
Not available Not available
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 for further guidance. To ensure safe use, never share your medication with others or take someone else's medication. 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; do not flush them down the toilet or pour them down the drain unless instructed to do so by a healthcare professional. 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. Additionally, some medications may have a separate 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 medical attention. Be prepared to provide information about the medication taken, the amount, and the time of ingestion to ensure prompt and effective treatment.