Lidocaine 0.5% Inj, 50ml
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; Amide-type local anesthetic
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 won't feel pain during a procedure or for a short time afterward. It's often used for minor surgeries, dental work, or to relieve pain from certain conditions.
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.
For proper storage and disposal, consult with your doctor, nurse, or pharmacist to determine the best approach if you need to store this medication at home.
If you miss a dose, contact your doctor promptly to receive guidance on the appropriate course of action.
For proper storage and disposal, consult with your doctor, nurse, or pharmacist to determine the best approach if you need to store this medication at home.
If you miss a dose, contact your doctor promptly to receive guidance on the appropriate course of action.
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.
- Report any unusual symptoms or discomfort during or after the procedure.
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. For infiltration anesthesia with 0.5% solution, typical doses range from 5 mL to 60 mL (25 mg to 300 mg lidocaine). Max single dose generally 4.5 mg/kg (not to exceed 300 mg) without epinephrine, or 7 mg/kg (not to exceed 500 mg) with epinephrine.
Dose Range:
25 - 300 mg
Condition-Specific Dosing:
Infiltration Anesthesia:
Up to 60 mL of 0.5% solution (300 mg lidocaine).
Peripheral Nerve Block:
Varies by nerve; e.g., intercostal nerve block: 3-5 mL of 0.5% solution per nerve.
Epidural Anesthesia:
Not typically used as 0.5% for epidural; higher concentrations (1-2%) are common. If used, large volumes would be needed.
Pediatric Dosing
Neonatal:
Not established for routine use; use with extreme caution. Max dose 2-3 mg/kg.
Infant:
Max dose 2-4 mg/kg (not to exceed 4.5 mg/kg).
Child:
Max dose 2-4 mg/kg (not to exceed 4.5 mg/kg).
Adolescent:
Max dose 2-4 mg/kg (not to exceed 4.5 mg/kg).
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment needed for single dose local anesthesia.
Moderate:
No specific adjustment needed for single dose local anesthesia.
Severe:
No specific adjustment needed for single dose local anesthesia. Caution with repeated doses or continuous infusions due to potential accumulation of metabolites.
Dialysis:
Not significantly dialyzable. Caution with repeated doses or continuous infusions.
Hepatic Impairment:
Mild:
No specific adjustment needed for single dose local anesthesia.
Moderate:
Reduce dose by 50% for continuous infusions or repeated doses. Monitor for toxicity.
Severe:
Reduce dose by 50-75% for continuous infusions or repeated doses. Monitor for toxicity. Avoid if possible.
Confidence:
Medium
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:
Variable (depends on site of administration, vascularity, presence of vasoconstrictor); 35% (oral, high first-pass metabolism)
Tmax:
Variable (e.g., 5-15 minutes for infiltration, longer for nerve blocks)
FoodEffect:
Not applicable for injectable formulation
Distribution:
Vd:
0.7-2.7 L/kg
ProteinBinding:
60-80% (primarily to alpha-1-acid glycoprotein)
CnssPenetration:
Yes (readily crosses blood-brain barrier and placenta)
Elimination:
HalfLife:
1.5-2 hours (prolonged in hepatic dysfunction)
Clearance:
10-20 mL/min/kg
ExcretionRoute:
Renal (less than 10% unchanged)
Unchanged:
<10%
Pharmacodynamics
OnsetOfAction:
2-5 minutes (infiltration)
PeakEffect:
5-15 minutes
DurationOfAction:
30-60 minutes (without epinephrine); 60-120 minutes (with epinephrine)
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 signs or symptoms, contact your doctor or seek medical attention immediately:
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, 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, or Seizures.
Other Symptoms: Feeling hot or cold, metallic taste, chest pain, or mood changes.
Additional Side Effects of Spinal Injection:
Sexual Dysfunction: Difficulty getting or maintaining an erection.
Motor Function Impairment: Inability to move or control bowel and bladder function.
Urinary Retention: Trouble passing urine.
Other Possible Side Effects
Not everyone experiences side effects, and many people have only minor or no side effects at all. However, if you notice any side effects that bother you or persist, contact your doctor for guidance. This is not an exhaustive list of possible side effects. If you have questions or concerns, 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. Your doctor can also provide medical advice on managing side effects.
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 medical attention immediately:
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, 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, or Seizures.
Other Symptoms: Feeling hot or cold, metallic taste, chest pain, or mood changes.
Additional Side Effects of Spinal Injection:
Sexual Dysfunction: Difficulty getting or maintaining an erection.
Motor Function Impairment: Inability to move or control bowel and bladder function.
Urinary Retention: Trouble passing urine.
Other Possible Side Effects
Not everyone experiences side effects, and many people have only minor or no side effects at all. However, if you notice any side effects that bother you or persist, contact your doctor for guidance. This is not an exhaustive list of possible side effects. If you have questions or concerns, 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. Your doctor can also provide medical advice on managing side effects.
Seek Immediate Medical Attention If You Experience:
- Dizziness or lightheadedness
- Numbness or tingling around the mouth
- Ringing in the ears (tinnitus)
- Blurred vision
- Tremors or muscle twitching
- Feeling anxious or restless
- Unusual drowsiness or confusion
- Slow or irregular heartbeat
- Difficulty breathing
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
To ensure safe treatment, inform your doctor about 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, disclose any history of:
+ Heart block
+ Severe bleeding
+ Severe infection
* If you have an infection at the planned injection site
It is essential 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 healthcare team will assess potential interactions and determine the safety of taking this medication with your other treatments.
Do not initiate, discontinue, or adjust 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 about 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, disclose any history of:
+ Heart block
+ Severe bleeding
+ Severe infection
* If you have an infection at the planned injection site
It is essential 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 healthcare team will assess potential interactions and determine the safety of taking this medication with your other treatments.
Do not initiate, discontinue, or adjust 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, 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.
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.
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, 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.
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.
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
- Respiratory arrest (stopping breathing)
- Severe low blood pressure
- Slow or irregular heartbeat leading to cardiac arrest
What to Do:
Seek immediate medical attention. Call 911 or your local emergency number. For general information, call Poison Control at 1-800-222-1222.
Drug Interactions
Major Interactions
- Antiarrhythmics (Class I, e.g., mexiletine, procainamide): Increased risk of cardiac depression and CNS toxicity.
- Beta-blockers (e.g., propranolol, metoprolol): May decrease lidocaine clearance, increasing plasma levels and toxicity risk.
- Cimetidine: May decrease lidocaine clearance, increasing plasma levels and toxicity risk.
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): May prolong neuromuscular blockade.
- Cholinesterase inhibitors (e.g., donepezil, rivastigmine): May increase risk of bradycardia or heart block.
Minor Interactions
- Phenytoin: May alter lidocaine metabolism.
- Local anesthetics (other): Additive systemic toxicity if combined.
Monitoring
Baseline Monitoring
Patient history (allergies, cardiac, hepatic, renal disease, medications)
Rationale: Identify contraindications, risk factors for toxicity, and potential drug interactions.
Timing: Prior to administration
Vital signs (heart rate, blood pressure, respiratory rate)
Rationale: Establish baseline and monitor for systemic effects.
Timing: Prior to administration
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; monitor for significant deviations.
Action Threshold: Bradycardia (<50 bpm), hypotension (SBP <90 mmHg or >20% drop), respiratory depression.
Neurological status (CNS toxicity)
Frequency: Continuously during and immediately after administration.
Target: Alert and oriented, no signs of agitation, confusion, or seizures.
Action Threshold: Lightheadedness, dizziness, tinnitus, circumoral numbness, muscle twitching, seizures, altered mental status.
ECG monitoring (if large doses or high-risk patient)
Frequency: Continuous during administration of large doses or in patients with cardiac disease.
Target: Normal sinus rhythm, no arrhythmias.
Action Threshold: Arrhythmias (e.g., bradycardia, heart block, ventricular arrhythmias).
Symptom Monitoring
- Lightheadedness
- Dizziness
- Tinnitus
- Blurred vision
- Numbness around the mouth (circumoral paresthesia)
- Tremors
- Muscle twitching
- Seizures
- Drowsiness
- Confusion
- Slurred speech
- Nausea/vomiting
- Bradycardia
- Hypotension
- Cardiac arrest
Special Patient Groups
Pregnancy
Generally considered safe for use as a local anesthetic during pregnancy when administered in appropriate doses. Lidocaine crosses the placenta but is rapidly metabolized by the fetus. Category B.
Trimester-Specific Risks:
First Trimester:
Low risk; no evidence of increased congenital anomalies.
Second Trimester:
Low risk.
Third Trimester:
Low risk; commonly used for epidural anesthesia during labor. Monitor for fetal bradycardia if used in large doses.
Lactation
Considered safe for use during breastfeeding. Lidocaine is excreted into breast milk in small amounts, but the relative infant dose is low, and oral bioavailability in the infant is poor. L2 (Safer).
Infant Risk:
Low risk of adverse effects to the breastfed infant.
Pediatric Use
Use with caution, especially in neonates and infants, due to immature hepatic metabolism and higher risk of systemic toxicity. Dosing must be carefully calculated based on weight (mg/kg) and not exceed recommended maximums. Monitor closely for signs of CNS and cardiovascular toxicity.
Geriatric Use
Reduced doses may be necessary in elderly patients due to decreased hepatic blood flow, reduced protein binding, and potential for decreased renal function, which can lead to higher plasma concentrations and increased risk of toxicity. Start with lower doses and titrate carefully. Monitor closely for CNS and cardiovascular effects.
Clinical Information
Clinical Pearls
- Always aspirate prior to injection to avoid inadvertent intravascular administration, which can lead to rapid systemic toxicity.
- The addition of epinephrine prolongs the duration of action and reduces systemic absorption, allowing for higher total doses, but should be avoided in areas with end-arterial circulation (e.g., fingers, toes, nose, penis, earlobes) due to risk of ischemia.
- Systemic toxicity typically manifests as CNS symptoms first (e.g., circumoral numbness, tinnitus, lightheadedness, seizures), followed by cardiovascular depression (e.g., bradycardia, hypotension, arrhythmias, cardiac arrest).
- Lipid emulsion therapy (Intralipid) is the antidote for severe local anesthetic systemic toxicity (LAST).
- 0.5% Lidocaine is a low concentration, often chosen for large volume infiltration or for patients where systemic toxicity is a particular concern.
Alternative Therapies
- Bupivacaine (longer duration of action)
- Ropivacaine (less cardiotoxic than bupivacaine, similar duration)
- Mepivacaine (intermediate duration)
- Chloroprocaine (short duration, ester-type)
- Topical anesthetics (e.g., EMLA cream for superficial procedures)
- Cryoanalgesia (cold therapy)
- Non-pharmacological pain management techniques
Cost & Coverage
Average Cost:
$10 - $50 per 50ml vial of 0.5% solution
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, 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; do not flush them down the toilet or pour them down the drain unless specifically instructed to do so. 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 quantity, and the time of ingestion.