Xylocaine 2% 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; Antiarrhythmic
Pharmacologic Class
Voltage-gated sodium channel blocker; Class IB Antiarrhythmic
Pregnancy Category
Category B
FDA Approved
Aug 1948
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 medical procedures. It works by temporarily blocking nerve signals in that area.
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
- Inform your healthcare provider about all medications, supplements, and herbal products you are taking.
- 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.
Available Forms & Alternatives
Available Strengths:
- Xylocaine 4% Top Soln
- Xylocaine-Mpf 2% Inj, 10ml
- Xylocaine 2% Inj, 10ml
- Xylocaine-Mpf 1% Inj, 5ml
- Xylocaine 2% Inj, 20ml
- Xylocaine-Mpf 1% Inj, 30ml
- Xylocaine 2% Inj, 50ml
- Xylocaine-Mpf 0.5% Inj, 50ml
- Xylocaine-Mpf 1% Inj, 2ml
- Xylocaine-Mpf 2% Inj, 5ml
- Xylocaine 1% Inj, 20ml
- Xylocaine-Mpf 2% Inj, 2ml
- Xylocaine-Mpf 1% Inj, 10ml
- Xylocaine 1% Inj, 50ml
- Xylocaine 0.5% Inj, 50ml
Dosing & Administration
Adult Dosing
Standard Dose:
Varies significantly by procedure and site of administration. For infiltration anesthesia: 0.5% to 1% solution, max 4.5 mg/kg (not to exceed 300 mg) without epinephrine, or 7 mg/kg (not to exceed 500 mg) with epinephrine.
Condition-Specific Dosing:
infiltration_anesthesia:
0.5% to 1% solution, max 4.5 mg/kg (300 mg total) without epinephrine; max 7 mg/kg (500 mg total) with epinephrine.
nerve_block:
1% to 2% solution, dose varies by block type (e.g., intercostal: 30 mg; paravertebral: 30-50 mg; caudal/epidural: 200-300 mg).
epidural_anesthesia:
1% to 2% solution, 200-300 mg (10-20 mL of 2% solution).
spinal_anesthesia:
Not typically used for spinal anesthesia in this concentration/volume for single dose.
Pediatric Dosing
Neonatal:
Not established for routine use; extreme caution due to immature hepatic function. Max 2-3 mg/kg.
Infant:
Max 4.5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine).
Child:
Max 4.5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine).
Adolescent:
Max 4.5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine).
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment required.
Moderate:
No specific adjustment required.
Severe:
No specific adjustment required, but monitor for systemic toxicity due to potential accumulation of active metabolites.
Dialysis:
Lidocaine is not significantly removed by hemodialysis. No specific adjustment, but monitor for toxicity.
Hepatic Impairment:
Mild:
Consider dose reduction in patients with severe hepatic impairment.
Moderate:
Reduce dose by 50% or more, monitor plasma concentrations if possible.
Severe:
Significant dose reduction required (e.g., 50-75%), monitor plasma concentrations closely due to impaired metabolism.
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 and presence of vasoconstrictors (e.g., epinephrine). Systemic absorption from local injection sites is rapid.
Tmax:
5-15 minutes (after subcutaneous injection), varies by site.
FoodEffect:
Not applicable for injectable formulation.
Distribution:
Vd:
0.7-2.7 L/kg (adults)
ProteinBinding:
60-80% (primarily to alpha-1-acid glycoprotein and albumin)
CnssPenetration:
Yes (crosses blood-brain barrier)
Elimination:
HalfLife:
1.5-2 hours (adults); prolonged in neonates and patients with hepatic impairment or CHF.
Clearance:
10-20 mL/min/kg
ExcretionRoute:
Renal (less than 10% unchanged)
Unchanged:
Less than 10%
Pharmacodynamics
OnsetOfAction:
2-5 minutes (infiltration)
PeakEffect:
5-15 minutes
DurationOfAction:
1-3 hours (without epinephrine); 2-6 hours (with epinephrine)
Confidence:
Medium
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, 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, such as slow, shallow, or troubled 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
If you receive this medication via spinal injection, you may also experience:
Erectile dysfunction
Loss of movement or mobility
Loss of bladder or bowel control
Urination difficulties
Other Possible Side Effects
Like all medications, this drug can cause side effects, although not everyone will experience them. If you have any side effects that bother you or persist, contact your doctor for advice. Some people may not experience any side effects at all.
If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online 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, 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, such as slow, shallow, or troubled 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
If you receive this medication via spinal injection, you may also experience:
Erectile dysfunction
Loss of movement or mobility
Loss of bladder or bowel control
Urination difficulties
Other Possible Side Effects
Like all medications, this drug can cause side effects, although not everyone will experience them. If you have any side effects that bother you or persist, contact your doctor for advice. Some people may not experience any side effects at all.
If you have questions or concerns about side effects, consult your doctor. You can also 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:
- Dizziness or lightheadedness
- Ringing in the ears (tinnitus)
- Metallic taste in the mouth
- Numbness or tingling around the mouth
- Drowsiness or confusion
- Muscle twitching or tremors
- Difficulty breathing
- Slow or irregular heartbeat
- Seizures
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 reactions you experienced.
If you are scheduled to receive this medication via spinal injection, tell your doctor if you have:
+ Heart block
+ Severe bleeding
+ Severe infection
+ An infection at the injection site
This list is not exhaustive. It is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine if it is safe to take this medication alongside your other treatments. Never start, stop, or adjust the dosage of any medication without consulting your doctor first.
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 reactions you experienced.
If you are scheduled to receive this medication via spinal injection, tell your doctor if you have:
+ Heart block
+ Severe bleeding
+ Severe infection
+ An infection at the injection site
This list is not exhaustive. It is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine if it is safe to take this medication alongside your other treatments. Never start, stop, or adjust the dosage of any medication without consulting your doctor first.
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 performing tasks 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 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.
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 performing tasks 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 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.
Overdose Information
Overdose Symptoms:
- Severe dizziness or lightheadedness
- Seizures
- Unconsciousness
- Respiratory arrest
- Cardiac arrest
What to Do:
Immediate medical attention is required. Call 911 or your local emergency number. Management includes maintaining airway, breathing, and circulation, administering anticonvulsants for seizures, and lipid emulsion therapy for severe systemic toxicity.
Drug Interactions
Major Interactions
- Antiarrhythmics (e.g., mexiletine, amiodarone, procainamide, quinidine, propafenone): Increased risk of cardiac depression and arrhythmias.
- Beta-blockers (e.g., propranolol, metoprolol): Decreased hepatic metabolism of lidocaine, leading to increased lidocaine levels and toxicity.
- Cimetidine: Decreased hepatic metabolism of lidocaine, leading to increased lidocaine levels and toxicity.
Moderate Interactions
- CYP1A2/3A4 inhibitors (e.g., macrolide antibiotics, azole antifungals, protease inhibitors): May increase lidocaine levels.
- Skeletal muscle relaxants (e.g., succinylcholine): Prolonged neuromuscular blockade.
- Phenytoin: Increased risk of cardiac depression.
- Local anesthetics (other): Additive systemic toxicity.
Minor Interactions
- Cholinergic agents: May antagonize effects.
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 (BP, HR, RR)
Rationale: To establish baseline and detect early signs of systemic toxicity.
Timing: Prior to administration
Routine Monitoring
Vital signs (BP, HR, RR)
Frequency: Every 5-15 minutes during and immediately after administration, then as clinically indicated.
Target: Within patient's normal range, stable.
Action Threshold: Significant changes (e.g., hypotension, bradycardia, respiratory depression) require immediate intervention.
Level of consciousness, neurological status
Frequency: Continuously during and immediately after administration.
Target: Alert and oriented, no signs of CNS toxicity (e.g., dizziness, tinnitus, seizures).
Action Threshold: Signs of CNS toxicity (e.g., circumoral numbness, metallic taste, lightheadedness, tinnitus, drowsiness, muscle twitching, seizures) require immediate intervention.
ECG monitoring (if large doses or systemic absorption concern)
Frequency: Continuous during and after administration.
Target: Normal sinus rhythm, no conduction abnormalities.
Action Threshold: Arrhythmias, widened QRS, prolonged PR/QT intervals.
Symptom Monitoring
- Lightheadedness
- Dizziness
- Tinnitus
- Metallic taste
- Numbness of lips/tongue (circumoral numbness)
- Drowsiness
- Confusion
- Muscle twitching
- Tremors
- Seizures
- Bradycardia
- Hypotension
- Respiratory depression
- Cardiac arrest
Special Patient Groups
Pregnancy
Generally considered safe for use during pregnancy when clinically indicated. Category B. Studies in animals have not shown fetal harm, and human data suggest no increased risk of malformations.
Trimester-Specific Risks:
First Trimester:
Low risk, no evidence of increased malformations.
Second Trimester:
Low risk.
Third Trimester:
Low risk, but caution with paracervical block due to potential for fetal bradycardia.
Lactation
Considered compatible with breastfeeding (L2). Lidocaine is excreted into breast milk in small amounts, but the relative infant dose is low, and systemic absorption by the infant is minimal.
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 function and higher risk of systemic toxicity. Dosing must be carefully calculated based on weight and age. Monitor closely for signs of toxicity.
Geriatric Use
Use with caution. Elderly patients may be more susceptible to systemic toxicity due to decreased hepatic function, reduced protein binding, and underlying cardiovascular disease. Lower doses may be required.
Clinical Information
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 circulation (e.g., fingers, toes, nose, ears, penis) due to risk of ischemia.
- Monitor for early signs of CNS toxicity (e.g., circumoral numbness, metallic taste, tinnitus, lightheadedness) as these often precede more severe symptoms like seizures.
- Systemic toxicity can be managed with supportive care, benzodiazepines for seizures, and lipid emulsion therapy for severe cases.
- The 2% concentration is potent; ensure appropriate dilution or volume for the intended procedure to stay within safe dose limits.
Alternative Therapies
- Bupivacaine (longer acting local anesthetic)
- Ropivacaine (longer acting local anesthetic, less cardiotoxic than bupivacaine)
- Mepivacaine (intermediate acting local anesthetic)
- Procaine (ester-type local anesthetic)
- Chloroprocaine (ester-type local anesthetic, very short acting)
Cost & Coverage
Average Cost:
Varies widely per 50ml vial
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 (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 your safety and the safety of others, never share your medication with anyone, and do not take medication prescribed to someone else.
All medications should be stored in a secure location, out of the reach of children and pets, to prevent accidental ingestion. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless specifically instructed to do so by a healthcare professional or pharmacist. Instead, consult with your pharmacist to determine the best disposal method, as some communities have drug take-back programs in place.
Additionally, some medications may come with a separate patient information leaflet; your pharmacist can provide this information if available. If you have any questions or concerns about your medication, it is crucial to 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 detailed information about the overdose, including the name of the medication, the amount taken, and the time it occurred, to ensure prompt and effective treatment.
All medications should be stored in a secure location, out of the reach of children and pets, to prevent accidental ingestion. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless specifically instructed to do so by a healthcare professional or pharmacist. Instead, consult with your pharmacist to determine the best disposal method, as some communities have drug take-back programs in place.
Additionally, some medications may come with a separate patient information leaflet; your pharmacist can provide this information if available. If you have any questions or concerns about your medication, it is crucial to 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 detailed information about the overdose, including the name of the medication, the amount taken, and the time it occurred, to ensure prompt and effective treatment.