Xylocaine-Mpf 2% Inj, 10ml

Manufacturer FRESENIUS KABI Active Ingredient Lidocaine Injection Solution (Anesthetic)(LYE doe kane) Pronunciation LYE-doe-kane
It is used to numb an area before a procedure.It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Local Anesthetic, Antiarrhythmic (Class IB)
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Pharmacologic Class
Voltage-gated sodium channel blocker
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Pregnancy Category
Category B
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FDA Approved
Jun 1948
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Lidocaine is a medication used to numb a specific area of your body to prevent pain during medical procedures, such as minor surgery, dental work, or childbirth. It works by temporarily blocking nerve signals in the area where it's injected.
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How to Use This Medicine

To use this medication correctly, follow your doctor's instructions and carefully read all accompanying information. Take this medication exactly as directed, and adhere to all provided guidelines. 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.
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Lifestyle & Tips

  • Inform your healthcare provider about all medications you are taking, including over-the-counter drugs, supplements, and herbal products.
  • Report any unusual sensations or discomfort during or after the injection.
  • Avoid eating or drinking until sensation returns if the injection affects your mouth or throat to prevent choking or biting your tongue/cheek.

Dosing & Administration

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Adult Dosing

Standard Dose: Varies significantly by procedure and site of injection. For infiltration: 0.5% to 1% solution. For peripheral nerve block: 1% to 2% solution. For epidural anesthesia: 1% to 2% solution. Max single dose typically 4.5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine), not to exceed 300 mg (without epinephrine) or 500 mg (with epinephrine).
Dose Range: 0.5 - 7 mg

Condition-Specific Dosing:

infiltration: 0.5% to 1% solution, up to 4.5 mg/kg (max 300 mg)
peripheralNerveBlock: 1% to 2% solution, up to 4.5 mg/kg (max 300 mg)
epiduralAnesthesia: 1% to 2% solution, up to 4.5 mg/kg (max 300 mg)
withEpinephrine: Up to 7 mg/kg (max 500 mg)
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Pediatric Dosing

Neonatal: Not established for routine use; extreme caution if used. Max 2-3 mg/kg.
Infant: Max 3-5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine), not to exceed 300 mg. Use lowest effective concentration and volume.
Child: Max 3-5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine), not to exceed 300 mg. Use lowest effective concentration and volume.
Adolescent: Max 3-5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine), not to exceed 300 mg. Use lowest effective concentration and volume.
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment generally needed, but monitor for toxicity.
Moderate: No specific adjustment generally needed, but monitor for toxicity.
Severe: Use with caution; consider reduced doses due to potential accumulation of metabolites. Monitor for toxicity.
Dialysis: Lidocaine is not significantly removed by hemodialysis. Use with caution; monitor for toxicity.

Hepatic Impairment:

Mild: Use with caution; consider reduced doses.
Moderate: Reduced doses recommended (e.g., 50% of usual dose). Monitor for toxicity.
Severe: Significantly reduced doses recommended (e.g., 50% or more reduction). Contraindicated in severe hepatic dysfunction for some indications. Monitor for toxicity.

Pharmacology

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Mechanism of Action

Lidocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action. It blocks voltage-gated sodium channels in the neuronal cell membrane, preventing the influx of sodium ions and thus inhibiting depolarization and nerve impulse propagation.
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Pharmacokinetics

Absorption:

Bioavailability: Variable; depends on site of administration, vascularity of tissue, presence of vasoconstrictor (e.g., epinephrine). Rapidly absorbed from injection sites.
Tmax: Variable; 5-15 minutes for epidural, 10-20 minutes for intercostal block, 30-60 minutes for subcutaneous infiltration.
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 impairment, heart failure, and in neonates)
Clearance: Approximately 10 mL/min/kg
ExcretionRoute: Renal (less than 10% as unchanged drug)
Unchanged: Less than 10%
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Pharmacodynamics

OnsetOfAction: Rapid; 2-5 minutes (infiltration, nerve block, epidural)
PeakEffect: Variable; 5-30 minutes depending on site and concentration.
DurationOfAction: 30-60 minutes (without epinephrine); 60-120 minutes (with epinephrine), depending on concentration and site.

Safety & Warnings

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Side Effects

Urgent Side Effects: Seek Medical Help Right Away

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek 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, abnormal 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, abnormal 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.
Neurological Symptoms: Feeling lightheaded, sleepy, confused, or experiencing blurred vision.
Cardiovascular Issues: Slow heartbeat.
Nervous System Symptoms: 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 extremely 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

Like all medications, this drug can cause side effects, although many people may not experience any or may only have mild symptoms. If you notice any side effects that bother you or persist, contact your doctor for guidance. 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. Your doctor can also provide medical advice on managing side effects.
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Seek Immediate Medical Attention If You Experience:

  • Dizziness or lightheadedness
  • Ringing in the ears (tinnitus)
  • Numbness or tingling around the mouth
  • Metallic taste in the mouth
  • Blurred or double vision
  • Tremors or muscle twitching
  • Feeling unusually sleepy or confused
  • Slow or irregular heartbeat
  • Difficulty breathing
  • Seizures
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

To ensure safe treatment, inform your doctor of the following:

Any allergies you have to this medication, its components, or other substances, including foods and drugs. Describe the allergic reaction you experienced, such as symptoms and signs.
If you are scheduled to receive this medication via spinal injection, notify your doctor if you have:
+ Heart block
+ Severe bleeding
+ Severe infection
+ An infection at the injection site

This list is not exhaustive, and it is crucial to discuss all your health conditions and medications with your doctor.

Share the following information with your doctor and pharmacist:

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

It is essential to verify that this medication is safe to use with all your other medications and health conditions. Never start, stop, or adjust the dosage of any medication without consulting your doctor first.
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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 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 sensation returns.

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 into the Spine
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 normal feeling and motor function have returned.

Mouth and Dental Considerations
Do not eat while your mouth is numb, as you may inadvertently bite your tongue.
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Overdose Information

Overdose Symptoms:

  • Severe CNS depression (drowsiness, unconsciousness)
  • Seizures
  • Respiratory arrest
  • Cardiovascular collapse (severe hypotension, bradycardia, asystole)
  • 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 oxygen, managing seizures (e.g., with benzodiazepines), and treating cardiovascular depression (e.g., with vasopressors, atropine, lipid emulsion therapy for severe toxicity). Call 1-800-222-1222 for Poison Control.

Drug Interactions

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Major Interactions

  • Amiodarone (increased risk of cardiac depression/arrhythmias)
  • Beta-blockers (e.g., Propranolol, Metoprolol - decreased lidocaine clearance, increased toxicity risk)
  • Cimetidine (decreased lidocaine clearance, increased toxicity risk)
  • Other antiarrhythmics (e.g., Class I antiarrhythmics - additive cardiac effects)
  • Skeletal muscle relaxants (prolonged neuromuscular blockade)
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Moderate Interactions

  • Phenytoin (increased lidocaine metabolism, but also potential for additive cardiac effects)
  • Succinylcholine (prolonged neuromuscular blockade)
  • Local anesthetics (additive systemic toxicity if multiple agents used)
  • CYP1A2/3A4 inhibitors (e.g., Macrolide antibiotics, Azole antifungals - increased lidocaine levels)
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Minor Interactions

  • Not available

Monitoring

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Baseline Monitoring

Allergy history (especially to amide-type local anesthetics)

Rationale: To prevent anaphylaxis or severe hypersensitivity reactions.

Timing: Prior to administration

Vital signs (heart rate, blood pressure, respiratory rate)

Rationale: To establish baseline and identify pre-existing cardiovascular or respiratory compromise.

Timing: Prior to administration

Assessment of patient's general condition and comorbidities

Rationale: To identify factors that may alter lidocaine pharmacokinetics or increase risk of toxicity (e.g., hepatic/renal impairment, heart failure).

Timing: Prior to administration

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Routine Monitoring

Vital signs (heart rate, blood pressure, respiratory rate)

Frequency: Continuously during and immediately after administration, then periodically as clinically indicated.

Target: Within patient's normal physiological range.

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

Neurological status (e.g., mental status, signs of CNS toxicity)

Frequency: Continuously during and immediately after administration, then periodically as clinically indicated.

Target: Alert and oriented, absence of neurological symptoms.

Action Threshold: Signs of CNS toxicity (e.g., dizziness, tinnitus, perioral numbness, seizures) require immediate cessation and management.

ECG monitoring (especially with large doses or IV administration)

Frequency: Continuously during and immediately after administration, then periodically as clinically indicated.

Target: Normal sinus rhythm, absence of arrhythmias.

Action Threshold: Arrhythmias (e.g., bradycardia, heart block, ventricular arrhythmias) require immediate intervention.

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Symptom Monitoring

  • Lightheadedness
  • Dizziness
  • Tinnitus
  • Perioral numbness
  • Metallic taste
  • Blurred vision
  • Tremors
  • Muscle twitching
  • Seizures
  • Drowsiness
  • Confusion
  • Bradycardia
  • Hypotension
  • Respiratory depression

Special Patient Groups

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Pregnancy

Lidocaine is Pregnancy Category B. Studies in animals have not shown harm to the fetus, and there are no adequate and well-controlled studies in pregnant women. It is generally considered safe for use during pregnancy when clinically indicated, especially for local or regional anesthesia during labor and delivery. Use the lowest effective dose.

Trimester-Specific Risks:

First Trimester: Generally considered low risk; use only if clearly needed.
Second Trimester: Generally considered low risk; use only if clearly needed.
Third Trimester: Commonly used for epidural/spinal anesthesia during labor and delivery. Fetal bradycardia has been reported with paracervical block.
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Lactation

Lidocaine is excreted into breast milk in small amounts. The amount transferred to the infant is generally considered too small to cause adverse effects. It is considered compatible with breastfeeding by most experts. Monitor the infant for drowsiness or feeding difficulties.

Infant Risk: Low risk
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Pediatric Use

Children, especially infants and neonates, are more susceptible to systemic toxicity due to differences in metabolism, distribution, and higher relative doses per body weight. Use the lowest effective dose and concentration. Careful monitoring for signs of toxicity is crucial. Max doses are lower per kg than adults.

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Geriatric Use

Elderly patients may be more susceptible to systemic toxicity due to decreased hepatic function, reduced renal clearance of metabolites, and altered protein binding. Reduced doses may be necessary. Monitor closely for adverse effects, especially CNS and cardiovascular toxicity.

Clinical Information

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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, but should not be used in areas with end-arterial circulation (e.g., fingers, toes, nose, penis, ears) due to risk of ischemia.
  • Methylparaben-free (MPF) formulations are essential for epidural, spinal, and other neuraxial blocks to prevent neurotoxicity associated with preservatives.
  • Systemic toxicity typically manifests as CNS symptoms first (e.g., perioral numbness, tinnitus, dizziness, seizures), followed by cardiovascular depression (e.g., bradycardia, hypotension, arrhythmias).
  • Lipid emulsion therapy (Intralipid) is a critical antidote for severe local anesthetic systemic toxicity (LAST).
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Alternative Therapies

  • Bupivacaine (longer acting local anesthetic)
  • Ropivacaine (similar to bupivacaine, less cardiotoxic)
  • Mepivacaine (intermediate acting local anesthetic)
  • Chloroprocaine (short acting local anesthetic)
  • Procaine (short acting local anesthetic)
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Cost & Coverage

Average Cost: Varies widely by supplier and volume per 10ml vial
Generic Available: Yes
Insurance Coverage: Generally covered by most insurance plans as a generic injectable medication.
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General Drug Facts

If your symptoms or health problems persist or worsen, it is essential to contact your doctor promptly. To ensure safe use, never share your medication with others, and do not take medication prescribed for someone else. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion. Dispose of unused or expired medications properly. Unless instructed otherwise, avoid flushing medications down the toilet or pouring them down the 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 it occurred, as this will aid in receiving appropriate treatment.