Xylocaine-Mpf 2% Inj, 2ml

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
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Pharmacologic Class
Voltage-gated Sodium Channel Blocker; Class IB Antiarrhythmic
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Pregnancy Category
Category B
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FDA Approved
Jan 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 the body, preventing you from feeling pain during medical procedures. It works by temporarily blocking nerve signals in that area. It can also be used to treat certain heart rhythm problems.
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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 be sure to 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.

In the event that you miss a dose, contact your doctor promptly to receive guidance on the appropriate course of action.
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Lifestyle & Tips

  • Report any unusual sensations (e.g., dizziness, ringing in ears, numbness around mouth, muscle twitching) immediately during or after administration.
  • Avoid eating or drinking until sensation returns if the mouth or throat is numbed to prevent choking.
  • Avoid activities requiring fine motor skills or full sensation until the anesthetic effect wears off.

Dosing & Administration

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Adult Dosing

Standard Dose: Highly variable based on procedure and site of administration. For local infiltration: 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.
Dose Range: 0.5 - 7 mg

Condition-Specific Dosing:

Local Infiltration (without epinephrine): Max 4.5 mg/kg (300 mg total)
Local Infiltration (with epinephrine): Max 7 mg/kg (500 mg total)
Peripheral Nerve Block (e.g., brachial plexus): Up to 400 mg (e.g., 25-50 mL of 1% solution)
Epidural Anesthesia (lumbar): 250-300 mg (e.g., 12.5-15 mL of 2% solution)
Caudal Anesthesia: 225-300 mg (e.g., 11.25-15 mL of 2% solution)
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Pediatric Dosing

Neonatal: Not established for routine use; use with extreme caution. Max 2-3 mg/kg.
Infant: Max 4.5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine). Lower doses for neonates/infants due to immature hepatic function.
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).
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment needed.
Moderate: No specific adjustment needed.
Severe: No specific adjustment needed, as renal excretion of unchanged drug is minor. However, metabolites may accumulate.
Dialysis: Not significantly removed by hemodialysis. No specific dose adjustment for dialysis patients, but monitor for toxicity.

Hepatic Impairment:

Mild: Consider dose reduction, monitor for toxicity.
Moderate: Reduce dose by 50% or more; monitor plasma concentrations and clinical response.
Severe: Reduce dose significantly (e.g., 75% or more); monitor plasma concentrations and clinical response closely. Avoid if possible.

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 depolarization and propagation of action potentials.
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Pharmacokinetics

Absorption:

Bioavailability: Variable (depends on site of administration, presence of vasoconstrictor). Systemic absorption occurs from all sites of administration. IV bioavailability is 100%.
Tmax: Variable; depends on site of administration (e.g., intercostal block: 5-15 min; epidural: 10-20 min; subcutaneous: 30-60 min).
FoodEffect: Not applicable for injectable formulation.

Distribution:

Vd: 0.7-2.7 L/kg (average 1.1 L/kg in healthy adults)
ProteinBinding: 60-80% (primarily to alpha-1-acid glycoprotein and albumin); concentration-dependent.
CnssPenetration: Yes

Elimination:

HalfLife: 1.5-2 hours (prolonged in hepatic dysfunction, heart failure, and in neonates).
Clearance: Approximately 10 mL/min/kg.
ExcretionRoute: Renal (less than 10% as unchanged drug; metabolites excreted renally).
Unchanged: Less than 10%
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Pharmacodynamics

OnsetOfAction: 2-5 minutes (for local infiltration/nerve block).
PeakEffect: 5-15 minutes (for local infiltration/nerve block).
DurationOfAction: 30-60 minutes (without epinephrine); 2-6 hours (with epinephrine, depending on site and concentration).
Confidence: High

Safety & Warnings

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BLACK BOX WARNING

When lidocaine is used for epidural anesthesia, there have been rare reports of permanent injury or death following the use of lidocaine for obstetrical paracervical block. This is due to fetal bradycardia and acidosis. Lidocaine is also contraindicated for intravenous regional anesthesia (Bier block) in patients with known hypersensitivity to amide-type local anesthetics. Additionally, for oral viscous lidocaine, there is a warning regarding serious adverse events, including death, in infants and young children due to accidental ingestion or improper administration.
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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 immediately or seek emergency medical attention:

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: Difficulty breathing, slow breathing, or shallow breathing.
Neurological Symptoms: Feeling lightheaded, sleepy, confused, or experiencing blurred vision.
Cardiovascular Issues: Slow heartbeat.
Anxiety and Excitability: Feeling nervous and excitable.
Speech Difficulties: Trouble speaking.
Numbness or Tingling: A burning, numbness, or tingling sensation that is not normal.
Restlessness and Anxiety: Restlessness, anxiety, or changes in eyesight.
Other Symptoms: Ringing in the ears, dizziness or fainting, severe headache, twitching, shakiness, seizures, 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.
Mobility Issues: Inability to move or control bowel and bladder function.
Urinary Problems: Difficulty passing urine.

Other Possible Side Effects:

Not all side effects are severe, and many people may experience no side effects or only minor ones. If you notice any side effects that bother you or persist, contact your doctor for advice. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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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 (perioral numbness)
  • Metallic taste in the mouth
  • Blurred or double vision
  • Tremors or muscle twitching
  • Confusion or drowsiness
  • Difficulty breathing
  • Slow or irregular heartbeat
  • 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.

Specific Considerations for Spinal Injection:
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 to avoid potential interactions. Always verify the safety of taking this medication with your other treatments and health issues. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
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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 condition called methemoglobinemia can occur with the use of this drug. 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.

Post-Treatment Precautions
Avoid driving and other activities that require alertness until the effects of this medication have worn off and you feel fully awake. 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 (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 normal sensation and motor function have returned.

Mouth and Dental Procedures
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 (coma, respiratory arrest)
  • Generalized seizures
  • Profound hypotension
  • Bradycardia
  • Cardiac arrest
  • Ventricular arrhythmias

What to Do:

Call 911 immediately. Management involves airway management, oxygenation, seizure control (e.g., benzodiazepines), circulatory support (vasopressors, IV fluids), and potentially lipid emulsion therapy for severe systemic toxicity. Call 1-800-222-1222 (Poison Control) for advice.

Drug Interactions

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Major Interactions

  • Amiodarone (increased risk of cardiac depression)
  • Beta-blockers (e.g., Propranolol, Metoprolol - decreased lidocaine clearance, increased toxicity risk)
  • Cimetidine (decreased lidocaine clearance, increased toxicity risk)
  • Class I Antiarrhythmics (e.g., Procainamide, Quinidine, Disopyramide - additive cardiac effects, increased toxicity risk)
  • Phenytoin (increased risk of cardiac depression, altered lidocaine metabolism)
  • Succinylcholine (prolonged neuromuscular blockade)
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Moderate Interactions

  • Anticonvulsants (e.g., Carbamazepine, Phenobarbital - may increase lidocaine metabolism)
  • Diltiazem, Verapamil (may decrease lidocaine clearance)
  • Local anesthetics (additive effects, increased risk of systemic toxicity if combined with other local anesthetics)
  • MAOIs (potential for enhanced pressor effects if lidocaine contains epinephrine)
  • Nitrates (may reduce efficacy of lidocaine in some settings)
  • Opioids (additive CNS depression)
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Minor Interactions

  • Herbal supplements (e.g., St. John's Wort - potential for altered metabolism)

Monitoring

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Baseline Monitoring

Patient history (allergies, cardiac/hepatic/renal disease, medications)

Rationale: To identify contraindications, risk factors for toxicity, and potential drug interactions.

Timing: Prior to administration.

Vital Signs (HR, BP, RR, SpO2)

Rationale: To establish baseline and detect early signs of systemic toxicity.

Timing: Prior to administration.

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Routine Monitoring

Vital Signs (HR, BP, RR, SpO2)

Frequency: Every 5-15 minutes during and immediately after administration, then as clinically indicated.

Target: Within patient's normal limits.

Action Threshold: Significant deviations (e.g., bradycardia, hypotension, respiratory depression) or signs of CNS toxicity.

Neurological status (mental status, seizures, tremors)

Frequency: Continuously during and immediately after administration.

Target: Alert and oriented, no abnormal movements.

Action Threshold: Drowsiness, dizziness, tinnitus, perioral numbness, tremors, seizures.

ECG monitoring (for large doses or high-risk patients)

Frequency: Continuous during and immediately after administration.

Target: Normal sinus rhythm, no significant arrhythmias.

Action Threshold: Bradycardia, heart block, ventricular arrhythmias.

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Symptom Monitoring

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

Special Patient Groups

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Pregnancy

Category B. Lidocaine crosses the placenta. While generally considered safe for use during pregnancy when clinically indicated, especially for local/regional anesthesia, caution is advised. Fetal bradycardia and acidosis have been reported with paracervical block.

Trimester-Specific Risks:

First Trimester: No evidence of increased risk of congenital anomalies.
Second Trimester: Generally considered safe for use.
Third Trimester: Generally considered safe for use, but monitor for fetal bradycardia if used for obstetrical procedures.
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Lactation

Lidocaine is excreted into breast milk in small amounts. The amount ingested by the infant is very low and unlikely to cause adverse effects. Considered L2 (safer drug).

Infant Risk: Low risk of adverse effects to the breastfed infant. Monitor for drowsiness or feeding difficulties, though unlikely.
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Pediatric Use

Children, especially infants and neonates, are more susceptible to systemic toxicity due to immature hepatic metabolism and higher relative doses. Use the lowest effective dose and monitor closely. Avoid formulations with preservatives for spinal/epidural use.

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Geriatric Use

Elderly patients may have reduced hepatic blood flow and/or impaired renal function, leading to decreased clearance and increased risk of systemic toxicity. Use lower doses and monitor closely. More susceptible to CNS and cardiovascular effects.

Clinical Information

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Clinical Pearls

  • Xylocaine-MPF indicates 'Methylparaben Free', which is critical for epidural, spinal, or other neuraxial blocks to prevent neurotoxicity from preservatives.
  • Always aspirate before 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.
  • Systemic toxicity typically manifests as CNS symptoms first (e.g., perioral numbness, tinnitus, lightheadedness, seizures), followed by cardiovascular depression (e.g., bradycardia, hypotension, arrhythmias, cardiac arrest).
  • Lipid emulsion therapy (Intralipid) is an antidote for severe local anesthetic systemic toxicity (LAST).
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Alternative Therapies

  • Bupivacaine (longer acting local anesthetic)
  • Ropivacaine (longer acting local anesthetic, less cardiotoxic than bupivacaine)
  • Mepivacaine (intermediate acting local anesthetic)
  • Chloroprocaine (short acting ester local anesthetic)
  • Procaine (short acting ester local anesthetic)
  • Non-pharmacological pain management techniques
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Cost & Coverage

Average Cost: Price varies significantly by concentration, volume, and supplier. Generally very inexpensive. per vial/ampule
Generic Available: Yes
Insurance Coverage: Tier 1 (Generic)
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General Drug Facts

If your symptoms or health problems do not improve or worsen over time, it is essential to contact your doctor for further evaluation and guidance. To ensure safe use, never share your prescription medications with others, and do not take medications prescribed to someone else.

Store all medications in a secure location, out of the reach of children and pets, to prevent accidental ingestion. Properly dispose of unused or expired medications. Unless instructed otherwise by a healthcare professional or pharmacist, do not dispose of medications by flushing them down the toilet or pouring them down the drain. If you are unsure about the correct disposal method, consult with your pharmacist, who can provide guidance on safe disposal practices and inform you about potential drug take-back programs in your area.

Some medications may come with an additional patient information leaflet; check with your pharmacist to see if this applies to your prescription. 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 was taken, to ensure prompt and effective treatment.