Xylocaine-Mpf 1% Inj, 30ml

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
Dec 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 stitches, minor surgery, or dental work. It works by temporarily blocking nerve signals in the area where it's injected, so you don't feel pain.
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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 immediately to receive guidance on the appropriate course of action.
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Lifestyle & Tips

  • Avoid touching or putting pressure on the numb area until sensation returns to prevent injury.
  • Follow post-procedure instructions carefully, especially regarding activity restrictions or wound care.

Dosing & Administration

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Adult Dosing

Standard Dose: Highly variable based on procedure, site, and individual patient factors. 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).

Condition-Specific Dosing:

infiltration: 0.5% to 1% solution; up to 4.5 mg/kg (max 300 mg) without epinephrine, or 7 mg/kg (max 500 mg) with epinephrine.
peripheralNerveBlock: 1% to 2% solution; 50-300 mg depending on nerve block.
epiduralBlock: 1% to 2% solution; 10-20 mL (100-400 mg) for lumbar/thoracic, 2-3 mL (20-30 mg) per segment for intercostal.
caudalBlock: 1% solution; 15-30 mL (150-300 mg).
intravenousRegionalAnesthesia: 0.5% solution; 1.5-3 mg/kg (max 300 mg).
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Pediatric Dosing

Neonatal: Not established for routine use; extreme caution due to immature hepatic function and higher risk of systemic toxicity. Max single dose 2-3 mg/kg.
Infant: Max single dose 3-5 mg/kg (without epinephrine), not to exceed 300 mg. Use lowest effective concentration and volume.
Child: Max single dose 3-5 mg/kg (without epinephrine), not to exceed 300 mg. Use lowest effective concentration and volume.
Adolescent: Max single dose 3-5 mg/kg (without 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 for local anesthetic use.
Moderate: No specific adjustment generally needed for local anesthetic use.
Severe: No specific adjustment generally needed for local anesthetic use, but monitor for signs of systemic toxicity if large doses or repeated administration.
Dialysis: Lidocaine is not significantly dialyzable. No specific adjustment for local anesthetic use, but caution with repeated doses.

Hepatic Impairment:

Mild: Consider dose reduction (e.g., 25% reduction) and careful monitoring.
Moderate: Significant dose reduction (e.g., 50% reduction) recommended. Monitor plasma levels if possible.
Severe: Contraindicated or extreme caution with significant dose reduction. Monitor plasma levels 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 blocking nerve impulse conduction. It specifically blocks voltage-gated sodium channels, preventing depolarization and propagation of action potentials.
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Pharmacokinetics

Absorption:

Bioavailability: Varies significantly by site of administration (e.g., 3% oral, 50-100% topical/mucosal, nearly 100% IV). For local injection, absorption is rapid and complete from the injection site, depending on vascularity.
Tmax: Varies by route: 5-15 minutes (epidural), 60-90 minutes (subcutaneous).
FoodEffect: Not applicable for injectable formulation.

Distribution:

Vd: 0.7-2.7 L/kg (adults); higher in neonates and infants.
ProteinBinding: 60-80% (primarily to alpha-1-acid glycoprotein and albumin); concentration-dependent.
CnssPenetration: Yes (readily crosses blood-brain barrier and placenta).

Elimination:

HalfLife: 1.5-2 hours (adults); prolonged in neonates, elderly, and patients with hepatic impairment or CHF.
Clearance: Approximately 10 mL/min/kg.
ExcretionRoute: Renal (less than 10% unchanged drug, metabolites excreted renally).
Unchanged: Less than 10%
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Pharmacodynamics

OnsetOfAction: 2-5 minutes (infiltration, nerve block); 5-15 minutes (epidural).
PeakEffect: Varies by route and dose; generally within 10-30 minutes for local anesthesia.
DurationOfAction: 30-60 minutes (without epinephrine); 60-120 minutes (with epinephrine).

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 immediately or seek emergency medical attention:

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, including:
+ 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, slow breathing, or shallow 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 extremely hot or cold
+ Metallic taste
+ Chest pain
+ Mood changes

Additional Side Effects

As with any medication, some people may experience side effects. If you notice any of the following symptoms, contact your doctor:

* Injection site reactions (if administered into the spine), such as:
+ Erectile dysfunction
+ Loss of mobility
+ Loss of bladder or bowel control
+ Urination difficulties

Reporting Side Effects

If you experience any side effects that bother you or do not go away, contact your doctor. 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
  • Blurred vision or double vision
  • Tremors or muscle twitching
  • Confusion or drowsiness
  • Unusual tiredness or weakness
  • 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, including any symptoms that occurred.
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 essential to disclose all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, as well as any existing health problems. This information will help your doctor and pharmacist assess potential interactions and ensure safe use of this medication. Do not initiate, discontinue, or modify 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 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 under 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 other 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 sensation has returned.

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 sensation 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 until the numbness in your mouth has resolved, as you may inadvertently bite your tongue.
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Overdose Information

Overdose Symptoms:

  • Severe dizziness or lightheadedness
  • Profound drowsiness or unconsciousness
  • Seizures
  • Slow or irregular heartbeat (bradycardia)
  • Very low blood pressure (hypotension)
  • Cardiac arrest
  • Respiratory arrest

What to Do:

Seek immediate medical attention. Call 911 or your local emergency number. In the US, you can also call Poison Control at 1-800-222-1222.

Drug Interactions

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Major Interactions

  • Class I antiarrhythmics (e.g., mexiletine, procainamide, quinidine, disopyramide): Increased risk of cardiac depression and arrhythmias.
  • Amiodarone: Increased risk of cardiac depression and arrhythmias.
  • Beta-blockers (e.g., propranolol, metoprolol): May decrease lidocaine clearance, leading to increased lidocaine levels and toxicity.
  • Cimetidine: May decrease lidocaine clearance, leading to increased lidocaine levels and toxicity.
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Moderate Interactions

  • Succinylcholine: Prolonged neuromuscular blockade.
  • Phenytoin: May alter lidocaine metabolism.
  • CYP1A2/CYP3A4 inhibitors (e.g., macrolide antibiotics, azole antifungals, protease inhibitors): May increase lidocaine levels.
  • CYP1A2/CYP3A4 inducers (e.g., rifampin, carbamazepine, phenobarbital): May decrease lidocaine levels.
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Minor Interactions

  • Other local anesthetics: Additive systemic toxicity.
  • Skeletal muscle relaxants: Potentiation of muscle relaxation.

Monitoring

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Baseline Monitoring

Allergy history

Rationale: To identify hypersensitivity reactions to lidocaine or other amide-type local anesthetics.

Timing: Prior to administration

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

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

Timing: Prior to administration

Patient's general condition and comorbidities

Rationale: To assess risk factors for toxicity (e.g., hepatic impairment, cardiac disease, elderly, pediatric).

Timing: Prior to administration

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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; significant deviations should prompt investigation.

Action Threshold: Bradycardia, hypotension, hypertension, or respiratory depression.

Neurological status (e.g., dizziness, tinnitus, perioral numbness, confusion, tremors, seizures)

Frequency: Continuously during and for several hours after administration.

Target: Absence of CNS symptoms.

Action Threshold: Any new or worsening CNS symptoms.

ECG monitoring (if large doses or systemic absorption is a concern)

Frequency: Continuous during and after administration.

Target: Normal sinus rhythm; absence of arrhythmias or conduction disturbances.

Action Threshold: Bradycardia, heart block, QRS widening, ventricular arrhythmias.

Injection site for local reactions (e.g., swelling, redness, pain)

Frequency: Visually inspect during and after procedure.

Target: Minimal local reaction.

Action Threshold: Excessive swelling, pain, or signs of infection.

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Symptom Monitoring

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

Special Patient Groups

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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, especially for local anesthesia.

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 and may cause fetal bradycardia or CNS depression if high maternal levels occur, especially during labor and delivery.
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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 rated L2 (likely compatible) by LactMed. Caution is advised, but generally considered safe for nursing mothers.

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

Pediatric patients, especially neonates and infants, are more susceptible to systemic toxicity due to immature hepatic function, higher body water content, and potentially higher peak plasma concentrations. Dosing must be carefully calculated based on weight, and the lowest effective dose should be used. Monitor closely for signs of CNS and cardiovascular toxicity.

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Geriatric Use

Elderly patients may have reduced hepatic function, decreased plasma protein binding, and reduced renal clearance, leading to increased plasma concentrations and prolonged half-life. A reduced dose may be necessary, and careful monitoring for systemic toxicity is crucial. Start with lower doses and titrate slowly.

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 be avoided 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, dizziness, seizures), followed by cardiovascular effects (e.g., bradycardia, hypotension, arrhythmias, cardiac arrest).
  • Lipid emulsion therapy (Intralipid) is an antidote for severe local anesthetic systemic toxicity (LAST).
  • Xylocaine-MPF (Methylparaben Free) formulations are typically used for neuraxial (epidural, spinal) anesthesia to avoid neurotoxicity associated with preservatives.
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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 local anesthetic)
  • Procaine (ester-type local anesthetic)
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Cost & Coverage

Average Cost: Varies widely by supplier and contract per 30ml vial
Generic Available: Yes
Insurance Coverage: Generally covered by most insurance plans, often as a Tier 1 or Tier 2 medication, especially for in-office procedures or hospital use.
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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 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 proper disposal method, consult your pharmacist, who can also inform you about potential drug take-back programs in your area. Additionally, some medications may come with 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 quantity, and the time of the incident.