Xylocaine-Mpf 1% Inj, 10ml

Manufacturer FRESENIUS KABI USA 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
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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
Jan 1970
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DEA Schedule
Not Controlled

Overview

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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 like stitches, minor surgery, or dental work. 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 guidelines 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

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

Dosing & Administration

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Adult Dosing

Standard Dose: Varies significantly by procedure and site of injection. For local infiltration with 1% solution: typically 5-30 mL (50-300 mg).
Dose Range: 50 - 300 mg

Condition-Specific Dosing:

local_infiltration_without_epinephrine: Maximum single dose: 4.5 mg/kg (not to exceed 300 mg). For 1% solution, this is up to 30 mL.
local_infiltration_with_epinephrine: Maximum single dose: 7 mg/kg (not to exceed 500 mg). For 1% solution, this is up to 50 mL.
nerve_block: Varies by block type (e.g., intercostal, brachial plexus, epidural). Consult specific guidelines.
epidural_anesthesia: Typically 200-300 mg (20-30 mL of 1% solution) for lumbar epidural, not to exceed 300 mg.
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Pediatric Dosing

Neonatal: Not established for routine use; extreme caution and reduced doses if used. Max 2-3 mg/kg.
Infant: Maximum single dose: 3-5 mg/kg (without epinephrine), 5-7 mg/kg (with epinephrine). Not to exceed 300 mg total.
Child: Maximum single dose: 3-5 mg/kg (without epinephrine), 5-7 mg/kg (with epinephrine). Not to exceed 300 mg total.
Adolescent: Maximum single dose: 3-5 mg/kg (without epinephrine), 5-7 mg/kg (with epinephrine). Not to exceed 300 mg total.
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment for single-dose local anesthesia.
Moderate: No specific adjustment for single-dose local anesthesia; caution with repeated doses or large volumes due to potential accumulation of metabolites.
Severe: No specific adjustment for single-dose local anesthesia; caution with repeated doses or large volumes due to potential accumulation of metabolites.
Dialysis: Lidocaine is not significantly removed by hemodialysis. Use with caution, monitor for toxicity.

Hepatic Impairment:

Mild: No specific adjustment for single-dose local anesthesia.
Moderate: Reduced doses may be necessary due to impaired metabolism and prolonged half-life. Monitor for signs of toxicity.
Severe: Significant dose reduction is necessary due to severely impaired metabolism. Monitor closely for toxicity. Consider alternative anesthetics.
Confidence: Medium

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 propagation of action potentials.
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Pharmacokinetics

Absorption:

Bioavailability: Not applicable for local injection; systemic absorption varies widely based on site of injection, vascularity, dose, and presence of vasoconstrictors (e.g., epinephrine).
Tmax: Highly variable; typically 5-15 minutes for onset, peak plasma levels can occur within 10-60 minutes depending on site.
FoodEffect: Not applicable

Distribution:

Vd: 0.7-2.7 L/kg
ProteinBinding: 60-80% (primarily to alpha-1-acid glycoprotein)
CnssPenetration: Yes (readily crosses blood-brain barrier if systemic levels are high)

Elimination:

HalfLife: 1.5-2 hours (prolonged in hepatic impairment or heart failure)
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; typically 2-5 minutes for local infiltration.
PeakEffect: Variable; depends on site of injection and presence of vasoconstrictor. Peak systemic levels usually within 10-60 minutes.
DurationOfAction: 0.5-3 hours (without epinephrine); 1-6 hours (with epinephrine), depending on dose, concentration, and site.

Safety & Warnings

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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:
+ 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 life-threatening condition):
+ 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
+ Shortness of breath
Signs of acidosis (too much acid in the blood):
+ Confusion
+ Rapid breathing
+ Rapid heartbeat
+ Abnormal heartbeat
+ Severe stomach pain, nausea, or vomiting
+ Excessive sleepiness
+ Shortness of breath
+ Feeling tired or weak
Other severe side effects:
+ Trouble breathing, slow breathing, or shallow breathing
+ Feeling lightheaded, sleepy, confused, or having blurred vision
+ Slow heartbeat
+ Feeling nervous and excitable
+ Trouble speaking
+ Burning, numbness, or tingling sensation
+ Restlessness
+ Anxiety
+ Changes in vision
+ Ringing in the ears
+ Dizziness or fainting
+ Severe headache
+ Twitching
+ Shakiness
+ Seizures
+ Feeling hot or cold
+ Metallic taste
+ Chest pain
+ Mood changes

Additional Side Effects of Spinal Injection

If you receive this medication via spinal injection, you may experience:

Erectile dysfunction
Loss of movement
Loss of bladder or bowel control
Trouble urinating

Other Possible Side Effects

Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to contact your doctor if you have any concerns. If you experience any side effects that bother you or do not go away, seek medical attention.

Reporting Side Effects

You can report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch. If you have questions about side effects, contact your doctor for medical advice.
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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
  • Unusual taste in the mouth (metallic taste)
  • Blurred vision or double vision
  • Tremors or muscle twitching
  • Feeling unusually sleepy or confused
  • Slow or irregular heartbeat
  • Difficulty breathing
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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.
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 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 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 while your mouth is numb, as you may inadvertently bite your tongue.
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Overdose Information

Overdose Symptoms:

  • Severe dizziness or lightheadedness
  • Seizures
  • Unconsciousness
  • Respiratory arrest (stopping breathing)
  • Severe low blood pressure (hypotension)
  • Bradycardia (slow heart rate)
  • Cardiac arrest

What to Do:

Seek immediate medical attention. Call 911 or your local emergency number. In the US, you can call Poison Control at 1-800-222-1222. Management involves supportive care, maintaining airway and breathing, managing seizures (e.g., with benzodiazepines), and treating cardiovascular collapse (e.g., with IV fluids, vasopressors, lipid emulsion therapy).

Drug Interactions

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Major Interactions

  • Antiarrhythmics (e.g., Class I antiarrhythmics like mexiletine, tocainide): Increased risk of cardiac depression and toxicity.
  • Beta-blockers (e.g., propranolol, metoprolol): May reduce hepatic blood flow, leading to decreased lidocaine clearance and increased plasma levels.
  • Cimetidine: Inhibits lidocaine metabolism, increasing plasma levels and risk of toxicity.
  • Other local anesthetics: Additive systemic toxicity.
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Moderate Interactions

  • Succinylcholine: Lidocaine may prolong the neuromuscular blockade of succinylcholine.
  • Phenytoin: May increase lidocaine metabolism; also, both can cause cardiac depression.
  • Amiodarone: Increased risk of cardiac effects.
  • CYP1A2 inhibitors (e.g., fluvoxamine, ciprofloxacin): May increase lidocaine levels.
  • CYP3A4 inhibitors (e.g., macrolide antibiotics, azole antifungals, protease inhibitors): May increase lidocaine levels.

Monitoring

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Baseline Monitoring

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

Rationale: To identify contraindications, precautions, and potential for altered drug metabolism/elimination.

Timing: Prior to administration

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

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

Timing: Prior to administration

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Routine Monitoring

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

Frequency: During and immediately after administration, then as clinically indicated.

Target: Within patient's normal range; significant deviations warrant investigation.

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

Neurological status (mental status, presence of dizziness, tinnitus, perioral numbness, tremors)

Frequency: During and immediately after administration, then as clinically indicated.

Target: Alert and oriented, absence of CNS symptoms.

Action Threshold: Signs of CNS excitation (e.g., tremors, seizures) or depression (e.g., somnolence, respiratory depression).

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

Frequency: Continuous during administration of large doses or in patients with cardiac disease.

Target: Normal sinus rhythm; absence of arrhythmias.

Action Threshold: Arrhythmias (e.g., 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
  • Hypotension
  • Bradycardia
  • Arrhythmias
  • Respiratory depression or arrest

Special Patient Groups

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Pregnancy

Lidocaine is generally considered safe for use during pregnancy when administered in appropriate doses for local anesthesia. It is classified as Pregnancy Category B.

Trimester-Specific Risks:

First Trimester: No evidence of increased risk of congenital anomalies.
Second Trimester: Generally considered safe.
Third Trimester: Generally considered safe; commonly used for epidural anesthesia during labor. Fetal bradycardia has been reported with paracervical block.
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Lactation

Lidocaine is excreted into breast milk in small amounts. However, the amount transferred to the infant is generally considered too small to cause adverse effects. It is rated L2 (safer) by LactMed.

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

Pediatric patients, especially infants and young children, are more susceptible to systemic toxicity due to differences in metabolism, distribution, and higher relative doses per body weight. Dosing must be carefully calculated based on weight, and the lowest effective dose should be used. Close monitoring for signs of toxicity is crucial.

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Geriatric Use

Elderly patients may be more susceptible to systemic toxicity due to age-related decreases in hepatic blood flow, reduced metabolic capacity, and potential for polypharmacy. Lower doses and slower administration rates may be necessary. Monitor closely for CNS and cardiovascular effects.

Clinical Information

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Clinical Pearls

  • Always aspirate prior to injection to ensure the needle is not in a blood vessel, especially when administering large volumes or in highly vascular areas.
  • The maximum dose of lidocaine should never be exceeded. Calculate the dose carefully based on the patient's weight and the concentration of the solution.
  • Adding epinephrine prolongs the duration of action and reduces systemic absorption, but it should not be used in areas with end-arterial blood supply (e.g., fingers, toes, nose, penis, ears) due to risk of ischemia.
  • Monitor patients for early signs of systemic toxicity (e.g., perioral numbness, tinnitus, dizziness) and intervene promptly.
  • Xylocaine-MPF (Methylparaben Free) is preferred for epidural or spinal anesthesia to avoid potential neurotoxicity associated with methylparaben.
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Alternative Therapies

  • Bupivacaine (longer duration of action)
  • Ropivacaine (less cardiotoxic than bupivacaine)
  • Mepivacaine (similar onset and duration to lidocaine, less vasodilation)
  • Prilocaine (lower CNS toxicity, but risk of methemoglobinemia with high doses)
  • Chloroprocaine (very short duration, rapid metabolism)
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Cost & Coverage

Average Cost: Highly variable per 10mL vial
Generic Available: Yes
Insurance Coverage: Generally covered by most insurance plans as a generic injectable.
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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, do not share your medication with others, and never take someone else's medication. Store all medications in a secure location, out of the reach of children and pets, to prevent accidental ingestion.

Proper disposal of unused or expired medications is crucial. Do not flush medications down the toilet or pour them down the drain unless specifically instructed to do so by a healthcare professional or pharmacist. If you are unsure about the best method for disposing of medications, consult with your pharmacist, who can provide guidance on safe disposal practices. Additionally, you may want to inquire about potential drug take-back programs in your area.

Some medications may come with an additional patient information leaflet. If you have questions or concerns about your medication, it is recommended that you consult with your pharmacist, doctor, nurse, 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, including the dosage, time of ingestion, and any other relevant details.