Xylocaine-Mpf 1% 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 1970
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Lidocaine is a medicine that numbs a specific area of your body to prevent pain during medical procedures, like stitches or minor surgery. 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.

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

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

Dosing & Administration

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Adult Dosing

Standard Dose: Highly variable based on procedure, site, and concentration. Max single dose typically 4.5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine), not exceeding 300-500 mg.

Condition-Specific Dosing:

infiltration: 0.5% to 1% solution; up to 4.5 mg/kg (max 300 mg)
peripheral nerve block: 1% to 2% solution; up to 4.5 mg/kg (max 300 mg)
epidural block: 1% to 2% solution; 200-300 mg (e.g., 10-20 mL of 1% or 2% solution)
caudal block: 1% solution; 15-30 mL (150-300 mg)
spinal block: Not typically used for spinal anesthesia; hyperbaric lidocaine is used for this purpose.
intravenous regional anesthesia (Bier block): 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. Max 2-4 mg/kg.
Infant: Max 4.5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine) per single dose. Not to exceed 300 mg. Dosing must be individualized based on weight and procedure.
Child: Max 4.5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine) per single dose. Not to exceed 300 mg. Dosing must be individualized based on weight and procedure.
Adolescent: Max 4.5 mg/kg (without epinephrine) or 7 mg/kg (with epinephrine) per single dose. Not to exceed 300 mg. Dosing must be individualized based on weight and procedure.
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment typically required.
Moderate: No specific adjustment typically required, but monitor for signs of toxicity.
Severe: Use with caution; consider reduced doses due to accumulation of active metabolites (MEGX, GX) and potential for increased free drug concentration. Monitor closely.
Dialysis: Lidocaine is not significantly removed by hemodialysis. Use with caution in ESRD; monitor for toxicity.

Hepatic Impairment:

Mild: Consider reduced dose; monitor for toxicity.
Moderate: Significant dose reduction (e.g., 50%) may be necessary due to impaired metabolism. Monitor plasma levels if possible.
Severe: Contraindicated or use with extreme caution at significantly reduced doses. Monitor closely 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 blocking nerve impulse conduction. It primarily acts by reversibly blocking 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: Highly variable depending on administration route (e.g., 35% oral due to first-pass, nearly 100% IV, variable for local injection based on vascularity of site).
Tmax: Varies by route: IV (minutes), local infiltration (5-15 minutes), epidural (10-20 minutes).
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). Binding is concentration-dependent and can be reduced in renal/hepatic impairment.
CnssPenetration: Yes, readily crosses the blood-brain barrier and placenta.

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: Rapid; 2-5 minutes for local infiltration/nerve block, 5-15 minutes for epidural.
PeakEffect: Varies by route and concentration; generally within 10-30 minutes.
DurationOfAction: 30-60 minutes (without epinephrine); 60-120 minutes (with epinephrine, depending on site and concentration).

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 when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate 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 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 mobility
Loss of bowel or bladder control
Urination difficulties

Other Possible Side Effects

As with any medication, you may experience side effects. While many people do not experience significant side effects, some may have mild or moderate reactions. If you notice any side effects that bother you or persist, contact your doctor for guidance.

Remember, this is not an exhaustive list of potential side effects. If you have concerns or questions, 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.
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Seek Immediate Medical Attention If You Experience:

  • Feeling dizzy or lightheaded
  • Ringing in your ears (tinnitus)
  • Numbness or tingling around your mouth
  • Metallic taste in your mouth
  • Blurred 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 reactions you experienced.
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 crucial to disclose all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, as well as any health problems you are experiencing. This will enable your doctor and pharmacist to assess potential interactions and ensure safe use of this medication. 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

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 before using this medication, as some products may contain sulfites.

Caution with Daily Activities
Avoid driving and engaging in 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 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 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
  • Confusion
  • Slurred speech
  • Severe tremors or muscle twitching
  • Seizures
  • Unconsciousness
  • Slow or irregular heartbeat
  • Low blood pressure
  • Cardiac arrest
  • Respiratory depression or arrest

What to Do:

Seek immediate medical attention. Call 911 or your local emergency number. For poison control, call 1-800-222-1222.

Drug Interactions

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Major Interactions

  • Amiodarone (increased risk of cardiac depression/arrhythmias)
  • Other Class I antiarrhythmics (e.g., procainamide, quinidine, disopyramide - additive cardiac effects)
  • Flecainide (additive cardiac effects)
  • Propafenone (additive cardiac effects)
  • Beta-blockers (e.g., propranolol, metoprolol - decreased hepatic clearance of lidocaine, leading to increased lidocaine levels and toxicity)
  • Cimetidine (decreased hepatic clearance of lidocaine, leading to increased lidocaine levels and toxicity)
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Moderate Interactions

  • Phenytoin (may alter lidocaine metabolism)
  • Succinylcholine (prolonged neuromuscular blockade)
  • Diltiazem, Verapamil (may decrease lidocaine clearance)
  • Rifampin (may increase lidocaine clearance)
  • Erythromycin (may inhibit lidocaine metabolism)
  • Ritonavir (may inhibit lidocaine metabolism)
  • St. John's Wort (may induce lidocaine metabolism)
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Minor Interactions

  • Local anesthetics of the ester type (e.g., procaine - competition for metabolism)

Monitoring

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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 immediate adverse reactions.

Timing: Prior to administration

ECG (if large doses or IV administration)

Rationale: To assess cardiac conduction and rhythm, especially if systemic absorption is anticipated or for antiarrhythmic use.

Timing: Prior to administration

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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; report significant deviations.

Action Threshold: Hypotension, bradycardia, or significant arrhythmias; signs of CNS toxicity.

Neurological status (CNS toxicity signs)

Frequency: Continuously during and after administration.

Target: Alert, oriented, no tremors, dizziness, or seizures.

Action Threshold: Drowsiness, dizziness, tinnitus, perioral numbness, muscle twitching, seizures.

ECG monitoring (if large doses or IV administration)

Frequency: Continuous during and immediately after administration.

Target: Normal sinus rhythm, no significant conduction delays or 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
  • Drowsiness
  • Confusion
  • Seizures
  • Bradycardia
  • Hypotension
  • Cardiac arrest

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; commonly used for epidural anesthesia during labor. Monitor for fetal bradycardia.
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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 (safer drug) by LactMed. Breastfeeding can usually be continued after lidocaine administration.

Infant Risk: Low risk of adverse effects to the breastfed infant.
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Pediatric Use

Use with caution. Dosing must be carefully calculated based on the child's weight and age to avoid systemic toxicity. Neonates and infants may have reduced protein binding and immature hepatic metabolism, increasing their susceptibility to toxicity. Monitor closely for signs of CNS and cardiovascular toxicity.

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Geriatric Use

Use with caution. Elderly patients may have reduced hepatic blood flow, decreased protein binding, and reduced renal function, leading to decreased clearance and increased plasma concentrations of lidocaine. Consider lower doses and monitor closely for signs of toxicity.

Clinical Information

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Clinical Pearls

  • Xylocaine-MPF (Methylparaben-Free) is crucial for epidural and spinal anesthesia to avoid neurotoxic effects associated with methylparaben.
  • 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.
  • Signs of systemic toxicity progress from CNS (lightheadedness, tinnitus, perioral numbness, tremors, seizures) to cardiovascular (bradycardia, hypotension, arrhythmias, cardiac arrest).
  • Lipid emulsion therapy (Intralipid) is the 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)
  • Prilocaine (intermediate acting local anesthetic, risk of methemoglobinemia)
  • Chloroprocaine (short acting local anesthetic, ester type)
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Cost & Coverage

Average Cost: Varies widely by supplier and volume (e.g., $5-$50 per 25-50 mL vial of 1% solution) per vial/ampule
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 persist or worsen, it is essential to contact your doctor for further evaluation and guidance. To ensure safe and effective treatment, never share your medication with others, and do not take medication prescribed for someone else.

Store all medications in a secure location, out of the reach of children and pets, to prevent accidental ingestion. Dispose of unused or expired medications properly. Unless instructed to do so by a healthcare professional or pharmacist, do not flush medications down the toilet or drain. If you are unsure about the proper 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 for more information. 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 information about the medication taken, including the dosage, time of ingestion, and any other relevant details to ensure prompt and effective treatment.