Xylocaine-Mpf 0.5% Inj, 50ml

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 to prevent pain during medical procedures, minor surgeries, or to relieve pain from certain conditions. 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.

For storage and disposal, consult with your doctor, nurse, or pharmacist to determine the best approach if you need to keep 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 symptoms or discomfort during or after the procedure.
  • Avoid touching or putting pressure on the numb area until sensation returns to prevent injury.

Dosing & Administration

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Adult Dosing

Standard Dose: Varies significantly by procedure and site of injection. For infiltration anesthesia with 0.5% solution: up to 300 mg (60 mL) without epinephrine, or up to 500 mg (100 mL) with epinephrine.

Condition-Specific Dosing:

infiltration_anesthesia_0.5%_without_epinephrine: Max 300 mg (60 mL)
infiltration_anesthesia_0.5%_with_epinephrine: Max 500 mg (100 mL)
nerve_block_brachial_plexus: 250-500 mg (50-100 mL of 0.5%)
epidural_anesthesia: 200-300 mg (40-60 mL of 0.5% or 1%)
caudal_anesthesia: 150-200 mg (30-40 mL of 0.5% or 1%)
spinal_anesthesia: 50-100 mg (10-20 mL of 0.5% or 1%)
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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).
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 typically needed for single-dose local anesthesia.
Moderate: No specific adjustment typically needed for single-dose local anesthesia.
Severe: Use with caution; consider lower doses due to potential accumulation of active metabolites. Monitor for toxicity.
Dialysis: Lidocaine is not significantly dialyzable. Use with caution, monitor for toxicity.

Hepatic Impairment:

Mild: Use with caution; consider lower doses.
Moderate: Reduce dose by 50% or more; monitor for toxicity. Prolonged half-life expected.
Severe: Contraindicated or significantly reduced dose (e.g., 75% reduction); monitor closely for toxicity. Prolonged half-life expected.

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 propagation of action potentials.
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Pharmacokinetics

Absorption:

Bioavailability: Highly variable depending on site of administration (e.g., 35% oral, nearly 100% IV, variable for local infiltration based on vascularity and presence of vasoconstrictor).
Tmax: Variable; 5-15 minutes for infiltration, longer for nerve blocks.
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 neonates)
Clearance: Approximately 10 mL/min/kg
ExcretionRoute: Renal (less than 10% unchanged)
Unchanged: Less than 10%
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Pharmacodynamics

OnsetOfAction: 2-5 minutes (for infiltration)
PeakEffect: 5-15 minutes
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 or seek immediate medical attention:

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 discoloration 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:
+ Breathing difficulties, slow breathing, or shallow breathing
+ Feeling lightheaded, sleepy, confused, or experiencing blurred vision
+ Slow heartbeat
+ Feeling nervous or excitable
+ Speech difficulties
+ Abnormal burning, numbness, or tingling sensations
+ 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

Additional Side Effects to Discuss with Your Doctor

If you are receiving this medication via spinal injection, you may also experience:

Erectile dysfunction
Loss of mobility
Loss of bladder or bowel control
Urination difficulties

Other Possible Side Effects

As with any medication, you may experience side effects that are not listed here. If you notice any symptoms that bother you or persist, contact your doctor for guidance. 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
  • Numbness or tingling around the mouth
  • Metallic taste in the mouth
  • Ringing in the ears (tinnitus)
  • Blurred vision or double vision
  • Slurred speech
  • 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 reactions you experienced.
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. They will help determine if it is safe to take this medication alongside your other treatments. 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 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 you have regained sensation.

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 while your mouth is numb, as you may accidentally 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
  • Slow heart rate (bradycardia)
  • Cardiac arrest

What to Do:

Immediate medical attention is required. Call 911 or emergency services. Management involves stopping the administration, ensuring airway patency, providing oxygen, managing seizures (e.g., with benzodiazepines), treating hypotension (e.g., with vasopressors), and managing arrhythmias. Intravenous lipid emulsion therapy may be considered for severe systemic toxicity.

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 Class I Antiarrhythmics (e.g., Procainamide, Quinidine, Disopyramide - additive cardiac effects, increased toxicity risk)
  • Succinylcholine (prolonged neuromuscular blockade)
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Moderate Interactions

  • Phenytoin (increased lidocaine metabolism, potential for reduced effect; also additive cardiac effects)
  • Rifampin (increased lidocaine metabolism, potential for reduced effect)
  • Erythromycin (potential for increased lidocaine levels)
  • Diltiazem, Verapamil (potential for increased lidocaine levels)
  • Local anesthetics (additive systemic toxicity if multiple agents used)
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Minor Interactions

  • Not available

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 (BP, HR, RR)

Rationale: To establish baseline and monitor for systemic effects.

Timing: Prior to administration

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Routine Monitoring

Signs of CNS toxicity (e.g., lightheadedness, dizziness, tinnitus, perioral numbness, tremors, seizures)

Frequency: Continuously during and immediately after administration, then periodically for several hours.

Target: Absence of symptoms

Action Threshold: Any new or worsening CNS symptom warrants immediate intervention (stop infusion, provide supportive care).

Signs of cardiovascular toxicity (e.g., hypotension, bradycardia, arrhythmias, cardiac arrest)

Frequency: Continuously during and immediately after administration, then periodically for several hours.

Target: Stable vital signs, normal ECG rhythm

Action Threshold: Significant changes in vital signs or new arrhythmias warrant immediate intervention.

Pain relief/anesthetic effect

Frequency: As needed to assess efficacy.

Target: Adequate anesthesia for procedure

Action Threshold: Inadequate anesthesia may require re-dosing or alternative approach.

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Symptom Monitoring

  • Lightheadedness
  • Dizziness
  • Tinnitus
  • Perioral numbness
  • Metallic taste
  • Slurred speech
  • Nystagmus
  • Tremors
  • Muscle twitching
  • Seizures
  • Drowsiness
  • Unconsciousness
  • Respiratory depression/arrest
  • Hypotension
  • Bradycardia
  • Cardiac arrhythmias
  • Cardiac arrest

Special Patient Groups

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Pregnancy

Generally considered safe for use as a local anesthetic during pregnancy when administered in appropriate doses. Category B. Studies in animals have not shown fetal harm, and human data suggest no increased risk of congenital anomalies.

Trimester-Specific Risks:

First Trimester: Low risk; no evidence of teratogenicity.
Second Trimester: Low risk.
Third Trimester: Low risk; commonly used for epidural anesthesia during labor. Monitor for maternal hypotension and fetal bradycardia.
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Lactation

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

Infant Risk: Low risk. Monitor infant for drowsiness or feeding difficulties, though unlikely.
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Pediatric Use

Use with caution. Children, especially infants, may be more susceptible to systemic toxicity due to differences in metabolism and distribution. Dosing must be carefully calculated based on weight (mg/kg) and maximum recommended doses should not be exceeded. Avoid concentrations higher than necessary. Monitor closely for signs of systemic toxicity.

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Geriatric Use

Use with caution. Elderly patients may have reduced hepatic or renal function, decreased protein binding, and increased sensitivity to the systemic effects of lidocaine. Consider lower doses and monitor closely for toxicity. Reduced lean body mass and cardiac output may also affect pharmacokinetics.

Clinical Information

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Clinical Pearls

  • Always aspirate prior to injection to avoid intravascular administration, which can lead to rapid systemic toxicity.
  • The addition of epinephrine prolongs the duration of action and reduces systemic absorption, allowing for higher total doses, but should not be used in areas with end-arterial circulation (e.g., fingers, toes, nose, penis, earlobe) due to risk of ischemia.
  • Systemic toxicity typically manifests as CNS symptoms first (e.g., perioral numbness, tinnitus, lightheadedness), followed by more severe CNS effects (seizures) and then cardiovascular depression.
  • The 'MPF' in Xylocaine-MPF stands for 'Methylparaben Free', which is important for certain uses like epidural or spinal anesthesia where preservatives can be neurotoxic.
  • Ensure resuscitation equipment and medications (e.g., lipid emulsion, benzodiazepines) are readily available when administering large volumes or high concentrations of lidocaine.
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Alternative Therapies

  • Bupivacaine (longer duration, higher potency)
  • Ropivacaine (similar to bupivacaine, less cardiotoxic)
  • Mepivacaine (intermediate duration)
  • Prilocaine (intermediate duration, risk of methemoglobinemia at high doses)
  • Chloroprocaine (short duration, ester type)
  • Topical anesthetics (e.g., EMLA cream, lidocaine patches for surface anesthesia)
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Cost & Coverage

Average Cost: Varies widely by concentration, volume, and manufacturer. Typically low cost. per vial/ampule
Generic Available: Yes
Insurance Coverage: Tier 1 (Generic)
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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 to do so by a healthcare professional, do not flush medications down the toilet or 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 quantity, and the time it occurred.