Lidocaine 1.5% Inj, 1 Ampule

Manufacturer HOSPIRA 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
Jan 1970
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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, preventing you from feeling pain during medical procedures like stitches, minor surgeries, 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 prescribed, 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

  • 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 local infiltration: 1.5% solution, typically 5-300 mg (0.33 mL - 20 mL of 1.5% solution). Max single dose: 4.5 mg/kg (not to exceed 300 mg) without epinephrine; 7 mg/kg (not to exceed 500 mg) with epinephrine.
Dose Range: 5 - 500 mg

Condition-Specific Dosing:

local_infiltration: Max 4.5 mg/kg (300 mg total) without epinephrine; 7 mg/kg (500 mg total) with epinephrine.
peripheral_nerve_block: Varies by nerve, e.g., brachial plexus block 225-300 mg (15-20 mL of 1.5% solution).
epidural_anesthesia: Varies by segment and desired effect, e.g., 225-300 mg (15-20 mL of 1.5% solution) for thoracic/lumbar.
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Pediatric Dosing

Neonatal: Not established for routine use; extreme caution if used. Max 2-3 mg/kg.
Infant: Max 4.5 mg/kg (not to exceed 300 mg) without epinephrine; 7 mg/kg (not to exceed 500 mg) with epinephrine. Use lowest effective dose.
Child: Max 4.5 mg/kg (not to exceed 300 mg) without epinephrine; 7 mg/kg (not to exceed 500 mg) with epinephrine. Use lowest effective dose.
Adolescent: Max 4.5 mg/kg (not to exceed 300 mg) without epinephrine; 7 mg/kg (not to exceed 500 mg) with epinephrine. Use lowest effective dose.
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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: No specific adjustment typically needed for single-dose local anesthesia, but caution with repeated doses or continuous infusion due to metabolite accumulation.
Dialysis: Considerations for continuous IV infusions; metabolites may accumulate. For single local injection, generally no specific adjustment.

Hepatic Impairment:

Mild: Caution, consider lower end of dosing range.
Moderate: Reduce dose by 50% or more, monitor for toxicity.
Severe: Significant dose reduction (e.g., 50-75%) required, monitor closely for toxicity. 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 specifically blocks voltage-gated sodium channels, preventing the propagation of action potentials along nerve fibers.
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Pharmacokinetics

Absorption:

Bioavailability: Not applicable for local injection (direct action). Systemic absorption varies based on site of administration, vascularity, dose, and presence of vasoconstrictors (e.g., epinephrine).
Tmax: Varies widely depending on site of injection (e.g., 5-15 minutes for intercostal block, longer for subcutaneous infiltration).
FoodEffect: Not applicable for injectable form.

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)

Elimination:

HalfLife: 1.5-2 hours (prolonged in hepatic impairment, heart failure, and in neonates)
Clearance: Approximately 10-20 mL/min/kg
ExcretionRoute: Renal (primarily as metabolites)
Unchanged: <10% (excreted unchanged in urine)
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Pharmacodynamics

OnsetOfAction: Rapid (2-5 minutes for infiltration, 5-15 minutes for nerve blocks)
PeakEffect: Varies with site of injection and procedure.
DurationOfAction: 30-60 minutes (without epinephrine); 60-120 minutes (with epinephrine, depending on concentration and site).

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
+ Irregular 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):
+ Confusion
+ Rapid breathing
+ Rapid heartbeat
+ Irregular heartbeat
+ Severe abdominal pain, nausea, or vomiting
+ Excessive sleepiness
+ Shortness of breath
+ Fatigue or weakness
Other severe side effects:
+ Breathing difficulties, slow breathing, or shallow breathing
+ Lightheadedness, drowsiness, confusion, or blurred vision
+ Slow heartbeat
+ Nervousness or excitability
+ 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

All medications can cause side effects, but many people experience none or only mild side effects. If you notice any side effects that bother you or persist, contact your doctor for guidance.

Injection-Specific Side Effects (if administered into the spine)

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

Reporting Side Effects

If you have questions or concerns about side effects, 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:

  • Feeling lightheaded or dizzy
  • Ringing in your ears (tinnitus)
  • Numbness or tingling around your mouth
  • Metallic taste in your mouth
  • Blurred vision
  • Tremors or muscle twitching
  • Confusion or drowsiness
  • Difficulty breathing
  • Slow or irregular heartbeat
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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.
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, and it is crucial to discuss all your health conditions and medications with your doctor.

Share the following with your doctor and pharmacist:
All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
* Your complete medical history

It is essential to verify that this medication is safe to take with your other medications and health conditions. Never start, stop, or adjust the dosage of any medication without consulting your doctor first.
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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.

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.

Protecting the Treated Area
If you are discharged before the numbness has resolved, take precautions to 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 (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 Considerations
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
  • Slow or irregular heartbeat
  • Low blood pressure
  • Respiratory arrest
  • Cardiac 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

  • Antiarrhythmics (Class I, III): Additive cardiac effects, increased risk of toxicity (e.g., procainamide, amiodarone, quinidine).
  • Beta-blockers (e.g., propranolol, metoprolol): May decrease hepatic clearance of lidocaine, increasing plasma levels and risk of toxicity.
  • Cimetidine: Decreases hepatic clearance of lidocaine, increasing plasma levels and risk of toxicity.
  • Succinylcholine: May prolong neuromuscular blockade.
  • Phenytoin (IV): Increased risk of cardiac depression.
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Moderate Interactions

  • CYP1A2 inhibitors (e.g., fluvoxamine, ciprofloxacin): May increase lidocaine levels.
  • CYP3A4 inhibitors (e.g., macrolide antibiotics, azole antifungals, protease inhibitors): May increase lidocaine levels.
  • CYP1A2 inducers (e.g., rifampin, omeprazole): May decrease lidocaine levels.
  • CYP3A4 inducers (e.g., carbamazepine, phenobarbital, St. John's Wort): May decrease lidocaine levels.
  • Local anesthetics (other): Additive systemic toxicity if combined.
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Minor Interactions

  • Nitrates: May cause methemoglobinemia when used with lidocaine (rare).

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 identify pre-existing cardiovascular or respiratory compromise.

Timing: Prior to administration

Patient's general condition and medical history

Rationale: To assess risk factors for systemic toxicity (e.g., hepatic impairment, heart failure, elderly, pediatric patients).

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 limits; monitor for significant changes.

Action Threshold: Bradycardia, hypotension, hypertension, or respiratory depression warrant immediate intervention.

Neurological status (CNS toxicity)

Frequency: Continuously during and after administration.

Target: Absence of CNS symptoms.

Action Threshold: Signs like lightheadedness, dizziness, tinnitus, perioral numbness, metallic taste, confusion, tremors, muscle twitching, or seizures require immediate cessation and management.

ECG monitoring (for large doses or IV use)

Frequency: Continuous during and after administration.

Target: Normal sinus rhythm, absence of arrhythmias.

Action Threshold: Arrhythmias (e.g., bradycardia, heart block, ventricular arrhythmias), QRS widening, or PR prolongation require immediate intervention.

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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
  • Apnea

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 and administered appropriately, especially for local anesthesia.

Trimester-Specific Risks:

First Trimester: Generally considered low risk; use only if clearly needed.
Second Trimester: Generally considered low risk; use only if clearly needed.
Third Trimester: Generally considered low risk; use only if clearly needed. Caution with paracervical block during labor due to potential 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 (likely compatible) by LactMed. Breastfeeding can usually continue after a single dose of local lidocaine.

Infant Risk: Low risk of adverse effects to the breastfed infant.
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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 CNS and cardiovascular toxicity is crucial.

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Geriatric Use

Elderly patients may have reduced hepatic function, decreased plasma protein binding, and reduced renal clearance, leading to higher plasma concentrations and increased risk of systemic toxicity. Lower doses and slower administration rates may be necessary. Monitor closely for adverse effects.

Clinical Information

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Clinical Pearls

  • Always aspirate prior to injection to ensure the needle is not in a blood vessel, which can lead to rapid systemic absorption and toxicity.
  • Use the lowest effective dose to achieve the desired anesthetic effect, especially in sensitive populations (pediatric, elderly, hepatic impairment).
  • The addition of epinephrine prolongs the duration of action and reduces systemic absorption, but should be avoided in areas with end-arterial supply (e.g., fingers, toes, nose, penis, ears) due to risk of ischemia.
  • Be prepared to manage systemic toxicity (CNS and cardiovascular) with appropriate resuscitation equipment and medications (e.g., lipid emulsion therapy for severe toxicity).
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Alternative Therapies

  • Bupivacaine (longer duration of action)
  • Ropivacaine (less cardiotoxic than bupivacaine, longer duration)
  • Mepivacaine (similar to lidocaine, slightly longer duration)
  • Prilocaine (lower CNS toxicity, but risk of methemoglobinemia)
  • Chloroprocaine (very short duration, ester-type)
  • Topical anesthetics (e.g., EMLA cream for superficial procedures)
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Cost & Coverage

Average Cost: Inexpensive per ampule/vial
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, 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 correct disposal method, 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, which can provide a safe and environmentally responsible way to dispose of unwanted medications.

Some medications may come with an additional patient information leaflet, so it is a good idea to check with your pharmacist to see if this is the case. If you have any questions or concerns about your medication, do not hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider for guidance and support.

In the event of a suspected overdose, it is critical to seek immediate medical attention. Call your local poison control center or visit the emergency room right away. When seeking help, be prepared to provide as much information as possible about the overdose, including the name of the medication, the amount taken, and the time it was taken. This information will help healthcare professionals provide the most effective treatment and care.