Lidocaine 4% Top Soln 50ml
It is used to manage pain.It is used to treat mouth sores.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Local Anesthetic
Pharmacologic Class
Amide-type Local Anesthetic
Pregnancy Category
Category B
FDA Approved
Jan 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
Lidocaine 4% topical solution is a numbing medicine used to relieve pain and discomfort in the mouth, throat, or other mucous membranes. It works by temporarily blocking nerve signals in the area where it's applied.
How to Use This Medicine
Taking Your Medication Correctly
To use this medication effectively, follow your doctor's instructions and read all accompanying information carefully. When using this medication as a rinse, swish it around your mouth for as long as possible, then swallow or spit it out as directed. If applying with a cotton swab, follow your doctor's or the label's instructions for proper application to the affected area. After using this medication, wait at least 60 minutes (1 hour) before eating. Before each use, shake the medication well and measure liquid doses accurately.
Storing and Disposing of Your Medication
Store this medication at room temperature, keeping it and all other medications in a safe location out of the reach of children and pets. 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. If you have questions about disposal, consult your pharmacist, who can also inform you about potential drug take-back programs in your area.
Missing a Dose
If you use this medication regularly, take a missed dose as soon as you remember. However, if it's close to the time for your next dose, skip the missed dose and resume your regular schedule. Do not apply two doses at once or take extra doses. Since this medication is sometimes used as needed, do not use it more frequently than your doctor advises.
To use this medication effectively, follow your doctor's instructions and read all accompanying information carefully. When using this medication as a rinse, swish it around your mouth for as long as possible, then swallow or spit it out as directed. If applying with a cotton swab, follow your doctor's or the label's instructions for proper application to the affected area. After using this medication, wait at least 60 minutes (1 hour) before eating. Before each use, shake the medication well and measure liquid doses accurately.
Storing and Disposing of Your Medication
Store this medication at room temperature, keeping it and all other medications in a safe location out of the reach of children and pets. 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. If you have questions about disposal, consult your pharmacist, who can also inform you about potential drug take-back programs in your area.
Missing a Dose
If you use this medication regularly, take a missed dose as soon as you remember. However, if it's close to the time for your next dose, skip the missed dose and resume your regular schedule. Do not apply two doses at once or take extra doses. Since this medication is sometimes used as needed, do not use it more frequently than your doctor advises.
Lifestyle & Tips
- For oral use, do not eat or drink for at least 1 hour after using the solution to prevent choking or biting your tongue/cheek while numb.
- Avoid hot foods or liquids while the area is numb to prevent burns.
- Do not swallow large amounts of the solution, as this can lead to serious side effects.
- Use a measuring device (e.g., syringe, measuring spoon) to ensure accurate dosing, especially for children.
Available Forms & Alternatives
Available Strengths:
- Lidocaine 4% Top Soln 50ml
- Lidocaine 2% Visc Oral Solution
- Lidocaine 1% Inj, 10ml
- Lidocaine 2% Inj, 2ml
- Lidocaine 4% Injection, 5ml
- Lidocaine 1% Inj, 5ml
- Lidocaine 1% Inj, 20ml
- Lidocaine 2% Inj, 20ml
- Lidocaine 1% Inj, 2ml
- Lidocaine 1% Inj, 50ml
- Lidocaine 2% Inj, 5ml
- Lidocaine 2% Inj, 10ml
- Lidocaine 1% Inj, 30ml
- Lidocaine 2% Inj, 50ml
- Lidocaine 2% Inj, 5ml
- Lidocaine 10mg/ml Inj, 5ml
- Lidocaine 3% Cream 28.35gm
- Lidocaine 3% Cream 85gm
- Lidocaine 2% Topical Jelly 5ml
- Lidocaine 2% Topical Jelly 10ml
- Lidocaine 2% Topical Jelly 20ml
- Lidocaine 20mg/ml Inj, 5ml
- Lidocaine 2% Jelly Gel (uro-Jet)5ml
- Lidocaine 0.5% Inj, 50ml
- Lidocaine 5% Patch
- Lidocaine 5% Topical Ointment 30gm
- Lidocaine 5% Topical Oint 35.44gm
- Lidocaine 5% Topical Ointment 50gm
- Lidocaine 1.5% Inj, 1 Ampule
- Lidocaine 5% Top/oral Oint 50gm
- Lidocaine 4% Cream 15gm
- Lidocaine 4% Cream 30gm
- Lidocaine 4% Cream 5gm
- Lidocaine 3% Cream 85gm
- Lidocaine Pain Relief 4% Patch
- Lidocaine 5% Top/oral Oint (sprmt)
- Lidocaine 5% Anorectal Cream
- Lidocaine 4% Cream 15gm
- Lidocaine 5% Topical Ointment 30gm
- Lidocaine 5% Anorectal Cream 15gm
- Lidocaine Pain Relief 4% Patch
- Lidocaine 5% Cream 30gm
- Lidocaine 2% Inj 25ml
- Lidocaine 5% Ointment 50gm
- Lidocaine 4% Cream 15gm
- Lidocaine 4% Topical Pain Patch
- Lidocaine 3%/hc 0.5% Cream 28.3gm
- Lidocaine 2% Topical Jelly 30ml
Dosing & Administration
Adult Dosing
Standard Dose:
Apply 15 mL (600 mg) of 4% solution to the affected area, swish and spit, or gargle and spit. May be used every 3 hours as needed.
Condition-Specific Dosing:
oral_mucosal_pain:
Do not exceed 8 doses (120 mL or 4800 mg) in a 24-hour period. For short-term use only.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established (use with extreme caution, typically not recommended for routine use due to high risk of systemic toxicity)
Child:
For children 3 years and older: Administer 4% solution based on weight (e.g., 4.5 mg/kg per dose, not to exceed 4 doses in 24 hours). Max single dose typically 5 mL (200 mg). Consult specific product labeling and pediatric guidelines.
Adolescent:
Similar to adult dosing, but caution with maximum daily dose to avoid systemic toxicity.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment for topical use, but monitor for systemic toxicity if significant absorption is expected.
Moderate:
No specific adjustment for topical use, but monitor for systemic toxicity if significant absorption is expected.
Severe:
No specific adjustment for topical use, but monitor for systemic toxicity due to potential accumulation of metabolites.
Dialysis:
Considerations: Lidocaine and its metabolites are dialyzable to some extent. Monitor closely for systemic toxicity if used.
Hepatic Impairment:
Mild:
Use with caution; monitor for signs of systemic toxicity.
Moderate:
Use with caution; consider reduced frequency or dose if significant systemic absorption is anticipated.
Severe:
Contraindicated or use with extreme caution due to impaired metabolism and increased risk of systemic toxicity.
Pharmacology
Mechanism of Action
Lidocaine is an amide-type local anesthetic. It stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of nerve impulses, thereby blocking the conduction of pain signals. It does this by reversibly binding to and blocking voltage-gated sodium channels in the neuronal membrane.
Pharmacokinetics
Absorption:
Bioavailability:
Variable; significant absorption can occur from mucous membranes (e.g., oral, pharyngeal, esophageal). Bioavailability from oral ingestion is low due to extensive first-pass metabolism.
Tmax:
Variable, typically 5-10 minutes for onset of action, peak plasma levels can occur within 30-60 minutes after mucosal application.
FoodEffect:
Not applicable for topical solution.
Distribution:
Vd:
0.7-2.7 L/kg (systemic)
ProteinBinding:
60-80% (primarily to alpha-1-acid glycoprotein and albumin)
CnssPenetration:
Yes, if systemic levels are high enough to cross the blood-brain barrier.
Elimination:
HalfLife:
1.5-2 hours (systemic, in healthy adults); prolonged in hepatic impairment.
Clearance:
Approximately 10 mL/min/kg (systemic)
ExcretionRoute:
Renal (less than 10% as unchanged drug; metabolites excreted renally).
Unchanged:
Less than 10%
Pharmacodynamics
OnsetOfAction:
1-5 minutes (topical)
PeakEffect:
5-10 minutes (topical)
DurationOfAction:
10-30 minutes (topical, depending on site and concentration)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
While 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 medical attention immediately:
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 acidosis (too much acid in the blood), such as:
+ Confusion
+ Fast breathing
+ Fast heartbeat
+ Irregular heartbeat
+ Severe stomach pain, nausea, or vomiting
+ Excessive sleepiness
+ Shortness of breath
+ Feeling extremely tired or weak
Signs of methemoglobinemia, a rare but potentially life-threatening condition, such as:
+ Blue or gray discoloration of the lips, nails, or skin
+ Irregular heartbeat
+ Seizures
+ Severe dizziness or fainting
+ Severe headache
+ Excessive sleepiness
+ Feeling extremely tired or weak
+ Shortness of breath
Breathing difficulties, such as:
+ Trouble breathing
+ Slow breathing
+ Shallow breathing
Severe numbness and tingling
Feeling lightheaded, sleepy, confused, or experiencing blurred vision
Seizures
Changes in vision
Feeling nervous and excitable
Dizziness or fainting
Ringing in the ears
Nausea or vomiting
Feeling excessively hot or cold
Shakiness
Twitching
Slow heartbeat
Chest pain
Other Possible Side Effects
Like all medications, this drug can cause side effects. However, many people may not experience any side effects or may only have mild ones. If you notice any of the following side effects or any other unusual symptoms, contact your doctor for advice:
Irritation at the site of application
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, 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.
While 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 medical attention immediately:
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 acidosis (too much acid in the blood), such as:
+ Confusion
+ Fast breathing
+ Fast heartbeat
+ Irregular heartbeat
+ Severe stomach pain, nausea, or vomiting
+ Excessive sleepiness
+ Shortness of breath
+ Feeling extremely tired or weak
Signs of methemoglobinemia, a rare but potentially life-threatening condition, such as:
+ Blue or gray discoloration of the lips, nails, or skin
+ Irregular heartbeat
+ Seizures
+ Severe dizziness or fainting
+ Severe headache
+ Excessive sleepiness
+ Feeling extremely tired or weak
+ Shortness of breath
Breathing difficulties, such as:
+ Trouble breathing
+ Slow breathing
+ Shallow breathing
Severe numbness and tingling
Feeling lightheaded, sleepy, confused, or experiencing blurred vision
Seizures
Changes in vision
Feeling nervous and excitable
Dizziness or fainting
Ringing in the ears
Nausea or vomiting
Feeling excessively hot or cold
Shakiness
Twitching
Slow heartbeat
Chest pain
Other Possible Side Effects
Like all medications, this drug can cause side effects. However, many people may not experience any side effects or may only have mild ones. If you notice any of the following side effects or any other unusual symptoms, contact your doctor for advice:
Irritation at the site of application
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, 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.
Seek Immediate Medical Attention If You Experience:
- Feeling dizzy, lightheaded, or drowsy
- Confusion or unusual behavior
- Ringing in your ears (tinnitus)
- Blurred vision or double vision
- Tremors or muscle twitching
- Seizures
- Slow or irregular heartbeat
- Difficulty breathing or swallowing
- Severe irritation or allergic reaction at the application site (rash, itching, swelling)
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced as a result of the allergy.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This information will help your doctor and pharmacist assess potential interactions between this medication and other substances.
* Any existing health problems, as this medication may interact with certain conditions.
To ensure your safety, it is crucial to verify that this medication can be taken safely with all your other medications and health conditions. Always consult your doctor before starting, stopping, or changing the dose of any medication.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced as a result of the allergy.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This information will help your doctor and pharmacist assess potential interactions between this medication and other substances.
* Any existing health problems, as this medication may interact with certain conditions.
To ensure your safety, it is crucial to verify that this medication can be taken safely with all your other medications and health conditions. Always consult your doctor before starting, stopping, or changing the dose of any medication.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
There is a risk of developing a severe blood condition called methemoglobinemia associated with this type of drug. Certain factors may increase this risk, including:
- Having glucose-6-phosphate dehydrogenase (G6PD) deficiency
- Pre-existing heart problems
- Pre-existing lung problems
- Taking specific other medications
- Being an infant under 6 months of age
If you have a history of methemoglobinemia, be sure to discuss this with your doctor.
When considering this medication for a child, it's crucial to note that different brands may be suitable for different age groups. Consult with your doctor before administering this drug to a child. Additionally, exercise caution when using this medication in children, as they may be at a higher risk for certain side effects.
To avoid accidental injury, do not eat while your mouth feels numb, as you may inadvertently bite your tongue.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
If you are pregnant, planning to become pregnant, or are breast-feeding, inform your doctor. It is necessary to discuss the potential benefits and risks of this medication to both you and your baby.
There is a risk of developing a severe blood condition called methemoglobinemia associated with this type of drug. Certain factors may increase this risk, including:
- Having glucose-6-phosphate dehydrogenase (G6PD) deficiency
- Pre-existing heart problems
- Pre-existing lung problems
- Taking specific other medications
- Being an infant under 6 months of age
If you have a history of methemoglobinemia, be sure to discuss this with your doctor.
When considering this medication for a child, it's crucial to note that different brands may be suitable for different age groups. Consult with your doctor before administering this drug to a child. Additionally, exercise caution when using this medication in children, as they may be at a higher risk for certain side effects.
To avoid accidental injury, do not eat while your mouth feels numb, as you may inadvertently bite your tongue.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
If you are pregnant, planning to become pregnant, or are breast-feeding, inform your doctor. It is necessary to discuss the potential benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Numbness around the mouth
- Lightheadedness, dizziness
- Tinnitus
- Blurred vision
- Tremors, muscle twitching
- Seizures
- Respiratory depression or arrest
- Bradycardia, hypotension, cardiac arrest
What to Do:
Immediately discontinue use. Call 911 or your local emergency number. For less severe symptoms, call a poison control center (1-800-222-1222 in the US). Supportive care, including airway management, oxygen, IV fluids, and anticonvulsants (e.g., benzodiazepines) for seizures, may be necessary. Lipid emulsion therapy may be considered for severe systemic toxicity.
Drug Interactions
Contraindicated Interactions
- Known hypersensitivity to amide-type local anesthetics
Major Interactions
- Antiarrhythmics (Class I antiarrhythmics like mexiletine, tocainide): Additive cardiac effects, increased risk of adverse reactions.
- Other local anesthetics: Increased risk of systemic toxicity.
Moderate Interactions
- Beta-blockers (e.g., propranolol, metoprolol): May decrease hepatic blood flow, reducing lidocaine clearance and increasing plasma concentrations.
- Cimetidine: Inhibits hepatic metabolism of lidocaine, increasing plasma concentrations.
- CYP1A2 inhibitors (e.g., fluvoxamine, ciprofloxacin): May increase lidocaine levels.
- CYP3A4 inhibitors (e.g., ketoconazole, erythromycin, ritonavir): May increase lidocaine levels.
- Phenytoin: May increase lidocaine levels and risk of toxicity.
- Succinylcholine: Prolongs neuromuscular blockade.
Minor Interactions
- Not many clinically significant minor interactions for topical use unless excessive systemic absorption occurs.
Monitoring
Baseline Monitoring
Patient history (allergies, cardiac/hepatic/renal conditions)
Rationale: To identify contraindications or risk factors for systemic toxicity.
Timing: Prior to initiation of therapy.
Assessment of pain/symptoms
Rationale: To establish baseline for efficacy monitoring.
Timing: Prior to each dose.
Routine Monitoring
Effectiveness of pain relief
Frequency: After each dose, as needed.
Target: Acceptable pain reduction.
Action Threshold: Lack of efficacy may indicate need for alternative treatment or re-evaluation of dose/application.
Signs of local irritation (e.g., redness, swelling, burning)
Frequency: With each application and throughout treatment.
Target: Absence of significant irritation.
Action Threshold: Discontinue if severe irritation occurs.
Signs of systemic toxicity (e.g., dizziness, drowsiness, confusion, tinnitus, blurred vision, tremors, seizures, bradycardia, hypotension)
Frequency: Especially during initial applications and with higher doses/frequent use.
Target: Absence of these symptoms.
Action Threshold: Immediately discontinue use and seek medical attention if any signs of systemic toxicity appear.
Symptom Monitoring
- Numbness or tingling beyond the treated area
- Difficulty swallowing or breathing
- Dizziness or lightheadedness
- Drowsiness or confusion
- Tinnitus (ringing in ears)
- Blurred or double vision
- Tremors or muscle twitching
- Seizures
- Slow or irregular heartbeat
- Low blood pressure
- Anxiety or agitation
Special Patient Groups
Pregnancy
Lidocaine is classified as Pregnancy Category B. Studies in animals have not shown harm to the fetus, but there are no adequate and well-controlled studies in pregnant women. It is generally considered safe for topical use during pregnancy when used as directed and systemic absorption is minimal. Use only if clearly needed.
Trimester-Specific Risks:
First Trimester:
Low risk, but use with caution and only if necessary.
Second Trimester:
Low risk, generally considered safe for topical use.
Third Trimester:
Low risk, generally considered safe for topical use.
Lactation
Lidocaine is excreted into breast milk in small amounts. The amount transferred to the infant is generally very low, especially with topical application. It is considered L2 (moderately safe) by LactMed. Monitor the infant for sedation or feeding difficulties.
Infant Risk:
Low risk of adverse effects to the breastfed infant with typical topical use.
Pediatric Use
Use with extreme caution in infants and young children due to a higher risk of systemic toxicity from accidental ingestion or excessive absorption. Children have a larger surface area to body weight ratio and less developed metabolic pathways. Strict adherence to weight-based dosing and maximum daily limits is crucial. Not recommended for children under 3 years unless specifically directed by a healthcare professional.
Geriatric Use
Use with caution in elderly patients, who may be more susceptible to systemic toxicity due to age-related decreases in hepatic function, renal function, and cardiac output. Start with lower doses and monitor closely for adverse effects.
Clinical Information
Clinical Pearls
- Always use a measuring device (e.g., syringe, measuring spoon) for accurate dosing, especially in children, to prevent accidental overdose.
- Advise patients not to eat or drink for at least 1 hour after oral application to prevent aspiration or biting injuries due to numbness.
- Warn patients about the risk of systemic toxicity, especially if large amounts are swallowed or applied to broken skin/mucosa.
- Lidocaine topical solution is for temporary relief; address the underlying cause of pain.
- Do not use on large areas of skin or for prolonged periods without medical supervision.
Alternative Therapies
- Oral analgesics (e.g., acetaminophen, ibuprofen) for systemic pain relief
- Other topical anesthetics (e.g., dyclonine, phenol)
- Antiseptic mouthwashes for oral irritation
- Cryotherapy (ice chips) for oral pain
Cost & Coverage
Average Cost:
$15 - $50 per 50 mL bottle of 4% solution
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (preferred generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide detailed information about the overdose, including the medication taken, the amount, and the time it occurred.