Xylocaine 4% Top Soln
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; Voltage-gated Sodium Channel Blocker
Pregnancy Category
Category B
FDA Approved
Jan 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
Lidocaine is a medicine that numbs a specific area of your body. Xylocaine 4% Topical Solution is used to numb the inside of your mouth, throat, or other mucous membranes to relieve pain or discomfort, or before certain medical procedures. It works by 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 the information provided. If you are using it as a mouth rinse, swish it around your mouth for as long as possible, then either swallow or spit it out as directed. If applying it with a cotton swab, put it on the affected area as instructed by your doctor or the label. After using this medication, wait at least 60 minutes (1 hour) before eating. Before each use, shake the medication well and measure liquid doses carefully.
Storing and Disposing of Your Medication
Store this medication at room temperature, keeping it in a safe place out of the reach of children and pets. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so. Instead, check with your pharmacist for guidance on the best disposal method. You may also want to inquire about drug take-back programs in your area.
Missing a Dose
If you use this medication on a regular basis and miss a dose, take it as soon as you remember. However, if it is close to the time for your next dose, skip the missed dose and resume your normal schedule. Do not apply two doses at once or take extra doses. If you use this medication as needed, do not use it more frequently than directed by your doctor.
To use this medication effectively, follow your doctor's instructions and read all the information provided. If you are using it as a mouth rinse, swish it around your mouth for as long as possible, then either swallow or spit it out as directed. If applying it with a cotton swab, put it on the affected area as instructed by your doctor or the label. After using this medication, wait at least 60 minutes (1 hour) before eating. Before each use, shake the medication well and measure liquid doses carefully.
Storing and Disposing of Your Medication
Store this medication at room temperature, keeping it in a safe place out of the reach of children and pets. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so. Instead, check with your pharmacist for guidance on the best disposal method. You may also want to inquire about drug take-back programs in your area.
Missing a Dose
If you use this medication on a regular basis and miss a dose, take it as soon as you remember. However, if it is close to the time for your next dose, skip the missed dose and resume your normal schedule. Do not apply two doses at once or take extra doses. If you use this medication as needed, do not use it more frequently than directed by your doctor.
Lifestyle & Tips
- Do not eat or drink for at least 1 hour after using this medicine in your mouth or throat, or until the numbness wears off, to prevent choking or biting your tongue/cheek.
- Avoid hot foods or liquids while the area is numb to prevent burns.
- Do not apply to large areas of skin, broken skin, or for prolonged periods, as this can lead to too much medicine being absorbed into your body.
- Keep this medicine out of reach of children. Accidental ingestion can be very dangerous and even fatal for children.
Available Forms & Alternatives
Available Strengths:
- Xylocaine 4% Top Soln
- Xylocaine-Mpf 2% Inj, 10ml
- Xylocaine 2% Inj, 10ml
- Xylocaine-Mpf 1% Inj, 5ml
- Xylocaine 2% Inj, 20ml
- Xylocaine-Mpf 1% Inj, 30ml
- Xylocaine 2% Inj, 50ml
- Xylocaine-Mpf 0.5% Inj, 50ml
- Xylocaine-Mpf 1% Inj, 2ml
- Xylocaine-Mpf 2% Inj, 5ml
- Xylocaine 1% Inj, 20ml
- Xylocaine-Mpf 2% Inj, 2ml
- Xylocaine-Mpf 1% Inj, 10ml
- Xylocaine 1% Inj, 50ml
- Xylocaine 0.5% Inj, 50ml
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
Apply 15 mL (600 mg lidocaine) to the affected area, not to exceed 30 mL (1200 mg lidocaine) in a 12-hour period.
Condition-Specific Dosing:
oral_mucosa:
For topical anesthesia of accessible mucous membranes of the oral and pharyngeal cavities: Apply 15 mL (600 mg) as a gargle or rinse, then spit out. May be repeated every 3 hours as needed, not to exceed 8 doses (120 mL or 4800 mg) in a 24-hour period. For painful oral lesions, apply directly with a cotton applicator.
endoscopy:
For topical anesthesia prior to endoscopy: Administer 15 mL (600 mg) as a gargle or rinse, then spit out, 5-10 minutes prior to procedure.
Pediatric Dosing
Neonatal:
Not established (Use with extreme caution, high risk of systemic toxicity)
Infant:
Not established (Use with extreme caution, high risk of systemic toxicity)
Child:
For children over 3 years: Administer 4-5 mg/kg/dose (0.1-0.125 mL/kg/dose of 4% solution), not to exceed 4.5 mg/kg or 300 mg (7.5 mL) per dose, whichever is less. Max 4 doses in 12 hours. Use with extreme caution due to risk of systemic toxicity, especially in children under 3 years or those with compromised mucosa. Accidental ingestion can be fatal.
Adolescent:
Similar to adult dosing, but consider lower doses for smaller adolescents. Max 4.5 mg/kg or 300 mg per dose, whichever is less, not to exceed 1200 mg in 12 hours.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended for topical use, but monitor for systemic toxicity if significant absorption is expected.
Moderate:
No specific adjustment recommended for topical use, but monitor for systemic toxicity if significant absorption is expected.
Severe:
No specific adjustment recommended for topical use, but monitor for systemic toxicity if significant absorption is expected. Metabolites are renally excreted.
Dialysis:
Considerations: Lidocaine is not significantly dialyzable. Monitor for systemic toxicity.
Hepatic Impairment:
Mild:
Use with caution; consider lower doses or extended dosing intervals due to reduced metabolism.
Moderate:
Use with caution; consider lower doses or extended dosing intervals due to reduced metabolism. Monitor for systemic toxicity.
Severe:
Contraindicated or use with extreme caution at significantly reduced doses. Monitor closely for systemic toxicity due to impaired metabolism.
Pharmacology
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.
Pharmacokinetics
Absorption:
Bioavailability:
Variable (depends on site of application, integrity of mucous membrane, and duration of exposure). Significant systemic absorption can occur from mucous membranes.
Tmax:
Variable (typically 5-10 minutes for onset, peak systemic levels can be 30-60 minutes after application to mucous membranes).
FoodEffect:
Not applicable for topical solution.
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 neonates)
Clearance:
Approximately 10 mL/min/kg
ExcretionRoute:
Renal (less than 10% as unchanged drug; primarily as metabolites)
Unchanged:
Less than 10%
Pharmacodynamics
OnsetOfAction:
1-5 minutes (for topical anesthesia)
PeakEffect:
5-10 minutes (for topical anesthesia)
DurationOfAction:
10-30 minutes (for topical anesthesia, depending on site and concentration)
Safety & Warnings
BLACK BOX WARNING
Cases of severe adverse events, including seizures, cardiorespiratory arrest, and death, have been reported in patients, including children, who were administered lidocaine viscous 2% solution. These events have resulted from accidental ingestion, inappropriate use, and/or overdose. Lidocaine 4% topical solution carries similar risks of systemic toxicity if ingested or applied excessively, especially in children. Keep out of reach of children. Do not exceed recommended dosage and frequency.
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, 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
+ Abnormal 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
+ Abnormal heartbeat
+ Seizures
+ Severe dizziness or fainting
+ Severe headache
+ Excessive sleepiness
+ Feeling extremely tired or weak
+ Shortness of breath
Other severe side effects, including:
+ Trouble breathing, slow breathing, or 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 extremely 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 do not experience any side effects or 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 all 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.
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, 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
+ Abnormal 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
+ Abnormal heartbeat
+ Seizures
+ Severe dizziness or fainting
+ Severe headache
+ Excessive sleepiness
+ Feeling extremely tired or weak
+ Shortness of breath
Other severe side effects, including:
+ Trouble breathing, slow breathing, or 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 extremely 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 do not experience any side effects or 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 all 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:
- Dizziness or lightheadedness
- Feeling nervous or restless
- Ringing in your ears (tinnitus)
- Blurred vision
- Numbness or tingling around your mouth
- Tremors or muscle twitching
- Seizures
- Slow or irregular heartbeat
- Difficulty breathing
- Unusual drowsiness or confusion
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.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins.
* Any existing health problems, as this medication may interact with other drugs or health conditions.
To ensure your safety, it is crucial to verify that it is safe to take this medication with all your current 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.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins.
* Any existing health problems, as this medication may interact with other drugs or health conditions.
To ensure your safety, it is crucial to verify that it is safe to take this medication with all your current 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.
A rare but serious blood condition called methemoglobinemia has been associated with drugs similar to this one. Your risk may be increased if you have a deficiency of the enzyme glucose-6-phosphate dehydrogenase (G6PD), heart problems, or lung problems. Additionally, the risk may be higher when taking certain other medications or in infants 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 approved for use in different age groups. Consult with your doctor before administering this drug to a child. Furthermore, when using this medication in children, caution is advised, as the risk of certain side effects may be higher in this population.
To avoid accidental injury, do not eat until the numbness in your mouth has resolved, 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 breastfeeding, inform your doctor. It is necessary to discuss the potential benefits and risks of this medication to both you and your baby to make an informed decision.
A rare but serious blood condition called methemoglobinemia has been associated with drugs similar to this one. Your risk may be increased if you have a deficiency of the enzyme glucose-6-phosphate dehydrogenase (G6PD), heart problems, or lung problems. Additionally, the risk may be higher when taking certain other medications or in infants 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 approved for use in different age groups. Consult with your doctor before administering this drug to a child. Furthermore, when using this medication in children, caution is advised, as the risk of certain side effects may be higher in this population.
To avoid accidental injury, do not eat until the numbness in your mouth has resolved, 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 breastfeeding, inform your doctor. It is necessary to discuss the potential benefits and risks of this medication to both you and your baby to make an informed decision.
Overdose Information
Overdose Symptoms:
- Severe dizziness, lightheadedness, or fainting
- Numbness or tingling spreading to other parts of the body
- Slurred speech
- Confusion or disorientation
- Seizures
- Slow or irregular heartbeat
- Low blood pressure
- Difficulty breathing or stopping breathing
- Coma
What to Do:
If you suspect an overdose, seek immediate medical attention. Call 911 or your local emergency number. For poison control, call 1-800-222-1222.
Drug Interactions
Major Interactions
- Class I Antiarrhythmics (e.g., mexiletine, tocainide): Increased risk of cardiac depression and CNS effects.
- Other Local Anesthetics: Additive systemic toxicity.
Moderate Interactions
- Beta-blockers (e.g., propranolol, metoprolol): May decrease hepatic blood flow, reducing lidocaine clearance and increasing plasma levels.
- Cimetidine: Inhibits lidocaine metabolism (CYP1A2, CYP3A4), increasing plasma levels.
- Phenytoin: May increase lidocaine metabolism (CYP3A4 induction) or have additive cardiac effects.
- Amiodarone: Increased risk of cardiac depression and CNS effects.
- Skeletal Muscle Relaxants (e.g., succinylcholine): Prolonged neuromuscular blockade.
Minor Interactions
- CYP3A4 Inducers (e.g., rifampin, carbamazepine): May decrease lidocaine levels.
- CYP3A4 Inhibitors (e.g., macrolide antibiotics, azole antifungals): May increase lidocaine levels.
Monitoring
Baseline Monitoring
Patient history (allergies, cardiac/hepatic/renal disease, concomitant medications)
Rationale: To identify contraindications, risk factors for systemic toxicity, and potential drug interactions.
Timing: Prior to initiation of therapy
Assessment of mucous membrane integrity
Rationale: Damaged or inflamed mucosa can increase systemic absorption and risk of toxicity.
Timing: Prior to application
Routine Monitoring
Signs and symptoms of systemic toxicity (CNS and cardiovascular)
Frequency: During and immediately after application, especially with higher doses or repeated use.
Target: Absence of symptoms
Action Threshold: Any signs of toxicity (e.g., dizziness, tinnitus, perioral numbness, seizures, bradycardia, hypotension) require immediate discontinuation and supportive care.
Effectiveness of anesthesia
Frequency: As needed
Target: Adequate pain relief/anesthesia
Action Threshold: Inadequate effect may indicate need for re-application (within dose limits) or alternative therapy.
Symptom Monitoring
- Lightheadedness
- Dizziness
- Tinnitus (ringing in ears)
- Blurred vision
- Numbness or tingling around the mouth (perioral numbness)
- Tremors
- Muscle twitching
- Seizures
- Drowsiness
- Confusion
- Bradycardia (slow heart rate)
- Hypotension (low blood pressure)
- Cardiac arrest (severe toxicity)
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 should be used during pregnancy only if clearly needed and the potential benefits outweigh the potential risks.
Trimester-Specific Risks:
First Trimester:
Generally considered low risk, but use only if clearly indicated.
Second Trimester:
Generally considered low risk, but use only if clearly indicated.
Third Trimester:
Generally considered low risk, but use only if clearly indicated. Monitor for potential effects on the neonate if used close to delivery.
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 when used topically at recommended doses. It is rated L2 (Safer) by LactMed.
Infant Risk:
Low risk of adverse effects to the breastfed infant. Monitor infant for unusual drowsiness or feeding difficulties, though unlikely with topical use.
Pediatric Use
Use with extreme caution, especially in children under 3 years of age. Children are more susceptible to systemic toxicity due to higher absorption rates from mucous membranes and lower body weight. Strict adherence to weight-based dosing and maximum daily limits is critical. Accidental ingestion can be fatal. Keep out of reach of children.
Geriatric Use
Elderly patients may be more susceptible to systemic toxicity due to decreased hepatic function, reduced protein binding, and/or reduced renal clearance of metabolites. Use lower doses and monitor closely for adverse effects.
Clinical Information
Clinical Pearls
- Always measure doses carefully, especially in pediatric patients, to avoid systemic toxicity.
- Instruct patients not to swallow the solution when used as a gargle/rinse for oral/pharyngeal anesthesia.
- Warn patients about the risk of biting their tongue/cheek or burning themselves with hot food/drinks while the area is numb.
- Systemic toxicity can occur even with topical application, especially if applied to large areas, broken skin, or if the maximum dose is exceeded.
- Be vigilant for early signs of CNS toxicity (e.g., perioral numbness, dizziness, tinnitus) as these often precede more severe symptoms like seizures.
Alternative Therapies
- Benzocaine topical (e.g., Orajel)
- Dyclonine topical solution
- Phenol topical solution
- Oral rinses (e.g., salt water, magic mouthwash)
- Systemic analgesics (e.g., NSAIDs, acetaminophen) for pain relief
Cost & Coverage
Average Cost:
Not available per bottle
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 (Generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it's 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 be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to 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 details about the medication taken, the amount, and the time it occurred.