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Lidocaine 5% Ointment 50gm

Manufacturer MACLEODS PHARMACEUTICALS Active Ingredient Lidocaine Ointment(LYE doe kane) Pronunciation LYE doe kane
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.
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Drug Class
Local Anesthetic
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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
Jun 1948
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Lidocaine 5% Ointment is a medicine applied to the skin to numb the area and relieve pain or itching. It works by temporarily blocking nerve signals in the skin.
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How to Use This Medicine

Proper Use of This Medication

To use this medication correctly, follow your doctor's instructions and read all the information provided.

Application to the Skin:

Do not take this medication by mouth. It is for skin use only.
 Avoid getting the medication in your mouth, nose, or eyes, as it may cause burning. If accidental contact occurs, rinse the area thoroughly with water.
Wash your hands before and after applying the medication, unless your hand is the treated area. In that case, do not wash your hand after application.
 Before applying, clean the affected area and dry it thoroughly.
Apply the medication to clean, dry, healthy skin.
 Do not cover the treated area with bandages or dressings unless instructed to do so by your doctor.

Oral Application (if applicable):

If using a cotton swab to apply the medication, follow your doctor's or the label's instructions for application to the affected area.
 After applying the medication, wait at least 60 minutes (1 hour) before eating.

Storage and Disposal:

Store the medication at room temperature.
 Do not freeze the medication.
Keep all medications in a safe place, 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. Consult your pharmacist for guidance on the best disposal method, and consider participating in local drug take-back programs.

Missing a Dose:

If you use this medication on a regular schedule and miss a dose, apply it as soon as you remember.
 If it is close to the time for your next dose, skip the missed dose and resume your regular application schedule.
Do not apply two doses at once or use extra doses.
 If you use this medication as needed, do not apply it more frequently than directed by your doctor.
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Lifestyle & Tips

  • Wash hands thoroughly before and after applying the ointment.
  • Apply only a thin layer to the affected area. Do not rub it in vigorously.
  • Do not apply to large areas of the body, especially if the skin is broken, cut, or irritated, as this can lead to too much medicine being absorbed into the body.
  • Do not cover the treated area with bandages or plastic wrap unless specifically instructed by your doctor, as this can increase absorption.
  • Avoid contact with eyes, nose, mouth, and other mucous membranes. If contact occurs, rinse thoroughly with water.
  • Keep out of reach of children and pets. Store safely.
  • Do not use heat (e.g., heating pads) on the treated area, as this can increase absorption.
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Available Forms & Alternatives

Available Strengths:

Dosing & Administration

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Adult Dosing

Standard Dose: Apply a thin layer to the affected area as needed, typically every 6-8 hours.

Condition-Specific Dosing:

painRelief: Apply a thin layer to the affected area. Do not exceed 60 grams (3000 mg lidocaine) in a 24-hour period. Maximum single application should not exceed 5 grams (250 mg lidocaine) over a 4-hour period.
pruritus: Apply a thin layer to the affected area as needed, typically every 6-8 hours. Do not exceed recommended daily limits.
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Pediatric Dosing

Neonatal: Not established. Use with extreme caution and under medical supervision due to risk of systemic toxicity.
Infant: Not established. Use with extreme caution and under medical supervision due to risk of systemic toxicity.
Child: Not established for routine use. For children 2-12 years, use with extreme caution and under medical supervision. Dosing should be based on weight and surface area, not exceeding 3 mg/kg per application. Do not exceed 4 applications in 24 hours. Consult a physician.
Adolescent: For adolescents 12 years and older, adult dosing may be considered, but caution is advised, especially with large areas or broken skin. Do not exceed adult maximums.
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Dose Adjustments

Renal Impairment:

Mild: No specific dose adjustment recommended for topical use, but monitor for signs of systemic toxicity if large areas or prolonged use.
Moderate: No specific dose adjustment recommended for topical use, but monitor for signs of systemic toxicity if large areas or prolonged use.
Severe: No specific dose adjustment recommended for topical use, but monitor for signs of systemic toxicity if large areas or prolonged use. Use with caution.
Dialysis: Not applicable for topical use, but systemic absorption could lead to accumulation of metabolites. Use with caution.

Hepatic Impairment:

Mild: No specific dose adjustment recommended for topical use, but monitor for signs of systemic toxicity if large areas or prolonged use.
Moderate: Use with caution; monitor for signs of systemic toxicity due to reduced metabolism.
Severe: Use with extreme caution; monitor closely for signs of systemic toxicity due to significantly reduced metabolism. Consider lower doses or less frequent application.

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 exerting a local anesthetic action. It blocks voltage-gated sodium channels, preventing depolarization and propagation of action potentials in nerve fibers.
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Pharmacokinetics

Absorption:

Bioavailability: Variable (generally low for intact skin, but increases significantly with damaged skin, large application areas, prolonged exposure, or occlusion). Systemic absorption can be up to 30% or more under occlusive dressings.
Tmax: Variable, typically 2-10 hours after topical application, depending on formulation and application site.
FoodEffect: Not applicable for topical formulation.

Distribution:

Vd: Approximately 1.1 L/kg (systemic absorption)
ProteinBinding: 60-80% (primarily to alpha-1-acid glycoprotein and albumin)
CnssPenetration: Yes (if systemic absorption occurs, crosses blood-brain barrier)

Elimination:

HalfLife: Approximately 1.5-2 hours (systemic)
Clearance: Approximately 0.95 L/min (systemic)
ExcretionRoute: Renal (less than 10% unchanged drug, primarily metabolites)
Unchanged: Less than 10%
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Pharmacodynamics

OnsetOfAction: 2-5 minutes (topical)
PeakEffect: 15-60 minutes (topical)
DurationOfAction: 30-60 minutes (topical, can be longer under occlusion)

Safety & Warnings

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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 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
+ Difficulty 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
+ Rapid breathing
+ Rapid 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
 Signs of skin infection, such as:
+ Oozing
+ Heat
+ Swelling
+ Redness
+ Pain
Respiratory problems, such as:
+ Difficulty 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 hot or cold
Shakiness
 Twitching
Slow heartbeat
 Chest pain

Other Possible Side Effects

Like all medications, this drug can cause side effects. 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
 Swelling
Redness
 Changes in skin color

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.
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Seek Immediate Medical Attention If You Experience:

  • Dizziness or lightheadedness
  • Numbness or tingling around the mouth
  • Blurred vision or ringing in the ears
  • Tremors or muscle twitching
  • Feeling unusually tired or drowsy
  • Slow or irregular heartbeat
  • Difficulty breathing
  • Severe redness, swelling, or blistering at the application site
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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 to this medication, its components, or other substances, including foods and drugs. Be sure to describe the allergic reaction and its symptoms.
 The presence of an infection at the site where the medication will be applied.
Any broken skin or open wounds at the intended application site.
 Swollen skin, numbness, or loss of sensation at the application site, as these conditions may affect the medication's absorption or increase the risk of adverse reactions.
If a large area of your body needs to be treated, as this may require special consideration and dosing adjustments.

Additionally, this medication may interact with other drugs or health conditions. Therefore, it is crucial to provide your doctor and pharmacist with a comprehensive list of:

 All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
 Your existing health problems

Your doctor will assess the safety of taking this medication with your other drugs and health conditions. Do not initiate, stop, or modify the dose of any medication without first consulting your doctor to ensure your safety.
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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 can occur with the use of this drug. 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.

Before using any other medications or skin products, including soaps, consult with your doctor. Do not use this medication for a longer period than prescribed by your doctor. While your skin is numb, avoid scratching or rubbing the area, and protect it from extreme temperatures.

Apply this medication only to intact skin, unless your doctor specifically instructs you to use it on cuts, scrapes, or damaged skin. Avoid exposure to heat sources such as sunlamps, tanning beds, heating pads, electric blankets, heat lamps, saunas, hot tubs, and heated waterbeds. Also, avoid taking long, hot baths or sunbathing, as these can cause your body temperature to rise and lead to excessive absorption of the medication.

If this medication is accidentally swallowed, immediately contact a doctor or a poison control center. Note that different brands of this medication may be suitable for children of different ages, so consult with your doctor before administering it to a child. When using this medication in children, exercise caution, as they may be at a higher risk for certain side effects.

If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects. Pregnant or breastfeeding women, or those planning to become pregnant, should discuss the potential benefits and risks of using this medication with their doctor.
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Overdose Information

Overdose Symptoms:

  • Severe dizziness or drowsiness
  • Nausea or vomiting
  • Tremors or muscle twitching
  • Seizures
  • Slow or irregular heartbeat
  • Low blood pressure
  • Difficulty breathing
  • Coma

What to Do:

Immediately wash off the ointment with soap and water. Seek emergency medical attention or call Poison Control at 1-800-222-1222. Be prepared to provide information about the amount used and when it was applied.

Drug Interactions

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Major Interactions

  • Antiarrhythmics (Class I, e.g., mexiletine, tocainide): Increased risk of cardiac effects.
  • Other local anesthetics: Additive systemic toxicity.
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Moderate Interactions

  • Beta-blockers (e.g., propranolol, metoprolol): May decrease hepatic metabolism of lidocaine, increasing systemic levels.
  • Cimetidine: May inhibit lidocaine metabolism, increasing systemic levels.
  • CYP3A4 inhibitors (e.g., ketoconazole, erythromycin, ritonavir): May increase lidocaine levels.
  • CYP1A2 inhibitors (e.g., fluvoxamine, ciprofloxacin): May increase lidocaine levels.
  • Succinylcholine: Prolonged neuromuscular blockade.
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Minor Interactions

  • Not available

Monitoring

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Baseline Monitoring

Skin integrity of application site

Rationale: Damaged or broken skin increases systemic absorption and risk of toxicity.

Timing: Prior to first application

Patient's medical history (cardiac, hepatic, renal disease, seizures)

Rationale: Identifies risk factors for systemic toxicity or altered metabolism/excretion.

Timing: Prior to first application

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Routine Monitoring

Application site for irritation, redness, swelling

Frequency: With each application

Target: Absence of significant irritation

Action Threshold: Discontinue if severe irritation or allergic reaction occurs.

Signs/symptoms of systemic toxicity (CNS: dizziness, confusion, tremors, seizures; Cardiovascular: bradycardia, hypotension, arrhythmias)

Frequency: During and after application, especially with large areas, prolonged use, or compromised skin

Target: Absence of symptoms

Action Threshold: Immediately discontinue use and seek medical attention if symptoms occur.

Total amount of ointment used

Frequency: Daily

Target: Within recommended maximums (e.g., 60g/24 hours for adults)

Action Threshold: Do not exceed maximum recommended dose to prevent systemic toxicity.

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Symptom Monitoring

  • Dizziness
  • Lightheadedness
  • Numbness around the mouth
  • Tingling sensations
  • Blurred vision
  • Tremors
  • Muscle twitching
  • Confusion
  • Seizures
  • Bradycardia (slow heart rate)
  • Hypotension (low blood pressure)
  • Arrhythmias
  • Difficulty breathing
  • Skin irritation (redness, swelling, rash, itching) at application site

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, but there are no adequate and well-controlled studies in pregnant women. Topical use with limited systemic absorption is generally considered low risk, but use only if clearly needed and potential benefits outweigh potential risks.

Trimester-Specific Risks:

First Trimester: Generally considered low risk with appropriate topical use, but caution advised.
Second Trimester: Generally considered low risk with appropriate topical use.
Third Trimester: Generally considered low risk with appropriate topical use.
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Lactation

Lidocaine is excreted into breast milk in small amounts. The amount transferred to the infant via breast milk after topical maternal application is generally considered to be very low and unlikely to cause adverse effects in a nursing infant. L2 (Safer).

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

Use with extreme caution, especially in children under 2 years of age, due to higher risk of systemic toxicity from greater surface area to body weight ratio and thinner skin. Dosing must be carefully calculated based on weight and surface area. Avoid large application areas, prolonged use, or occlusive dressings. Monitor closely for signs of systemic toxicity.

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Geriatric Use

No specific dose adjustments are typically needed for topical use in the elderly, but caution is advised due to potential for decreased hepatic function, which could lead to higher systemic levels if significant absorption occurs. Start with lower doses and monitor for adverse effects.

Clinical Information

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Clinical Pearls

  • Topical lidocaine ointment is for external use only. Do not ingest.
  • The 5% ointment is potent; use sparingly and only on the affected area.
  • Systemic toxicity is rare with proper use but can occur if applied to large areas, broken skin, or under occlusion, or if the maximum dose is exceeded.
  • Symptoms of systemic toxicity (e.g., dizziness, tremors, confusion, seizures, cardiac effects) require immediate medical attention.
  • Advise patients to avoid applying heat (e.g., heating pads) to the treated area, as this can increase systemic absorption.
  • Patients should be instructed on the maximum amount of ointment that can be safely applied per day and per application.
  • Not for use on mucous membranes or in the eyes.
  • Consider alternative pain relief methods if the patient has extensive skin damage or a history of severe cardiac or hepatic impairment.
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Alternative Therapies

  • Topical NSAIDs (e.g., diclofenac gel)
  • Capsaicin cream
  • Menthol/Camphor topical analgesics
  • Oral analgesics (e.g., acetaminophen, NSAIDs)
  • Ice/cold packs
  • Heat therapy (with caution)
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Cost & Coverage

Average Cost: $15 - $40 per 50gm tube of 5% ointment
Generic Available: Yes
Insurance Coverage: Tier 1 or 2 (Generic)
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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 medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it occurred.