Lidocaine 4% Cream 15gm

Manufacturer RUGBY LABORATORIES Active Ingredient Lidocaine Cream(LYE doe kane) Pronunciation LYE doe kane
It is used to manage pain.It is used to treat signs of hemorrhoids or rectal irritation. 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
FDA Approved
Jan 1970
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Lidocaine 4% cream is a numbing medicine applied to the skin to relieve pain, itching, or discomfort. It works by temporarily blocking nerve signals in the area where it's applied.
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How to Use This Medicine

Taking Your Medication Correctly

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

Using Rectal Products

1. Wash your hands before and after applying the medication.
2. Apply the medication to clean, dry skin as directed by your doctor or according to the package labeling.

Using Skin Products

1. Do not ingest this medication. It is for skin use only.
2. Avoid getting the medication in your mouth, nose, or eyes, as it may cause irritation. If accidental contact occurs, rinse the area thoroughly with water.
3. Wash your hands before and after applying the medication, unless your hand is the treated area.
4. Clean and dry the affected area before applying the medication.
5. Apply the medication to clean, dry, healthy skin.
6. Do not cover the treated area with bandages or dressings unless instructed to do so by your doctor.

Storing and Disposing of Your Medication

1. Store the medication at room temperature.
2. Do not freeze the medication.
3. Keep all medications in a safe place, out of the reach of children and pets.
4. 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.
5. Consult your pharmacist for guidance on the best disposal method. Local drug take-back programs may also be available.

Missing a Dose

If you use this medication regularly:
- Take a missed dose as soon as you remember.
- If it is 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 extra doses.

If you use this medication as needed:
- Do not use it more frequently than directed by your doctor.
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Lifestyle & Tips

  • Wash hands thoroughly before and after applying the cream.
  • Apply only a thin layer to the affected area as directed by your doctor or pharmacist.
  • Do not apply to large areas of the body, open wounds, broken, or irritated skin.
  • Avoid covering the treated area with bandages or tight dressings unless specifically instructed by a healthcare professional, as this can increase absorption and risk of side effects.
  • Do not use heat (e.g., heating pads) on the treated area, as this can also 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 to prevent accidental ingestion.

Dosing & Administration

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Adult Dosing

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

Condition-Specific Dosing:

Maximum Application: Do not exceed 3-4 applications in a 24-hour period. Do not apply to large areas of the body or to broken or irritated skin. Maximum recommended dose is 0.5 g of cream per 10 cm² area, not exceeding 60 g per 24 hours for adults.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Use with extreme caution and under medical supervision. Lower concentrations (e.g., 2%) are generally preferred. Dosage must be carefully calculated based on weight and body surface area to avoid systemic toxicity. Max dose typically 3 mg/kg per application.
Adolescent: Use with caution, consider adult dosing with careful monitoring for systemic absorption, especially if applied to large or broken skin areas.
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment typically needed for topical use.
Moderate: Use with caution due to potential for accumulation of metabolites if significant systemic absorption occurs. Monitor for signs of toxicity.
Severe: Use with caution and reduced frequency/amount due to potential for accumulation of lidocaine and its metabolites. Monitor closely for systemic toxicity.
Dialysis: Considerations: Lidocaine and its metabolites are dialyzable to some extent, but systemic absorption from topical application is usually low. Use with caution and monitor for toxicity.

Hepatic Impairment:

Mild: No specific adjustment typically needed for topical use.
Moderate: Use with caution and reduced frequency/amount due to impaired metabolism of lidocaine. Monitor closely for systemic toxicity.
Severe: Contraindicated or use with extreme caution and significantly reduced dose/frequency due to severely impaired metabolism, leading to increased risk of systemic toxicity. Monitor closely.

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 specifically blocks voltage-gated sodium channels, preventing depolarization and propagation of action potentials.
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Pharmacokinetics

Absorption:

Bioavailability: Variable; generally low (approx. 3-10%) after topical application to intact skin, but can increase significantly (up to 60%) with prolonged application, large surface areas, occlusive dressings, or compromised skin.
Tmax: Variable, typically 2-4 hours after topical application, but can be longer depending on formulation and application conditions.
FoodEffect: Not applicable for topical formulation.

Distribution:

Vd: Approximately 1.1 L/kg (after IV administration, systemic absorption from topical is lower).
ProteinBinding: Approximately 60-80% (primarily to alpha-1-acid glycoprotein and albumin).
CnssPenetration: Limited at therapeutic topical doses; significant penetration occurs with systemic toxicity.

Elimination:

HalfLife: Approximately 1.5-2 hours (for parent drug after systemic absorption); metabolites have longer half-lives.
Clearance: Approximately 10-20 mL/min/kg (systemic clearance).
ExcretionRoute: Renal (primarily metabolites).
Unchanged: Less than 10% of lidocaine is excreted unchanged in the urine.
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Pharmacodynamics

OnsetOfAction: Within 5-15 minutes after application.
PeakEffect: Variable, typically 20-60 minutes, depending on skin penetration and concentration.
DurationOfAction: Approximately 1-3 hours, depending on the amount applied and individual variability.

Safety & Warnings

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Side Effects

Serious 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 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
+ 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
Signs of skin infection, such as:
+ Oozing
+ Heat
+ Swelling
+ Redness
+ Pain
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 hot or cold
Shakiness
Twitching
Slow heartbeat
Chest pain

Additional Side Effects of Rectal Products

If you are using a rectal product, you may also experience:

Bleeding from the rectum
Rectal pain

Other Possible Side Effects

Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to contact your doctor if you notice any of the following:

Irritation at the site of application
Swelling
Redness
Changes in skin color

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:

  • Signs of too much medicine absorbed (systemic toxicity): Dizziness, lightheadedness, drowsiness, confusion, ringing in the ears (tinnitus), blurred vision, numbness or tingling around the mouth, muscle twitching, tremors, or seizures. Seek immediate medical attention if these occur.
  • Signs of allergic reaction: Rash, itching, hives, swelling of the face/lips/tongue/throat, severe dizziness, trouble breathing. Seek immediate medical attention.
  • Severe skin irritation 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. Describe the allergic reaction and its symptoms.
The presence of an infection at the site where the medication will be applied.
Broken skin or open wounds at the application site.
Swollen skin, numbness, or loss of sensation at the application site.
* The need to treat a large area with this medication.

This list is not exhaustive, and 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 use this medication with your other treatments and health issues. Never start, stop, or adjust the dosage of any medication without consulting your doctor first.
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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.

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 or 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.

Before using any other medications or products on your skin, including soaps, consult with your doctor.

Adhere to your doctor's instructions regarding the duration of use for this medication. Do not exceed the recommended treatment period.

While using this medication, avoid scratching or rubbing the treated skin area, as it may be numb. Additionally, protect the area from extreme temperatures.

Unless instructed by your doctor, do not apply this medication to cuts, scrapes, or damaged skin.

To minimize the risk of increased drug absorption, avoid exposure to heat sources such as:
- Sunlamps
- Tanning beds
- Heating pads
- Electric blankets
- Heat lamps
- Saunas
- Hot tubs
- Heated waterbeds
Also, avoid taking long, hot baths or sunbathing, as these activities may cause your body temperature to rise.

If this medication is accidentally swallowed, immediately contact a doctor or a poison control center, as it may cause harm.

When considering use in children, note that different brands of this medication may be approved for different age groups. Consult with your doctor before administering this medication to a child.

If the patient is a child, exercise caution when using this medication, as the risk of certain side effects may be higher in this population.

For individuals 65 years of age 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 breastfeeding, discuss the potential benefits and risks of using this medication with your doctor to make an informed decision.
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Overdose Information

Overdose Symptoms:

  • Nervousness, dizziness, blurred vision, tremors, drowsiness, seizures, unconsciousness.
  • Slow heart rate (bradycardia), low blood pressure (hypotension), irregular heart rhythm, cardiac arrest.
  • Difficulty breathing, respiratory arrest.
  • Methemoglobinemia (rare, but serious, characterized by bluish skin discoloration, shortness of breath, fatigue).

What to Do:

Immediately remove the cream and wash the area. Call 911 or your local emergency number. For non-emergencies, call a poison control center at 1-800-222-1222. Medical management may include supportive care, airway management, anticonvulsants for seizures, and vasopressors for hypotension.

Drug Interactions

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Major Interactions

  • Class I Antiarrhythmics (e.g., tocainide, mexiletine): Increased risk of cardiac adverse effects due to additive sodium channel blockade.
  • Other Local Anesthetics: Increased risk of systemic toxicity (CNS, cardiovascular) due to additive effects.
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Moderate Interactions

  • Beta-blockers (e.g., propranolol, metoprolol): May reduce hepatic blood flow, potentially decreasing lidocaine clearance and increasing systemic levels.
  • Cimetidine: Inhibits CYP450 enzymes (CYP3A4, CYP1A2), potentially increasing lidocaine plasma concentrations.
  • Phenytoin: May increase lidocaine metabolism (CYP3A4 induction) or have additive cardiac effects.
  • Amide-type Local Anesthetics (e.g., bupivacaine, ropivacaine): Additive systemic toxicity if significant absorption occurs.

Monitoring

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Baseline Monitoring

Skin integrity and area of application

Rationale: To assess risk of increased systemic absorption and local irritation.

Timing: Prior to first application

Pain level

Rationale: To establish baseline for efficacy assessment.

Timing: Prior to first application

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Routine Monitoring

Local skin reactions (redness, swelling, rash, itching)

Frequency: With each application and daily

Target: Absence of significant irritation

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

Signs of systemic toxicity (CNS, cardiovascular)

Frequency: Daily, especially with large area/prolonged use

Target: Absence of symptoms

Action Threshold: Discontinue and seek medical attention if dizziness, drowsiness, confusion, tremors, seizures, bradycardia, or hypotension occur.

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Symptom Monitoring

  • Dizziness
  • Lightheadedness
  • Drowsiness
  • Confusion
  • Numbness around the mouth
  • Tingling sensations
  • Tremors
  • Muscle twitching
  • Seizures
  • Blurred vision
  • Tinnitus
  • Bradycardia (slow heart rate)
  • Hypotension (low blood pressure)
  • Skin irritation (redness, rash, itching, swelling, blistering)

Special Patient Groups

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Pregnancy

Lidocaine is Pregnancy Category B. Studies in animals have not shown harm to the fetus. Topical absorption is generally low, making it a relatively safe option for pain relief during pregnancy when used appropriately and for limited durations/areas. Consult with a healthcare provider.

Trimester-Specific Risks:

First Trimester: Low risk, but use with caution and only if clearly needed.
Second Trimester: Low risk, generally considered safe for topical use.
Third Trimester: Low risk, generally considered safe for topical use, but avoid large areas or prolonged use near term.
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Lactation

Lidocaine is rated L2 (likely compatible) for lactation. It is excreted into breast milk in small amounts, but systemic absorption from topical application is low, making infant exposure minimal. Use on the breast area should be avoided immediately prior to nursing to prevent infant ingestion.

Infant Risk: Low risk of adverse effects to the breastfed infant when used topically by the mother.
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Pediatric Use

Children, especially infants and young children, are more susceptible to systemic toxicity from lidocaine due to their higher surface area to weight ratio and immature metabolic pathways. Use of 4% cream is generally not recommended for children under 12 years unless specifically directed and monitored by a physician. Lower concentrations (e.g., 2%) are preferred if topical lidocaine is necessary, and dosage must be carefully calculated based on weight and body surface area. Strict adherence to dosage and application instructions is crucial.

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Geriatric Use

Elderly patients may be more sensitive to the systemic effects of lidocaine due to age-related decreases in hepatic function, renal function, and cardiac output, which can affect lidocaine metabolism and clearance. Use with caution, starting with lower doses or less frequent application, and monitor closely for signs of systemic toxicity.

Clinical Information

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Clinical Pearls

  • Always advise patients to use the smallest effective amount for the shortest duration.
  • Emphasize that topical lidocaine is not for internal use, nor for application to mucous membranes or broken/irritated skin, as this significantly increases systemic absorption and toxicity risk.
  • Warn against using occlusive dressings or external heat sources (e.g., heating pads) over the application site, as this can dramatically increase systemic absorption.
  • Be aware of the risk of methemoglobinemia, especially in infants or patients with certain genetic predispositions (e.g., G6PD deficiency), though rare with topical lidocaine alone.
  • Educate patients on the signs of systemic toxicity (CNS and cardiac symptoms) and when to seek immediate medical attention.
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Alternative Therapies

  • Other topical anesthetics (e.g., benzocaine, tetracaine)
  • Topical NSAIDs (e.g., diclofenac gel)
  • Topical capsaicin cream
  • Oral analgesics (e.g., acetaminophen, NSAIDs)
  • Ice packs or cold therapy
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Cost & Coverage

Average Cost: $15 - $50 per 15gm tube
Generic Available: Yes
Insurance Coverage: Tier 1 or Tier 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 details. 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 information about the medication taken, the amount, and the time it happened.