Lidocaine 5% Anorectal Cream 15gm

Manufacturer PATRIN Active Ingredient Lidocaine Rectal Cream and Gel(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
Amide-type local anesthetic; 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 5% Anorectal Cream is a numbing medicine used to relieve pain, itching, soreness, or burning caused by conditions like hemorrhoids, anal fissures, or other irritations in the rectal area. It works by temporarily blocking nerve signals in the skin, reducing discomfort.
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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 the information provided with your medication. Before and after applying the medication, wash your hands thoroughly. Clean the affected area before use and make sure it is completely dry. Apply the medication as directed by your doctor or according to the package labeling.

Storing and Disposing of Your Medication

Store your medication at room temperature, avoiding freezing. Keep all medications in a secure 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 disposing of your medication, consult your pharmacist. You may also want to check if there are drug take-back programs available in your area.

Missing a Dose

If you use this medication regularly, take a missed dose as soon as you remember. However, 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 take 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

  • Maintain good anal hygiene by gently cleaning the area after bowel movements.
  • Avoid excessive straining during bowel movements.
  • Increase dietary fiber and fluid intake to promote softer stools and reduce straining.
  • Avoid prolonged sitting on the toilet.
  • Follow your doctor's advice on diet and lifestyle changes for underlying conditions.

Dosing & Administration

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Adult Dosing

Standard Dose: Apply a small amount (e.g., pea-sized or up to 1 gram) to the affected area up to 3 to 4 times daily. Max 60 grams in 24 hours for extensive use, but typically much less for anorectal application.

Condition-Specific Dosing:

anorectal_pain_itching: Apply a small amount to the affected area up to 3-4 times daily. Do not exceed recommended frequency or amount.
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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: Not established (not recommended for children under 12 years without physician consultation; if used, apply lowest effective dose to smallest area)
Adolescent: Not established (for adolescents 12 years and older, consult physician; may use adult dosing with caution and close monitoring)
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment typically needed for topical use with low systemic absorption.
Moderate: No specific adjustment typically needed for topical use with low systemic absorption.
Severe: No specific adjustment typically needed for topical use with low systemic absorption. Use with caution if extensive application or impaired skin barrier due to potential for increased systemic exposure.
Dialysis: No specific adjustment typically needed for topical use with low systemic absorption. Use with caution if extensive application or impaired skin barrier.

Hepatic Impairment:

Mild: No specific adjustment typically needed for topical use with low systemic absorption.
Moderate: Use with caution. Lidocaine is primarily metabolized by the liver. While systemic absorption from topical use is low, significant impairment could theoretically increase systemic levels if absorption is high.
Severe: Use with extreme caution. Significant hepatic impairment can reduce lidocaine clearance, increasing risk of systemic toxicity if absorption occurs. Avoid extensive 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 effecting local anesthetic action. It specifically blocks voltage-gated sodium channels in the neuronal membrane.
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Pharmacokinetics

Absorption:

Bioavailability: Variable (depends on application site, skin integrity, dose, and duration of application; generally low for intact skin, higher for mucous membranes or broken skin)
Tmax: Variable (e.g., 30-60 minutes for topical application, if significant systemic absorption occurs)
FoodEffect: Not applicable (topical administration)

Distribution:

Vd: 1.1-2.1 L/kg (systemic)
ProteinBinding: 60-80% (primarily alpha-1-acid glycoprotein)
CnssPenetration: Limited (with proper topical application; can occur with significant systemic absorption)

Elimination:

HalfLife: 1.5-2 hours (parent drug, systemic)
Clearance: 0.95 L/min (systemic)
ExcretionRoute: Renal (metabolites)
Unchanged: <10% (parent drug in urine)
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Pharmacodynamics

OnsetOfAction: 2-5 minutes (topical)
PeakEffect: 10-20 minutes (topical)
DurationOfAction: 30-60 minutes (topical, depending on formulation and site)

Safety & Warnings

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Side Effects

Serious Side Effects: Seek Medical Help Immediately

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you experience any of the following symptoms, contact your doctor or seek medical attention right away:

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
Respiratory problems, 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
Rectal bleeding or pain

Other Possible Side Effects

Like all medications, this drug can cause side effects. However, many people experience no side effects or only mild ones. If you experience any of the following side effects or any other symptoms that concern you, contact your doctor:

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:

  • Signs of an allergic reaction: rash, hives, itching, swelling (especially of the face, tongue, or throat), severe dizziness, trouble breathing.
  • Signs of systemic toxicity: dizziness, lightheadedness, blurred vision, ringing in the ears, numbness or tingling around the mouth, tremors, confusion, slow heart rate, low blood pressure, difficulty breathing, or seizures. Seek immediate medical attention if these occur.
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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, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction and its symptoms.
The presence of an infection at the site where this medication will be applied.
Any broken skin or open wounds at the application site.
If you have swollen skin, numbness, or a loss of sensation at the application site, which may affect your ability to feel pain.

This list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. They will help you determine if it is safe to take this medication with your other medications and health conditions.

Remember, do not start, stop, or change 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.

There is a risk of developing a severe blood disorder called methemoglobinemia associated with this type of drug. This risk may be increased in individuals with certain conditions, such as glucose-6-phosphate dehydrogenase (G6PD) deficiency, 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 products on your skin, including soaps, consult with your doctor. It is crucial to follow your doctor's instructions regarding the use of this medication and not exceed the recommended duration of treatment.

To minimize potential complications, avoid scratching or rubbing the skin while it is numb, and do not expose it to extreme temperatures. Do not apply this medication to cuts, scrapes, or damaged skin unless specifically instructed to do so by your doctor.

Avoid using heat sources, such as sunlamps, tanning beds, heating pads, electric blankets, heat lamps, saunas, hot tubs, or heated waterbeds, as they can cause your body temperature to rise and lead to excessive absorption of the medication. Also, avoid taking long, hot baths or sunbathing.

If this medication is accidentally ingested, seek immediate medical attention by calling a doctor or poison control center. Be aware that different brands of this medication may be suitable for children of varying ages, so consult with your doctor before administering it to a child.

When using this medication in children, exercise caution, as they may be more susceptible to certain side effects. Similarly, if you are 65 or older, use this medication with caution, as you may be more prone to experiencing side effects.

If you are pregnant, planning to become pregnant, or breastfeeding, discuss the potential benefits and risks of this medication with your doctor to ensure the best possible outcome for you and your baby.
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Overdose Information

Overdose Symptoms:

  • Severe dizziness or lightheadedness
  • Numbness or tingling around the mouth
  • Blurred vision or double vision
  • Ringing in the ears (tinnitus)
  • Tremors or muscle twitching
  • Confusion or disorientation
  • Slurred speech
  • Seizures
  • Slow or irregular heartbeat (bradycardia, arrhythmias)
  • Low blood pressure (hypotension)
  • Difficulty breathing
  • Loss of consciousness

What to Do:

If you suspect an overdose, seek immediate emergency medical attention. Call 911 or your local poison control center (e.g., 1-800-222-1222 in the US).

Drug Interactions

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Major Interactions

  • Other local anesthetics (additive systemic toxicity)
  • Class I antiarrhythmics (e.g., mexiletine, tocainide - additive cardiac effects)
  • Antiarrhythmics (e.g., amiodarone, propafenone - increased risk of cardiac depression)
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Moderate Interactions

  • Beta-blockers (e.g., propranolol - may reduce hepatic blood flow, potentially increasing lidocaine levels)
  • Cimetidine (inhibits CYP enzymes, potentially increasing lidocaine levels)
  • Succinylcholine (may prolong neuromuscular blockade)
  • Phenytoin (may increase lidocaine clearance, but also potential for additive cardiac effects)
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Confidence Interactions

Monitoring

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Baseline Monitoring

Assessment of skin integrity

Rationale: Broken or irritated skin can increase systemic absorption and risk of toxicity.

Timing: Prior to first application

History of allergies to local anesthetics

Rationale: To identify potential hypersensitivity reactions.

Timing: Prior to first application

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Routine Monitoring

Local irritation (redness, swelling, itching, burning)

Frequency: With each application and as needed

Target: Absence of symptoms

Action Threshold: Discontinue use if severe or persistent; consult healthcare provider.

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

Frequency: With each application and as needed, especially with extensive use or compromised skin

Target: Absence of symptoms

Action Threshold: Discontinue use immediately and seek emergency medical attention.

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Symptom Monitoring

  • Burning
  • Stinging
  • Rash
  • Itching
  • Swelling
  • Increased pain
  • Dizziness
  • Lightheadedness
  • Blurred vision
  • Ringing in ears (tinnitus)
  • Numbness or tingling around the mouth
  • Tremors
  • Confusion
  • Slow heart rate (bradycardia)
  • Low blood pressure (hypotension)
  • Difficulty breathing
  • Seizures

Special Patient Groups

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Pregnancy

Lidocaine is Pregnancy Category B. Generally considered safe for topical use during pregnancy when used at recommended doses and for limited periods. Use only if clearly needed and potential benefits outweigh potential risks.

Trimester-Specific Risks:

First Trimester: Low risk based on animal studies, but human data are limited. Use with caution.
Second Trimester: Generally considered safe for topical use at recommended doses.
Third Trimester: Generally considered safe for topical use at recommended doses.
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Lactation

Lidocaine is excreted into breast milk in small amounts. It is generally considered compatible with breastfeeding when used topically at recommended doses. Monitor the infant for any signs of adverse effects (e.g., drowsiness, feeding difficulties).

Infant Risk: Low (L2)
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Pediatric Use

Use with extreme caution in children, especially infants and young children, due to a higher risk of systemic toxicity from absorption. Children have a larger surface area to body weight ratio and less mature metabolic pathways. Dosing must be carefully calculated based on weight and surface area, and application should be limited to the smallest effective area for the shortest duration. Not recommended for children under 12 years without medical supervision.

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Geriatric Use

Use with caution. Elderly patients may be more susceptible to systemic adverse effects due to decreased hepatic metabolism, reduced renal clearance, and/or potential for underlying cardiac conditions. Start with lower doses and monitor closely for signs of systemic toxicity.

Clinical Information

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Clinical Pearls

  • Apply sparingly to the affected area. Do not use on large areas of skin, on broken or irritated skin, or under occlusive dressings for prolonged periods without medical advice, as this significantly increases systemic absorption and the risk of toxicity.
  • Wash hands thoroughly before and after application.
  • Avoid contact with eyes. If contact occurs, rinse thoroughly with water.
  • Systemic toxicity, though rare with proper topical use, can be serious and manifest as CNS (e.g., dizziness, confusion, tremors, seizures) or cardiovascular (e.g., bradycardia, hypotension, arrhythmias) effects. Educate patients on these warning signs.
  • This cream is for external use only on the anorectal area. Do not ingest.
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Alternative Therapies

  • Other topical anesthetics (e.g., pramoxine, benzocaine)
  • Topical corticosteroids (e.g., hydrocortisone cream for inflammation)
  • Astringents (e.g., witch hazel pads)
  • Protectants (e.g., zinc oxide, petrolatum, preparation H)
  • Oral analgesics (for systemic pain relief)
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Cost & Coverage

Average Cost: $10 - $30 per 15gm tube
Generic Available: Yes
Insurance Coverage: Tier 1 or Tier 2 (most insurance plans)
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General Drug Facts

If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, 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 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 happened.