Lidocaine 5% Anorectal Cream

Manufacturer NIVAGEN PHARMACEUTICALS 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
Voltage-gated sodium channel blocker
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Pregnancy 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 applied to the skin around the anus to relieve pain, itching, and discomfort caused by conditions like hemorrhoids or anal fissures. 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 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

  • Clean and dry the affected area before applying the cream.
  • Wash hands thoroughly before and after application.
  • Apply a thin layer of cream; do not use more than directed.
  • Avoid contact with eyes, nose, and mouth.
  • Do not use on large areas of skin or on broken/inflamed skin unless directed by a doctor, as this can increase absorption and risk of side effects.
  • Avoid prolonged use without consulting a doctor.
  • Maintain good bowel habits to prevent straining (e.g., high-fiber diet, adequate hydration).

Dosing & Administration

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Adult Dosing

Standard Dose: Apply to the affected area up to 6 times daily, as needed.

Condition-Specific Dosing:

Hemorrhoids and Anal Fissures: Apply a thin layer to the affected area up to 6 times daily. Do not exceed 20g per 24 hours for extensive use.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established for self-administration; consult a physician for use in children under 12 years.
Adolescent: For adolescents 12 years and older, adult dosing may apply under medical supervision.
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment needed for topical use due to minimal systemic absorption.
Moderate: No specific adjustment needed for topical use due to minimal systemic absorption.
Severe: No specific adjustment needed for topical use due to minimal systemic absorption. Use with caution if extensive application on compromised skin, as systemic absorption may increase.
Dialysis: No specific adjustment needed for topical use. Use with caution if extensive application on compromised skin.

Hepatic Impairment:

Mild: No specific adjustment needed for topical use due to minimal systemic absorption.
Moderate: No specific adjustment needed for topical use due to minimal systemic absorption. Use with caution if extensive application on compromised skin, as systemic absorption may increase.
Severe: No specific adjustment needed for topical use due to minimal systemic absorption. Use with caution if extensive application on compromised skin, as systemic absorption may increase.

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 the generation and propagation of nerve impulses.
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Pharmacokinetics

Absorption:

Bioavailability: Low (variable, depends on application site, skin integrity, and duration of exposure); systemic absorption is minimal from intact skin/mucosa but increases with inflamed or broken skin.
Tmax: Variable (typically 2-10 minutes for onset of action, peak effect within 5-15 minutes for topical application).
FoodEffect: Not applicable for topical formulation.

Distribution:

Vd: 0.7-2.7 L/kg (if systemically absorbed)
ProteinBinding: 60-80% (primarily to alpha-1-acid glycoprotein and albumin)
CnssPenetration: Limited (if systemically absorbed, crosses blood-brain barrier)

Elimination:

HalfLife: 1.5-2 hours (systemic)
Clearance: Approximately 0.95 L/min (systemic)
ExcretionRoute: Renal (primarily as metabolites)
Unchanged: <10% (systemic)
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Pharmacodynamics

OnsetOfAction: 2-5 minutes (topical)
PeakEffect: 5-15 minutes (topical)
DurationOfAction: 30 minutes to 3 hours (topical, depending on site and concentration)

Safety & Warnings

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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
+ 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 extremely 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 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:

Irritation at the site of application
Swelling
Redness
Skin discoloration

This is not an exhaustive list of possible side effects. If you have 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:

  • Increased redness, swelling, or irritation at the application site.
  • Rash, hives, or itching that spreads beyond the application area.
  • Difficulty breathing or swallowing (signs of allergic reaction).
  • Dizziness, lightheadedness, drowsiness, confusion.
  • Blurred vision or ringing in the ears.
  • Numbness or tingling around the mouth.
  • Tremors or muscle twitching.
  • Slow or irregular heartbeat.
  • If symptoms do not improve or worsen after 7 days of use, consult a doctor.
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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, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine if it is safe to take this medication in conjunction with your other treatments and health issues. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
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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 has been associated with drugs similar to this one. Your risk may be increased if you have a condition called 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 ever had methemoglobinemia, be sure to tell 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 it, and do not expose it to extreme temperatures.

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

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

If you are 65 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 with your doctor to ensure the best decision for you and your baby.
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Overdose Information

Overdose Symptoms:

  • Severe dizziness or drowsiness
  • Nausea, vomiting
  • Blurred vision, double vision
  • Ringing in the ears (tinnitus)
  • Numbness or tingling around the mouth
  • Tremors, muscle twitching
  • Seizures
  • Slow or irregular heartbeat (bradycardia)
  • Low blood pressure (hypotension)
  • Difficulty breathing, respiratory depression
  • Coma

What to Do:

If you suspect an overdose, seek immediate medical attention or call a poison control center (1-800-222-1222). Overdose with topical lidocaine is rare but can occur with excessive application, especially on broken skin. Management involves supportive care, maintaining airway, breathing, and circulation, and treating symptoms (e.g., benzodiazepines for seizures, vasopressors for hypotension, atropine for bradycardia).

Drug Interactions

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Moderate Interactions

  • Antiarrhythmics (Class I, e.g., tocainide, mexiletine): Increased risk of cardiac effects if significant systemic absorption occurs.
  • Beta-blockers (e.g., propranolol): May reduce hepatic metabolism of lidocaine, increasing systemic levels if significant absorption occurs.
  • Cimetidine: May inhibit lidocaine metabolism, increasing systemic levels if significant absorption occurs.
  • Other local anesthetics: Additive systemic effects if significant absorption occurs.

Monitoring

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Routine Monitoring

Local skin reaction (redness, irritation, swelling)

Frequency: Daily, with each application

Target: Absence of significant irritation

Action Threshold: Discontinue use and consult physician if severe irritation, rash, or allergic reaction occurs.

Effectiveness of pain/itching relief

Frequency: Daily, with each application

Target: Symptom improvement

Action Threshold: Consult physician if symptoms persist or worsen after several days of use.

Signs of systemic toxicity (rare with proper topical use)

Frequency: Monitor for symptoms

Target: Absence of systemic symptoms

Action Threshold: Seek immediate medical attention if dizziness, drowsiness, blurred vision, ringing in ears, tremors, nervousness, or seizures occur.

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Symptom Monitoring

  • Local irritation (redness, itching, rash, swelling, burning)
  • Allergic reactions (hives, difficulty breathing, swelling of face/lips/tongue/throat)
  • Signs of systemic toxicity (dizziness, lightheadedness, drowsiness, confusion, blurred vision, ringing in ears, numbness/tingling around mouth, tremors, muscle twitching, seizures, slow heart rate, low blood pressure, difficulty breathing)

Special Patient Groups

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Pregnancy

Lidocaine is generally considered safe for topical use during pregnancy when used as directed, due to minimal systemic absorption. Consult a healthcare provider before use.

Trimester-Specific Risks:

First Trimester: Low risk; minimal systemic absorption.
Second Trimester: Low risk; minimal systemic absorption.
Third Trimester: Low risk; minimal systemic absorption.
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Lactation

Lidocaine is considered compatible with breastfeeding (L2). Minimal amounts are excreted into breast milk after topical application, and systemic absorption in the infant is unlikely to cause adverse effects.

Infant Risk: Low risk
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Pediatric Use

Use with caution in children, especially those under 12 years of age. Pediatric skin may absorb more lidocaine, increasing the risk of systemic toxicity. Dosing should be carefully calculated by a healthcare professional based on weight and surface area, and application should be limited to the smallest effective amount for the shortest duration. Self-administration in children is not recommended.

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Geriatric Use

No specific dose adjustments are typically needed for topical lidocaine in geriatric patients. However, elderly patients may be more sensitive to the systemic effects if significant absorption occurs due to potential age-related changes in liver or kidney function, or reduced protein binding. Use the lowest effective dose and monitor for adverse effects.

Clinical Information

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Clinical Pearls

  • Lidocaine 5% anorectal cream is for external use only. Do not ingest.
  • Always wash hands thoroughly before and after applying the cream.
  • Do not apply to large areas of skin, open wounds, or severely damaged skin without medical advice, as this increases the risk of systemic absorption and toxicity.
  • Avoid using occlusive dressings (e.g., plastic wrap) over the treated area unless specifically instructed by a healthcare professional, as this can also increase absorption.
  • If using for hemorrhoids, apply gently to the external area. For internal hemorrhoids, an applicator tip may be provided, but use with caution and as directed.
  • Discontinue use and seek medical attention if you experience severe burning, stinging, swelling, or signs of an allergic reaction or systemic toxicity.
  • Keep out of reach of children and pets.
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Alternative Therapies

  • Phenylephrine (vasoconstrictor for hemorrhoids)
  • Hydrocortisone (topical corticosteroid for inflammation and itching)
  • Witch hazel (astringent)
  • Zinc oxide (skin protectant)
  • Stool softeners (to prevent straining)
  • Sitz baths (for comfort and hygiene)
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Cost & Coverage

Average Cost: $15 - $50 per 30g tube
Generic Available: Yes
Insurance Coverage: Tier 1 or Tier 2 (often covered by most insurance plans as a generic)
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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.