Tacrolimus 0.1% Ointment 30gm

Manufacturer PERRIGO Active Ingredient Tacrolimus 0.1% Ointment(ta KROE li mus) Pronunciation ta KROE li mus
WARNING: All products:Long-term safety of this drug is not known. Lymphoma, skin cancer, and other types of cancer have rarely happened in people treated with this drug. It is not known if this drug caused this effect. Do not use this drug without a break for a long time unless told to do so by the doctor. Use only on the affected skin. If you have questions, talk with the doctor.This drug is not approved for use in children younger than 16 years of age. Talk with the doctor. @ COMMON USES: It is used to treat eczema.It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Topical immunomodulator
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Pharmacologic Class
Calcineurin inhibitor
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Pregnancy Category
Category C
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FDA Approved
Dec 2000
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Tacrolimus ointment is a non-steroidal medication used to treat moderate to severe eczema (atopic dermatitis) in adults and children aged 2 years and older. It works by calming the immune system in the skin, which helps to reduce inflammation, redness, and itching.
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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. This medication is for topical use only, meaning it should be applied directly to the affected area of your skin. Avoid getting it in your mouth, nose, or eyes, as it may cause burning.

Before applying the medication, wash your hands thoroughly. If the affected area is on your hand, you do not need to wash that hand after application. Clean the affected area before use and make sure it is completely dry. Then, apply a thin layer of the medication to the affected skin and gently rub it in.

Important Application Instructions

- Apply the medication only to the affected skin area. Do not apply it to healthy skin.
- Unless directed by your doctor, do not cover the treated area with bandages or dressings.
- After applying the medication, wait for some time before bathing, showering, or swimming.
- Continue using the medication until the health problem is resolved, as directed by your doctor.

Managing Skin Reactions

To help manage any skin reactions, moisturize your skin as advised by your doctor. If your symptoms do not improve after 6 weeks of treatment, consult with your doctor.

Storage and Disposal

Store this medication at room temperature in a dry place, avoiding storage in a bathroom. Keep the container tightly closed and store all medications in a safe location out of the reach of children and pets.

Missed Dose

If you miss a dose, apply it as soon as you remember. However, if it is close to the time for your next dose, skip the missed dose and continue with your regular schedule. Do not apply two doses at the same time or extra doses.
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Lifestyle & Tips

  • Apply a thin layer only to the affected skin areas. Do not apply to healthy skin.
  • Wash your hands thoroughly after applying the ointment, unless your hands are the treated area.
  • Avoid excessive exposure to natural or artificial sunlight (e.g., tanning beds, sunlamps) while using this medication. Use sunscreen and wear protective clothing.
  • Do not cover the treated skin with bandages or other occlusive dressings, as this may increase absorption.
  • Avoid alcohol consumption if you experience facial flushing or skin irritation after drinking.
  • Do not use on skin that is broken, infected, or has open wounds.

Dosing & Administration

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Adult Dosing

Standard Dose: Apply a thin layer to affected skin areas twice daily.

Condition-Specific Dosing:

atopicDermatitis: Apply a thin layer to affected skin areas twice daily. Discontinue after signs and symptoms resolve. If symptoms persist for more than 6 weeks, re-evaluate diagnosis.
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Pediatric Dosing

Neonatal: Not established (contraindicated for children under 2 years of age)
Infant: Not established (contraindicated for children under 2 years of age)
Child: For children 2 years and older: Apply a thin layer to affected skin areas twice daily. Discontinue after signs and symptoms resolve. If symptoms persist for more than 6 weeks, re-evaluate diagnosis.
Adolescent: Apply a thin layer to affected skin areas twice daily. Discontinue after signs and symptoms resolve. If symptoms persist for more than 6 weeks, re-evaluate diagnosis.
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Dose Adjustments

Renal Impairment:

Mild: No dosage adjustment needed due to minimal systemic absorption.
Moderate: No dosage adjustment needed due to minimal systemic absorption.
Severe: No dosage adjustment needed due to minimal systemic absorption.
Dialysis: No specific considerations for topical use due to minimal systemic absorption.

Hepatic Impairment:

Mild: No dosage adjustment needed due to minimal systemic absorption.
Moderate: No dosage adjustment needed due to minimal systemic absorption.
Severe: No dosage adjustment needed due to minimal systemic absorption.

Pharmacology

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Mechanism of Action

Tacrolimus is a calcineurin inhibitor. It binds to the cytosolic protein FKBP-12 (FK506 binding protein), forming a complex that inhibits calcineurin, a calcium-dependent phosphatase. This inhibition prevents the dephosphorylation of nuclear factor of activated T-cells (NF-AT), thereby inhibiting its translocation to the nucleus and subsequent transcription of early T-cell activation genes (e.g., interleukin-2, interferon-gamma). This leads to inhibition of T-lymphocyte activation and proliferation, and inhibition of inflammatory mediator release from mast cells and basophils.
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Pharmacokinetics

Absorption:

Bioavailability: Minimal (<0.5%) systemic absorption after topical application.
Tmax: Variable; often undetectable plasma concentrations. If detectable, typically within hours.
FoodEffect: Not applicable for topical administration.

Distribution:

Vd: Not clinically relevant due to minimal systemic absorption.
ProteinBinding: Not clinically relevant due to minimal systemic absorption (systemically, >98.8% bound).
CnssPenetration: Not clinically relevant due to minimal systemic absorption.

Elimination:

HalfLife: Not clinically relevant for topical use; systemic half-life is long (e.g., 25-100 hours) if absorbed.
Clearance: Not clinically relevant for topical use.
ExcretionRoute: Primarily fecal excretion if systemically absorbed.
Unchanged: Not clinically relevant for topical use.
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Pharmacodynamics

OnsetOfAction: Clinical improvement typically observed within 1-2 weeks.
PeakEffect: Continued improvement over several weeks of treatment.
DurationOfAction: Effect persists as long as applied, or for some time after discontinuation.

Safety & Warnings

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BLACK BOX WARNING

Long-term safety of topical calcineurin inhibitors has not been established. Rare cases of malignancy (e.g., skin cancer and lymphoma) have been reported in patients treated with topical calcineurin inhibitors, including tacrolimus ointment. A causal relationship has not been established. Continuous long-term use of topical calcineurin inhibitors, in the absence of data establishing safety, is not recommended. Tacrolimus ointment is not indicated for use in children younger than 2 years of age.
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Side Effects

Serious Side Effects: Seek Medical Attention Immediately

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 help 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 skin infection, including:
+ Oozing
+ Heat
+ Swelling
+ Redness
+ Pain
Signs of kidney problems, such as:
+ Inability to pass urine
+ Changes in urine output
+ Blood in the urine
+ Sudden weight gain
Fever
Ear pain
Skin lump or growth
Swollen gland
Muscle 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 discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical help:

Skin tingling
Skin irritation
Sensitivity to heat or cold
Headache
Cough
Stuffy nose
Flu-like symptoms
Pimples (acne)
Hair bumps
Upset stomach

Reporting Side Effects

This list is not exhaustive, and you may experience other 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:

  • Worsening of your skin condition or no improvement after 6 weeks.
  • Signs of a skin infection (e.g., pus, spreading redness, warmth, fever, pain).
  • New or changing skin lesions, moles, or lumps.
  • Swollen lymph nodes (glands) in your neck, armpits, or groin.
  • Severe burning, stinging, or itching that does not go away.
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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 you experienced, including any symptoms that occurred.
Certain health conditions, including:
+ Skin areas with cancer or precancerous lesions
+ Netherton's syndrome, a specific skin disease
+ Other skin problems that may weaken the skin
+ Active skin infections, such as chickenpox or herpes
+ A weakened immune system

This list is not exhaustive, and it is crucial to discuss all your health problems and medications with your doctor.

To ensure safe treatment, inform your doctor and pharmacist about:
All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
* Your complete medical history, including any health problems

Do not start, stop, or modify the dosage of any medication without first consulting your doctor to confirm it is safe to do so in conjunction with this medication.
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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. Adhere to the prescribed treatment duration, and do not use this drug for an extended period beyond what your doctor has recommended.

To minimize the risk of adverse effects, avoid exposure to direct sunlight, sunlamps, and tanning beds. When going outside, use a broad-spectrum sunscreen with a high sun protection factor (SPF) and wear protective clothing and eyewear to shield your skin from the sun. Additionally, refrain from undergoing any form of light therapy while using this medication.

Before consuming alcohol, consult with your doctor to discuss potential interactions and risks. It is also crucial to talk to your doctor before using any other medications or skin products, including soaps, to avoid potential interactions.

Regular skin checks are vital; follow your doctor's instructions for scheduling these examinations. Common side effects of this medication may include burning, stinging, soreness, or itching at the application site. These effects typically occur during the initial days of treatment and subside as your skin improves. However, if these symptoms are severe, persistent, or bothersome, contact your doctor for guidance.

In the event of accidental ingestion, this medication can be harmful. If you swallow this drug, immediately contact a doctor or a poison control center for assistance.

If you are pregnant, planning to become pregnant, or breastfeeding, inform your doctor. It is necessary to discuss the potential benefits and risks of this medication to both you and your baby to ensure informed decision-making.
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Overdose Information

Overdose Symptoms:

  • Unlikely with topical application due to minimal systemic absorption.
  • If ingested, symptoms could include systemic tacrolimus effects such as kidney problems, tremor, headache, nausea, vomiting, or diarrhea.

What to Do:

If swallowed, seek immediate medical attention or call a Poison Control Center (1-800-222-1222). Management is supportive; activated charcoal may be considered if ingestion is recent.

Drug Interactions

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Moderate Interactions

  • Live attenuated vaccines (theoretical risk due to potential systemic immunosuppression, though minimal with topical use)
  • Other systemic immunosuppressants (caution advised, though systemic absorption is minimal)
  • Excessive UV exposure (sunlight, tanning beds, phototherapy) due to theoretical risk of skin malignancy
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Minor Interactions

  • Alcohol (facial flushing or skin irritation has been reported in some patients)

Monitoring

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Baseline Monitoring

Skin assessment

Rationale: To evaluate the extent and severity of atopic dermatitis.

Timing: Prior to initiation of treatment.

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Routine Monitoring

Skin assessment

Frequency: Periodically, as clinically indicated, or at follow-up visits.

Target: Reduction in erythema, pruritus, and lesion severity.

Action Threshold: If no improvement after 6 weeks, re-evaluate diagnosis. If worsening, assess for infection or other causes.

Signs of skin infection

Frequency: With each visit and patient self-monitoring.

Target: Absence of new or worsening signs of infection (e.g., pus, spreading redness, fever).

Action Threshold: Discontinue use and treat infection if present.

Signs of malignancy (lymphoma, skin cancer)

Frequency: Periodically, especially with long-term use.

Target: Absence of new or changing skin lesions, or swollen lymph nodes.

Action Threshold: Refer for dermatological evaluation if suspicious lesions or lymphadenopathy develop.

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Symptom Monitoring

  • Local burning sensation
  • Itching (pruritus)
  • Erythema (redness)
  • Folliculitis
  • Acne
  • Headache
  • Flu-like symptoms
  • Alcohol intolerance (facial flushing, irritation)

Special Patient Groups

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Pregnancy

Category C. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Minimal systemic absorption is expected with topical use.

Trimester-Specific Risks:

First Trimester: Limited data, but minimal systemic absorption suggests low risk.
Second Trimester: Limited data, but minimal systemic absorption suggests low risk.
Third Trimester: Limited data, but minimal systemic absorption suggests low risk.
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Lactation

Caution advised. It is unknown whether tacrolimus is excreted in human milk after topical application. Systemic tacrolimus is excreted into breast milk. Weigh the benefits of breastfeeding against the potential risks to the infant.

Infant Risk: Low risk due to minimal maternal systemic absorption, but potential for infant exposure is unknown.
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Pediatric Use

Approved for children 2 years of age and older. Not recommended for children younger than 2 years due to potential for increased systemic absorption and theoretical risk of malignancy.

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Geriatric Use

No specific dosage adjustments are needed for elderly patients. Clinical studies did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. However, minimal systemic absorption suggests no age-related concerns.

Clinical Information

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Clinical Pearls

  • Tacrolimus ointment is a second-line treatment for atopic dermatitis, used when other therapies (e.g., topical corticosteroids) are not appropriate or effective.
  • Patients may experience transient burning or itching upon initial application, which usually subsides within a week as the skin condition improves.
  • Use intermittently for flares of atopic dermatitis, rather than continuously long-term.
  • Avoid applying to areas of active skin infection; treat the infection first.
  • Educate patients about the black box warning regarding potential malignancy risk and the importance of avoiding excessive sun exposure.
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Alternative Therapies

  • Topical corticosteroids (e.g., hydrocortisone, triamcinolone, fluticasone)
  • Crisaborole ointment (Eucrisa)
  • Ruxolitinib cream (Opzelura)
  • Pimecrolimus cream (Elidel)
  • Phototherapy (UVB, UVA)
  • Systemic therapies for severe atopic dermatitis (e.g., dupilumab, tralokinumab, cyclosporine, methotrexate)
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Cost & Coverage

Average Cost: $100 - $300+ per 30gm tube
Generic Available: Yes
Insurance Coverage: Tier 2 or Tier 3 (Specialty)
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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.

This medication is accompanied by a Medication Guide, which is a valuable resource that provides additional information. Please read this guide carefully and review it again whenever you receive a refill of your medication. If you have any questions or concerns about your medication, don't hesitate to discuss them with your doctor, 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 reporting the incident, be prepared to provide details about the medication taken, the amount consumed, and the time it occurred.