Tacrolimus 0.1% Ointment 60gm

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 medication applied to the skin to treat moderate to severe eczema (atopic dermatitis). It works by calming down the overactive immune system in your skin, which helps reduce redness, itching, and inflammation associated with eczema.
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How to Use This Medicine

Using Your Medication Correctly

To use this medication safely and effectively, follow your doctor's instructions carefully. Read all the information provided to you and follow the instructions closely.

Applying the Medication

Do not take this medication by mouth. It is for use on your skin only.
Avoid getting the medication in your mouth, nose, or eyes, as it may cause burning.
Wash your hands before and after applying the medication, unless your hand is the area being treated.
Clean the affected area before applying the medication and dry it thoroughly.
Apply a thin layer of the medication to the affected skin and gently rub it in.
Only apply the medication to the affected skin, avoiding healthy skin.
Do not cover the treated area with bandages or dressings unless your doctor instructs you to do so.
Avoid bathing, showering, or swimming immediately after applying the medication.

Continuing Treatment

Stop using the medication when your skin condition has improved.
To help manage skin reactions, moisturize your skin as directed by your doctor.
If your symptoms do not improve after 6 weeks of treatment, consult your doctor.

Storing and Disposing of Your Medication

Store the medication at room temperature in a dry place, away from the bathroom.
Keep the lid tightly closed.
Keep all medications in a safe place, out of the reach of children and pets.

Missing a Dose

If you 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 schedule.
* Do not apply two doses at the same time or take extra doses.
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Lifestyle & Tips

  • Apply a thin layer of ointment only to the affected areas of your skin.
  • Do not use occlusive dressings (like bandages or wraps) over the treated areas, as this can increase absorption.
  • Avoid excessive exposure to natural or artificial sunlight (e.g., tanning beds) while using this medication. Use sunscreen and wear protective clothing.
  • Do not use on skin that is broken, infected, or has open wounds.
  • Wash your hands thoroughly after applying the ointment, unless your hands are the treated area.
  • This medication is for short-term and intermittent use; avoid continuous long-term application.

Dosing & Administration

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Adult Dosing

Standard Dose: Apply a thin layer of Tacrolimus 0.1% Ointment to affected skin areas twice daily.

Condition-Specific Dosing:

atopicDermatitis: Apply a thin layer to affected skin areas twice daily. Discontinue when symptoms resolve. If symptoms recur, treatment can be reinitiated. Chronic continuous use should be avoided.
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Pediatric Dosing

Neonatal: Not established (contraindicated for children younger than 2 years of age)
Infant: Not established (contraindicated for children younger than 2 years of age)
Child: For children aged 2-15 years, Tacrolimus 0.03% Ointment is typically used. Apply a thin layer to affected skin areas twice daily. Tacrolimus 0.1% Ointment is not indicated for this age group.
Adolescent: For adolescents 16 years and older, Tacrolimus 0.1% Ointment can be used. Apply a thin layer to affected skin areas twice daily.
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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 immunophilin FKBP-12, 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. This leads to the inhibition of transcription of early T-cell activation genes (e.g., interleukin-2, interferon-gamma, TNF-alpha), ultimately suppressing T-lymphocyte activation and proliferation. It also inhibits the release of inflammatory mediators from mast cells and basophils.
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Pharmacokinetics

Absorption:

Bioavailability: Minimal, <0.5% systemically (highly variable)
Tmax: Variable, often undetectable in blood after topical application
FoodEffect: Not applicable for topical administration

Distribution:

Vd: Not well-defined for topical administration; if absorbed systemically, high
ProteinBinding: >98.8% (primarily to albumin and alpha-1-acid glycoprotein, if systemically absorbed)
CnssPenetration: Limited (if systemically absorbed)

Elimination:

HalfLife: Not well-defined for topical; if systemically absorbed, ~30-40 hours
Clearance: Not well-defined for topical
ExcretionRoute: Primarily fecal (if systemically absorbed), with minimal renal excretion
Unchanged: Minimal (if systemically absorbed)
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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

Cases of malignancy, including cutaneous and other lymphomas, and skin cancer, have been reported in patients treated with topical calcineurin inhibitors, including tacrolimus ointment. A causal relationship has not been established. Chronic continuous use of topical calcineurin inhibitors should be avoided in any age group, and application should be limited to areas of involvement with atopic dermatitis. Topical 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, this medication can cause severe and potentially life-threatening side effects. If you experience 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, 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 skin condition or no improvement after a few weeks of use.
  • Signs of a skin infection (e.g., pus, fever, spreading redness, warmth, pain).
  • Swollen lymph nodes (glands) in your neck, armpits, or groin.
  • Development of any new or unusual skin lesions, moles, or changes in existing ones.
  • Severe burning, stinging, or itching that does not subside after the first few days of treatment.
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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 symptoms you experienced as a result of the allergy.
Certain health conditions, including:
+ Skin areas with cancer or precancerous lesions
+ Netherton's syndrome, a specific skin disease
+ Other skin problems that may compromise skin integrity
+ 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 (OTC) medications you are taking
Any natural products or vitamins you are using
* All your health problems, including those not listed above

Before starting, stopping, or changing the dose of any medication, including this one, consult with your doctor to confirm it is safe to do so.
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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 products on your skin, 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 side effects are severe, persistent, or bothersome, contact your doctor for guidance.

In the event that this medication is ingested, it can cause harm. If accidental ingestion occurs, 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 using this medication during these situations to ensure the well-being of both you and your baby.
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Overdose Information

Overdose Symptoms:

  • If ingested (swallowed): Nausea, vomiting, abdominal pain, headache, tremor, paresthesia (tingling/numbness), and potential kidney dysfunction.
  • Topical overdose is unlikely to cause systemic toxicity due to poor absorption.

What to Do:

If swallowed, seek immediate medical attention or call Poison Control at 1-800-222-1222.

Drug Interactions

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Moderate Interactions

  • Live vaccines (theoretical concern if significant systemic absorption occurs, but generally not an issue for topical use)
  • Other immunosuppressants (additive immunosuppression, but unlikely to be clinically relevant with topical use due to minimal systemic absorption)

Monitoring

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Baseline Monitoring

Assessment of skin condition

Rationale: To establish baseline severity of atopic dermatitis and identify any contraindications (e.g., skin infections, malignancy).

Timing: Prior to initiation of therapy.

Patient history for skin malignancy or lymphoproliferative disorders

Rationale: Due to potential, though unproven, association with malignancy.

Timing: Prior to initiation of therapy.

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Routine Monitoring

Skin condition

Frequency: Regularly during treatment and follow-up

Target: Reduction in erythema, pruritus, and inflammation

Action Threshold: Worsening symptoms, signs of infection, or development of new skin lesions warrant re-evaluation.

Signs of skin infection (e.g., bacterial, viral, fungal)

Frequency: At each follow-up visit and as reported by patient

Target: Absence of infection

Action Threshold: Presence of infection requires appropriate treatment and potential temporary discontinuation of tacrolimus.

Lymphadenopathy

Frequency: Periodically

Target: Absence of persistent or significant lymphadenopathy

Action Threshold: Persistent or significant lymphadenopathy should be investigated.

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Symptom Monitoring

  • Burning sensation at application site (common, usually transient)
  • Itching
  • Stinging
  • Erythema (redness)
  • Folliculitis
  • Acne
  • Herpes simplex infection (cold sores, eczema herpeticum)
  • Varicella zoster infection (chickenpox, shingles)
  • Lymphadenopathy (swollen lymph nodes)
  • Unusual skin changes or new skin lesions

Special Patient Groups

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Pregnancy

Category C. Use only if the potential benefit justifies the potential risk to the fetus. While systemic absorption from topical application is minimal, data are limited.

Trimester-Specific Risks:

First Trimester: Limited data, theoretical risk based on systemic exposure.
Second Trimester: Limited data, theoretical risk based on systemic exposure.
Third Trimester: Limited data, theoretical risk based on systemic exposure.
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Lactation

L3 (Moderately Safe). Tacrolimus is excreted in breast milk after systemic administration. While systemic absorption from topical application is minimal, caution is advised. Consider the potential for infant exposure versus the maternal benefit. A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Infant Risk: Low risk of adverse effects to the infant due to minimal systemic absorption, but potential for exposure exists.
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Pediatric Use

Approved for children 2 years and older. Tacrolimus 0.03% ointment is typically used for children aged 2-15 years. Tacrolimus 0.1% ointment is indicated for adults and adolescents 16 years and older. Contraindicated for children younger than 2 years of age. Long-term safety in children is still under investigation.

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Geriatric Use

No specific dosage adjustments are needed. However, geriatric patients may have more fragile skin or other comorbidities, so monitor for skin integrity and potential for increased systemic absorption if the skin barrier is compromised.

Clinical Information

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Clinical Pearls

  • Tacrolimus ointment is a second-line therapy for atopic dermatitis, typically used when first-line therapies (e.g., topical corticosteroids) are ineffective or not tolerated, or for sensitive areas like the face and skin folds.
  • Patients may experience transient burning, stinging, or itching upon initial application, which usually subsides within a few days of continued use.
  • Emphasize the black box warning regarding potential malignancy risk; advise patients on intermittent, short-term use and limiting application to affected areas.
  • Strict sun protection (sunscreen, protective clothing) is crucial due to theoretical increased risk of skin cancer.
  • Avoid use on acutely infected skin lesions; treat infections before initiating tacrolimus.
  • Avoid bathing immediately after application to prevent washing off the ointment.
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Alternative Therapies

  • Topical corticosteroids (e.g., hydrocortisone, triamcinolone, fluocinonide)
  • Pimecrolimus cream (another topical calcineurin inhibitor)
  • Crisaborole ointment (Eucrisa)
  • Topical ruxolitinib cream (Opzelura)
  • Phototherapy (UVB)
  • Systemic immunosuppressants (e.g., cyclosporine, methotrexate, azathioprine) for severe cases
  • Biologic agents (e.g., dupilumab, tralokinumab) for severe cases
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Cost & Coverage

Average Cost: $100 - $400+ per 60gm tube of 0.1% ointment (generic)
Generic Available: Yes
Insurance Coverage: Tier 3 or higher, often requires prior authorization
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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. This medication is accompanied by a Medication Guide, which provides crucial information for patients. Please read this guide carefully and review it again whenever your prescription is refilled. If you have any questions or concerns about this medication, consult 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, and the time it occurred.