Tacrolimus 0.03% Ointment 60gm

Manufacturer PERRIGO Active Ingredient Tacrolimus 0.03% Ointment(ta KROE li mus) Pronunciation ta KROE li mus
WARNING: 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 2 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
Immunosuppressant
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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 prescription medicine 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. It is typically used when other treatments haven't worked or aren't suitable.
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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. It is essential to use this medication only as directed.

Apply this medication topically, directly to the affected skin area. Do not ingest it or apply it to mucous membranes, such as the mouth, nose, or eyes, as it may cause irritation or burning.
Before and after applying the medication, wash your hands thoroughly, unless the treated area is on your hand. In that case, do not wash your hand after application.
Clean the affected area before applying the medication and ensure it is completely dry.
Gently rub a thin layer of the medication onto the affected skin. Avoid applying it to healthy skin.
Unless instructed by your doctor, do not cover the treated area with bandages or dressings.
After applying the medication, wait for a while before bathing, showering, or swimming.
Continue using the medication until the skin condition has resolved. If your symptoms persist or worsen after 6 weeks of treatment, consult your doctor.
To minimize skin reactions, follow your doctor's advice on moisturizing your skin.

Storage and Disposal

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

Missed Dose

If you forget to apply a dose, do so as soon as you remember.
If it is close to the time for your next scheduled dose, skip the missed dose and resume your regular application schedule.
Do not apply extra doses or double doses to make up for a missed dose.
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Lifestyle & Tips

  • Apply a thin layer only to the affected skin areas, as directed by your doctor. Do not use more than prescribed.
  • Wash your hands thoroughly after applying the ointment.
  • Avoid contact with eyes, nose, mouth, and genitals. If contact occurs, rinse thoroughly with water.
  • Do not apply to skin that is broken, infected, or has open wounds.
  • Do not cover the treated skin with bandages, wraps, or tight clothing unless specifically instructed by your doctor, as this may increase absorption.
  • Limit your exposure to natural or artificial sunlight (e.g., tanning beds) while using this medication. Wear protective clothing and use sunscreen if you must be in the sun.
  • Avoid using other topical products on the same area at the same time unless advised by your doctor.
  • This medication is not for continuous, long-term use. Use it only when you have symptoms of eczema and stop when your skin clears up.

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 when signs and symptoms resolve. If symptoms persist after 6 weeks, re-evaluate diagnosis.
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Pediatric Dosing

Neonatal: Not established (contraindicated in children younger than 2 years of age).
Infant: Not established (contraindicated in children younger than 2 years of age).
Child: For children 2 to 15 years of age: Apply a thin layer of Tacrolimus 0.03% Ointment to affected skin areas twice daily. Discontinue when signs and symptoms resolve. If symptoms persist after 6 weeks, re-evaluate diagnosis.
Adolescent: For adolescents 16 years of age and older: Apply a thin layer of Tacrolimus 0.03% Ointment to affected skin areas twice daily. Discontinue when signs and symptoms resolve. If symptoms persist after 6 weeks, re-evaluate diagnosis.
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Dose Adjustments

Renal Impairment:

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

Hepatic Impairment:

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

Pharmacology

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Mechanism of Action

Tacrolimus is a calcineurin inhibitor. It inhibits T-lymphocyte activation by binding to an intracellular protein, FKBP-12. This complex then inhibits calcineurin, a calcium-dependent phosphatase, thereby preventing the dephosphorylation and nuclear translocation of nuclear factor of activated T-cells (NF-AT). NF-AT is essential for the transcription of genes encoding early cytokines (e.g., interleukin-2, IL-3, IL-4, IL-5, GM-CSF, and TNF-alpha), which are involved in the initiation and progression of atopic dermatitis.
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Pharmacokinetics

Absorption:

Bioavailability: Very low systemic absorption (<0.5% in most patients with moderate to severe atopic dermatitis).
Tmax: Not well-defined for topical application; variable and low.
FoodEffect: Not applicable for topical administration.

Distribution:

Vd: Not well-defined for topical application due to minimal systemic absorption.
ProteinBinding: High (>98.8% to plasma proteins and erythrocytes) for systemically absorbed drug.
CnssPenetration: Limited/No for topical application.

Elimination:

HalfLife: Not well-defined for topical application; systemic half-life is highly variable (e.g., 25-60 hours).
Clearance: Not well-defined for topical application.
ExcretionRoute: Primarily fecal (for systemically absorbed drug), minimal renal excretion.
Unchanged: Minimal unchanged drug excreted.
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Pharmacodynamics

OnsetOfAction: Clinical improvement typically observed within days to weeks.
PeakEffect: Peak therapeutic effect may take several weeks of consistent application.
DurationOfAction: Requires continuous application for sustained effect; not a single-dose therapy.

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 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 signs and symptoms of atopic dermatitis, is not recommended. Limit application to areas of involvement with atopic dermatitis.
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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 unusual 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 not mentioned here. 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 a new skin infection (e.g., pus, spreading redness, warmth, fever)
  • Severe burning, stinging, or itching that does not go away or worsens after a few days of treatment
  • Swollen glands (lymph nodes) in your neck, armpits, or groin
  • New skin growths or changes in existing moles
  • Signs of an allergic reaction (e.g., rash, hives, swelling of the face/lips/tongue, difficulty breathing)
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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 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 side effects are severe, persistent, or bothersome, contact your doctor for guidance.

In the event that this medication is ingested, it can be harmful. If you or someone else accidentally swallows 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 using this medication during these situations to ensure the best possible outcome for you and your baby.
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Overdose Information

Overdose Symptoms:

  • Topical overdose is unlikely due to minimal systemic absorption. If a large amount is accidentally ingested, symptoms could include systemic tacrolimus toxicity (e.g., kidney problems, tremor, headache, nausea, vomiting, abdominal pain).

What to Do:

If you suspect an overdose or accidental ingestion, seek immediate medical attention. Call your doctor or Poison Control (1-800-222-1222) right away. For topical, wash off excess ointment with soap and water.

Drug Interactions

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Moderate Interactions

  • Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, erythromycin, diltiazem, grapefruit juice): Theoretical risk of increased systemic tacrolimus levels if significant systemic absorption occurs (e.g., on large areas of compromised skin or with occlusive dressings). Clinical significance is generally low for topical use.

Monitoring

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Baseline Monitoring

Skin condition assessment (e.g., Eczema Area and Severity Index - EASI)

Rationale: To establish baseline severity of atopic dermatitis and guide treatment.

Timing: Prior to initiation of therapy.

Lymph node examination

Rationale: To assess for lymphadenopathy, especially given the black box warning regarding lymphoma.

Timing: Prior to initiation of therapy.

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Routine Monitoring

Skin condition assessment

Frequency: Periodically, as clinically indicated (e.g., every 2-4 weeks initially, then less frequently once controlled).

Target: Improvement in signs and symptoms of atopic dermatitis (e.g., reduced erythema, pruritus, lichenification).

Action Threshold: Lack of significant improvement or worsening of symptoms after 6 weeks, or signs of skin infection.

Signs of skin infection (e.g., impetigo, folliculitis, herpes simplex)

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

Target: Absence of active infection.

Action Threshold: Presence of infection; treatment should be initiated or tacrolimus temporarily discontinued.

Lymph node examination

Frequency: Periodically, as clinically indicated.

Target: Absence of new or worsening lymphadenopathy.

Action Threshold: New or persistent lymphadenopathy; further investigation may be warranted.

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Symptom Monitoring

  • Burning sensation at application site
  • Itching (pruritus)
  • Stinging
  • Erythema (redness)
  • Folliculitis
  • Acne
  • Herpes simplex infection (cold sores, eczema herpeticum)
  • Skin irritation
  • Headache
  • Flu-like symptoms
  • Swollen lymph nodes
  • New skin lesions or changes in existing moles

Special Patient Groups

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Pregnancy

Tacrolimus ointment should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. While systemic absorption from topical application is minimal, oral tacrolimus is classified as Pregnancy Category C, indicating animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans.

Trimester-Specific Risks:

First Trimester: Limited data for topical. Oral tacrolimus: potential for developmental toxicity (e.g., malformations) at high doses in animal studies.
Second Trimester: Limited data for topical. Oral tacrolimus: potential for developmental toxicity at high doses.
Third Trimester: Limited data for topical. Oral tacrolimus: potential for premature birth, hyperkalemia, and renal dysfunction in neonates exposed in utero.
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Lactation

Use with caution. Tacrolimus is excreted in breast milk following systemic administration. Due to minimal systemic absorption of topical tacrolimus, infant exposure is expected to be low, but the potential for adverse effects on the breastfed infant cannot be excluded. 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: L3 (Moderately Safe) - limited human data, but low systemic absorption suggests low infant exposure. Monitor infant for adverse effects (e.g., immunosuppression, renal dysfunction).
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Pediatric Use

Approved for children 2 years of age and older. Not recommended for children under 2 years due to potential for increased systemic absorption in immature skin and lack of established safety/efficacy in this age group. Use the 0.03% concentration for children 2-15 years of age.

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Geriatric Use

No specific dose adjustment is needed for elderly patients. While elderly patients may have thinner skin, potentially leading to slightly increased absorption, tacrolimus ointment is generally well-tolerated in this population. Clinical studies did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects.

Clinical Information

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Clinical Pearls

  • Tacrolimus ointment is a second-line therapy for atopic dermatitis, typically reserved for patients who have not responded adequately to other topical prescription treatments or for whom those treatments are not advisable.
  • Patients should be advised to use the lowest effective concentration (0.03% for most, 0.1% for adults if needed) and apply only to affected areas.
  • Avoid continuous long-term use; use intermittently for flares of atopic dermatitis.
  • Sun protection is crucial due to the theoretical risk of skin malignancy associated with topical calcineurin inhibitors.
  • A burning or stinging sensation at the application site is a common side effect, especially at the start of treatment, and usually resolves within a few days.
  • Inform patients about the black box warning regarding potential malignancy risk, emphasizing that a causal relationship has not been established and the importance of intermittent use.
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Alternative Therapies

  • Pimecrolimus cream (another topical calcineurin inhibitor)
  • Topical corticosteroids (e.g., hydrocortisone, triamcinolone, fluocinonide)
  • Crisaborole ointment (topical phosphodiesterase-4 (PDE4) inhibitor)
  • Ruxolitinib cream (topical Janus kinase (JAK) inhibitor)
  • Dupilumab (injectable biologic for moderate-to-severe atopic dermatitis)
  • Tralokinumab (injectable biologic for moderate-to-severe atopic dermatitis)
  • Phototherapy (UVB, UVA)
  • Systemic immunosuppressants (e.g., cyclosporine, methotrexate, azathioprine - for severe, refractory cases)
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Cost & Coverage

Average Cost: $200 - $600 per 60gm 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 is essential to contact your doctor promptly. To ensure safe use, 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 you receive a refill of this medication. 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 quantity, and the time it occurred.