Tacrolimus 0.03% Ointment 100gm
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.
Drug Class
Topical immunomodulator; Calcineurin inhibitor
Pharmacologic Class
Calcineurin inhibitor
Pregnancy Category
Category C
FDA Approved
Dec 2000
DEA Schedule
Not Controlled
Overview
What is this medicine?
Tacrolimus ointment is a medication applied to the skin to treat eczema (atopic dermatitis). It works by calming down the immune system in your skin to reduce redness, itching, and inflammation. It is not a steroid.
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.
- Avoid bathing, showering, or swimming immediately after applying the medication.
- Continue using the medication until the health problem is resolved.
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 lid tightly closed and ensure all medications are kept 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.
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.
- Avoid bathing, showering, or swimming immediately after applying the medication.
- Continue using the medication until the health problem is resolved.
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 lid tightly closed and ensure all medications are kept 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.
Lifestyle & Tips
- Apply a thin layer only to the affected skin areas. Do not use on large areas of the body or under occlusive dressings (bandages, wraps) unless directed by your doctor.
- Wash your hands before and after applying the ointment.
- Avoid contact with eyes, mouth, and nose. If contact occurs, rinse thoroughly with water.
- Avoid excessive exposure to natural or artificial sunlight (tanning beds, UVA/UVB light therapy) while using this medication, as it may increase the risk of skin cancer. Use sunscreen and wear protective clothing.
- Do not bathe, shower, or swim immediately after applying the ointment, as this may wash off the medication.
- Do not use on skin that is broken, infected, or has open wounds.
- Limit alcohol consumption, as it may cause flushing or warmth of the skin when using tacrolimus ointment.
Available Forms & Alternatives
Available Strengths:
- Tacrolimus 1mg Capsules
- Tacrolimus 0.5mg (half Mg) Capsules
- Tacrolimus 5mg (five Mg) Capsules
- Tacrolimus 1mg Caps (bx)
- Tacrolimus 0.5mg (half Mg) Cap(bx)
- Tacrolimus 5mg (five Mg)caps (bx)
- Tacrolimus 0.03% Ointment 30gm
- Tacrolimus 0.03% Ointment 60gm
- Tacrolimus 0.03% Ointment 100gm
- Tacrolimus 0.1% Ointment 30gm
- Tacrolimus 0.1% Ointment 60gm
- Tacrolimus 0.1% Ointment 100gm
Dosing & Administration
Adult Dosing
Standard Dose:
Apply a thin layer to affected skin areas twice daily. Rub in gently and completely. Discontinue when signs and symptoms of atopic dermatitis resolve.
Condition-Specific Dosing:
atopicDermatitis:
Apply a thin layer to affected skin areas twice daily. Rub in gently and completely. Discontinue when signs and symptoms of atopic dermatitis resolve. Continue for up to 6 weeks if symptoms persist, or until resolution. Intermittent long-term use may be considered for prevention of flares.
Pediatric Dosing
Neonatal:
Not established (contraindicated in children <2 years of age)
Infant:
Not established (contraindicated in children <2 years of age)
Child:
For children 2 to 15 years of age: Tacrolimus 0.03% ointment. Apply a thin layer to affected skin areas twice daily. Rub in gently and completely. Discontinue when signs and symptoms of atopic dermatitis resolve.
Adolescent:
For adolescents ≥16 years of age: Tacrolimus 0.03% or 0.1% ointment. Apply a thin layer to affected skin areas twice daily. Rub in gently and completely. Discontinue when signs and symptoms of atopic dermatitis resolve.
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed (minimal systemic absorption)
Moderate:
No adjustment needed (minimal systemic absorption)
Severe:
No adjustment needed (minimal systemic absorption)
Dialysis:
No adjustment needed (minimal systemic absorption)
Hepatic Impairment:
Mild:
No adjustment needed (minimal systemic absorption)
Moderate:
No adjustment needed (minimal systemic absorption)
Severe:
No adjustment needed (minimal systemic absorption)
Pharmacology
Mechanism of Action
Tacrolimus is a macrolactam immunomodulator. It inhibits calcineurin, a phosphatase, thereby blocking the transcription of early T-cell activation genes (e.g., IL-2, IL-3, IL-4, IL-5, GM-CSF, TNF-alpha). This leads to the inhibition of T-lymphocyte activation and proliferation, and also inhibits the release of pro-inflammatory cytokines from mast cells and basophils, reducing inflammation in atopic dermatitis.
Pharmacokinetics
Absorption:
Bioavailability:
Minimal (<0.5% to 1% systemically absorbed after topical application, varies with skin integrity and surface area)
Tmax:
Variable (systemic concentrations are generally low and often undetectable)
FoodEffect:
Not applicable for topical formulation
Distribution:
Vd:
Not well-defined for topical application due to minimal systemic absorption. If absorbed systemically, highly distributed.
ProteinBinding:
Highly protein bound (>98.8%) to plasma proteins (albumin and alpha-1-acid glycoprotein) if absorbed systemically.
CnssPenetration:
Limited (minimal systemic absorption)
Elimination:
HalfLife:
Systemic half-life is long (e.g., 25-60 hours) if absorbed, but topical application results in very low systemic exposure.
Clearance:
Not well-defined for topical application due to minimal systemic absorption.
ExcretionRoute:
Primarily fecal (92.6%) and urinary (2.1%) if absorbed systemically.
Unchanged:
Less than 1% of dose excreted unchanged in urine if absorbed systemically.
Pharmacodynamics
OnsetOfAction:
Improvement in symptoms typically seen within 1-2 weeks.
PeakEffect:
Peak therapeutic effect may take several weeks of consistent use.
DurationOfAction:
Effects persist as long as treatment is continued; flares may recur upon discontinuation.
Safety & Warnings
BLACK BOX WARNING
Long-term safety of topical calcineurin inhibitors has not been established. Although a causal relationship 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. Therefore, continuous long-term use of topical calcineurin inhibitors in any age group should be avoided, and application should be limited to areas of involvement. Tacrolimus ointment is not indicated for use in children younger than 2 years of age.
Side Effects
Urgent 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:
+ Unable to pass urine
+ Change in how much urine is passed
+ 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. However, many people do not experience any side effects or only have mild ones. If you are bothered by any of the following side effects or if they 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
This is not an exhaustive list of possible 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.
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:
+ Unable to pass urine
+ Change in how much urine is passed
+ 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. However, many people do not experience any side effects or only have mild ones. If you are bothered by any of the following side effects or if they 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
This is not an exhaustive list of possible 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.
Seek Immediate Medical Attention If You Experience:
- Severe burning, stinging, or itching that does not improve or worsens
- Signs of skin infection (e.g., pus, spreading redness, fever, warmth)
- Swollen lymph nodes (glands) in your neck, armpits, or groin
- New or worsening skin lesions, moles, or changes in skin color
- Unusual tiredness, unexplained weight loss, or night sweats (rare, but report to doctor)
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.
Certain health conditions, including:
+ Skin areas with cancer or precancerous lesions
+ Netherton's syndrome, a specific skin disease
+ Other skin problems that may weaken your 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 medications and health problems with your doctor.
To ensure your safety, provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter (OTC) medications you are taking
Natural products and vitamins you are using
* Any health problems you have
Before starting, stopping, or changing the dose of any medication, including this one, consult with your doctor to confirm it is safe for you to do so.
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.
Certain health conditions, including:
+ Skin areas with cancer or precancerous lesions
+ Netherton's syndrome, a specific skin disease
+ Other skin problems that may weaken your 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 medications and health problems with your doctor.
To ensure your safety, provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter (OTC) medications you are taking
Natural products and vitamins you are using
* Any health problems you have
Before starting, stopping, or changing the dose of any medication, including this one, consult with your doctor to confirm it is safe for you to do so.
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 sunlight, sunlamps, and tanning beds. When going outside, use sunscreen 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 any potential interactions. It is also crucial to talk to your doctor before using any other medications or products on your skin, including soaps.
Regular skin checks are necessary, so be sure to follow your doctor's instructions for scheduling these examinations.
Common side effects of this medication 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 that this medication is ingested, it can be harmful. 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 this medication to both you and your baby to ensure informed decision-making.
To minimize the risk of adverse effects, avoid exposure to sunlight, sunlamps, and tanning beds. When going outside, use sunscreen 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 any potential interactions. It is also crucial to talk to your doctor before using any other medications or products on your skin, including soaps.
Regular skin checks are necessary, so be sure to follow your doctor's instructions for scheduling these examinations.
Common side effects of this medication 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 that this medication is ingested, it can be harmful. 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 this medication to both you and your baby to ensure informed decision-making.
Overdose Information
Overdose Symptoms:
- Topical overdose is unlikely due to minimal systemic absorption. If accidentally ingested, systemic effects could occur, but are rare for the ointment.
What to Do:
If accidental ingestion occurs, contact a poison control center or seek immediate medical attention. Call 1-800-222-1222.
Drug Interactions
Moderate Interactions
- Live vaccines (theoretical risk of reduced immune response, though systemic absorption is minimal)
- Immunosuppressants (concurrent use with other systemic immunosuppressants is not recommended due to potential for additive immunosuppression, though systemic absorption of topical tacrolimus is minimal)
Minor Interactions
- CYP3A4 inhibitors (e.g., erythromycin, itraconazole, ketoconazole, diltiazem, grapefruit juice) - theoretical risk of increased systemic tacrolimus levels if significant absorption occurs, but generally not clinically relevant for topical use.
- UV light therapy (phototherapy) - concurrent use is not recommended due to potential for increased skin cancer risk.
Monitoring
Routine Monitoring
Skin condition (e.g., erythema, pruritus, lichenification)
Frequency: Regularly during treatment
Target: Improvement or resolution of symptoms
Action Threshold: Lack of improvement, worsening symptoms, or signs of infection warrant re-evaluation.
Signs of skin infection
Frequency: Regularly during treatment
Target: Absence of infection (e.g., pus, spreading redness, fever)
Action Threshold: Presence of infection requires appropriate treatment and potential discontinuation of tacrolimus.
Symptom Monitoring
- Burning or stinging sensation at application site (common, usually transient)
- Pruritus (itching)
- Erythema (redness)
- Folliculitis
- Acne
- Headache
- Flu-like symptoms
- Signs of skin infection (e.g., pus, warmth, spreading redness, fever)
- Swollen lymph nodes (lymphadenopathy)
Special Patient Groups
Pregnancy
Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Systemic absorption is minimal, but animal studies have shown adverse effects at high systemic doses. Category C.
Trimester-Specific Risks:
First Trimester:
Limited human data; animal studies show developmental toxicity at high systemic doses.
Second Trimester:
Limited human data.
Third Trimester:
Limited human data.
Lactation
Tacrolimus is excreted in human milk after systemic administration. It is not known whether topical application results in sufficient systemic absorption to produce detectable quantities in breast milk. Caution should be exercised when tacrolimus ointment is administered to a nursing woman. Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for tacrolimus ointment and any potential adverse effects on the breastfed infant from tacrolimus ointment or from the underlying maternal condition.
Infant Risk:
L3 - Moderate concern (potential for systemic exposure, though low for topical; monitor infant for adverse effects).
Pediatric Use
Contraindicated in children younger than 2 years of age. For children 2 to 15 years of age, only the 0.03% strength is recommended. Long-term safety has not been established. Use for shortest duration necessary.
Geriatric Use
No specific dosage adjustment is required. Clinical studies did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. However, systemic exposure is minimal, so age-related pharmacokinetic changes are unlikely to be clinically significant.
Clinical Information
Clinical Pearls
- Tacrolimus ointment is a second-line therapy for atopic dermatitis in patients who have failed to respond adequately to other topical prescription treatments, or when those treatments are not advisable.
- It is important to inform patients about the Black Box Warning regarding potential malignancy risk and to emphasize avoiding continuous long-term use and excessive sun exposure.
- Initial application may cause transient burning or stinging, which usually subsides with continued use.
- Avoid using on acutely infected skin lesions. Treat infections before starting tacrolimus.
- Do not use occlusive dressings over the treated area, as this may increase systemic absorption.
Alternative Therapies
- Pimecrolimus cream (Elidel) - another topical calcineurin inhibitor
- Topical corticosteroids (e.g., hydrocortisone, triamcinolone, fluocinonide)
- Crisaborole ointment (Eucrisa) - phosphodiesterase-4 (PDE4) inhibitor
- Ruxolitinib cream (Opzelura) - Janus kinase (JAK) inhibitor
- Systemic therapies for severe atopic dermatitis (e.g., dupilumab, tralokinumab, oral JAK inhibitors, systemic immunosuppressants)
- Phototherapy
Cost & Coverage
Average Cost:
$150 - $400 per 100gm tube
Generic Available:
Yes
Insurance Coverage:
Tier 2 or Tier 3 (Specialty/Non-preferred Brand)
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, a patient fact sheet that provides crucial information. 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 amount, and the time it occurred.