Tacrolimus 0.1% Ointment 100gm
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.
Drug Class
Topical immunosuppressant
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 medicine applied to the skin to treat eczema (atopic dermatitis). It works by calming down the overactive immune system in your skin that causes eczema symptoms like redness and itching. It's 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. It is essential to use this medication only as directed.
Apply this medication topically, directly to the affected area of your skin. Do not ingest it or apply it to your mouth, nose, or eyes, as it may cause irritation or burning.
Before and after applying the medication, wash your hands thoroughly, unless your hand is the area being treated. 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 to do so, 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 this medication until your skin condition improves. If your symptoms persist after 6 weeks of treatment, consult your doctor for further guidance.
To minimize skin reactions, moisturize your skin as advised by your doctor.
Storage and Disposal
To maintain the medication's effectiveness and safety:
Store it at room temperature in a dry place, avoiding bathrooms.
Keep the container tightly closed.
* Store all medications in a secure 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 scheduled dose, skip the missed dose and resume your regular application schedule. Do not apply two doses at once or use extra doses to make up for a missed one.
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 area of your skin. Do not ingest it or apply it to your mouth, nose, or eyes, as it may cause irritation or burning.
Before and after applying the medication, wash your hands thoroughly, unless your hand is the area being treated. 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 to do so, 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 this medication until your skin condition improves. If your symptoms persist after 6 weeks of treatment, consult your doctor for further guidance.
To minimize skin reactions, moisturize your skin as advised by your doctor.
Storage and Disposal
To maintain the medication's effectiveness and safety:
Store it at room temperature in a dry place, avoiding bathrooms.
Keep the container tightly closed.
* Store all medications in a secure 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 scheduled dose, skip the missed dose and resume your regular application schedule. Do not apply two doses at once or use extra doses to make up for a missed one.
Lifestyle & Tips
- Apply a thin layer only to the affected skin areas.
- Wash hands thoroughly after applying the ointment, unless hands are the treated area.
- Avoid prolonged or unnecessary sun exposure, including tanning beds and UV light therapy, while using this medication. Use sunscreen and wear protective clothing.
- Do not cover the treated area with bandages or wraps unless directed by your doctor.
- Avoid bathing, showering, or swimming immediately after application to allow the ointment to absorb.
- 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.
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.
Condition-Specific Dosing:
atopicDermatitis:
Apply a thin layer to affected skin areas twice daily. Continue for 1 week after clearing of signs and symptoms.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established for infants under 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. Rub in gently and completely. Continue for 1 week after clearing of signs and symptoms. Tacrolimus 0.1% Ointment is generally not recommended for children under 16 years.
Adolescent:
For adolescents 16 years of age and older: Apply a thin layer of Tacrolimus 0.1% Ointment to affected skin areas twice daily. Rub in gently and completely. Continue for 1 week after clearing of signs and symptoms.
Dose Adjustments
Renal Impairment:
Mild:
No dosage adjustment generally needed due to minimal systemic absorption.
Moderate:
No dosage adjustment generally needed due to minimal systemic absorption.
Severe:
No dosage adjustment generally needed due to minimal systemic absorption. Use with caution in patients with severe renal impairment due to potential for increased systemic exposure if skin barrier is compromised.
Dialysis:
No specific recommendations; use with caution.
Hepatic Impairment:
Mild:
No dosage adjustment generally needed due to minimal systemic absorption.
Moderate:
No dosage adjustment generally needed due to minimal systemic absorption.
Severe:
No dosage adjustment generally needed due to minimal systemic absorption. Use with caution in patients with severe hepatic impairment due to potential for increased systemic exposure if skin barrier is compromised.
Pharmacology
Mechanism of Action
Tacrolimus is a macrolactam immunomodulator. It inhibits calcineurin, a phosphatase, thereby blocking the transcription of early T-cell activation genes, such as interleukin-2 (IL-2). This leads to the inhibition of T-lymphocyte activation and proliferation, and also inhibits the release of pro-inflammatory cytokines and mediators from mast cells and basophils.
Pharmacokinetics
Absorption:
Bioavailability:
Minimal systemic absorption (typically <1%) after topical application, but can increase with compromised skin barrier or large surface area application.
Tmax:
Variable, generally 1-2 days for detectable systemic levels, if any.
FoodEffect:
Not applicable for topical formulation.
Distribution:
Vd:
Not well characterized for topical application due to minimal systemic absorption. Systemically, highly protein bound.
ProteinBinding:
Approximately 98.8% (systemic)
CnssPenetration:
Limited (systemic)
Elimination:
HalfLife:
Variable, generally 40-70 hours (systemic, if absorbed).
Clearance:
Not well characterized for topical application.
ExcretionRoute:
Primarily fecal (systemic), with minor renal excretion.
Unchanged:
<1% (systemic)
Pharmacodynamics
OnsetOfAction:
Improvement in symptoms typically seen within 1 week.
PeakEffect:
Maximal therapeutic effect may take several weeks.
DurationOfAction:
Effects persist as long as treatment is continued; long-term remission can be achieved with intermittent therapy.
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 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 the absence of clinical signs and symptoms of atopic dermatitis, should be avoided. Limit application to areas of involvement. Tacrolimus ointment is not indicated for use in children younger than 2 years of age.
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.
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.
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, worsening pain).
- Swollen lymph nodes (glands) in the neck, armpits, or groin.
- New or unusual skin lesions or moles.
- Any signs of allergic reaction (e.g., rash, hives, swelling of face/lips/tongue, difficulty breathing).
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 pre-cancerous lesions
+ Netherton's syndrome, a specific skin disease
+ Other skin problems that may weaken your skin
+ Active skin infections, such as chicken pox 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, tell your doctor and pharmacist about:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
* Your complete medical history, including all health problems
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 pre-cancerous lesions
+ Netherton's syndrome, a specific skin disease
+ Other skin problems that may weaken your skin
+ Active skin infections, such as chicken pox 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, tell your doctor and pharmacist about:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
* Your complete medical history, including all health problems
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 longer than recommended by your doctor.
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 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 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 few 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.
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 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 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 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 few 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.
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.
Overdose Information
Overdose Symptoms:
- Systemic overdose is unlikely with topical application due to minimal absorption. If ingested, symptoms could include nausea, vomiting, abdominal pain, headache, tremor, and kidney dysfunction (similar to systemic tacrolimus toxicity).
What to Do:
If accidental ingestion occurs, seek immediate medical attention or call a poison control center (1-800-222-1222). For topical overuse, wash off excess ointment. Management is generally supportive.
Drug Interactions
Contraindicated Interactions
- Not applicable for topical tacrolimus under normal use conditions. Avoid live vaccines during treatment if significant systemic absorption is suspected.
Major Interactions
- Systemic immunosuppressants (e.g., cyclosporine, corticosteroids): Concomitant use with topical tacrolimus is not recommended due to potential for additive immunosuppression, though systemic absorption is minimal.
- CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, erythromycin, diltiazem, grapefruit juice): While systemic absorption is low, theoretical risk of increased systemic tacrolimus levels if applied to large areas or compromised skin.
Moderate Interactions
- Vaccines (live attenuated): Avoid administration of live vaccines during treatment, especially if there is concern for systemic absorption, due to potential for reduced vaccine efficacy or increased risk of infection.
Minor Interactions
- Not applicable for topical formulation under normal use.
Monitoring
Baseline Monitoring
Skin assessment
Rationale: To evaluate the extent and severity of atopic dermatitis.
Timing: Prior to initiation of therapy.
Routine Monitoring
Clinical response (skin lesions, pruritus)
Frequency: Regularly during treatment, typically at follow-up visits.
Target: Improvement or resolution of signs and symptoms.
Action Threshold: Lack of improvement after 6 weeks, worsening symptoms, or development of adverse reactions should prompt re-evaluation.
Signs of skin infection
Frequency: At each visit and patient self-monitoring.
Target: Absence of new or worsening infections.
Action Threshold: Presence of infection requires appropriate treatment; consider temporary discontinuation of tacrolimus.
Signs of malignancy (lymphadenopathy, skin lesions)
Frequency: Periodically, especially during long-term use.
Target: Absence of suspicious findings.
Action Threshold: Any suspicious findings require prompt investigation.
Symptom Monitoring
- Burning sensation at application site
- Itching (pruritus)
- Erythema (redness)
- Folliculitis
- Acne
- Headache
- Flu-like symptoms
- Signs of skin infection (e.g., pus, spreading redness, fever)
- Swollen lymph nodes
Special Patient Groups
Pregnancy
Tacrolimus ointment is classified as Pregnancy Category C. Animal studies have shown adverse effects on the fetus, but there are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Systemic absorption is minimal, but caution is advised.
Trimester-Specific Risks:
First Trimester:
Potential for developmental toxicity observed in animal studies; human data limited.
Second Trimester:
Limited human data; animal studies suggest potential for adverse effects.
Third Trimester:
Limited human data; animal studies suggest potential for adverse effects.
Lactation
Tacrolimus is excreted in human milk after systemic administration. While systemic absorption from topical application is minimal, 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 or from the underlying maternal condition.
Infant Risk:
L3 (Moderate risk) - Low systemic absorption suggests low infant exposure, but potential for adverse effects cannot be completely ruled out.
Pediatric Use
Approved for use in children 2 years of age and older. The 0.03% ointment is generally recommended for children aged 2 to 15 years. The 0.1% ointment is approved for patients 16 years and older. Not recommended for children younger than 2 years of age due to potential for increased systemic absorption and unknown long-term effects.
Geriatric Use
No specific dosage adjustments are recommended 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, systemic absorption is minimal, and no age-related differences in safety or efficacy are expected.
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.
- Patients should be advised about the Black Box Warning regarding potential malignancy risk and the importance of using the lowest effective dose for the shortest duration necessary.
- Avoid use on large surface areas, broken skin, or for prolonged periods without medical supervision.
- Sun protection is crucial during treatment due to potential photosensitivity and theoretical increased risk of skin cancer.
- Initial application may cause transient burning, stinging, or itching, which usually improves with continued use.
- Do not use occlusive dressings over the treated area.
- Patients should avoid live vaccines during treatment, especially if there is concern for systemic absorption.
Alternative Therapies
- Topical corticosteroids (e.g., hydrocortisone, triamcinolone, fluocinonide)
- Topical phosphodiesterase-4 (PDE4) inhibitors (e.g., crisaborole ointment)
- Topical JAK inhibitors (e.g., ruxolitinib cream)
- Phototherapy (UVB, UVA)
- Systemic immunosuppressants (e.g., cyclosporine, methotrexate, dupilumab, tralokinumab) for severe cases.
Cost & Coverage
Average Cost:
$200 - $600 per 100gm tube
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (often requires prior authorization)
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 for guidance. 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.