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Tacrolimus
Tacrolimus is an immunosuppressive medication used to prevent organ transplant rejection and to treat certain skin conditions such as atopic dermatitis (eczema). It works by suppressing the immune system to prevent the body from attacking the transplanted organ or reducing inflammation in autoimmune skin conditions. Tacrolimus is available in oral forms, injections, and topical formulations.
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Frequently Asked Questions
How long do I need to use tacrolimus after a transplant?
Tacrolimus is usually taken long-term to prevent organ rejection. Your doctor will monitor your progress and make dose adjustments over time based on your response to the medication and blood levels.
Can I use tacrolimus ointment on my face?
Yes, tacrolimus ointment can be used on the face for treating atopic dermatitis, but avoid contact with the eyes and mucous membranes. Only use it as directed by your doctor.
How long does it take for tacrolimus to start working?
For organ transplant patients, it can take several days for tacrolimus to reach therapeutic levels in the blood. For topical use in atopic dermatitis, improvement can typically be seen within 1 to 3 weeks of consistent use.
Can tacrolimus cause weight gain?
Tacrolimus is not commonly associated with significant weight gain. However, it can cause water retention, especially when used with other immunosuppressants.
Is it safe to drink alcohol while using tacrolimus?
There are no specific interactions between alcohol and tacrolimus, but alcohol can increase the risk of liver toxicity. It is best to consult your doctor regarding alcohol use.
Comprehensive Drug Guide
How Does Tacrolimus Work?
Tacrolimus works by inhibiting calcineurin, a protein involved in the activation of T-cells in the immune system. By blocking calcineurin, tacrolimus prevents T-cells from producing cytokines, substances that signal the immune system to attack perceived foreign threats. This suppression of T-cell activity helps prevent the immune system from rejecting transplanted organs and reduces inflammation in autoimmune skin conditions.
Common Dosages
- Oral capsules (Prograf): 0.5 mg, 1 mg, 5 mg (taken twice daily).
- Topical ointment (Protopic): 0.03% and 0.1% strength.
- IV injection: Dosage based on body weight and the specific condition being treated.
Typical Dosing
- For organ transplant rejection prevention:
- Oral capsules: The typical starting dose is 0.1 to 0.2 mg/kg/day, divided into two doses, with dose adjustments based on blood levels and organ function.
- IV injection: For patients unable to take oral medications, tacrolimus can be administered via IV at a dose of 0.03 to 0.05 mg/kg/day.
- For atopic dermatitis (topical ointment):
- Adults and children aged 16 years and older: Apply 0.1% ointment twice daily to the affected areas.
- Children aged 2 to 15 years: Apply 0.03% ointment twice daily to the affected areas.
Typical Dosing
FDA Approved Indications
- Prevention of organ transplant rejection, particularly in kidney, liver, and heart transplants.
- Moderate to severe atopic dermatitis (eczema) in adults and children over 2 years old (topical ointment).
Who Shouldn't Take Tacrolimus?
- Hypersensitivity to tacrolimus or any component of the formulation.
- Severe liver disease without proper monitoring.
- Breastfeeding, as tacrolimus can pass into breast milk.
Advice From The Pharmacist
- Oral tacrolimus should be taken at the same time each day, and it is essential to take it either consistently with or without food, as food can affect its absorption.
- Topical tacrolimus should be applied only to the affected skin areas, and avoid using it on infected skin or open wounds. Do not cover the treated area with bandages unless directed by your doctor.
- Avoid excessive sunlight and UV exposure while using tacrolimus, as it may increase your skin's sensitivity to the sun.
- Monitor your blood levels regularly if you are taking tacrolimus for transplant rejection, as the dose may need adjustment to maintain the correct therapeutic level and avoid toxicity.
Side Effects of Tacrolimus
Common Side Effects
- Headache
- Diarrhea
- Nausea or vomiting
- Insomnia
- Tremors
For topical tacrolimus, side effects may include:
- Burning or itching at the application site
- Skin redness or irritation
- Increased risk of skin infections
Uncommon/Severe Side Effects
- Kidney damage (nephrotoxicity)
- High blood pressure (hypertension)
- Increased risk of infections due to immune suppression
- Increased risk of certain cancers, including lymphoma and skin cancer (especially with long-term use)
Risks and Warnings of Tacrolimus
- Infection Risk: Tacrolimus suppresses the immune system, which increases the risk of infections, including viral, bacterial, and fungal infections. Patients should report signs of infection (fever, chills, cough) to their doctor immediately.
- Kidney Damage: Tacrolimus can cause nephrotoxicity, particularly at higher doses. Kidney function should be regularly monitored, especially in transplant patients.
- Lymphoma and Skin Cancer: Long-term use of tacrolimus, especially in organ transplant patients, may increase the risk of lymphoma and skin cancer. Patients should avoid prolonged sun exposure and use sun protection.
Interactions with Tacrolimus
Common Drug Interactions
- CYP3A4 inhibitors (such as ketoconazole, erythromycin): These medications can increase tacrolimus blood levels, leading to a higher risk of toxicity.
- CYP3A4 inducers (such as rifampin, phenytoin): These medications can reduce tacrolimus levels, reducing its effectiveness.
- NSAIDs (such as ibuprofen): Combining NSAIDs with tacrolimus can increase the risk of kidney damage.
- Live vaccines: Avoid live vaccines while taking tacrolimus, as the immune suppression can reduce the vaccine's effectiveness or increase the risk of infection from the vaccine.
Alternatives to Tacrolimus
- Cyclosporine (Neoral, Sandimmune): Another calcineurin inhibitor used for transplant rejection and autoimmune conditions.
- Pimecrolimus (Elidel): A topical immunosuppressant used to treat atopic dermatitis, similar to tacrolimus but with a different profile.
- Mycophenolate mofetil (CellCept): Another immunosuppressant often used in organ transplant patients in combination with tacrolimus or other agents.