Tacrolimus

Tacrolimus is used along with other medications to prevent rejection (attack of a transplanted organ by the immune system of a person receiving the organ) in people who have received kidney, liver, or heart transplants. It is also used as a topical agent for treating eczema that has not responded to other medications.

Tacrolimus is in a class of medications called immunosupressants. It works by decreasing the activity of the immune system.

This medication comes in an immediate-release capsule form that is taken twice a day and extended-release capsule and tablet forms that are taken once a day. It is also available as an injectable form that is given as an ongoing infusion after the transplant surgery.

Tacrolimus is also available as a topical ointment that is applied to the affected skin twice a day.

Common side effects of oral and injectable tacrolimus include infection, altered renal function, increased blood pressure, headache, tremor, and nausea. Common side effects of topical tacrolimus include soreness or irritation at the application site.

Tacrolimus can also cause blurred vision, drowsiness, and dizziness. Do not drive or operate heavy machinery until you know how tacrolimus affects you.

Oral/Injectable:

Tacrolimus is used along with other medications to prevent rejection (attack of a transplanted organ by the immune system of a person receiving the organ) in people who have received kidney, liver, or heart transplants. It works by decreasing the activity of the immune system to prevent it from attacking the transplanted organ.

Topical:

Tacrolimus is used for treating eczema that has not responded to other medications. It works by stopping the immune system from producing substance that may cause eczema.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Tacrolimus may be found in some form under the following brand names:

• Astagraf

• Envarsus XR

• Hecoria

• Prograf

• Protopic

Serious side effects have been reported with Tacrolimus. See the “Tacrolimus Precautions” section.

Oral/injectable:

Common side effects of oral and injectable tacrolimus include the following:

• headache
• uncontrollable shaking of a part of the body
• diarrhea
• constipation
• nausea
• vomiting
• heartburn
• stomach pain
• loss of appetite
• difficulty falling asleep or staying asleep
• dizziness
• weakness
• back or joint pain
• burning, numbness, pain or tingling in the hands or feet

Topical:

Common side effects of topical tacrolimus include the following:

• skin burning, stinging, redness or soreness
• tingling skin
• increased sensitivity of the skin to hot or cold temperatures
• itching
• acne
• swollen or infected hair follicles
• headache
• muscle or back pain
• flu-like symptoms
• stuffy or runny nose
• nausea

This is not a complete list of tacrolimus side effects. Ask your doctor or pharmacist for more information.

Tell your doctor if you have any side effect that bothers you or that does not go away.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your doctor if you take:

• amphotericin B (Abelcet, Ambisome, Amphotec)
• antacids
• certain antibiotics including aminoglycosides such as amikacin, gentamicin, neomycin (Neo-Fradin), streptomycin, and tobramycin (Tobi), and macrolides such as clarithromycin (Biaxin), and erythromycin (EES, E-Mycin, Erythrocin)
• antifungal medications such as clotrimazole (Lotrimin, Mycelex), fluconazole (Diflucan), itraconazole (Sporanox), ketoconazole (Nizoral) and voriconazole (Vfend)
• bromocriptine (Parlodel)
• calcium channel blockers such as diltiazem (Cardizem), nicardipine (Cardene), nifedipine (Adalat, Procardia), and verapamil (Calan, Covera, Isoptin)
• caspofungin (Cancidas)
• chloramphenicol
• cimetidine (Tagamet)
• cisplatin (Platinol)
• cyclosporine (Gengraf, Neoral, Sandimmune)
• danazol (Danocrine)
• diuretics ('water pills')
• ganciclovir (Cytovene)
• hormonal contraceptives (birth control pills, patches, rings, inserts, or injections)
• HIV protease inhibitors such as indinavir (Crixivan), nelfinavir (Viracept), and ritonavir (Norvir)
• lansoprazole (Prevacid)
• medications for seizures such as carbamazepine (Tegretol), phenobarbital, and phenytoin (Dilantin)
• methylprednisolone (Medrol)
• metoclopramide (Reglan)
• nefazodone
• omeprazole (Prilosec)
• rifabutin (Mycobutin)
• rifampin (Rifadin, Rimactane)
• sirolimus (Rapamune)

This is not a complete list of tacrolimus drug interactions. Ask your doctor or pharmacist for more information.

Oral/injectable:

Serious side effects have been reported with tacrolimus including the following:

• Lymphoma and other malignancies. The risk of lymphomas after transplant appears related to intensity and duration of use of tacrolimus. Avoid prolonged exposure to UV light and sunlight.
• Serious infections. Patients receiving tacrolimus are at increased risk of bacterial, viral, fungal and protozoal infections, including opportunistic infections: combination immunosuppression should be used with caution.
• Diabetes mellitus. Patients are at risk for new onset diabetes after transplant and this risk may be increased by tacrolimus. Monitor blood glucose closely.
• Nephrotoxicity. Harm to the kidneys may be acute and/or chronic; if kidney function worsens, reduce the dose of tacrolimus. Use caution with other nephrotoxic drugs.
• Hypertension. Tacrolimus poses a risk for increased blood pressure that may require antihypertensive therapy. Monitor blood pressure regularly, and review medication list for relevant drug-drug interactions that may influence blood pressure.
• Anaphylactic reactions with IV formulation. Patients receiving tacrolimus injection may show signs and symptoms of anaphylaxis, including hives, rash, itching, and difficulty breathing or swallowing.

Tell your healthcare provider right away if you have any of the following signs or symptoms while receiving tacrolimus, which may suggest a serious reaction:

• decreased urination
• pain or burning on urination
• swelling of the arms, hands, feet, ankles or lower legs
• weight gain
• unusual bleeding or bruising
• seizures
• coma (loss of consciousness for a period of time)

Topical:

Serious side effects have been reported with topical tacrolimus including the following:

• Lymphoma and other malignancies: The risk of lymphomas after transplant appears related to intensity and duration of use of tacrolimus. Avoid prolonged exposure to UV light and sunlight.
• Nephrotoxicity: Harm to the kidneys may be acute and/or chronic; if kidney function worsens, reduce the dose of tacrolimus. Use caution with other nephrotoxic drugs.

Tell your healthcare provider right away if you have any of the following signs or symptoms while using tacrolimus ointment, which may suggest a serious reaction:

• swollen glands
• rash
• crusting, oozing, blistering or other signs of skin infection
• cold sores
• chicken pox or other blisters
• swelling of the hands, arms, feet, ankles, or lower legs

Tacrolimus can cause blurred vision, dizziness, and drowsiness. Do not drive or operate heavy machinery until you know how tacrolimus affects you.

Do not take tacrolimus if you are allergic to allergic to tacrolimus or to any of its ingredients.

Grapefruit and grapefruit juice may interact with tacrolimus and lead to potentially dangerous effects. Discuss the use of grapefruit products with your doctor.

Before taking tacolimus, tell your doctor about all of your medical conditions. Especially tell your doctor if you:

• are allergic to tacrolimus to any of its ingredients
• have or have had kidney disease
• have or have had liver disease
• have or have had heart disease
• are pregnant or breastfeeding

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements.

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X - are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

Tacrolimus falls into category C. There are no well-controlled studies that have been done in pregnant women. Tacrolimus should be used during pregnancy only if the possible benefit outweighs the possible risk to the unborn baby.

Tell your doctor if you are breastfeeding or plan to breastfeed.

Tacrolimus has been detected in human breast milk. Because of the possibility for adverse reactions in nursing infants from tacrolimus, a choice should be made whether to stop nursing or to stop use of this medication. The importance of the drug to the mother should be considered.

Oral/injectable:

Take tacrolimus exactly as prescribed.

This medication comes in an immediate-release capsule form that is taken twice a day and extended-release capsule and tablet forms that are taken once a day. It is also available as an injectable form that is given as an ongoing infusion after the transplant surgery.

If you miss a dose, take the missed dose as soon as you remember. If it is almost time for the next dose, skip the missed dose and take your next dose at the regular time. Do not take 2 doses of tacrolimus at the same time.

Avoid receiving live vaccines while using tacrolimus.

Topical:

Take tacrolimus exactly as prescribed.

Tacrolimus is also available as a topical ointment that is applied to the affected skin twice a day.

If you miss a dose, take the missed dose as soon as you remember. If it is almost time for the next dose, skip the missed dose and take your next dose at the regular time. Do not take 2 doses of tacrolimus at the same time.

Avoid prolonged exposure to the sun or UV light while using tacrolimus, even when the ointment is not on the skin.

Take this medication exactly as prescribed by your doctor. Follow the directions on your prescription label carefully.

Oral/injectable:

The dose your doctor recommends may be based on the following:

• the condition being treated
• other medical conditions you have
• other medications you are taking
• how you respond to this medication
• your weight

The recommended dose of tacolimus to prevent rejection after organ transplantation is based on the organ that was transplanted, the patient’s weight, and other medications that the patient is taking. The dose may be increased or decreased according to patient response and tolerability.

Topical:

The dose your doctor recommends may be based on the following:

• the condition being treated
• other medical conditions you have
• how you respond to this medication
• your age

The recommended dose of tacolimus to treat eczema is application of a thin layer of the ointment to the affected skin twice daily. Children aged 2 to 15 years should use the 0.03% ointment and adults can use either the 0.03% or 0.1% ointment. Treatment should be discontinued when signs and symptoms of eczema resolve.

If you take too much tacrolimus, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

If tacrolimus is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur. However, if overdose is suspected, seek emergency medical attention.

Oral/injectable:

• Store tacrolimus at room temperature.
• Keep this and all medicines out of the reach of children.

Topical:

• Store tacrolimus at room temperature.
• Keep this and all medicines out of the reach of children.

BOXED WARNING - MALIGNANCIES AND SERIOUS INFECTIONS

Increased risk of development of lymphoma and other malignancies, particularly of the skin, due to immunosuppression.

Increased susceptibility to bacterial, viral, fungal, and protozoal infections, including opportunistic infections.

Only physicians experienced in immunosuppressive therapy and management of organ transplant patients should prescribe tacrolimus. Patients receiving the drug should be managed in facilities equipped and staffed with adequate laboratory and supportive medical resources. The physician responsible for maintenance therapy should have complete information requisite for the follow-up of the patient.