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tacrolimus

Pronunciation

Generic Name: tacrolimus (oral and injection) (ta KROE li mus)
Brand Name: Astagraf XL, Hecoria, Prograf

What is tacrolimus?

Tacrolimus lowers your body's immune system. The immune system helps your body fight infections. The immune system can also fight or "reject" a transplanted organ such as a liver or kidney. This is because the immune system treats the new organ as an invader.

Tacrolimus is used together with other medicines to prevent your body from rejecting a heart, liver, or kidney transplant.

Tacrolimus may also be used for purposes not listed in this medication guide.

What is the most important information I should know about tacrolimus?

Tacrolimus may increase your risk of developing serious infections, cancer, or transplant failure. Talk with your doctor about the risks and benefits of using this medication.

Slideshow: 2014 Update - First Time Brand-to-Generic Switches

Call your doctor right away if you have any signs of infection, such as fever, chills, body aches, skin warmth or redness, or flu symptoms.

What should I discuss with my healthcare provider before taking tacrolimus?

You should not use this medication if you are allergic to tacrolimus or hydrogenated castor oil, or if you have used cyclosporine (Neoral, Sandimmune, Gengraf) within the past 24 hours.

Tacrolimus can lower blood cells that help your body fight infections, or cause your body to produce too much of a certain type of white blood cell. This can lead to serious and sometimes fatal conditions, including cancer, a severe brain infection that can lead to disability or death, or a virus that can cause failure of a transplanted kidney.

Using tacrolimus may increase your risk of developing skin cancer, especially if you are treated over long periods of time with drugs that weaken the immune system. Talk with your doctor about your specific risk.

Some people taking tacrolimus after a kidney transplant have developed diabetes. This effect has been seen most commonly in people who are Hispanic or African-American. Talk with your doctor about your individual risk of diabetes if you have concerns.

To make sure tacrolimus is safe for you, tell your doctor if you have:

  • kidney or liver disease;

  • heart disease, high blood pressure, high cholesterol or triglycerides (a type of fat in the blood);

  • a heart rhythm disorder or history of long QT syndrome;

  • if you take heart rhythm medication;

  • if you use other medicines to prevent rejection of a transplanted organ; or

  • if you use other medications that can weaken your immune system.

FDA pregnancy category C. It is not known whether tacrolimus will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication.

Tacrolimus can pass into breast milk and may harm a nursing baby. You should not breast-feed while you are using tacrolimus.

How should I take tacrolimus?

Follow all directions on your prescription label. Your doctor may occasionally change your dose to make sure you get the best results. Do not take this medicine in larger or smaller amounts or for longer than recommended.

You may receive an injection of tacrolimus shortly after your transplant. Tacrolimus injection is given until you are ready to take the pill form of tacrolimus.

The tacrolimus capsule is usually taken every 12 hours. Take the medicine at the same time each day. You may take tacrolimus with or without food, but take it the same way each time.

Do not crush, chew, break, or open an extended-release capsule. Swallow it whole.

While using tacrolimus, you may need frequent blood tests. Your blood pressure will need to be checked often.

Store at room temperature away from moisture and heat.

What happens if I miss a dose?

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while taking tacrolimus?

Avoid being near people who are sick or have infections. Tell your doctor at once if you develop signs of infection.

Do not receive a "live" vaccine while using tacrolimus, or you could develop a serious infection. Live vaccines include measles, mumps, rubella (MMR), rotavirus, typhoid, yellow fever, varicella (chickenpox), zoster (shingles), and nasal flu (influenza) vaccine.

Grapefruit and grapefruit juice may interact with tacrolimus and lead to unwanted side effects. Avoid the use of grapefruit products while taking tacrolimus.

Avoid exposure to sunlight or tanning beds. Tacrolimus can make you sunburn more easily. Wear protective clothing and use sunscreen (SPF 30 or higher) when you are outdoors.

Tacrolimus side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

  • swelling, rapid weight gain, little or no urinating;

  • chest pain, shortness of breath, feeling like you might pass out;

  • headache, tremors, numbness and tingly feeling, seizure (convulsions);

  • bloody or tarry stools, coughing up blood or vomit that looks like coffee grounds;

  • high blood pressure--severe headache, blurred vision, buzzing in your ears, anxiety, chest pain, shortness of breath, uneven heartbeats;

  • high blood sugar--increased thirst, increased urination, hunger, fruity breath odor, nausea, loss of appetite, drowsiness, blurred vision, confusion;

  • high potassium--slow heart rate, weak pulse, muscle weakness, tingly feeling;

  • low magnesium or phosphate--bone pain, jerky muscle movements, muscle weakness or limp feeling, slow reflexes;

  • signs of infection in the brain--change in your mental state, problems with speech or walking, decreased vision (may start gradually and get worse quickly); or

  • symptoms of a new infection--sudden weakness or ill feeling, fever, chills, sore throat, painful mouth sores, pain when swallowing, skin sores, cold or flu symptoms, cough, trouble breathing, pale skin, easy bruising, unusual bleeding.

Common side effects may include:

  • diarrhea, constipation, stomach pain;

  • weakness, mild headache;

  • sleep problems (insomnia); or

  • swelling in your hands or feet.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

See also: Side effects (in more detail)

Tacrolimus dosing information

Usual Adult Dose for Organ Transplant -- Rejection Prophylaxis:

For use in the prophylaxis of allograft rejection in transplant recipients:

INTRAVENOUS INJECTION:
-Kidney and Liver Transplant:
Initial Dose: 0.03 to 0.05 mg/kg/day as a continuous IV infusion
-Heart Transplant: 0.01 mg/kg/day as a continuous IV infusion

-Doses as high as 0.1 mg/kg/day as a continuous IV infusion may be appropriate.
-Continuous IV infusion of tacrolimus injection should be continued only until the patient can tolerate oral administration of the capsules. This usually occurs within 2 to 3 days.

IMMEDIATE RELEASE CAPSULE:
-Kidney Transplant:
In combination with azathioprine: 0.2 mg/kg/day orally
In combination with MMF/IL-2 receptor antagonist: 0.1 mg/kg/day orally
-Liver Transplant: 0.1 to 0.15 mg/kg/day orally
-Heart Transplant: 0.075 mg/kg/day orally

-Daily doses should be administered as two divided doses, every 12 hours.
-Doses as high as 0.3 mg/kg/day administered every 12 hours in 2 divided doses may be appropriate.
-The initial dose of should be administered no sooner than 6 hours after transplantation in liver and heart transplant patients. In kidney transplant patients, the initial dose may be administered within 24 hours of transplantation, but should be delayed until renal function has recovered.
-It is important to take immediate release capsules consistently every day either with or without food because the presence and composition of food decreases the bioavailability.
-Patients should not eat grapefruit or drink grapefruit juice.

EXTENDED RELEASE CAPSULE:
Kidney Transplant only:
-With basiliximab induction: 0.15 mg/kg/day orally as a single daily dose. Give first dose prior to or within 48 hours after transplant completion; may delay therapy initiation until renal function has recovered.
-Without induction:
0.1 mg/kg/day orally, preoperatively, as a single daily dose. Give preoperative dose within 12 hours prior to reperfusion.
0.2 mg/kg/day orally, postoperatively, as a single daily dose. Give first postoperative dose within 12 hours after reperfusion but not less than 4 hours after preoperative dose.

-Take tacrolimus extended release capsules once daily in the morning, preferably on an empty stomach; do not take with an alcoholic beverage or grapefruit juice; do not chew, divide or crush capsules.

Comments:
-Adult patients should receive doses at the lower end of the dosing range.
-Dosing of tacrolimus should be titrated based on clinical assessments of rejection and tolerability, and to maintain recommended trough concentration ranges. Monitoring of whole blood tacrolimus trough concentrations is recommended.
-Typical whole blood trough concentrations usually range from 5 to 20 ng/mL. Monitoring of tacrolimus blood levels is considered an essential component of toxicity evaluation. The incidence of adverse effects increase as blood levels rise above the typical range. Extra caution and closer monitoring are recommended when graft function changes or drug interactions are suspected.
-In a patient initially receiving an IV infusion of tacrolimus, the first dose of oral therapy should be given 8 to 12 hours after discontinuing the IV infusion.
-African-American kidney transplant patients may require higher doses of tacrolimus to attain comparable trough concentrations compared to Caucasian patients.
-Tacrolimus should not be used simultaneously with cyclosporine. Tacrolimus or cyclosporine should be discontinued at least 24 hours before initiating the other.
-Extended-release capsules are not interchangeable or substitutable with tacrolimus immediate-release capsules.

Usual Adult Dose for Graft Versus Host Disease:

(Not approved by FDA)
Prevention:
Initial dose: 0.03 mg/kg/day (based on lean body weight) as a continuous infusion. Treatment should begin at least 24 hours prior to stem cell infusion and continued only until oral medication can be tolerated.

Treatment:
Initial dose: 0.03 mg/kg/day (based on lean body weight) as a continuous infusion.

Conversion from IV to oral dose (1:4 ratio): Multiply total daily IV dose times 4 and administer in 2 divided oral doses per day, every 12 hours.

Usual Pediatric Dose for Organ Transplant -- Rejection Reversal:

Liver transplant:
Oral: Initial dose: 0.15 to 0.2 mg/kg/day divided every 12 hours
IV: 0.03 to 0.05 mg/kg/day as a continuous infusion
Dose adjustments may be required. Doses as high as 0.15 mg/kg/day IV or 0.3 mg/kg/day orally have been used.

Heart transplant:
Oral: Initial dose: 0.1 to 0.3 mg/kg/day divided every 12 hours
IV: 0.01 to 0.03 mg/kg/day as a continuous infusion

Kidney transplant:
Oral: Initial dose: 0.2 to 0.3 mg/kg/day divided every 12 hours
IV: 0.06 mg/kg/day as a continuous infusion

Usual Pediatric Dose for Graft Versus Host Disease:

(Not approved by FDA)
Prevention:
Initial dose: 0.03 mg/kg/day (based on lean body weight) as continuous infusion. Treatment should begin at least 24 hours prior to stem cell infusion and continued only until oral medication can be tolerated.
Conversion from IV to oral dose (1:4 ratio): Multiply total daily IV dose times 4 and administer in 2 divided oral doses per day, every 12 hours.

What other drugs will affect tacrolimus?

Tacrolimus can harm your kidneys. This effect is increased when you also use certain other medicines, including: antivirals, chemotherapy, injected antibiotics, medicine for bowel disorders, injectable osteoporosis medication, and some pain or arthritis medicines (including aspirin, Tylenol, Advil, and Aleve).

Many medicines can interact with tacrolimus and should not be used at the same time. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible drug interactions are listed in this medication guide. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.

Where can I get more information?

  • Your pharmacist can provide more information about tacrolimus.
  • Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.
  • Disclaimer: Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

Copyright 1996-2012 Cerner Multum, Inc. Version: 7.01. Revision Date: 2013-11-14, 10:09:39 AM.

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