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Tacrolimus (oral and injection)

Generic name: tacrolimus (oral/injection) [ ta-KROE-li-mus ]
Brand names: Astagraf XL, Envarsus XR, Prograf, Hecoria
Dosage forms: intravenous solution (5 mg/mL), oral capsule (0.5 mg; 1 mg; 5 mg), oral capsule, extended release (0.5 mg; 1 mg; 5 mg), ... show all 5 dosage forms
Drug class: Calcineurin inhibitors

Medically reviewed by Drugs.com on Jul 31, 2023. Written by Cerner Multum.

What is tacrolimus?

Tacrolimus is used together with other medicines in people who have had a heart, kidney, liver, or lung transplant.

Tacrolimus weakens your immune system to prevent your body from "rejecting" the transplanted organ.

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

Tacrolimus side effects

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

You may get infections more easily, even serious or fatal infections. Call your doctor right away if you have signs of infection such as: fever, chills, flu symptoms, cough, sweating, painful skin sores, skin warmth or redness, or muscle aches.

Also call your doctor at once if you have:

Common side effects of tacrolimus may include:

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.

Warnings

Tacrolimus may increase your risk of developing a serious infection, skin cancer, or lymphoma. Talk with your doctor about the risks and benefits of using tacrolimus.

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

Before taking this medicine

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

Using tacrolimus may increase your risk of developing serious infections or certain types of cancer, such as lymphoma or skin cancer. Your risk may be higher if you are treated over long periods of time with drugs that weaken the immune system. Ask your doctor about this risk and about symptoms to watch for.

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.

Tell your doctor if you have ever had:

Tell your doctor if you plan to get pregnant. Tacrolimus may harm an unborn baby, and can worsen conditions such as diabetes or high blood pressure in the mother. Use effective birth control before and during treatment with tacrolimus.

If you are pregnant, your name may be listed on a pregnancy registry to track the effects of tacrolimus on the baby.

If you are a man, use birth control before and during treatment with tacrolimus if your sex partner is able to get pregnant.

Pregnancy may be less likely to occur while the mother or the father is using this medicine. Both men and women should still use birth control to prevent pregnancy because the medicine can harm an unborn baby.

Ask a doctor if it is safe to breastfeed while using this medicine.

How should I take tacrolimus?

Follow all directions on your prescription label and read all medication guides or instruction sheets. Your doctor may occasionally change your dose. Use the medicine exactly as directed.

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.

Take oral tacrolimus at the same time each day, with a full glass of water.

Swallow the tablet or capsule whole and do not crush, chew, break, or open it.

Mix tacrolimus oral granules with water right before you take them. Do not save this mixture for later use. Do not get the powder or mixture on your skin or in your eyes. If this happens, wash your skin with soap and water or rinse your eyes with water.

Take Astragraf XL or Envarsus XR in the morning on an empty stomach, at least 1 hour before or 2 hours after a meal.

You may take Prograf with or without food, but take it the same way each time.

Your dose needs may change if you switch to a different brand, strength, or form of tacrolimus. All forms of tacrolimus are not equivalent and may not have the same dose or schedule. Avoid medication errors by using only the form and strength your doctor prescribes.

You will need frequent medical tests, and 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?

For Prograf: Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose.

For Astragraf XL: Take the medicine as soon as you can, but skip the missed dose if you are more than 14 hours late for the dose.

For Envarsus XR: Take the medicine as soon as you can, but skip the missed dose if you are more than 15 hours late for the dose.

Do not take two doses at one time.

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 receiving a "live" vaccine. The vaccine may not work as well while you are using tacrolimus. Live vaccines include measles, mumps, rubella (MMR), rotavirus, typhoid, yellow fever, varicella (chickenpox), and zoster (shingles).

Grapefruit may interact with tacrolimus and cause side effects. Avoid consuming grapefruit products.

What other drugs will affect tacrolimus?

Sometimes it is not safe to use certain medications at the same time. Some drugs can affect your blood levels of other drugs you take, which may increase side effects or make the medications less effective.

Tacrolimus can harm your kidneys, especially if you also use certain medicines for infections, cancer, osteoporosis, organ transplant rejection, bowel disorders, high blood pressure, or pain or arthritis (including Advil, Motrin, and Aleve).

Tell your doctor about all your current medicines. Many drugs can affect tacrolimus, especially:

This list is not complete and many other drugs may affect tacrolimus. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible drug interactions are listed here.

Further information

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.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.