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Overview: Tacrolimus is used to help keep your body from rejecting a transplanted organ. The medicine works by reducing your immune system’s activity. Common side effects include tremor and high blood pressure. Try to use this medicine at the same time each day, and do not miss or skip doses. Do not start or stop any other medicines including any over-the-counter (OTC) medicines without talking with your healthcare provider.

Uses

What is tacrolimus used for?

Tacrolimus is commonly used to prevent organ rejection after certain organ transplants.

Tacrolimus may also be used for other conditions as determined by your healthcare provider.

How does tacrolimus work (mechanism of action)?

Tacrolimus works by inhibiting certain types of cells called T-cells that are a part of your immune system. As a result, your immune system is less active. Thus, you are less likely to reject an organ like a kidney that you have received.

How is tacrolimus supplied (dosage forms)?

Brand and other names

  • Astagraf XL
  • Envarsus XR
  • Prograf

Dosage forms and strengths

  • 0.5 mg, 1 mg, 5 mg oral capsules
  • 0.5 mg, 1 mg, 5 mg extended-release oral capsules
  • 0.75 mg, 1 mg, 4 mg extended-release oral tablets
  • 0.2 mg/packet and 1 mg/packet granules for oral suspension

See also: Tacrolimus topical 

Tacrolimus is also available in injectable forms.

How should I store tacrolimus?

Oral Products. Tacrolimus capsules, extended-release capsules and tablets, and granules to make an oral liquid should be stored at room temperature, between 68 F to 77 F (20 C to 25 C). It can be exposed to temperatures between 59 F to 86 F (15 C to 30 C) for shorter periods of time, such as when transporting it. Store in a cool, dry place.

Injectable. Tacrolimus injection is usually given by a healthcare provider in a hospital or clinic. You will not store it at home.

Side Effects

What are the most common side effects of tacrolimus?

The most common side effects of tacrolimus are listed below. Tell your healthcare provider if you have any of these side effects that bother you.

  • Infections (see below)
  • Uncontrollable shakiness that most commonly happens in the hands, arms, or legs
  • Fluid build up in hands, arms, feet, or ankles
  • Nerve problems (see below)
  • Constipation, diarrhea, nausea, and stomach pain
  • High blood pressure (see below)
  • Kidney problems (see below)
  • Headache 
  • Low electrolyte levels, such as magnesium or phosphate
  • High potassium level (see below)
  • High cholesterol levels
  • High blood sugar (see below)
  • Anemia
  • Trouble sleeping

There may be other side effects of tacrolimus that are not listed here. Contact your healthcare provider if you think you are having a side effect of a medicine. In the U.S., you can report side effects to the FDA at www.fda.gov/medwatch or by calling 800-FDA-1088. In Canada, you can report side effects to Health Canada at www.health.gc.ca/medeffect or by calling 866-234-2345.

What are the serious side effects of tacrolimus?

While less common, the most serious side effects of tacrolimus are described below, along with what to do if they happen.

Severe Allergic Reactions. Tacrolimus may cause allergic reactions, which can be serious. Stop using tacrolimus and get help right away if you have any of the following symptoms of a serious allergic reaction.

  • Breathing problems or wheezing
  • Racing heart
  • Fever or general ill feeling
  • Swollen lymph nodes
  • Swelling of the face, lips, mouth, tongue, or throat
  • Trouble swallowing or throat tightness
  • Itching, skin rash, or pale red bumps on the skin called hives
  • Nausea or vomiting
  • Dizziness, feeling lightheaded, or fainting
  • Stomach cramps
  • Joint pain

Kidney Problems. An acute kidney injury can happen when using tacrolimus. Keep all appointments to have your blood checked. Call your healthcare provider right away if you have any of the following symptoms. 

  • Reduced need to pee
  • Swelling in your feet, ankles, or legs
  • Weakness or unusual tiredness
  • Difficulty catching your breath or chest pain/pressure
  • Confusion
  • Nausea
  • Seizures

High Potassium Level (Hyperkalemia).Tacrolimus can cause a high potassium level, which can be serious and may lead to death. Your healthcare provider may check your potassium levels while you are using tacrolimus, especially if you take certain other medicines. Call your healthcare provider right away if you have any of the following symptoms of a high potassium level. 

  • Muscle cramping or weakness 
  • Slow heartbeat or feeling of skipped heartbeats
  • Trouble breathing
  • Nausea, vomiting, or diarrhea
  • Abnormal heart rhythm 

High Blood Pressure (Hypertension). Tacrolimus may increase your blood pressure or make it worse if you have a history of high blood pressure. Call your healthcare provider if your blood pressure increases while using this medicine.

Blood Clotting Problems. Tacrolimus can lead to a serious problem with blood clotting. Tell your healthcare provider right away if you have any of the following symptoms.

  • Fever
  • Shortness of breath
  • Pale or yellowish skin
  • Your skin or the whites of your eyes turning yellowish in color (also called jaundice)
  • Changes in your vision
  • Unusual weakness or tiredness
  • Headache, confusion, or slurred speech
  • Fast heartbeat
  • Purplish spots or red dots on the skin or in the mouth due to bleeding under the skin
  • Low amount of pee or pee that is pink or has blood in it

Infections. Tacrolimus can increase your risk of infections, including serious infections that can lead to death. Call your healthcare provider right away if you have an infection or any of the following symptoms.

  • Fever, sweats, chills, or muscle aches
  • Feeling more tired than usual
  • Sore throat
  • Cough or coughing up blood
  • Burning or stinging when you pee
  • Shortness of breath
  • Diarrhea or stomach pain
  • Weight loss
  • Area on your skin that is warm, red, or painful

Progressive Multifocal Leukoencephalopathy (PML). People using tacrolimus may develop a rare brain disease called PML. It is caused by a virus called the JC virus. PML is very serious and can lead to death. Stop using tacrolimus and call your healthcare provider right away if you have any of the following symptoms of PML.

  • Clumsiness or loss of coordination
  • Difficulty walking or speaking
  • Facial drooping
  • Vision problems
  • Thinking, memory, or personality changes
  • Weakness on one side of your body that gets worse
  • Seizures

Cancer. Tacrolimus can cause a new cancer to develop, including blood or skin cancer, or cause a previously treated cancer to recur. Try to limit the time you spend in the sun and make sure you are protecting yourself by wearing protective clothing and/or sunscreen. Tell your healthcare provider about any new symptoms that you may get.

Nerve Problems. Nerves are the fibers that carry sensations from your body to your brain. Tacrolimus may cause problems with these nerves, which can be serious. For example, tacrolimus may cause a rare but serious brain condition called posterior reversible encephalopathy syndrome (PRES). PRES involves swelling and narrowing of blood vessels in your brain. If PRES is not treated, it can lead to a stroke. Call your healthcare provider right away if you have any of the following symptoms of nerve problems.

  • Headache 
  • Vision changes 
  • Difficulty moving or controlling parts of your body 
  • Uncontrollable shakiness that most commonly happens in the hands, arms, or legs
  • Change in mental status such as confusion or trouble thinking clearly
  • Seizures 
  • Muscle weakness
  • Numbness or tingling
  • Dizziness

High Blood Sugar. Tacrolimus can cause high blood sugar levels (hyperglycemia) or diabetes. Keep all appointments with your healthcare provider to check your blood work. Call your healthcare provider if you develop any of the following symptoms of high blood sugar.

  • Thirsty more than usual
  • Peeing more than usual
  • Increase or decrease in hunger
  • Tiredness
  • Feeling sick to your stomach
  • Confusion
  • Your breath smelling fruity
  • Nausea, vomiting, or stomach pain

Heart Rhythm Changes. Tacrolimus may cause a rare, dangerous heart rhythm problem called QT prolongation and torsade de pointes. Some people have a higher risk of this, including people who are older, have other people in their family who have had these conditions, have low potassium or magnesium levels, or who take other medicines that can prolong the QT interval. Tell your healthcare provider right away if you faint or have changes in your heart rate or rhythm, such as a fast or skipping heartbeat.

Enlarged Heart Muscle (Myocardial Hypertrophy). Tacrolimus may cause your heart muscle to grow larger than normal. There is a greater chance of this happening when the amount of tacrolimus in your body is high. Call your healthcare provider if you have any of the following symptoms.

  • Shortness of breath
  • Chest pain or discomfort
  • Abnormal heart rhythm 
  • Tiredness
  • Feeling lightheaded, dizziness, or fainting

Low Red Blood Cell Levels (Pure Red Cell Aplasia). Tacrolimus may cause a condition called pure red cell aplasia, which is when your body is not making enough red blood cells. Keep all your appointments to have your blood checked. Tell your healthcare provider right away if you have any of the following symptoms.

  • Unusual weakness or tiredness
  • Cold hands and feet
  • Fast or abnormal heartbeat
  • Pale or yellowish skin
  • Dizziness, lightheadedness, or feeling like you are about to pass out
  • Shortness of breath

Warnings & Precautions

Who should not use tacrolimus?

Allergies to Ingredients. People who are allergic to any of the following should not use tacrolimus.

  • Tacrolimus
  • Prograf
  • Envarsus XR
  • Astagraf XL
  • Any of the ingredients in the specific product dispensed

Your pharmacist can tell you all of the ingredients in the specific tacrolimus products they stock.

What should I know about tacrolimus before using it?

Do not use tacrolimus unless it has been prescribed to you by a healthcare provider. Use it as prescribed. Try to use tacrolimus around the same time each day. This will help to keep your blood levels consistent.

Do not stop using tacrolimus unless told to do so by your healthcare provider. Stopping tacrolimus may lead to organ rejection.

Do not share tacrolimus with other people, even if they have the same condition as you. It may harm them.

Do not chew, open, divide, dissolve or crush tacrolimus capsules, extended-release capsules, or extended-release tablets. They should be swallowed whole.

Follow the “Instructions for Use” for how to mix and take the oral liquid if you are using the tacrolimus granules.

Tacrolimus products are not always interchangeable. Always check the medicine and the label on your tacrolimus before using any to make sure you are using the correct one. Call your healthcare provider if your tacrolimus looks different than usual or if the directions change, and you do not understand why.

Keep all appointments, including lab appointments before and after starting tacrolimus.

Keep tacrolimus out of the reach of children.

If you are able to get pregnant or get your partner pregnant, use effective birth control before and while using tacrolimus.  

Tacrolimus may make it difficult for you to get pregnant or get your partner pregnant in the future. Talk to your healthcare provider if you have concerns.

What should I tell my healthcare provider before using tacrolimus?

Tell your healthcare provider about all of your health conditions and any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are taking. This will help them determine if tacrolimus is right for you.

In particular, make sure that you discuss any of the following.

Vaccines. Talk with your healthcare provider about any vaccines that you may need. You should not receive certain vaccines right before or while using tacrolimus. Tell your healthcare provider about any vaccines you have recently received or have scheduled.

Current and Past Health Conditions. Tell your healthcare provider if you have any of the following.

  • Kidney or liver problems
  • Heart problems, including heart failure 
  • Infections 
  • High blood pressure
  • High blood sugar
  • Cancer
  • Cystic fibrosis
  • Electrolyte imbalance, including potassium, calcium, and magnesium

Other Medicines and Supplements. Tacrolimus may interact with other medicines and supplements. Before using tacrolimus, tell your healthcare provider about any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are using. See the Interactions section for more details.

Pregnancy. Tacrolimus may cause harm to an unborn baby. You should use effective birth control before and while using tacrolimus if you can become pregnant or if you can get your partner pregnant. Tell your healthcare provider if you or your partner are pregnant or plan to become pregnant. If you or your partner become pregnant while using tacrolimus, you can register for the Transplant Pregnancy Registry International by calling 877-955-6877 or at www.transplantpregnancyregistry.org. This registry collects safety information about the use of tacrolimus during pregnancy. 

Breastfeeding. Tacrolimus passes into breast milk. Tell your healthcare provider if you are breastfeeding or plan to breastfeed. Your healthcare provider will advise you if you should use tacrolimus while breastfeeding.

Interactions

Does tacrolimus interact with foods or drinks?

Grapefruit or grapefruit juice can cause the amount of tacrolimus in your body to go up. Do not eat grapefruit or drink grapefruit juice while using tacrolimus.

Tacrolimus extended-release tablets and extended-release capsules should be taken on an empty stomach, at least one hour before or two hours after eating a meal. Do not drink alcohol. Alcohol may change how quickly the medicine is released into your body. 

Food may affect how tacrolimus capsules or granules are absorbed by your body. Make sure you are consistent about taking the capsules or granules always either with or without food. It is best to limit the amount of alcohol you drink with tacrolimus capsules or granules. The risk of confusion or headache may be increased if you drink alcohol while taking tacrolimus capsules or granules.

Does tacrolimus interact with other medicines (drug interactions)?

Tacrolimus interacts with many other medicines. Always tell your healthcare provider about any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are taking.

In particular, make sure that you discuss if you are taking any of the following before using tacrolimus.

  • A non-steroidal anti-inflammatory drug (NSAID), such as ibuprofen (Motrin, Advil), naproxen (Aleve), diclofenac, sulindac and others, which are contained in many prescription and OTC products for pain, swelling, and fever
  • An angiotensin-converting enzyme (ACE) inhibitor, such as enalapril or lisinopril, which is a medicine for high blood pressure, heart failure, and certain kidney problems
  • Certain antibiotics, such as an aminoglycoside, clarithromycin, or erythromycin, which is a medicine used to treat bacterial infections
  • A calcium channel blocker, such as diltiazem (Cardizem CD and others), verapamil (Verelan, Verelan PM), nifedipine (Procardia), or nicardipine, which is a medicine used for high blood pressure or other conditions
  • Amiodarone (Pacerone and others), which is a medicine used for an irregular heart rhythm 
  • A medicine for HIV or AIDS
  • A medicine for high blood pressure
  • Ketoconazole, itraconazole (Sporanox, Tolsura), posaconazole (Noxafil), voriconazole (Vfend), fluconazole, caspofungin, or amphotericin B (Abelcet, AmBisome), which is a medicine used for fungal infections
  • A barbiturate, such as phenobarbital, or primidone, which is a medicine that may be used to treat seizures
  • Carbamazepine (Tegretol, Carbatrol, and others) or oxcarbazepine (Trileptal), which is a medicine commonly used to treat seizures or nerve pain
  • St. John’s wort, which is a supplement that may be used to treat depression
  • Rifampin (Rifadin), which is a medicine commonly used to treat an infection called tuberculosis
  • Rifabutin (Mycobutin), which is a medicine used to prevent Mycobacterium avium complex infection
  • A diuretic, also called a water pill, which is a medicine used to reduce edema (fluid retention) and blood pressure
  • A corticosteroid, such as dexamethasone, methylprednisolone, or prednisone, which is a medicine for certain inflammatory conditions, asthma, or COPD
  • Cyclosporine, sirolimus, mycophenolic acid, or everolimus, which is a medicine that suppresses your immune system
  • Medicines that can cause QT prolongation, which is a potentially dangerous heart rhythm problem
  • Cimetidine, omeprazole, lansoprazole, or an antacid containing magnesium or aluminum
  • Ethinyl estradiol, which is in many birth control pills
  • Cannabidiol (Epidiolex), which is a medicine for certain types of seizures

Many other medicines may alter the blood levels of tacrolimus. Tell your healthcare provider about all medicines that you take or have recently taken.

This may not be a complete list of medicines that can interact with tacrolimus. Always check with your healthcare provider.

Does interact with other drugs you are taking?

Enter your medication into the WebMD interaction checker

Overdose/Missed Dose

What should I do if I accidentally use too much tacrolimus?

If you or someone else has used too much tacrolimus, get medical help right away, call 911, or contact a Poison Control center at 800-222-1222.

What should I do if I miss a dose of tacrolimus?

Missing doses of tacrolimus can cause it to not work as well over time. So, it is important not to miss or skip doses.

Oral Capsules or Granules. If you miss a dose, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose and only take the next dose. Do not take double or extra doses.

Extended-Release Capsules. If you miss a tacrolimus extended-release capsule dose, take it as soon as you remember but only if 14 hours or less have passed since you were supposed to take it. If more than 14 hours have passed, skip the missed dose and take your next dose at the regular time. Do not take double or extra doses.

Extended-Release Tablets. If you miss a tacrolimus extended-release tablet dose, take it as soon as you remember but only if 15 hours or less have passed since you were supposed to take it. If more than 15 hours have passed, skip the missed dose and take your next dose at the regular time. Do not take double or extra doses.

Injection. Tacrolimus injection is usually given by a healthcare provider in a hospital. Your healthcare provider will make sure you are receiving tacrolimus as scheduled. If you miss an appointment to get your tacrolimus injection dose, call to make another appointment as soon as possible.