What is tacrolimus? What are the uses for tacrolimus?

  • Tacrolimus, previously known as FK506, is a macrolide immunosuppressant produced by the bacteria Streptomyces tsukubaensis.
  • Tacrolimus is used for the prevention of rejection of transplanted kidneys, liver, or heart.
  • It can be combined with steroids, azathioprine (Imuran Azasan) or mycophenolate mofetil (CellCept).

What brand names are available for tacrolimus?

Prograf, Astagraf XL, Envarsus XR

Is tacrolimus available as a generic drug?

Yes

Do I need a prescription for tacrolimus?

Yes

What are the side effects of tacrolimus?

Tacrolimus is associated with many and various side effects. These include:

Other side effects include

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What is the dosage for tacrolimus?

  • Oral tacrolimus is taken twice daily.
  • Starting doses range between 0.075 mg/kg/day to 0.2 mg/kg/day (immediate release capsules).
  • Doses vary widely and are based on tests that measure the amount of tacrolimus in the blood.
  • Taking tacrolimus with food can reduce some of the abdominal pain that can occur with this medicine; however, food can reduce the amount of tacrolimus that is absorbed. This is especially true with fatty foods.
  • Capsules should be taken consistently with or without food in order to avoid major swings in blood levels.
  • Grapefruit juice increases blood levels of tacrolimus and should be avoided.
  • The injection is only used for patients who cannot tolerate tacrolimus capsules.

What drugs interact with tacrolimus?

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 may interact with tacrolimus and lead to unwanted side effects. Avoid the use of grapefruit products.
  • Avoid drinking alcohol. It may increase your risk of side effects.
  • Avoid being near people who are sick or have infections. Tell your doctor at once if you develop signs of infection.
  • Tacrolimus could make you sunburn more easily. Avoid sunlight or tanning beds. Wear protective clothing and use sunscreen (SPF 30 or higher) when you are outdoors.
  • Tacrolimus can harm your kidneys, especially if you also use certain medicines for infections, cancer, osteoporosis, bowel disorders, or pain or arthritis (including aspirin, Tylenol, Advil, 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.

Is tacrolimus safe to take if I'm pregnant or breastfeeding?

  • Tacrolimus crosses the placenta, but there have been no adequate studies in pregnant women to assess the effects on the fetus. Among women who have received tacrolimus while pregnant, high potassium levels and kidney injury in newborns have been reported. Therefore, tacrolimus should be used during pregnancy only when it is clearly needed.
  • Tacrolimus passes into breast milk. It is recommended that breastfeeding be discontinued while women are receiving oral tacrolimus.

What else should I know about tacrolimus?

What preparations of tacrolimus are available?

  • Capsule: 0.5, 1, and 5 mg
  • Tablets: 0.75, 1, 4 mg
  • Injection: 5 mg/ml

How should I keep tacrolimus stored?

Tacrolimus should be stored at room temperature between 15 C and 30 C (59 F and 86 F).

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Summary

Tacrolimus (Prograf, Astagraf XL, Envarsus XR) is a medication prescribed for the prevention of rejection of transplanted liver, heart, or kidneys. Side effects may include nausea, vomiting, itching, fever, tremor, headache, baldness, anemia, rash, and abdominal pain. Drug interactions, dosing, and pregnancy and breastfeeding safety information should be reviewed prior to taking this medication. The brand Hecoria has been discontinued in the US.

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See more info: tacrolimus on RxList
Medically Reviewed on 7/10/2019
References
FDA Prescribing Information
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