tacrolimus (Prograf, Astagraf XL, Envarsus XR)

• 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

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

• baldness,
• anemia,
• loss of appetite,
• diarrhea,
• high concentrations of potassium in the blood,
• high blood pressure,
• nausea,
• vomiting,
• tingling sensation in the extremities,
• itching,
• tremor,
• fever,
• headache,
• rash,
• high blood sugar concentrations, and
• abdominal pain.

Other side effects include

• confusion,
• painful joints,
• increased sensitivity to light,
• blurred vision,
• insomnia,
• infection,
• jaundice (yellowing of the skin due to effects on the liver),
• kidney injury,
• swollen ankles, and
• seizures.

• 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.

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:

• amiodarone;
• cyclosporine;
• sirolimus;
• antibiotic, antifungal, or antiviral medicines; or
• blood pressure medication, such as a diuretic or "water pill."

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.

• 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 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).