Description
Tacrolimus is used together with other medicines to prevent the body from rejecting a transplanted organ (eg, kidney, liver, heart, or lung). This medicine may be used with steroids, azathioprine, basiliximab, or mycophenolate mofetil. Tacrolimus belongs to a group of medicines known as immunosuppressive agents.
When a patient receives an organ transplant, the body's white blood cells will try to get rid of (reject) the transplanted organ. Tacrolimus works by suppressing the immune system to prevent the white blood cells from trying to get rid of the transplanted organ.
Tacrolimus is a very strong medicine. It can cause side effects that can be very serious, such as kidney problems. It may also decrease the body's ability to fight infections. You and your doctor should talk about the benefits of this medicine as well as the risks of using it.
This medicine is available only with your doctor's prescription.
This product is available in the following dosage forms:
- Tablet, Extended Release
- Capsule
- Capsule, Extended Release
- Granule
Before Using
In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:
Allergies
Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.
Pediatric
Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of Astagraf XL® in children 4 years of age and older. Safety and efficacy have been established.
Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of Prograf® in children with liver, kidney, heart, or lung transplants. Safety and efficacy have been established.
Appropriate studies have not been performed on the relationship of age to the effects of Envarsus XR® in the pediatric population. Safety and efficacy have not been established.
Geriatric
Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of tacrolimus in the elderly. However, elderly patients are more likely to have kidney, liver, or heart problems, which may require caution and an adjustment in the dose for patients receiving tacrolimus.
Breastfeeding
There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.
Drug Interactions
Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.
Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.
- Bepridil
- Cisapride
- Dronedarone
- Fluconazole
- Lefamulin
- Mesoridazine
- Mifepristone
- Nelfinavir
- Pimozide
- Piperaquine
- Posaconazole
- Ritonavir
- Saquinavir
- Sparfloxacin
- Terfenadine
- Thioridazine
- Ziprasidone
Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
- Abacavir
- Abametapir
- Abrocitinib
- Aceclofenac
- Acemetacin
- Adagrasib
- Adenovirus Vaccine Type 4, Live
- Adenovirus Vaccine Type 7, Live
- Alefacept
- Alfuzosin
- Amikacin
- Amiloride
- Amiodarone
- Amisulpride
- Amitriptyline
- Amlodipine
- Amphotericin B
- Amprenavir
- Amtolmetin Guacil
- Anagrelide
- Apalutamide
- Apixaban
- Apomorphine
- Aprepitant
- Aranidipine
- Aripiprazole
- Aripiprazole Lauroxil
- Armodafinil
- Arsenic Trioxide
- Asciminib
- Asenapine
- Aspirin
- Astemizole
- Atazanavir
- Avacopan
- Azilsartan
- Azilsartan Medoxomil
- Azithromycin
- Bacillus of Calmette and Guerin Vaccine, Live
- Bedaquiline
Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
- Aluminum Carbonate, Basic
- Aluminum Hydroxide
- Aluminum Phosphate
- Dihydroxyaluminum Aminoacetate
- Dihydroxyaluminum Sodium Carbonate
- Ertapenem
- Magaldrate
- Magnesium Carbonate
- Magnesium Hydroxide
- Magnesium Oxide
- Magnesium Peroxide
- Magnesium Trisilicate
- Tigecycline
Other Interactions
Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.
Using this medicine with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.
- Ethanol
- Grapefruit Juice
Other Medical Problems
The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:
- Congestive heart failure or
- Diabetes or
- Heart disease or
- Heart rhythm problems (eg, QT prolongation), or history of or
- Hyperkalemia (high potassium in the blood) or
- Hypertension (high blood pressure) or
- Myocardial hypertrophy (heart is larger than normal), history of or
- Paresthesia (numbness or tingling in the hands, arms, legs, or feet), history of or
- Seizures (convulsions), history of or
- Tremors—Use with caution. May make these conditions worse.
- Cystic fibrosis—May require a higher dose for patients with this condition.
- Infection, active (eg, bacteria, fungus, or virus)—May decrease your body's ability to fight an infection.
- Kidney disease or
- Liver disease—Use with caution. The effects may be increased because of slower removal of the medicine from the body.
Proper Use
Take this medicine exactly as directed by your doctor. Do not take more or less of it and do not take it more often than your doctor ordered. Using too much will increase the chance for side effects, while using too little may cause rejection of your transplanted organ.
This medicine comes with a Medication Guide or a patient information insert and patient instructions. Read and follow the instructions carefully. Ask your doctor if you have questions.
This medicine is always used together with other medicines. Make sure you understand when to take all of your medicines during the day. Your doctor will give you a daily plan for taking your medicines.
You may take the immediate-release capsule or oral liquid with or without food. But take it the same way each time.
If you are using the extended-release capsule:
- Swallow the capsule whole with liquid. Do not crush, break, chew, or divide it.
- Take the capsule every morning, preferably on an empty stomach, at least 1 hour before or at least 2 hours after a meal.
- Do not drink alcohol with the capsule.
If you are using the extended-release tablet:
- Take it on an empty stomach in the morning, at least 1 hour before or 2 hours after a meal, at the same time every day.
- Swallow the tablet whole with liquid (preferably water). Do not crush, chew, divide, or dissolve it.
- Do not drink alcohol with the tablet.
If you are using the granule for oral suspension, you may take it with or without food, but you should take it the same way each time. To prepare the oral liquid:
- Empty the contents of the packet in a glass cup filled with 1 to 2 tablespoons (15 to 30 milliliters) of room temperature water and mix. Use a metal spoon to stir the mixture. Do not use plastic.
- Drink it right away after preparing.
- Refill the glass cup with the same amount of water and gently swirl to mix any remaining granules to get the full dose of this medicine.
- You may also use an oral syringe to give this medicine.
- Do not inhale the granules or let the oral liquid come in contact with your skin or eyes. If you get the granules or the oral liquid on your skin, wash the area well with soap and water. If you get them into your eyes, rinse with water.
- Do not save the prepared oral liquid for later use.
You should not eat grapefruit or drink grapefruit juice while you are using this medicine. Grapefruit and grapefruit juice will increase the amount of medicine in the body.
Do not stop using this medicine without first checking with your doctor. You might have to take this medicine for the rest of your life to prevent your body from rejecting the transplant.
Use only the brand of this medicine that your doctor prescribed. Different brands may not work the same way.
Do not use Prograf® together with cyclosporine. Tacrolimus or cyclosporine should be stopped at least 24 hours before starting the other.
Dosing
The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
- For oral dosage form (capsules, granules):
- To prevent heart or lung transplant rejection:
- Adults—Dose is based on body weight and must be determined by your doctor. The starting dose is usually 0.075 milligram per kilogram (mg/kg) of body weight per day, divided into 2 doses and taken every 12 hours. Your doctor may adjust the dose as needed.
- Children—0.3 mg/kg per day, divided in 2 doses, given every 12 hours. Your doctor may adjust your dose as needed.
- To prevent kidney transplant rejection:
- Adults—Dose is based on body weight and must be determined by your doctor. The starting dose is usually 0.1 to 0.2 milligram per kilogram (mg/kg) of body weight per day, divided into 2 doses and taken every 12 hours. Your doctor may adjust the dose as needed.
- Children—0.3 mg/kg per day, divided in 2 doses, given every 12 hours.
- To prevent liver transplant rejection:
- Adults—Dose is based on body weight and must be determined by your doctor. The starting dose is usually 0.1 to 0.15 milligram per kilogram (mg/kg) of body weight per day, divided into 2 doses and taken every 12 hours. Your doctor may adjust the dose as needed.
- Children—Dose is based on body weight and must be determined by your doctor. The starting dose is usually 0.15 to 0.2 mg/kg of body weight per day, divided into 2 doses and taken every 12 hours.
- To prevent heart or lung transplant rejection:
- For oral dosage form (extended-release capsules):
- To prevent kidney transplant rejection:
- Adults
- With basiliximab, mycophenolate mofetil, and steroids—Dose is based on body weight and must be determined by your doctor. The dose is usually between 0.15 to 0.2 milligram per kilogram (mg/kg) of body weight once a day before reperfusion (return of blood flow to the blocked organ) or within 48 hours after transplant.
- With mycophenolate mofetil and steroids—Dose is based on body weight and must be determined by your doctor. The dose is 0.1 milligram per kilogram (mg/kg) of body weight within 12 hours before reperfusion, then 0.2 mg/kg once a day at least 4 hours after pre-operation dose and within 12 hours after reperfusion.
- Children 4 years of age and older—0.3 mg/kg of body weight given once a day within 24 hours after reperfusion. Your doctor may adjust the dose as needed.
- Children younger than 4 years of age—Use and dose must be determined by your doctor.
- Adults
- To prevent kidney transplant rejection:
- For oral dosage form (extended-release tablets):
- To prevent kidney transplant rejection:
- Adults—Dose is based on body weight and must be determined by your doctor. At first, 0.14 milligram (mg) per kilogram (kg) per day. Your doctor may adjust your dose as needed and tolerated.
- Children—Use and dose must be determined by your doctor.
- To prevent kidney transplant rejection:
Missed Dose
If you miss a dose of Astagraf XL® and it is less than 14 hours since the regular time, take the missed dose right away. If more than 14 hours have passed since the regular time, skip the missed dose and return to your regular schedule.
If you miss a dose of Envarsus XR® and it is less than 15 hours since the regular time, take the missed dose right away. If more than 15 hours have passed since the regular time, skip the missed dose and return to your regular schedule.
Storage
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Ask your healthcare professional how you should dispose of any medicine you do not use.
Precautions
It is very important that your doctor check your or your child's progress at regular visits to make sure that this medicine is working properly. Blood and urine tests may be needed to check for unwanted effects.
Using this medicine while you are pregnant can harm your unborn baby. It may also cause birth defects if the father is using it when his sexual partner becomes pregnant. If you think you have become pregnant while using this medicine, tell your doctor right away.
Do not use Prograf® together with sirolimus (Rapamune®).
This medicine may increase your risk of getting skin cancer or cancer of the lymph system (lymphoma). Talk to your doctor if you have concerns about this risk.
This medicine may increase your risk of developing infections. Avoid being near people who are sick while you are using this medicine. Wash your hands often. Tell your doctor if you have any kind of infection before you start using this medicine. Tell your doctor if you have ever had an infection that would not go away or an infection that kept coming back.
While you are being treated with tacrolimus, and after you stop treatment with it, do not have any immunizations (vaccines) without your doctor's approval. Tacrolimus may lower your body's resistance and the vaccine may not work as well or you might get the infection the vaccine is meant to prevent. In addition, you should not be around other persons living in your household who receive live virus vaccines because there is a chance they could pass the virus on to you. Some examples of live vaccines include measles, mumps, influenza (nasal flu vaccine), poliovirus (oral form), rotavirus, and rubella. Do not get close to them and do not stay in the same room with them for very long. If you have questions about this, talk to your doctor.
This medicine may increase your risk for developing a rare and serious virus infection with the BK polyoma virus. This virus may affect how your kidneys work and cause a transplanted kidney to fail. Check with your doctor right away if you have bloody urine, decreased frequency or amount of urine, increased thirst, loss of appetite, lower back or side pain, nausea, swelling of the face, fingers, or lower legs, trouble breathing, unusual tiredness or weakness, vomiting, or weight gain.
This medicine may cause kidney problems. Check with your doctor right away if you have blood in your urine, change in frequency of urination or amount of urine, drowsiness, increased thirst, loss of appetite, nausea or vomiting, swelling of your feet or lower legs, trouble breathing, or weakness.
This medicine may increase your risk of developing a serious and rare brain infection called progressive multifocal leukoencephalopathy (PML). Check with your doctor right away if you have vision changes, loss of coordination, clumsiness, confusion, memory loss, difficulty speaking or understanding what others say, or weakness in the legs.
This medicine may cause serious brain or nerve problems (eg, posterior reversible encephalopathy syndrome). Tell your doctor right away if you have blurred vision, confusion, dizziness, headache, mental changes, seizures, high blood pressure, unusual drowsiness, tiredness, or weakness, or a fast heartbeat.
Hyperkalemia (high potassium in the blood) may occur while you are using this medicine. Check with your doctor right away if you have confusion, difficulty with breathing, an irregular heartbeat, nausea or vomiting, nervousness, numbness or tingling in the hands, feet, or lips, stomach pain, or weakness or heaviness of the legs.
Tacrolimus may cause a condition called pure red cell aplasia (PRCA). This is a very rare condition where the body no longer makes red blood cells and the patient has severe anemia. Check with your doctor right away if you have a fever and sore throat, pale skin, unusual bleeding or bruising, or unusual tiredness or weakness.
Tell your doctor if you have African or Hispanic relatives. You may be at an increased risk for diabetes after transplant. If you are African-American, you might need a higher dose of this medicine. Talk to your doctor if you have concerns.
Use sunscreen or sunblock lotion with a sun protection factor (SPF) of at least 15 on a regular basis when you are outdoors. Wear protective clothing and hats, and stay out of direct sunlight between the hours of 10 am and 3 pm. Avoid sunlamps and tanning beds.
If you plan to have children, talk with your doctor before using this medicine. Some men and women using this medicine have become infertile (unable to have children).
This medicine may cause thrombotic microangiopathy (damage in the smallest blood vessels), hemolytic uremic syndrome, and thrombotic thrombocytopenic purpura. Tell your doctor right away if you have a change in mental status, dark or bloody urine, decreased urine output, difficulty speaking, fever, pale color of the skin, pinpoint red spots on the skin, seizures, severe chest pain, sudden weakness in the arms or legs, unusual bleeding or bruising, or yellow eyes or skin.
Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal (eg, cannabidiol, St. John's wort) or vitamin supplements.
Side Effects
Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.
Check with your doctor immediately if any of the following side effects occur:
More common
- Abnormal dreams
- agitation
- chills
- blurred vision
- confusion
- cough
- diarrhea
- dizziness
- dry mouth
- fever
- flushed, dry skin
- frequent urination
- fruit-like breath odor
- general feeling of discomfort or illness
- headache
- increased hunger
- increased thirst
- increased urination
- itching, skin rash
- joint pain
- loss of appetite
- loss of consciousness
- loss of energy or weakness
- mental depression
- muscle pains, trembling, or twitching
- nausea
- pale skin
- runny nose
- seeing or hearing things that are not there
- seizures
- shivering
- sore throat
- stomach pain
- sweating
- swelling of the feet or lower legs
- tingling
- trembling and shaking of the hands
- trouble breathing
- trouble sleeping
- unexplained weight loss
- unusual bleeding or bruising
- unusual tiredness or weakness
- vomiting
Less common
- Chest pain
- increased sensitivity to pain
- muscle cramps
- numbness or pain in the legs
- ringing in the ears
Rare
- Enlarged heart
- flushing of the face or neck
- weight loss
Incidence not known
- Black, tarry stools
- blistering, peeling, or loosening of the skin
- bloating
- bloody nose
- bloody urine
- change in mental status
- constipation
- drowsiness
- fainting
- fast, slow, or irregular heartbeat
- heartburn
- heavier menstrual periods
- indigestion
- joint pain
- lightheadedness
- lower back or side pain
- pain and fullness in the right upper stomach
- pinpoint red spots on the skin
- pounding or rapid pulse
- red skin lesions, often with a purple center
- red, irritated eyes
- skin sores
- ulcers or white spots in the mouth or on the lips
- weakness
- weight gain
- yellow eyes or skin
Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:
More common
- Belching
- difficulty with moving
- lack or loss of strength
- muscle stiffness
Less common
- Body aches or pain
- burning or stinging of the skin
- cracks in the skin
- crying
- dysphoria
- excessive muscle tone
- false beliefs that cannot be changed by facts
- false or unusual sense of well-being
- feeling of constant movement of self or surroundings
- feeling of unreality
- feeling that others are watching you or controlling your behavior
- feeling that others can hear your thoughts
- increased sensitivity of the skin to sunlight
- large, flat, blue or purplish patches in the skin
- muscle tension or tightness
- painful blisters on the trunk of the body
- painful cold sores or blisters on the lips, nose, eyes, or genitals
- paranoia
- poor insight and judgment
- problems with memory or speech
- quick to react or overreact emotionally
- rapidly changing moods
- redness or other discoloration of the skin
- restlessness
- scaly skin
- sensation of spinning
- sense of detachment from self or body
- severe mood or mental changes
- severe sunburn
- sleepiness or unusual drowsiness
- sore mouth or tongue
- sores on the skin
- swelling or inflammation of the mouth
- tender, swollen glands in the neck
- trouble recognizing objects
- trouble thinking and planning
- trouble walking
- unusual behavior
- white patches in the mouth, tongue, or throat
Incidence not known
- Change in color vision
- decreased weight
- difficulty seeing at night
- feeling hot and cold
- hearing loss
Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.
Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.
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