Tacrolimus Oral, Intravenous

ta-KROE-li-mus

Intravenous routeSolution

Increased susceptibility to infection and the possible development of lymphoma may result from immunosuppression. Only physicians experienced in immunosuppressive therapy and management of organ transplant patients should prescribe tacrolimus. Patients receiving the drug should be managed in facilities equipped and staffed with adequate laboratory and supportive medical resources. The physician responsible for maintenance therapy should have complete information requisite for the follow-up of the patient .

Increased susceptibility to infection and the possible development of lymphoma may result from immunosuppression. Only physicians experienced in immunosuppressive therapy and management of organ transplant patients should prescribe, and they should have complete information requisite for the follow-up of the patient .

Oral routeCapsule

Increased susceptibility to infection and the possible development of lymphoma may result from immunosuppression. Only physicians experienced in immunosuppressive therapy and management of organ transplant patients should prescribe tacrolimus. Patients receiving the drug should be managed in facilities equipped and staffed with adequate laboratory and supportive medical resources. The physician responsible for maintenance therapy should have complete information requisite for the follow-up of the patient .

Increased susceptibility to infection and the possible development of lymphoma may result from immunosuppression. Only physicians experienced in immunosuppressive therapy and management of organ transplant patients should prescribe, and they should have complete information requisite for the follow-up of the patient .

Topical routeOintment

Long-term safety of topical calcineurin inhibitors has not been established. Although a causal relationship has not been established, rare cases of malignancy (eg, skin and lymphoma) have been reported in patients treated with topical calcineurin inhibitors, including tacrolimus ointment. Therefore: Continuous long-term use of topical calcineurin inhibitors, including tacrolimus ointment, in any age group should be avoided, and application limited to areas of involvement with atopic dermatitis. Tacrolimus ointment is not indicated for use in children less than 2 years of age. Only 0.03% tacrolimus ointment is indicated for use in children 2-15 years of age .

Long-term safety of topical calcineurin inhibitors has not been established and rare cases of malignancy (eg, skin and lymphoma) have been reported in patients treated with topical calcineurin inhibitors, including tacrolimus ointment. Avoid continuous long-term use in any age group, and apply to limited areas of involvement with atopic dermatitis. Not indicated for use in children less than 2 years of age. Only 0.03% tacrolimus ointment is indicated for use in children 2-15 years of age .

Commonly used brand name(s):

In the U.S.

  • Prograf

Available Dosage Forms:

  • Capsule
  • Solution

Therapeutic Class: Immune Suppressant

Uses For tacrolimus

Tacrolimus belongs to a group of medicines known as immunosuppressive agents. It is used to lower the body's natural immunity in patients who receive organ (for example, kidney, liver, pancreas, lung, and heart) transplants.

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 preventing the white blood cells from getting rid of the transplanted organ.

Tacrolimus may also be used for other indications, as determined by your doctor.

Tacrolimus is a very strong medicine. It can cause side effects that can be very serious, such as kidney problems. It may also reduce the body's ability to fight infections. You and your doctor should talk about the good tacrolimus will do as well as the risks of using it.

Tacrolimus is available only with your doctor's prescription.

Once a medicine has been approved for marketing for a certain use, experience may show that it is also useful for other medical problems. Although not specifically included in the product labeling, tacrolimus is used in certain patients with the following medical conditions:

  • Bone marrow transplantation
  • Uveitis, severe, refractory (an eye condition)

For patients receiving bone marrow transplantation, tacrolimus may work by preventing the cells from the transplanted bone marrow from attacking the cells of the patient. The dose of tacrolimus for patients receiving bone marrow transplantation is based on body weight. The usual dose is 0.12 to 0.3 mg per kg (0.05 to 0.14 mg per pound) of body weight a day for patients taking tacrolimus by mouth, and 0.04 to 0.1 mg per kg (0.018 to 0.045 mg per pound) of body weight a day for patients receiving tacrolimus by injection.

The dose of tacrolimus for patients with severe, refractory uveitis is based on body weight. For severe, refractory uveitis, the usual dose is 0.1 to 0.15 mg per kg (0.045 to 0.068 mg per pound) of body weight a day.

Before Using tacrolimus

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 tacrolimus, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to tacrolimus 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

tacrolimus does not cause different types of side effects or problems in children than it does in adults, although some side effects may occur more or less often than they do in adult patients.

Geriatric

There is no specific information comparing the use of tacrolimus in the elderly with the use in other age groups. Tacrolimus is not expected to cause different side effects or problems in older people than it does in younger adults. However, older patients may need lower doses of tacrolimus.

Pregnancy

Pregnancy CategoryExplanation
All TrimestersCAnimal studies have shown an adverse effect and there are no adequate studies in pregnant women OR no animal studies have been conducted and there are no adequate studies in pregnant women.

Breast Feeding

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.

Interactions with Medicines

Using tacrolimus 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.

  • Ziprasidone

Using tacrolimus 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.

  • Aceclofenac
  • Acemetacin
  • Alclofenac
  • Amikacin
  • Amiloride
  • Amiodarone
  • Apazone
  • Bacillus of Calmette and Guerin Vaccine, Live
  • Basiliximab
  • Benoxaprofen
  • Bromfenac
  • Bufexamac
  • Carbamazepine
  • Carprofen
  • Caspofungin
  • Cisplatin
  • Clometacin
  • Clonixin
  • Colchicine
  • Cyclosporine
  • Darunavir
  • Dexketoprofen
  • Dibekacin
  • Diclofenac
  • Diflunisal
  • Dipyrone
  • Droxicam
  • Efavirenz
  • Etodolac
  • Etofenamate
  • Etravirine
  • Felbinac
  • Fenbufen
  • Fenoprofen
  • Fentiazac
  • Floctafenine
  • Flufenamic Acid
  • Flurbiprofen
  • Gentamicin
  • Ibuprofen
  • Indomethacin
  • Indoprofen
  • Isoxicam
  • Itraconazole
  • Kanamycin
  • Ketoprofen
  • Ketorolac
  • Lornoxicam
  • Measles Virus Vaccine, Live
  • Meclofenamate
  • Mefenamic Acid
  • Meloxicam
  • Mumps Virus Vaccine, Live
  • Nabumetone
  • Naproxen
  • Nefazodone
  • Neomycin
  • Netilmicin
  • Niflumic Acid
  • Nimesulide
  • Oxaprozin
  • Oxyphenbutazone
  • Pazopanib
  • Phenobarbital
  • Phenylbutazone
  • Phenytoin
  • Pirazolac
  • Piroxicam
  • Pirprofen
  • Poliovirus Vaccine, Live
  • Posaconazole
  • Propyphenazone
  • Proquazone
  • Rifabutin
  • Rifampin
  • Rotavirus Vaccine, Live
  • Rubella Virus Vaccine, Live
  • Sirolimus
  • Smallpox Vaccine
  • Spironolactone
  • St John's Wort
  • Streptomycin
  • Sulindac
  • Suprofen
  • Tenidap
  • Tenoxicam
  • Tiaprofenic Acid
  • Tobramycin
  • Tolmetin
  • Triamterene
  • Typhoid Vaccine
  • Varicella Virus Vaccine
  • Voriconazole
  • Yellow Fever Vaccine
  • Zomepirac

Using tacrolimus 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
  • Amprenavir
  • Chloramphenicol
  • Clarithromycin
  • Clotrimazole
  • Dalfopristin
  • Danazol
  • Dihydroxyaluminum Aminoacetate
  • Dihydroxyaluminum Sodium Carbonate
  • Diltiazem
  • Erythromycin
  • Fluconazole
  • Fosphenytoin
  • Ketoconazole
  • Magnesium Carbonate
  • Magnesium Hydroxide
  • Magnesium Oxide
  • Magnesium Trisilicate
  • Metoclopramide
  • Metronidazole
  • Mibefradil
  • Nelfinavir
  • Nevirapine
  • Nifedipine
  • Quinupristin
  • Rifapentine
  • Ritonavir
  • Saquinavir
  • Schisandra sphenanthera
  • Telithromycin
  • Theophylline

Interactions with Food/Tobacco/Alcohol

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. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Using tacrolimus with any of the following may cause an increased risk of certain side effects but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use tacrolimus, or give you special instructions about the use of food, alcohol, or tobacco.

  • Grapefruit Juice

Other Medical Problems

The presence of other medical problems may affect the use of tacrolimus. Make sure you tell your doctor if you have any other medical problems, especially:

  • Cancer—Tacrolimus can make this condition worse.
  • Chickenpox (including recent exposure) or
  • Herpes zoster (shingles)—The risk of severe disease affecting other parts of the body may be increased.
  • Diabetes mellitus (sugar diabetes)—Tacrolimus can increase the amount of sugar in the blood.
  • Hepatitis or
  • Kidney disease or
  • Liver disease—Tacrolimus can have harmful effects on the kidney in patients with these conditions; a lower dose of tacrolimus may be needed in patients with these conditions.
  • Hyperkalemia (high amount of potassium in the blood) or
  • Nervous system problems—Tacrolimus can make these conditions worse.
  • Infection—Tacrolimus decreases the body's ability to fight infection.

Proper Use of tacrolimus

Take tacrolimus only as directed by your doctor. Do not take more or less of it and do not take it more often than your doctor ordered. The exact amount of medicine you need has been carefully worked out. Taking too much may increase the chance of side effects, while taking too little may lead to rejection of your transplanted organ.

To help you remember to take your medicine, try to get into the habit of taking it at the same time each day. This will also help tacrolimus work better by keeping a constant amount in the blood.

Absorption of tacrolimus may be changed if you change your diet. tacrolimus should be taken consistently with respect to meals. You should not change the type or amount of food you eat unless you discuss it with your health care professional.

Grapefruit and grapefruit juice may increase the effects of tacrolimus by increasing the amount of tacrolimus in the body. You should not eat grapefruit or drink grapefruit juice while you are taking tacrolimus.

Do not stop taking tacrolimus without first checking with your doctor. You may have to take medicine for the rest of your life to prevent your body from rejecting the transplant.

Dosing

The dose of tacrolimus 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 tacrolimus. 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):
    • Adults, teenagers, or children—Dose is based on body weight and will be determined by your doctor.
  • For injection dosage form:
    • Adults, teenagers, or children—Dose is based on body weight and will be determined by your doctor..

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.

Precautions While Using tacrolimus

The effects of tacrolimus may cause increased infections and delayed healing. Dental work, whenever possible, should be completed prior to beginning tacrolimus.

It is very important that your doctor check your progress at regular visits. Your doctor will want to do laboratory tests to make sure that tacrolimus is working properly and to check for unwanted effects.

Tacrolimus may increase your risk for getting skin cancer when exposed to sunlight.

  • Stay out of direct sunlight, especially between the hours of 10:00 AM and 3:00 PM if possible.
  • Wear protective clothing , including a hat. Also, wear sunglasses
  • Apply a sun block product that has a skin protection factor (SPF) of 15 or higher. If you have questions about this, check with your health care professional.
  • Apply a sun block lipstick that has an SPF of at least 15 to protect your lips.
  • Do not use a sun lamp or a tanning bed.
  • If you notice any unusual changes to your skin, check with your doctor.

While you are taking tacrolimus, it is important to maintain good dental hygiene and see a dentist regularly for teeth cleaning.

Raw oysters or other shellfish may contain bacteria that can cause serious illness, and possibly death. This is more likely to be a problem if these foods are eaten by patients with certain medical conditions. Even eating oysters from "clean" water or good restaurants does not guarantee that the oysters do not contain the bacteria. Symptoms of this infection include sudden chills, fever, nausea, vomiting, blood poisoning, and sometimes death. Eating raw shellfish is not a problem for most healthy people; however, patients with the following conditions may be at greater risk: cancer, immune disorders, organ transplantation, long-term corticosteroid use (as for asthma, arthritis, or organ transplantation), liver disease (including viral hepatitis), excess alcohol intake (2 to 3 drinks or more per day), diabetes, stomach problems (including previous stomach surgery and low stomach acid), and hemochromatosis (an iron disorder). Do not eat raw oysters or other shellfish while you are taking tacrolimus. Be sure oysters and shellfish are fully cooked.

While you are being treated with tacrolimus, and after you stop treatment with it, it is important to see your doctor about the immunizations (vaccinations) you should receive. Do not get any immunizations without your doctor's approval. Tacrolimus lowers your body's resistance. For some immunizations, there is a chance you might get the infection the immunization is meant to prevent. For other immunizations, it may be especially important to receive the immunization to prevent a disease. In addition, other persons living in your house should not take oral poliovirus vaccine since there is a chance they could pass the poliovirus on to you. Also, avoid persons who have recently taken oral poliovirus vaccine. Do not get close to them, and do not stay in the same room with them for very long. If you cannot take these precautions, you should consider wearing a protective face mask that covers the nose and mouth.

Treatment with tacrolimus may also increase the chance of getting other infections. If you can, avoid people with colds or other infections. If you think you are getting a cold or other infection, check with your doctor.

Tacrolimus is not available in all countries. If you are traveling to another country, be sure you will have an adequate supply of your medicine.

tacrolimus Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Some side effects will have signs or symptoms that you can see or feel. Your doctor will watch for others by doing certain tests.

Also, because of the way tacrolimus acts on the body, there is a chance that it may cause effects that may not occur until years after the medicine is used. These delayed effects may include certain types of cancer, such as lymphomas or skin cancers.

Check with your doctor immediately if any of the following side effects occur:

More common
  • Abdominal pain
  • abnormal dreams
  • agitation
  • anxiety
  • chills
  • confusion
  • convulsions (seizures)
  • diarrhea
  • dizziness
  • fever and sore throat
  • flu-like symptoms
  • frequent urination
  • hallucinations (seeing or hearing things that are not there)
  • headache
  • infection
  • itching
  • loss of appetite
  • loss of energy or weakness
  • mental depression
  • muscle trembling or twitching
  • nausea
  • nervousness
  • pale skin
  • shortness of breath
  • skin rash
  • swelling of feet or lower legs
  • tingling
  • trembling and shaking of hands
  • trouble in sleeping
  • unusual bleeding or bruising
  • unusual tiredness or weakness
  • vomiting
Less common
  • Blurred vision
  • chest pain
  • increased sensitivity to pain
  • muscle cramps
  • numbness or pain in legs
  • ringing in ears
  • sweating
Rare
  • Enlarged heart
  • flushing of face or neck
  • general feeling of discomfort or illness
  • weight loss
  • wheezing
Incidence not determined - Observed during clinical practice with tacrolimus; estimates of frequency cannot be determined.
  • Black, tarry stools
  • blistering, peeling, loosening of skin
  • bloating
  • blood in urine
  • blurred vision
  • constipation
  • convulsions (seizures)
  • cough
  • cramping or burning
  • drowsiness
  • fainting
  • fast, slow, or irregular heartbeat
  • heartburn
  • increased blood pressure
  • increased thirst
  • indigestion
  • irregular heartbeat
  • itching
  • joint or muscle pain
  • lightheadedness
  • loss of appetite
  • lower back or side pain
  • nausea
  • pinpoint red spots on skin
  • pounding or rapid pulse
  • recurrent fainting
  • red, irritated eyes
  • red skin lesions, often with a purple center
  • shortness of breath
  • sores
  • stomach pain
  • sugar in the urine
  • troubled breathing
  • ulcers or white spots in mouth or on lips
  • weakness
  • weight gain
  • yellow eyes or skin

tacrolimus may also cause the following side effects that your doctor will watch for:

More common
  • Hyperkalemia (too much potassium in the blood)
  • hypomagnesemia (not enough magnesium in the blood)
  • kidney problems
Less common
  • Hyperlipidemia (high cholesterol)
  • hypertension (high blood pressure)

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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