Pronunciation:

ta-KROE-li-mus

Brand Names:

• Prograf

Dosage Forms:

• Solution
• Capsule

Warnings:

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 .

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 .

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 .

Classifications:

Therapeutic—

Immune Suppressant

Uses of This Medicine:

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 this medicine 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 This Medicine:

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.

Children—

This medicine 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.

Older adults—

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 Category	Explanation
All Trimesters	C	Animal 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.

Other medicines—

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.

• Ziprasidone

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

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:

• 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 This Medicine:

Take this medicine 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 this medicine may be changed if you change your diet. This medicine 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 this medicine in the body. You should not eat grapefruit or drink grapefruit juice while you are taking this medicine.

Do not stop taking this medicine 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 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):
  • 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 This Medicine:

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

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.

Side Effects of This Medicine:

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

This medicine 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.