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Tacrolimus (Oral route)

Pronunciation:

ta-KROE-li-mus

Brand Names:

  • Astagraf XL
  • Hecoria
  • Prograf

Dosage Forms:

  • Capsule
  • Capsule, Extended Release

Warnings:

Oral route(Capsule, Extended Release;Capsule)

Increased susceptibility to infection and the possible development of lymphoma and other malignancies may result from immunosuppression . Use of Astagraf XL(TM) in liver transplant recipients is not recommended, as increased mortality was seen in female liver transplant patients in a clinical trial . 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 .

Classifications:

Therapeutic—

Immune Suppressant

Pharmacologic—

Calcineurin Inhibitor

Uses of This Medicine:

Tacrolimus is used together with other medicines to prevent the body from rejecting a transplanted organ (eg, kidney, liver, or heart). This medicine may be used with steroids, azathioprine (Imuran®), basiliximab (Simulect®), or mycophenolate mofetil (Cellcept®). 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.

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 transplant.
  • Pancreas transplant.
  • Rheumatoid arthritis.

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—

Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of tacrolimus in children with liver transplants.

Appropriate studies have not been performed on the relationship of age to the effects of tacrolimus in children with kidney and heart transplants. Safety and efficacy have not been established.

Older adults—

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.

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.

Other medicines—

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.

  • Amifampridine
  • Dronedarone
  • Fluconazole
  • Mifepristone
  • Nelfinavir
  • Pimozide
  • Piperaquine
  • Posaconazole
  • 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.

  • Aceclofenac
  • Acemetacin
  • Adalimumab
  • Afatinib
  • Alefacept
  • Amikacin
  • Amiloride
  • Amiodarone
  • Amtolmetin Guacil
  • Aripiprazole
  • Artemether
  • Aspirin
  • Atazanavir
  • Bacillus of Calmette and Guerin Vaccine, Live
  • Basiliximab
  • Bedaquiline
  • Bromfenac
  • Bufexamac
  • Buserelin
  • Carbamazepine
  • Caspofungin
  • Celecoxib
  • Ceritinib
  • Choline Salicylate
  • Cisplatin
  • Citalopram
  • Clarithromycin
  • Clonixin
  • Clozapine
  • Colchicine
  • Crizotinib
  • Cyclosporine
  • Dabrafenib
  • Darunavir
  • Delamanid
  • Deslorelin
  • Dexibuprofen
  • Dexketoprofen
  • Dibekacin
  • Diclofenac
  • Diflunisal
  • Dipyrone
  • Domperidone
  • Efavirenz
  • Eliglustat
  • Enzalutamide
  • Erythromycin
  • Escitalopram
  • Eslicarbazepine Acetate
  • Esomeprazole
  • Etodolac
  • Etofenamate
  • Etoricoxib
  • Etravirine
  • Felbinac
  • Fenoprofen
  • Fepradinol
  • Feprazone
  • Floctafenine
  • Flufenamic Acid
  • Fluoxetine
  • Flurbiprofen
  • Fosphenytoin
  • Gentamicin
  • Gonadorelin
  • Goserelin
  • Haloperidol
  • Histrelin
  • Ibuprofen
  • Ibuprofen Lysine
  • Idelalisib
  • Iloperidone
  • Indomethacin
  • Infliximab
  • Itraconazole
  • Ivabradine
  • Kanamycin
  • Ketoconazole
  • Ketoprofen
  • Ketorolac
  • Lapatinib
  • Leuprolide
  • Lornoxicam
  • Loxoprofen
  • Lumefantrine
  • Lumiracoxib
  • Measles Virus Vaccine, Live
  • Meclofenamate
  • Mefenamic Acid
  • Meloxicam
  • Metronidazole
  • Mitotane
  • Morniflumate
  • Mumps Virus Vaccine, Live
  • Nabumetone
  • Nafarelin
  • Naproxen
  • Nefazodone
  • Neomycin
  • Nepafenac
  • Netilmicin
  • Niflumic Acid
  • Nilotinib
  • Nimesulide
  • Omeprazole
  • Ondansetron
  • Oxaprozin
  • Oxyphenbutazone
  • Parecoxib
  • Pazopanib
  • Phenobarbital
  • Phenylbutazone
  • Phenytoin
  • Piketoprofen
  • Piroxicam
  • Pixantrone
  • Poliovirus Vaccine, Live
  • Pranoprofen
  • Primidone
  • Proglumetacin
  • Propyphenazone
  • Proquazone
  • Quetiapine
  • Ranolazine
  • Rifabutin
  • Rifampin
  • Rofecoxib
  • Rotavirus Vaccine, Live
  • Rubella Virus Vaccine, Live
  • Salicylic Acid
  • Salsalate
  • Sevoflurane
  • Siltuximab
  • Simeprevir
  • Sirolimus
  • Smallpox Vaccine
  • Sodium Salicylate
  • Spironolactone
  • St John's Wort
  • Streptomycin
  • Sulindac
  • Sunitinib
  • Telaprevir
  • Telithromycin
  • Tenofovir
  • Tenoxicam
  • Tiaprofenic Acid
  • Ticagrelor
  • Tizanidine
  • Tobramycin
  • Tocophersolan
  • Tolfenamic Acid
  • Tolmetin
  • Triamterene
  • Triptorelin
  • Typhoid Vaccine
  • Ulipristal
  • Valdecoxib
  • Vandetanib
  • Varicella Virus Vaccine
  • Vemurafenib
  • Vilanterol
  • Vinflunine
  • Voriconazole
  • Yellow Fever Vaccine

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
  • Amprenavir
  • Boceprevir
  • Chloramphenicol
  • Clotrimazole
  • Dalfopristin
  • Danazol
  • Dihydroxyaluminum Aminoacetate
  • Dihydroxyaluminum Sodium Carbonate
  • Diltiazem
  • Ertapenem
  • Magnesium Carbonate
  • Magnesium Hydroxide
  • Magnesium Oxide
  • Magnesium Trisilicate
  • Metoclopramide
  • Mibefradil
  • Nevirapine
  • Nifedipine
  • Quinupristin
  • Rifapentine
  • Ritonavir
  • Saquinavir
  • Schisandra sphenanthera
  • Theophylline
  • 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 family 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
  • Paresthesias (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.
  • 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 of This Medicine:

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 you to reject your transplanted organ.

This medicine comes with a patient information insert. It is very important that you read and understand this information. Be sure to ask your doctor about anything you do not understand.

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 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 breakfast.
  • Do not drink alcohol with the capsule.

You should not eat grapefruit or drink grapefruit juice while you are taking this medicine. Grapefruit and grapefruit juice will increase the amount of medicine in the body.

Do not stop taking this medicine without first checking with your doctor. You might 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 (extended-release capsules):
    • To prevent kidney transplant rejection:
      • Adults and children 16 years of age and older—Dose is based on body weight and must be determined by your doctor. The dose is usually between 0.1 to 0.2 milligram (mg) per kilogram (kg) of body weight per day given as a single dose. Your doctor may adjust the dose as needed.
      • Children younger than 16 years of age—Use and dose must be determined by your doctor.
  • For oral dosage form (capsules):
    • To prevent heart transplant rejection:
      • Adults—Dose is based on body weight and must be determined by your doctor. The starting dose is usually 0.075 milligram (mg) per kilogram (kg) of body weight per day, divided into two doses and taken every 12 hours. Your doctor may adjust the dose as needed.
      • Children—Use and dose must be determined by your doctor.
    • 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 (mg) per kilogram (kg) of body weight per day, divided into two doses and taken every 12 hours. Your doctor may adjust the dose as needed.
      • Children—Use and dose must be determined by your doctor.
    • To prevent liver transplant rejection:
      • Adults and teenagers 16 years of age and older—Dose is based on body weight and must be determined by your doctor. The starting dose is usually 0.1 to 0.15 milligram (mg) per kilogram (kg) of body weight per day, divided into two doses and taken every 12 hours. Your doctor may adjust the dose as needed.
      • Teenagers and children younger than 16 years of age—Dose is based on body weight and must be determined by your doctor. The starting dose is usually 0.15 to 0.2 mg per kg of body weight per day, divided into two doses and taken every 12 hours. Your doctor may adjust the dose as needed.

Missed dose—

DRUG: GENERAL, MISS, STANDARD

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 dose and return to your regular schedule on the next day.

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 While Using This Medicine:

It is very important that your doctor check your 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.

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.

Use sunscreen or sunblock lotions 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.

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 are having more than one of these symptoms: bloody urine, a 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 increase your risk of developing a serious and rare brain infection called progressive multifocal leukoencephalopathy (PML). Check with your doctor right away if you are having more than one of these symptoms: vision changes, loss of coordination, clumsiness, confusion, memory loss, difficulty speaking or understanding what others say, or weakness in the legs.

This medicine may increase your risk of a stomach problem called gastrointestinal perforation. Talk to your doctor if you have concerns about this risk.

This medicine may cause serious nervous system problems. Tell your doctor right away if you have the following symptoms while using this medicine: blurred vision, dizziness, headache, mental changes, seizures, high blood pressure, 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 abdominal or stomach pain, confusion, difficulty with breathing, an irregular heartbeat, nausea or vomiting, nervousness, numbness or tingling in the hands, feet, or lips, 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.

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, St. John's wort) or vitamin supplements.

Side Effects of This Medicine:

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
Abdominal or stomach pain
abnormal dreams
agitation
chills
confusion
convulsions (seizures)
diarrhea
dizziness
fever and sore throat
flu-like symptoms
frequent urination
headache
itching
loss of appetite
loss of energy or weakness
mental depression
muscle trembling or twitching
nausea
pale skin
seeing or hearing things that are not there
shortness of breath
skin rash
swelling of the feet or lower legs
tingling
trembling and shaking of the hands
trouble 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 the legs
ringing in the ears
sweating
Rare
Enlarged heart
flushing of the face or neck
general feeling of discomfort or illness
weight loss
wheezing
Incidence not known
Black, tarry stools
blistering, peeling, loosening of the skin
bloating
bloody urine
constipation
cough
drowsiness
fainting
fast, slow, or irregular heartbeat
heartburn
increased thirst
indigestion
joint or muscle pain
lightheadedness
lower back or side pain
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
Acid or sour stomach
belching
difficulty with moving
lack or loss of strength
muscle pain or stiffness
Less common
Body aches or pain
burning or stinging of the skin
cracks in the skin
crying
delusions
dementia
depersonalization
dysphoria
euphoria
excessive muscle tone
feeling of constant movement of self or surroundings
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
loss of strength or energy
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
quick to react or overreact emotionally
rapidly changing moods
redness or other discoloration of the skin
restlessness
scaly skin
sensation of spinning
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
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
sudden sweating

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.


Last Updated: 11/4/2014

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