Tacrolimus (Intravenous)

Tacrolimus injection is used with other medicines to stop the body from rejecting a transplanted organ (such as a kidney, liver, heart, or lung). This medicine may be used with steroids, azathioprine, or mycophenolate mofetil. Tacrolimus is part of a group of medicines called immunosuppressive agents.

When a patient gets an organ transplant, the body's white blood cells will try to get rid of (reject) the transplanted organ. Tacrolimus helps by suppressing the immune system to stop the white blood cells from rejecting the transplanted organ.

Tacrolimus is a very strong medicine. It can cause side effects that can be very serious, like kidney problems. It may also lower the body's ability to fight infections. You and your doctor should discuss the benefits of this medicine along with the risks of using it.

This medicine is to be given only by or under the direct supervision of a doctor.

It is very important that your doctor checks your progress while you are using this medicine to ensure it 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.

You should not use this medicine together with sirolimus (Rapamune®).

Tacrolimus injection may cause serious allergic reactions, including anaphylaxis, which can be life-threatening and require immediate medical attention. Call your doctor or nurse right away if you experience itching, hives, hoarseness, trouble breathing or swallowing, or any swelling of your hands, face, or mouth after you receive this medicine.

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 sick people 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 receive 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. Additionally, you should not be around other people 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 of 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.

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.

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, and weakness in the legs.

This medicine may cause serious brain or nerve problems (e.g., 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, 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 breathing, 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.

Use sunscreen or sunblock lotion with a sun protection factor (SPF) of at least 15 regularly when you are outdoors. Wear protective clothing and hats, and stay out of direct sunlight between 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 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 (e.g., cannabidiol, St. John's wort) or vitamin supplements.

In deciding to use a medicine, the risks of using the drug must be weighed against the beneficial it will do. This is a decision you and your clinician will make. For this medicine, the following should be considered:

Allergies

Inform your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medications. Also inform 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 tacrolimus injection in children with liver, kidney, heart, or lung transplants.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific issues that would limit the usefulness of tacrolimus injection 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 injection.

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 chances before using this drug while breastfeeding.

Interactions with 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 clinician may want to change the dose, or other precautions may be necessary. When you are receiving this medicine, it is especially essential that your healthcare professional know if you are using 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 medications you take.

• Bepridil
• Cisapride
• Dronedarone
• Fluconazole
• Lefamulin
• Mesoridazine
• Mifepristone
• Nelfinavir
• Pimozide
• Piperaquine
• Posaconazole
• Ritonavir
• Saquinavir
• Sparfloxacin
• Terfenadine
• Thioridazine
• Ziprasidone

Using this medication with any of the following drugs is usually not recommended, but may be required in some cases. If both medications are prescribed together, your clinician may change the dose or how frequently you use one or both of the drugs.

• Abacavir
• Abametapir
• Abrocitinib
• Aceclofenac
• Acemetacin
• Adagrasib
• Adenovirus Vaccine, Live
• Alefacept
• Alfuzosin
• Amikacin
• Amiloride
• Amiodarone
• Amisulpride
• Amitriptyline
• Amlodipine
• Amphotericin B
• Amprenavir
• Amtolmetin Guacil
• Anagrelide
• Apalutamide
• Apomorphine
• Aprepitant
• Aripiprazole
• Aripiprazole Lauroxil
• Armodafinil
• Arsenic Trioxide
• Asciminib
• Asenapine
• Aspirin
• Astemizole
• Atazanavir
• Avacopan
• Azilsartan
• Azilsartan Medoxomil
• Azithromycin
• Bacillus of Calmette and Guerin Vaccine, Live
• Bedaquiline
• Belzutifan
• Benazepril
• Berotralstat
• Boceprevir
• Bosentan
• Bromfenac
• Bufexamac
• Buprenorphine
• Buserelin
• Candesartan
• Cannabidiol
• Cannabis
• Canrenoate
• Canrenone
• Capreomycin
• Captopril
• Carbamazepine
• Caspofungin
• Celecoxib
• Cenobamate
• Ceritinib
• Chloramphenicol
• Chloroquine
• Chlorpromazine
• Cholera Vaccine, Live
• Choline Salicylate
• Cimetidine
• Ciprofloxacin
• Cisplatin
• Citalopram
• Clarithromycin
• Clofazimine
• Clomipramine
• Clonixin
• Clothiapine
• Clotrimazole
• Clozapine
• Cobicistat
• Colchicine
• Conivaptan
• Crizotinib
• Cyclobenzaprine
• Cyclosporine
• Dabrafenib
• Dalfopristin
• Daridorexant
• Darunavir
• Dasabuvir
• Dasatinib
• Degarelix
• Delamanid
• Delavirdine
• Dengue Tetravalent Vaccine, Live
• Desipramine
• Deslorelin
• Deutetrabenazine
• Dexamethasone
• Dexibuprofen
• Dexketoprofen
• Dexmedetomidine
• Diclofenac
• Didanosine
• Diflunisal
• Diltiazem
• Dipyrone
• Disopyramide
• Dofetilide
• Dolasetron
• Domperidone
• Donepezil
• Doxepin
• Droperidol
• Droxicam
• Ebastine
• Ebola Zaire Vaccine, Live
• Echinacea
• Efavirenz
• Elacestrant
• Elagolix
• Elbasvir
• Eliglustat
• Eluxadoline
• Emtricitabine
• Enalapril
• Enalaprilat
• Enasidenib
• Encorafenib
• Entrectinib
• Enzalutamide
• Eplerenone
• Eprosartan
• Erdafitinib
• Eribulin
• Erythromycin
• Escitalopram
• Eslicarbazepine Acetate
• Esomeprazole
• Etodolac
• Etofenamate
• Etoricoxib
• Etrasimod
• Etravirine
• Famotidine
• Fedratinib
• Felbamate
• Felbinac
• Felodipine
• Fenoprofen
• Fentanyl
• Fepradinol
• Feprazone
• Fexinidazole
• Fingolimod
• Flecainide
• Floctafenine
• Flufenamic Acid
• Fluoxetine
• Flurbiprofen
• Fluvoxamine
• Formoterol
• Fosamprenavir
• Fosaprepitant
• Foscarnet
• Fosinopril
• Fosnetupitant
• Fosphenytoin
• Fostemsavir
• Galantamine
• Gatifloxacin
• Gemifloxacin
• Gentamicin
• Gepirone
• Glasdegib
• Glecaprevir
• Gonadorelin
• Goserelin
• Granisetron
• Grazoprevir
• Halofantrine
• Haloperidol
• Histrelin
• Hydroquinidine
• Hydroxychloroquine
• Hydroxyzine
• Ibuprofen
• Ibuprofen Lysine
• Ibutilide
• Idelalisib
• Iloperidone
• Imatinib
• Imipramine
• Indinavir
• Indomethacin
• Infliximab
• Influenza Virus Vaccine, Live
• Inotuzumab Ozogamicin
• Irbesartan
• Isavuconazonium Sulfate
• Itraconazole
• Ivabradine
• Ivacaftor
• Ivosidenib
• Kanamycin
• Ketoconazole
• Ketoprofen
• Ketorolac
• Lamivudine
• Lanreotide
• Lapatinib
• Larotrectinib
• Lasmiditan
• Lenacapavir
• Lenvatinib
• Letermovir
• Leuprolide
• Levamlodipine
• Levofloxacin
• Lisinopril
• Lofexidine
• Lomitapide
• Lopinavir
• Lorlatinib
• Lornoxicam
• Losartan
• Loxoprofen
• Lumacaftor
• Lumefantrine
• Lumiracoxib
• Macimorelin
• Mavacamten
• Measles Virus Vaccine, Live
• Meclofenamate
• Mefenamic Acid
• Mefloquine
• Meloxicam
• Methadone
• Methotrimeprazine
• Methylprednisolone
• Metoclopramide
• Metronidazole
• Mibefradil
• Mirtazapine
• Mitotane
• Mizolastine
• Mobocertinib
• Modafinil
• Moexipril
• Moricizine
• Morniflumate
• Moxifloxacin
• Mumps Virus Vaccine, Live
• Mycophenolic Acid
• Nabumetone
• Nafarelin
• Nafcillin
• Naproxen
• Nefazodone
• Neomycin
• Nepafenac
• Neratinib
• Netilmicin
• Netupitant
• Nevirapine
• Nicardipine
• Nifedipine
• Niflumic Acid
• Nilotinib
• Nimesulide
• Nimesulide Beta Cyclodextrin
• Nirmatrelvir
• Norfloxacin
• Octreotide
• Ofloxacin
• Olanzapine
• Olmesartan
• Omaveloxolone
• Ombitasvir
• Omeprazole
• Ondansetron
• Osilodrostat
• Osimertinib
• Oxaliplatin
• Oxaprozin
• Oxcarbazepine
• Oxyphenbutazone
• Ozanimod
• Pacritinib
• Palbociclib
• Paliperidone
• Panobinostat
• Papaverine
• Parecoxib
• Paritaprevir
• Paromomycin
• Paroxetine
• Pasireotide
• Pazopanib
• Pentamidine
• Perindopril
• Perphenazine
• Phenobarbital
• Phenylbutazone
• Phenytoin
• Piketoprofen
• Pimavanserin
• Pipamperone
• Piroxicam
• Pirtobrutinib
• Pitolisant
• Pixantrone
• Plazomicin
• Poliovirus Vaccine, Live
• Ponesimod
• Potassium Phosphate
• Prednisone
• Primidone
• Probucol
• Procainamide
• Prochlorperazine
• Proglumetacin
• Promethazine
• Propafenone
• Propionic Acid
• Propyphenazone
• Proquazone
• Protriptyline
• Quetiapine
• Quinapril
• Quinidine
• Quinine
• Quinupristin
• Quizartinib
• Ramipril
• Ranitidine
• Ranolazine
• Relugolix
• Remdesivir
• Ribociclib
• Rifabutin
• Rifampin
• Rifapentine
• Risperidone
• Ritlecitinib
• Rofecoxib
• Rotavirus Vaccine, Live
• Rubella Virus Vaccine, Live
• Salicylic Acid
• Salsalate
• Schisandra sphenanthera
• Selpercatinib
• Sertindole
• Sertraline
• Sevoflurane
• Simeprevir
• Siponimod
• Sirolimus
• Smallpox Monkeypox Vaccine, Live Non-Replicating
• Smallpox Vaccine
• Sodium Phosphate
• Sodium Phosphate, Dibasic
• Sodium Phosphate, Monobasic
• Sodium Salicylate
• Solifenacin
• Sorafenib
• Sotalol
• Sotorasib
• Sparsentan
• Spectinomycin
• Spirapril
• Spironolactone
• Stavudine
• St John's Wort
• Streptomycin
• Sulindac
• Sulpiride
• Sultopride
• Sunitinib
• Tamoxifen
• Taurursodiol
• Telaprevir
• Telavancin
• Telithromycin
• Telmisartan
• Tenofovir
• Tenoxicam
• Tepotinib
• Tetrabenazine
• Tiaprofenic Acid
• Tipranavir
• Tizanidine
• Tobramycin
• Tocilizumab
• Tofacitinib
• Tolfenamic Acid
• Tolmetin
• Tolterodine
• Toremifene
• Trandolapril
• Trazodone
• Triamterene
• Triclabendazole
• Trimipramine
• Triptorelin
• Trofinetide
• Tucatinib
• Typhoid Vaccine, Live
• Valdecoxib
• Valsartan
• Vandetanib
• Vardenafil
• Varicella Virus Vaccine, Live
• Vemurafenib
• Venlafaxine
• Verapamil
• Vilanterol
• Vilazodone
• Vinflunine
• Voclosporin
• Vonoprazan
• Voriconazole
• Vorinostat
• Voxelotor
• Voxilaprevir
• Yellow Fever Vaccine
• Zidovudine
• Zoster Vaccine, Live
• Zotepine
• Zuclopenthixol

Using this medicine with any of the following drugs may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both drugs are prescribed together, your doctor may change the dose or how frequently you use one or both of the medicines.

• Danazol
• Ertapenem
• Lansoprazole
• Tigecycline

Interactions with Food/Tobacco/Alcohol

Certain medications 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 additionally 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 frequently you use this medication, or give you special instructions about the use of food, alcohol, or tobacco.

• Grapefruit Juice

Other Medical Issues

The presence of other medical problems may affect the use of this medicine. Make sure you inform your doctor if you have any other medical issues, especially:

• Allergy to polyoxyl 60 hydrogenated castor oil—Should not be used in patients with this condition.

• Cystic fibrosis—May require a higher dose for patients with this condition.

• Diabetes or
• Heart disease or
• Heart rhythm issues (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.

• Infection, active (eg, bacteria, fungus, or virus)—May lower your body's ability to fight an infection.

• Kidney disease or
• Liver disease—Use with caution. The effects may be increased since of slower removal of the medicine from the body.

Along with its necessary effects, a medicine may cause some unwanted effects. Not all of these side effects may occur, but if they do, they may need medical attention.

Check with your doctor or nurse right away if any of the following side effects happen:

More common

• Abnormal dreams
• agitation
• anxiety
• blurred vision
• chills
• 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 aches and pains
• muscle trembling or twitching
• nausea
• nervousness
• 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 with 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
• bloated stomach
• bloating
• bloody nose
• bloody urine
• blurred vision
• change in mental status
• constipation
• drowsiness
• fainting
• fast, slow, or irregular heartbeat
• heartburn
• heavier menstrual periods
• increased blood pressure
• 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, irritated eyes
• red skin lesions, often with a purple center
• skin sores
• ulcers or white spots in mouth or on 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
• muscle stiffness

Less common

• Body aches or pain
• burning or stinging of the skin
• cracks in the skin
• crying
• delusions of persecution, mistrust, suspiciousness, or combativeness
• 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
• 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 happen 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.

In the U.S.

• Prograf

Available Dosage Forms:

• Solution

Therapeutic Class: Immune Suppressant

Pharmacologic Class: Calcineurin Inhibitor

A nurse or other trained health professional will give you this medicine in a hospital. It is given through a needle placed into one of your veins. The medicine must be injected slowly, so your IV tube will need to stay in place for 30 minutes.

You will only receive this medicine for a few days. Then your doctor will switch you to the oral (by mouth) form of tacrolimus.

This medicine comes with a patient information insert and patient instructions. Read and follow the instructions carefully. Ask your doctor if you have any questions.

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

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