Tacrolimus

For kidney, liver, or heart transplant patients, the dose of tacrolimus varies according to the circumstances and will be determined by your doctor. If you are unable to take capsules, the medication may be delivered by slow injection into a vein at the hospital.

Tacrolimus is usually taken every 12 hours. You should try to take your doses of tacrolimus at the same time every day. The doses should be spaced as evenly throughout the day as possible. Ask your transplant nurse or pharmacist about a dosing schedule that fits your lifestyle.

Tacrolimus may be taken with or without food, but it is best to be consistent. Tacrolimus should not be taken with grapefruit or grapefruit juice. The capsules should be swallowed whole and not cut, crushed, or chewed.

For the treatment of rheumatoid arthritis, the recommended adult dose of tacrolimus is 3 mg, taken once a day. People taking Tacrolimus for rheumatoid arthritis must be regularly monitored by their doctor for side effects.

Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are using the medication without consulting your doctor.

It is important to take Tacrolimus exactly as prescribed by the doctor. If even a few doses of tacrolimus are missed, your body may reject your transplanted organ. If you miss a dose of tacrolimus, do not try to catch up on your own, but call your doctor or pharmacist immediately for advice. Ask your doctor ahead of time what you should do about missed doses. Be sure to order your medication refills well ahead of time.

Tacrolimus is often given with other medications. Make sure you talk to your doctor about whether you need to stop or continue taking any other immunosuppressive medications.

Store Tacrolimus at room temperature, protect it from light and moisture, and keep it out of the reach of children.

Do not dispose of medications in wastewater (e.g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.

In addition to its desired action, this medication may cause some adverse effects, notably: it may cause headaches; it may cause diarrhea; it may cause stomach ache; it may cause sleep disturbances or insomnia; it may cause nausea or, rarely, vomiting; it may cause numbness and a decreased sensitivity to touch; it may make your skin more sensitive to UV rays (e.g., sunlight, tanning lamps) - avoid exposure to UV rays as much as possible and protect yourself when out in the sun. Each person may react differently to a treatment. If you think this medication may be causing adverse effects (including those described here, or others), talk to your health care professional. He or she can help you to determine whether or not the medication is the source of the problem.

0.5 mg
Each white-to-off-white powder-filled, size “4” capsule, with a light-yellow opaque body imprinted with “Z” in black and light yellow cap imprinted with “0.5 mg” in black, contains tacrolimus 0.5 mg. Nonmedicinal ingredients: croscarmellose sodium, hypromellose, lactose monohydrate, magnesium stearate. Capsule shell: gelatine, titanium dioxide and yellow iron oxide. Printing ink: black iron oxide, butyl alcohol, dehydrated alcohol, isopropyl alcohol, potassium hydroxide, propylene glycol, shellac, strong ammonia, and water.

1 mg
Each white-to-off-white powder-filled, size “4” capsule with white opaque body imprinted with “Z” in black and white cap imprinted with “1 mg” in black, contains tacrolimus 1 mg. Nonmedicinal ingredients: croscarmellose sodium, hypromellose, lactose monohydrate, magnesium stearate. Capsule shell: gelatine, and titanium dioxide. Printing ink: black iron oxide, butyl alcohol, dehydrated alcohol, isopropyl alcohol, potassium hydroxide, propylene glycol, shellac, strong ammonia, and water.

5 mg
Each white-to-off-white powder-filled, size “3” capsule with Swedish-orange-coloured opaque body imprinted with “Z” in black, and Swedish-orange-coloured cap imprinted with “5 mg” in black contains tacrolimus 5 mg. Nonmedicinal ingredients: croscarmellose sodium, hypromellose, lactose monohydrate, magnesium stearate. Capsule shell: gelatine, titanium dioxide, and red iron oxide. Printing ink: black iron oxide, butyl alcohol, dehydrated alcohol, isopropyl alcohol, potassium hydroxide, propylene glycol, shellac, strong ammonia, and water.

Do not take Tacrolimus if you are allergic to tacrolimus or any ingredients of the medication.

There may be an interaction between tacrolimus and any of the following:

• Acarbose
• alcohol
• Aliskiren
• Amiodarone
• antacids (e.g., aluminum hydroxide, magnesium carbonate)
• antifungal medications (e.g., ketoconazole, Clotrimazole, itraconazole, fluconazole, Voriconazole)
• antihistamines (e.g., cetirizine, doxylamine, Diphenhydramine, Hydroxyzine, Loratadine)
• antipsychotics (e.g., Chlorpromazine, Clozapine, Haloperidol, Olanzapine, Quetiapine, Risperidone)
• Aprepitant
• barbiturates (e.g., butalbital, Phenobarbital)
• BCG
• Bosentan
• Bromocriptine
• calcium channel blockers (e.g., Diltiazem, Verapamil, Nifedipine)
• Carbamazepine
• Carvedilol
• Celecoxib
• chloroquine
• Cinacalcet
• Cobicistat
• Colchicine
• conivaptan
• corticosteroids (e.g., Dexamethasone, Hydrocortisone, Prednisone)
• Cyclosporine
• daclatasvir
• Danazol
• Deferasirox
• Denosumab
• diabetes medications (e.g., chlorpropamide, Glyburide, insulin, Metformin, Rosiglitazone)
• Disopyramide
• dofetilide
• Domperidone
• Dronedarone
• echinacea
• Enzalutamide
• Eplerenone
• Fenofibrate
• Fingolimod
• Flecainide
• "gliptin" diabetes medications (e.g., Linagliptin, Saxagliptin, Sitagliptin)
• grapefruit juice
• H2 antagonists (e.g., Famotidine, Ranitidine)
• HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs; e.g., delavirdine, efavirenz, etravirine, nevirapine)
• HIV protease inhibitors (e.g., atazanavir, indinavir, ritonavir, saquinavir)
• Leflunomide
• macrolide antibiotics (e.g., erythromycin, clarithromycin)
• medications to treat cancer (e.g., Carboplatin, Cyclophosphamide, Doxorubicin, Ifosfamide, Vincristine)
• Methadone
• Methotrexate
• Metoclopramide
• mifepristone
• Modafinil
• nefazodone
• non-steroidal anti-inflammatory medications (NSAIDs; e.g., Diclofenac, Ibuprofen, Naproxen)
• Oxcarbazepine
• Phenytoin
• Pimecrolimus
• potassium-sparing diuretics (e.g., Amiloride, Spironolactone, triamterene)
• primidone
• procainamide
• Propafenone
• protein kinase inhibitors (e.g., Bosutinib, Crizotinib, Dabrafenib, imatinib, Nilotinib, Sunitinib)
• proton pump inhibitors (e.g., Lansoprazole, Omeprazole)
• quinidine
• quinine
• quinolone antibiotics (e.g., ciprofloxacin, Norfloxacin, Ofloxacin)
• rifabutin
• rifampin
• rilpivirine
• Roflumilast
• St. John's wort
• selective serotonin reuptake inhibitors (SSRIs; e.g., Citalopram, Fluoxetine, Paroxetine, Sertraline)
• serotonin antagonists (anti-emetic medications; e.g., Granisetron, Ondansetron)
• sevelamer
• Sildenafil
• siltuximab
• Sirolimus
• Sotalol
• "statin" cholesterol lowering medications (e.g., Atorvastatin, Lovastatin, Simvastatin)
• Tetrabenazine
• Tocilizumab
• Tofacitinib
• Trastuzumab
• tricyclic antidepressants (e.g., Amitriptyline, Clomipramine, Desipramine, Trimipramine)
• vaccines
• Vardenafil

If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

• stop taking one of the medications,
• change one of the medications to another,
• change how you are taking one or both of the medications, or
• leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.

Medications other than those listed above may interact with Tacrolimus. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the Nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.

Before you begin using a medication, be sure to inform your doctor of any medical conditions or Allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use Tacrolimus.

Abnormal heart rhythms: Tacrolimus may cause a heart rhythm problem called QT prolongation. If you have a history of QT prolongation, slow or irregular heartbeat, irregular heart rhythm, heart failure, Heart Attack, heart disease, taking other medications known to cause QT prolongation, or a family history of sudden cardiac death at less than 50 years of age, discuss with your doctor how Tacrolimus may affect your medical condition, or how your medical condition may affect the dosing and effectiveness of Tacrolimus. Your doctor will perform tests at regular intervals to monitor for any changes in your heart rhythm.

Blood pressure: Tacrolimus treatment commonly causes mild-to-moderate increases in blood pressure. Monitor your blood pressure, and inform your doctor if there is an indication that your blood pressure is rising.

Diabetes: Tacrolimus may cause an increase in blood sugar levels and glucose tolerance may change. People with diabetes may find it necessary to monitor their blood sugar more frequently while using Tacrolimus. Your doctor will help to monitor this, but be sure to report any signs of high blood sugar (e.g., increased thirst, urination, unusual tiredness) to your doctor.

If you have diabetes or are at risk for developing diabetes, discuss with your doctor how Tacrolimus may affect your medical condition, how your medical condition may affect the dosing and effectiveness of Tacrolimus, and whether any special monitoring is needed.

High potassium levels in the blood: Tacrolimus may cause an increase in potassium levels in the blood. Some foods (e.g., bananas or orange juice) and some medications may increase the risk of this problem. Be sure to tell your doctor and pharmacist about all the medications you are taking (including non-prescription medications) and to talk to them about potassium-rich foods.

Infections: Tacrolimus reduces resistance to infections and may delay healing. Ensure proper treatment to avoid infection (e.g., dental work, skin injury). Avoid activities that increase the risk of infection.

Because tacrolimus reduces the body’s response to infection, conditions caused by bacteria or viruses that have been dormant in the body, such as chicken pox, hepatitis B, or Tuberculosis may be reactivated.

Tell your doctor immediately if you notice signs of an infection, such as fever or chills, severe diarrhea, shortness of breath, prolonged dizziness, headache, stiff neck, weight loss, or listlessness.

Kidneys: Tacrolimus may affect kidney function. Your doctor will monitor your kidney function with laboratory tests while you are taking Tacrolimus. Be sure to immediately report to your doctor any evidence of changes in kidney function such as changes in the appearance of urine, frequency of urination, and amount of urine produced.

Liver function: Liver disease or reduced liver function may cause Tacrolimus to build up in the body, causing side effects. If you have liver problems, discuss with your doctor how Tacrolimus may affect your medical condition, how your medical condition may affect the dosing and effectiveness of Tacrolimus, and whether any special monitoring is needed. Your doctor may want to test your liver function regularly with blood tests while you are taking Tacrolimus.

If you experience symptoms of liver problems such as fatigue, feeling unwell, loss of appetite, nausea, yellowing of the skin or whites of the eyes, dark urine, pale stools, abdominal pain or swelling, and itchy skin, contact your doctor immediately.

Lymphoma and other malignancies: People taking immunosuppressant medications, such as tacrolimus, are at increased risk of developing a type of cancer known as lymphoma and certain types of Skin Cancer. This risk is related to the intensity and duration of treatment with immunosuppressant medications rather than to one specific medication.

Possible warning signs of cancer include a change in bowel or bladder habits, sores that don’t heal, unusual bleeding, change in appearance of a wart or mole, night sweats, a nagging cough or persistent and severe headaches. If you experience any of these, let your doctor know right away. This may help to detect any cancers early in their development.

Nerves: Tacrolimus may affect nerve function and cause symptoms such as tremors and headaches. Be sure to report any changes to your doctor at once.

Red blood cell aplasia: Tacrolimus has been reported to cause the body to stop producing red blood cells. If you experience symptoms of reduced red blood cell count such as shortness of breath, feeling unusually tired or pale skin, contact your doctor as soon as possible.

Reversible posterior leukoencephalopathy syndrome (RPLS): This is a rare disease of the brain that can occur when using tacrolimus. Make sure your doctor knows if you have experienced this condition before. If you experience signs and symptoms of RPLS, such as headache, seizures, change in awareness or consciousness or vision changes, contact your doctor immediately.

Pregnancy: Adequate studies have not been conducted on the use of tacrolimus by pregnant women. Reports of the use of tacrolimus during pregnancy has been associated with high blood potassium levels and kidney problems in the newborn.

Tacrolimus should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking Tacrolimus, contact your doctor immediately.

Breast-feeding: Tacrolimus passes into breast milk. Breast-feeding is not recommended while taking tacrolimus. If you are a breast-feeding mother and taking tacrolimus, it may affect your baby. Talk to your doctor.

This medication is typically used only once a day. However, your pharmacist may have suggested a different schedule that is more appropriate for you. Important: Follow the instructions on the label. Do not use more of this product, or more often, than prescribed. The capsule of this medication should not be opened, crushed or chewed. It must be used regularly and continuously to maintain its beneficial effects. Be sure to keep an adequate supply on hand. You should take this medication at approximately the same time each day. If you remember missing a dose within 14 hours of the time it is usually taken, take it as soon as you remember, then take the next dose at the regularly scheduled time. If the dose is missed by more than 14 hours, skip the missed dose. Do not double the next dose to catch up. This medication may be taken with or without food, but always the same way (always with or always without food). Avoid grapefruit and grapefruit juice during your treatment. Grapefruit can seriously affect how this medication works. If you drink alcohol, a moderate consumption is recommended. Talk to your health care professional to find out exactly how much alcohol you can drink.