Generic Name: Tacrolimus Brand Name(s): Generics only. No brands available.

Uses

What is Tacrolimus used for?

Tacrolimus is used with other medications to prevent rejection of a kidney, heart, or liver transplant. This medication belongs to a class of drugs known as immunosuppressants. It works by weakening your body’s defense system (immune system) to help your body accept the new organ as if it were your own.

How should I take Tacrolimus?

Take this medication by mouth with or without food, usually every 12 hours or as directed by your doctor. If you have nausea or an upset stomach, you may take this drug with food, although this may cause your body to absorb less of the drug. However, you must choose one way (with food or without food) and always take this medication the same way so that your body always absorbs the same amount of drug. Consult your doctor or pharmacist for more details.

Dosage is based on your weight, medical condition, blood test results (e.g., tacrolimus trough levels), and response to therapy.

Do not increase your dose or take this medication more often without your doctor’s approval. Your condition will not improve any faster and the risk of serious side effects may be increased. Also, do not stop taking this medication without your doctor’s approval.

Take this medication regularly in order to get the most benefit from it. It is important to take all doses on time to keep the amount of medicine in your body at a constant level. Remember to take it at the same times each day.

How do I store Tacrolimus?

Tacrolimus is best stored at room temperature away from direct light and moisture. To prevent drug damage, you should not store Tacrolimus in the bathroom or the freezer. There may be different brands of Tacrolimus that may have different storage needs. It is important to always check the product package for instructions on storage, or ask your pharmacist. For safety, you should keep all medicines away from children and pets.

You should not flush Tacrolimus down the toilet or pour them into a drain unless instructed to do so. It is important to properly discard this product when it is expired or no longer needed. Consult your pharmacist for more details about how to safely discard your product.

Precautions & warnings

What should I know before using Tacrolimus?

Before taking tacrolimus, tell your doctor or pharmacist if you are allergic to it; or to other macrolide medications (such as sirolimus); or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: mineral imbalances (such as high potassium), kidney disease, any recent/current infections, cancer, liver disease, high blood pressure, diabetes.

Tacrolimus may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away.

The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may cause QT prolongation. Before using tacrolimus, tell your doctor or pharmacist of all the drugs you take and if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).

Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/”water pills”) or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using tacrolimus safely.

This medication may increase your risk of developing skin cancer. Limit your time in the sun. Avoid tanning booths and sunlamps. Use sunscreen and wear protective clothing when outdoors.

Tacrolimus can make you more likely to get infections or may worsen any current infections. Therefore, wash your hands well to prevent the spread of infection. Avoid contact with people who have infections that may spread to others (such as chickenpox, measles, flu). Consult your doctor if you have been exposed to an infection or for more details.

Do not have immunizations/vaccinations without the consent of your doctor. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose).

This drug may increase your potassium levels. Before using potassium supplements or salt substitutes containing potassium, consult your doctor or pharmacist.

Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

Older adults may be more sensitive to the side effects of this drug, especially QT prolongation.

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.

This drug passes into breast milk and the effect on a nursing infant is unknown. Discuss the risks and benefits with your doctor before breast-feeding.

Is it safe during pregnancy or breast-feeding?

There are no adequate studies in women for determining risk when using this Tacrolimus during pregnancy or while breastfeeding. Please always consult with your doctor to weigh the potential benefits and risks before taking Tacrolimus. Tacrolimus is pregnancy risk category C according to the US Food and Drug Administration (FDA).

FDA pregnancy risk category reference below:

  • A=No risk,
  • B=No risk in some studies,
  • C=There may be some risk,
  • D=Positive evidence of risk,
  • X=Contraindicated,
  • N=Unknown

Side effects

What side effects can occur from Tacrolimus?

Shaking, headache, diarrhea, nausea/vomiting, upset stomach, loss of appetite, trouble sleeping, and tingling of the hands/feet may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if you have any serious side effects, including: mental/mood changes, dizziness, signs of kidney problems (such as change in the amount of urine), pounding heartbeat, symptoms of heart failure (such as shortness of breath, swelling ankles/feet, unusual tiredness, unusual/sudden weight gain), hearing problems (such as hearing loss, ringing in the ears), pain/redness/swelling of arms or legs, easy bruising/bleeding, muscle pain/cramp/weakness, yellowing skin/eyes, dark urine, persistent nausea/vomiting, severe stomach/abdominal pain, severe leg pain.

This medication may also increase your risk of getting a rare but very serious (sometimes fatal) brain infection (progressive multifocal leukoencephalopathy-PML). Get medical help right away if any of these rare but very serious side effects occur: clumsiness, loss of coordination, weakness, sudden change in your thinking (such as confusion, difficulty concentrating), difficulty moving your muscles, problems with speech, seizure, vision changes.

Get medical help right away if you have any very serious side effects, including: fainting, fast/irregular heartbeat, severe dizziness, chest/jaw/left arm pain, black stools, vomit that looks like coffee grounds.

This medication may raise your blood pressure. Check your blood pressure regularly and tell your doctor if the results are high. Your doctor may control your blood pressure with medication.

Tacrolimus may cause diabetes. Tell your doctor or pharmacist if you experience any of the following symptoms of high blood sugar: increased thirst/hunger, frequent urination.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

Not everyone experiences these side effects. There may be some side effects not listed above. If you have any concerns about a side-effect, please consult your doctor or pharmacist.

Interactions

What drugs may interact with Tacrolimus?

Some products that may interact with this drug include: aluminum/magnesium antacid, cyclosporine, sirolimus, temsirolimus, ziprasidone, other drugs that may increase the level of potassium in the blood (such as “water pills” including amiloride, spironolactone), other drugs that weaken the immune system/increase the risk of infection (such as natalizumab, rituximab).

Other medications can affect the removal of tacrolimus from your body, which may affect how tacrolimus works. Examples include cimetidine, danazol, nefazodone, ethinyl estradiol, methylprednisolone, St. John’s wort, azole antifungals (such as itraconazole, voriconazole), HIV and HCV protease inhibitors (such as nelfinavir, ritonavir, boceprevir, telaprevir), rifamycins (such as rifampin, rifabutin), certain anti-seizure drugs (such as phenobarbital, phenytoin), among others.

Tacrolimus may interact with other drugs that you are currently taking, which can change how your drug works or increase your risk for serious side effects. To avoid any potential drug interactions, you should keep a list of all the drugs you are using (including prescription drugs, nonprescription drugs and herbal products) and share it with your doctor and pharmacist. For your safety, do not start, stop, or change the dosage of any drugs without your doctor’s approval.

Does food or alcohol interact with Tacrolimus?

Tacrolimus may interact with food or alcohol by altering the way the drug works or increase the risk for serious side effects. Please discuss with your doctor or pharmacist any potential food or alcohol interactions before using this drug.

Avoid eating grapefruit or drinking grapefruit juice while being treated with this medication unless your doctor instructs you otherwise. Grapefruit can increase the amount of certain medications in your bloodstream. Consult your doctor or pharmacist for more details.

What health conditions may interact with Tacrolimus?

Tacrolimus may interact with your health condition. This interaction may worsen your health condition or alter the way the drug works. It is important to always let your doctor and pharmacist know all the health conditions you currently have.

Dosage

The information provided is not a substitute for any medical advice. You should ALWAYS consult with your doctor or pharmacist before using this Tacrolimus.

What is the dose of Tacrolimus for an adult?

Usual Adult Dose for Organ Transplant – Rejection Prophylaxis

KIDNEY TRANSPLANT:

IMMEDIATE RELEASE:

-In combination with azathioprine: Initial dose: 0.1 mg/kg orally every 12 hours. Initiate within 24 hours of surgery, but delay until renal function has recovered.

-In combination with mycophenolate mofetil (MMF)/interleukin-2 (IL-2) receptor antagonist: Initial dose: 0.05 mg/kg orally every 12 hours. Initiate within 24 hours of surgery, but delay until renal function has recovered.

Comments:

-Should be taken consistently either with or without food because the presence and composition of food decreases the bioavailability.

Use: Prophylaxis of organ rejection in patients receiving allogeneic liver, kidney or heart transplants; use concomitantly with adrenal corticosteroids; in kidney and heart transplant, use in conjunction with azathioprine or MMF

EXTENDED RELEASE:

-With Basiliximab Induction, MMF, and Corticosteroids: Initial dose: 0.15 mg/kg/day orally as a single dose. Give first dose prior to or within 48 hours of transplant completion. May delay initiation until renal function has recovered.

-With MMF and Corticosteroids, but Without Basiliximab Induction: Pre-operative dose: 0.1 mg/kg/day orally as a single dose within 12 hours prior to reperfusion; Post-operative dose: 0.2 mg/kg/day orally as a single dose. Give first post-operative dose within 12 hours after reperfusion but not less than 4 hours after the pre-operative dose.

Comments:

-Extended-release capsules are not interchangeable or substitutable with immediate-release capsules.

-Concomitant use with cyclosporine is not recommended.

-If switching from tacrolimus infusion, administer 8 to 12 hours after discontinuing infusion.

Use: Prophylaxis of organ rejection in patients receiving a kidney transplant with MMF and corticosteroids, with or without basiliximab induction

INTRAVENOUS:

-Initial dose: 0.03 to 0.05 mg/kg/day as a continuous IV infusion

Comments:

-Adult patients should receive doses at the lower end of the dosing range.

-IV administration should be reserved only for initiation in patients unable to take oral therapy.

-Convert to oral therapy as soon as it can be tolerated, usually within 2 to 3 days.

Use: Prophylaxis of organ rejection in patients receiving allogeneic liver, kidney or heart transplants; use concomitantly with adrenal corticosteroids; in kidney and heart transplant, use in conjunction with azathioprine or MMF

LIVER TRANSPLANT:

IMMEDIATE RELEASE:

-Initial dose: 0.05 to 0.075 mg/kg orally every 12 hours. Initiate no sooner than 6 hours after surgery.

Comments:

-Should be taken consistently either with or without food because the presence and composition of food decreases the bioavailability.

Use: Prophylaxis of organ rejection in patients receiving allogeneic liver, kidney or heart transplants; use concomitantly with adrenal corticosteroids; in kidney and heart transplant, use in conjunction with azathioprine or MMF

INTRAVENOUS:

-Initial dose: 0.03 to 0.05 mg/kg/day as a continuous IV infusion

Comments:

-Adult patients should receive doses at the lower end of the dosing range.

-IV administration should be reserved only for initiation in patients unable to take oral therapy.

-Convert to oral therapy as soon as it can be tolerated, usually within 2 to 3 days.

Use: Prophylaxis of organ rejection in patients receiving allogeneic liver, kidney or heart transplants; use concomitantly with adrenal corticosteroids; in kidney and heart transplant, use in conjunction with azathioprine or MMF

HEART TRANSPLANT:

IMMEDIATE RELEASE:

-Initial dose: 0.0375 mg/kg orally every 12 hours. Initiate no sooner than 6 hours after surgery

Comments:

-Should be taken consistently either with or without food because the presence and composition of food decreases the bioavailability.

Use: Prophylaxis of organ rejection in patients receiving allogeneic liver, kidney or heart transplants; use concomitantly with adrenal corticosteroids; in kidney and heart transplant, use in conjunction with azathioprine or MMF

INTRAVENOUS:

-Initial dose: 0.01 mg/kg/day as a continuous IV infusion

Comments:

-Adult patients should receive doses at the lower end of the dosing range.

-IV administration should be reserved only for initiation in patients unable to take oral therapy.

-Convert to oral therapy as soon as it can be tolerated, usually within 2 to 3 days.

Use: Prophylaxis of organ rejection in patients receiving allogeneic liver, kidney or heart transplants; use concomitantly with adrenal corticosteroids; in kidney and heart transplant, use in conjunction with azathioprine or MMF

Usual Adult Dose for Graft Versus Host Disease

Some experts recommend:

Prevention:

-Intravenous injection: Initial dose: 0.03 mg/kg/day (based on lean body weight) as a continuous infusion. Initiate at least 24 hours prior to stem cell infusion and continue only until oral medication can be tolerated.

Treatment:

-Intravenous injection: Initial dose: 0.03 mg/kg/day (based on lean body weight) as a continuous infusion.

Comments: To convert from IV to oral (1:4 ratio), multiply total daily IV dose times 4 and administer in 2 divided oral doses per day, every 12 hours.

Renal Dose Adjustments

KIDNEY TRANSPLANT:

IMMEDIATE RELEASE AND INTRAVENOUS:

Patients with post-operative oliguria: Initiate no sooner than 6 hours and within 24 hours of transplantation.

EXTENDED RELEASE:

Patients with post-operative oliguria: Initiate no sooner than 6 hours and within 48 hours of transplantation.

Liver Dose Adjustments

Severe liver impairment (Child-Pugh 10 or greater): May require lower doses

LIVER TRANSPLANT:

Patients experiencing post-transplant hepatic impairment may be associated with an increased risk of developing renal insufficiency related to high blood levels of this drug. Monitor closely and consider dose adjustments.

Dose Adjustments

Concomitant use of cyclosporine: Avoid concomitant use; discontinue tacrolimus or cyclosporine at least 24 hours prior to initiating the other. In the presence of elevated tacrolimus or cyclosporine concentrations, further delay dosing with the other drug.

Other Comments

Administration advice:

-Tacrolimus should not be used simultaneously with cyclosporine. Tacrolimus may be initiated at least 24 hours after stopping cyclosporine; however, dosing should be delayed if cyclosporine blood levels are elevated.

-Dosing should be titrated based on clinical assessments of rejection and tolerability, and to maintain recommended trough concentration ranges.

-Patients should not eat grapefruit or drink grapefruit juice with this drug.

Extended release:

-Should be taken once daily in the morning, preferably on an empty stomach at least 1 hour before or 2 hours after a meal; do not take with an alcoholic beverage; do not chew, divide, or crush.

-Take a missed dose as soon as possible but not more than 14 hours after the scheduled time. Beyond the 14-hour timeframe, the patient should wait until the usual scheduled time the following morning to take the next scheduled dose. Do not take 2 doses at the same time.

Reconstitution/preparation techniques: The manufacturer product information should be consulted.

Monitoring:

-Frequent monitoring of tacrolimus whole blood trough concentrations is recommended; the manufacturer product information should be consulted.

-Whole blood trough concentrations usually range from 5 to 20 ng/mL. Extra caution and closer monitoring are recommended when graft function changes or drug interactions are suspected.

-Monitoring of cyclosporine blood concentrations should be continued post-conversion as tacrolimus may affect the clearance of cyclosporine.

-Renal and liver function and tissue biopsies should be monitored regularly.

-Blood glucose and serum potassium should be monitored.

-Consider obtaining electrocardiograms and monitoring electrolytes periodically in patients at increased risk for QT prolongation.

Patient advice: Since this drug may cause visual and/or neurological disturbances, patients should be cautioned against driving or operating machinery if they are affected.

What is the dose of Tacrolimus for a child?

Usual Pediatric Dose for Organ Transplant – Rejection Reversal

LIVER TRANSPLANT:

IMMEDIATE RELEASE:

-Initial dose: 0.075 to 0.1 mg/kg orally every 12 hours

Comments:

-Should be taken consistently either with or without food because the presence and composition of food decreases the bioavailability.

Use: Prophylaxis of organ rejection in patients receiving allogeneic liver, kidney or heart transplants; use concomitantly with adrenal corticosteroids; in kidney and heart transplant, use in conjunction with azathioprine or mycophenolate mofetil (MMF)

INTRAVENOUS:

-Initial dose: 0.03 to 0.05 mg/kg/day as a continuous IV infusion

Comments:

-Pediatric patients without pre-existing renal or hepatic dysfunction have required and tolerated higher doses than adults to achieve similar blood concentrations.

-IV administration should be reserved only for initiation in patients unable to take oral therapy.

-Convert to oral therapy as soon as it can be tolerated, usually within 2 to 3 days.

Use: Prophylaxis of organ rejection in patients receiving allogeneic liver, kidney or heart transplants; use concomitantly with adrenal corticosteroids; in kidney and heart transplant, use in conjunction with azathioprine or MMF

Usual Pediatric Dose for Graft Versus Host Disease

Some experts recommend:

Prevention:

-Intravenous injection: Initial dose: 0.03 mg/kg/day (based on lean body weight) as continuous infusion. Initiate at least 24 hours prior to stem cell infusion and continue only until oral medication can be tolerated.

Comments: To convert from IV to oral (1:4 ratio), multiply total daily IV dose times 4 and administer in 2 divided oral doses per day, every 12 hours.

Precautions

Safety and efficacy have not been established in patients younger than 16 years for Astagraf XL(R).

How is Tacrolimus available?

Tacrolimus is available in the following dosage forms and strengths:

  • Oral capsule,
  • Oral capsule, extended release,
  • Intravenous solution,
  • Oral tablet, extended release.

What should I do in case of an emergency or overdose?

In case of an emergency or an overdose, call your local emergency services or go to your nearest emergency room.

What should I do if I miss a dose?

If you miss a dose of Tacrolimus, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and take your regular dose as scheduled. Do not take a double dose.

 

Hello Health Group does not provide medical advice, diagnosis or treatment.

Review Date: June 1, 2018 | Last Modified: June 1, 2018

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