General MedicinePrescription OnlyPregnancy Cat. Not classifiedFDA Yes
Tacrolimus
TACROLIMUS EXTENDED-RELEASE CAPSULES
1 INDICATIONS AND USAGE Tacrolimus extended-release capsules is indicated for the prophylaxis of organ rejection in kidney transplant patients in combination with other immunosuppressants in adult patients who can swallow capsules intact [see Clinical Studies ( 14.1 ), ( 14.2 )] . Pediatric use information is approved for Astellas Pharma US, Inc.'s ASTAGRAF XL (tacrolimus extended-release capsules). However, due to Astellas Pharma US, Inc.'s marketing exclusivity rights, this drug product is not...
Medically reviewed by MedCentralHub Medical Review Board, Licensed Pharmacists & Physicians ·
Brand names:tacrolimus
Quick Reference
Medicine ClassGeneral Medicine
FDA ApprovedYes
PregnancyCategory Not classified
Quick Facts
- Active ingredient
- TACROLIMUS EXTENDED-RELEASE CAPSULES
- Medicine class
- General Medicine
- Brand names
- tacrolimus
- Availability
- Prescription only (Rx)
- Pregnancy category
- Not classified
- Half-life
- half-life
- FDA approved
- Yes
What Is Tacrolimus?
1 INDICATIONS AND USAGE Tacrolimus extended-release capsules is indicated for the prophylaxis of organ rejection in kidney transplant patients in combination with other immunosuppressants in adult patients who can swallow capsules intact [see Clinical Studies ( 14.1 ), ( 14.2 )] . Pediatric use information is approved for Astellas Pharma US, Inc.'s ASTAGRAF XL (tacrolimus extended-release capsules). However, due to Astellas Pharma US, Inc.'s marketing exclusivity rights, this drug product is not...
Tacrolimus (TACROLIMUS EXTENDED-RELEASE CAPSULES) belongs to the General Medicine class of medications. It was first approved by the FDA in Yes. This medication requires a prescription from a licensed healthcare provider.
Key Safety Information
- •Always follow the dose recommended by your healthcare professional. Taking more than prescribed increases the risk of side effects including serious complications.
- •Seek emergency care if you experience signs of an allergic reaction — hives, swelling, difficulty breathing, or rash. Stop the medication and call your doctor immediately.
- •Some medications can increase the risk of cardiovascular events. Tell your doctor if you have high blood pressure, a history of heart attack or stroke, or any pre-existing health condition.
- •Avoid or limit alcohol while taking Tacrolimus. Do not drink alcohol without first discussing it with your healthcare provider as it may increase adverse effects.
- •Take Tacrolimus with food or a full glass of water if stomach upset occurs. Stop use and talk to your doctor if you experience persistent stomach pain or GI symptoms.
- •Tell your doctor about all medications, supplements, and vitamins you take. Some combinations significantly increase the risk of harm.
This is a summary only. Always read the full prescribing information and consult your healthcare provider for personalized medical advice.
Uses & Indications
Tacrolimus is prescribed for the following conditions. Some uses are FDA-approved indications; others may be evidence-based off-label uses. Consult your healthcare provider for personalized guidance.
1 INDICATIONS AND USAGE Tacrolimus extended-release capsules is indicated for the prophylaxis of organ rejection in kidney transplant patients in combination with other immunosuppressants in adult patients who can swallow capsules intact [see Clinical Studies ( 14.1 ), ( 14.2 )] .
Pediatric use information is approved for Astellas Pharma US, Inc.'s ASTAGRAF XL (tacrolimus extended-release capsules).
However, due to Astellas Pharma US, Inc.'s marketing exclusivity rights, this drug product is not labeled with that information.
Tacrolimus extended-release capsules is a calcineurin-inhibitor immunosuppressant indicated for the prophylaxis of organ rejection in kidney transplant patients in combination with other immunosuppressants in adult patients who can swallow capsules intact.
( 1 , 14.1 , 14.2 )
Dosage Guide
The following are general dosing guidelines only. Your actual dose should be determined by your healthcare provider based on your condition, renal/hepatic function, and other medications.
AD
Adult Dosage
2 DOSAGE AND ADMINISTRATION Capsules must be taken whole. ( 2.1 ) Take consistently every morning at the same time on an empty stomach at least 1 hour before a meal or at least 2 hours after a meal. ( 2.1 ) Avoid eating grapefruit or drinking grapefruit juice or alcohol. ( 2.1 ) African-American patients and patients with severe hepatic impairment may require dosing adjustments. ( 2.3 ) Frequent monitoring of trough concentrations is recommended. ( 2.4 ) For complete dosing information, see Full Prescribing Information. MMF = Mycophenolate mofetil Recommended Tacrolimus Extended-Release Capsules Initial Dosage Patient Population Initial Oral Dosage Whole Blood Trough Concentration Range ADULT With basiliximab, MMF and steroids 0.15 mg/kg to 0.2 mg/kg once daily prior to reperfusion or within 48 hours of completion of transplant Month 1: 7 ng/mL to 15 ng/mL Month 2 to Month 6: 5 ng/mL to 15 ng/mL More than 6 Months: 5 ng/mL to 10 ng/mL With MMF and steroids, without basiliximab inductio
Available Forms
Available Strengths
Side Effects
Common
- 6 ADVERSE REACTIONS The following clinically significant adverse drug reactions are discussed in greater detail in other sections of labeling: Lymphoma and Other Malignancies [see Warnings and Precautions ( 5.1 )] Serious Infections [see Warnings and Precautions ( 5.2 )] Increased Mortality in Female Liver Transplant Patients [see Warnings and Precautions ( 5.3 )] New Onset Diabetes after Transplant [see Warnings and Precautions ( 5.5 )] Nephrotoxicity due to Tacrolimus Extended-Release Capsules and Drug Interactions [see Warnings and Precautions ( 5.6 )] Neurotoxicity [see Warnings and Precautions ( 5.7 )] Hyperkalemia [see Warnings and Precautions ( 5.8 )] Hypertension [see Warnings and Precautions ( 5.9 )] QT Prolongation [see Warnings and Precautions ( 5.11 )] Pure Red Cell Aplasia [see Warnings and Precautions ( 5.13 )] Thrombotic Microangiopathy, Including Hemolytic Uremic Syndrome and Thrombotic Thrombocytopenic Purpura [see Warnings and Precautions (5.14) ] The most common adverse reactions (≥ 30%) are: diarrhea, constipation, nausea, peripheral edema, tremor and anemia.
- ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact eVenus Pharmaceutical Laboratories, Inc.
- at 1-609-395-8625 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
- 6.1 Clinical Studies Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
- In addition, the clinical trials were not designed to establish comparative differences across study arms with regards to the adverse reactions discussed below.
- Kidney transplant patients were treated with tacrolimus extended-release capsules (N=214) or tacrolimus immediate-release product (N=212) and concomitant immunosuppressants (median duration of exposure of 12 months) in a randomized, open-label, active-controlled trial of mostly U.S.
- patients (Study 1) [see Clinical Studies ( 14.1 )] .
Serious
- 5 WARNINGS AND PRECAUTIONS Not Interchangeable with Other Tacrolimus Products-Medication Errors: Instruct patients or caregivers to recognize the appearance of tacrolimus extended-release capsules.
- ( 5.4 ) New onset diabetes after transplant: Monitor blood glucose.
- ( 5.5 ) Nephrotoxicity (acute and/or chronic): May occur due to tacrolimus extended-release capsules, drug interactions, concomitant nephrotoxic drugs.
- Monitor renal function;
- consider dosage reduction.
Rare
Medicine Interactions
Always inform your healthcare provider and pharmacist about ALL medications you take, including prescriptions, OTC medicines, vitamins, and supplements.
MajorModerateMinor
Warnings & Contraindications
5 WARNINGS AND PRECAUTIONS Not Interchangeable with Other Tacrolimus Products-Medication Errors: Instruct patients or caregivers to recognize the appearance of tacrolimus extended-release capsules. ( 5.4 ) New onset diabetes after transplant: Monitor blood glucose. ( 5.5 ) Nephrotoxicity (acute and/or chronic): May occur due to tacrolimus extended-release capsules, drug interactions, concomitant n
How Tacrolimus Works
12.1 Mechanism of Action Tacrolimus binds to an intracellular protein, FKBP-12. A complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin (a ubiquitous mammalian intracellular enzyme) is then formed and the phosphatase activity of calcineurin is inhibited. Such inhibition prevents the dephosphorylation and translocation of various factors such as the nuclear factor of activated T-cells (NF-AT), and nuclear factor kappa-light-chain-enhancer of activated B-cells (NF-κB). Tacrolimus inhibits the expression and/or production of several cytokines that include interleukin (IL)-1 beta, IL‑2, IL-3, IL-4, IL-5, IL-6, IL-8, IL-10, gamma interferon, tumor necrosis factor-alpha, and granulocyte macrophage colony-stimulating factor. Tacrolimus also inhibits IL-2 receptor expression and nitr
Pharmacokinetics
Absorption
Absorption In healthy subjects, the administration of escalating tacrolimus extended-release capsules doses ranging from 1
Half-Life
half-life
Metabolism
Metabolism The desired pharmacological activity of tacrolimus is primarily due to the parent drug
Excretion
Excretion In a mass balance study of orally-administered radiolabeled tacrolimus to 6 healthy subjects, the mean recovery of the radiolabel was 94
Pregnancy & Breastfeeding Safety
Not classified
Breastfeeding
Many medications pass into breast milk in varying amounts. Before using Tacrolimuswhile breastfeeding, discuss the benefits and risks with your healthcare provider or pharmacist — they can weigh your dose, your infant's age, and available lactation safety data to find the safest option for you and your baby.
Storage & Handling
Store at room temperature. Keep away from moisture and heat. Keep out of reach of children.
Frequently Asked Questions
Related on MedCentralHub
- Class hub
General Medicine alternatives
Compare all General Medicine medications — uses, side effects, and cost differences
- Detail
Tacrolimus dosage guide
Adult, pediatric, renal, and hepatic dosing for Tacrolimus
- Detail
Tacrolimus side effects
Complete adverse effect profile including common, serious, and rare reactions
Sources & References
- • FDA Prescribing Information — Official labeling and package insert for Tacrolimus
- • U.S. National Library of Medicine — MedlinePlus drug information
- • American Hospital Formulary Service (AHFS) — Clinical pharmacology monograph
- • PubMed / MEDLINE — View clinical studies
Last reviewed by MedCentralHub Medical Review Board · MedCentralHub Editorial Policy
Medical Disclaimer
The information on this page is for educational purposes only and is not intended as medical advice, diagnosis, or treatment. Always consult your doctor, pharmacist, or qualified healthcare provider before starting, stopping, or changing any medication.