Tacrolimus

Prescription ·Exploratory record · not publication-reviewed ·Updated July 13, 2026

Tacrolimus is a calcineurin inhibitor used to prevent rejection after kidney, liver, heart, lung, and other organ transplants depending on formulation and protocol. It has a narrow therapeutic index and major risks including nephrotoxicity, neurotoxicity, hyperkalemia, hypomagnesemia, hypertension, diabetes, QT concerns, serious infections, malignancy, and strong CYP3A4/P-glycoprotein interactions.

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Publication status

Exploratory record, not a reviewed medical publication.

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This generated database record has not completed a claim-level review by a qualified human medical reviewer. Bibliography links and evidence labels are not approval. The page remains available for reference and is excluded from search indexing.

In short

What the research says.

A quick, data-only summary. The full evidence, dosing, and sources are below.

Tacrolimus is a calcineurin inhibitor used to prevent rejection after kidney, liver, heart, lung, and other organ transplants depending on formulation and protocol. NutriStack rates the supporting evidence as strong. Common adult dosing is Systemic transplant dosing is individualized by organ, formulation, genotype, interacting drugs, and target trough concentration. Immediate-release capsules are commonly divided every 12 hours; extended-release products are not interchangeable milligram-for-milligram without specialist direction., though a prescriber sets the actual dose. With long-term use it can deplete magnesium. This profile indexes 3 sources.

What it's good for

Prevention of organ transplant rejection^2,1
Core immunosuppressive therapy in kidney, liver, heart, and lung transplant protocols^1,2
Treatment of selected refractory autoimmune conditions off-label
Topical formulation use for inflammatory skin disease, separate from systemic transplant dosing

What to watch for

Nephrotoxicity
Tremor
Headache
Known hypersensitivity to tacrolimus or formulation components^2,3
Use only under clinicians experienced with immunosuppression and therapeutic drug monitoring²

The bottom line

Evidence rating strong. Most-documented uses: prevention of organ transplant rejection, core immunosuppressive therapy in kidney, liver, heart, and lung transplant protocols, treatment of selected refractory autoimmune conditions off-label. 3 sources indexed (1995–2026), with 0 interaction records on file.

The science

How it works, mechanistically.

Core mechanism

Tacrolimus binds FKBP-12 to form a complex that inhibits calcineurin, preventing NFAT activation and interleukin-2 transcription in T cells. This suppresses T-cell activation and transplant rejection. CYP3A4/5 and P-glycoprotein determine much of its exposure, while renal vasoconstriction and tubular effects produce nephrotoxicity and electrolyte abnormalities.^2,3

Class

Calcineurin inhibitor immunosuppressant

Absorption

Fat-soluble; take with food

Dosing

Dosing & protocol.

Common range

Systemic transplant dosing is individualized by organ, formulation, genotype, interacting drugs, and target trough concentration. Immediate-release capsules are commonly divided every 12 hours; extended-release products are not interchangeable milligram-for-milligram without specialist direction.

Recommended form

Exact prescribed tacrolimus formulation with trough-guided monitoring; do not interchange immediate-release and extended-release products without specialist supervision

Take consistently with regard to food and time of day. Avoid grapefruit products and notify the transplant team before starting or stopping supplements.

Depletions

What it depletes.

Nutrients this medication can lower over time, and what to replace.

Magnesium

Significant

Tacrolimus can cause renal magnesium wasting and clinically significant hypomagnesemia.

Replace Magnesium GlycinateMonitor Serum magnesiumOnset Days to months after initiation, especially post-transplant

Full Tacrolimus depletion and interaction guide →

Safety

Full safety detail.

Side effects

Nephrotoxicity
Tremor
Headache
Seizures or posterior reversible encephalopathy syndrome rarely
Hyperkalemia
Hypomagnesemia
Hypertension
New-onset diabetes after transplant
QT prolongation risk
Serious infections
Lymphoma and skin cancers
Gastrointestinal upset

Contraindications

Known hypersensitivity to tacrolimus or formulation components^2,3
Use only under clinicians experienced with immunosuppression and therapeutic drug monitoring²
Avoid unsupervised formulation switches
Use caution with kidney dysfunction, hyperkalemia, QT risk, infection, malignancy risk, and interacting CYP3A4/P-gp drugs or supplements^1,3

Sources

Sources, by evidence tier.

Numbered references. Citations throughout the page link here.

Reviews & position papers

1KDIGO Clinical Practice Guideline for the Care of Kidney Transplant RecipientsKidney Disease: Improving Global Outcomes · American Journal of Transplantation · 2009
Guideline supports therapeutic monitoring and surveillance for nephrotoxicity, electrolytes, infection, and malignancy.
2Tacrolimus in solid organ transplantationVenkataramanan R et al. · Clinical Pharmacokinetics · 1995
Review describes pharmacokinetics, monitoring, and adverse effects.

Reference material

3Tacrolimus Capsules US Prescribing InformationURLU.S. National Library of Medicine · DailyMed · 2026
Labeling describes boxed warning, therapeutic drug monitoring, nephrotoxicity, hyperkalemia, infections, malignancies, and CYP3A interactions.

FAQ

Common questions.

Quick answers about Tacrolimus, drawn from the data on this page.

What is Tacrolimus?

What is Tacrolimus used for?

Commonly cited benefits of Tacrolimus include: Prevention of organ transplant rejection; Core immunosuppressive therapy in kidney, liver, heart, and lung transplant protocols; Treatment of selected refractory autoimmune conditions off-label; Topical formulation use for inflammatory skin disease, separate from systemic transplant dosing. NutriStack rates the overall evidence as strong.

What is a typical dose of Tacrolimus?

A typical adult dose of Tacrolimus is Systemic transplant dosing is individualized by organ, formulation, genotype, interacting drugs, and target trough concentration. Immediate-release capsules are commonly divided every 12 hours; extended-release products are not interchangeable milligram-for-milligram without specialist direction.. The commonly recommended form is Exact prescribed tacrolimus formulation with trough-guided monitoring; do not interchange immediate-release and extended-release products without specialist supervision. These are general ranges, not personalized advice; confirm the right dose with a clinician.

What are the side effects of Tacrolimus?

Reported side effects include nephrotoxicity, tremor, headache, seizures or posterior reversible encephalopathy syndrome rarely, hyperkalemia, hypomagnesemia. This is educational information; check with a healthcare professional before use.

How strong is the evidence for Tacrolimus?

NutriStack rates this as Strong, meaning multiple high-quality meta-analyses or systematic reviews converge on the same finding. Full tier criteria are at https://nutristackapp.com/methodology/evidence-tiers.

Use this with your stack

Tacrolimus in NutriStack.

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