Tacrolimus and Nicardipine: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Tacrolimus
Nicardipine
How we grade severity & evidence
Severity levels
- Contraindicated: These should generally not be used together.
- Major: Potentially serious — often needs a change or close monitoring.
- Moderate: Can be significant — usually manageable with monitoring.
- Minor: Usually limited clinical impact.
Evidence grades
- Established: Well documented — supported by controlled studies or strong clinical data.
- Probable: Good supporting evidence, though not definitively proven.
- Suspected: Some evidence suggests this interaction, but it is not well established.
- Possible: Limited or conflicting evidence; the interaction may occur.
- Theoretical: Predicted from the drugs' pharmacology; not yet confirmed in people.
Ratings come from the documented interaction literature and are reviewed by a pharmacist. They describe the documented risk of the combination, not what will necessarily happen to you — your dose, timing, and health picture all matter.
What happens
Increased tacrolimus exposure and an increased risk of toxicity
Interaction Deep Dive
Concomitant administration of oral or IV niCARdipine1 and tacrolimus may result in inhibition of CYP3A-mediated tacrolimus metabolism by niCARdipine, thereby increasing tacrolimus whole blood concentrations and the risk of serious adverse events such as neurotoxicity or QT prolongation 2. Concomitant administration of niCARdipine and tacrolimus in CYP3A5 non-expressors resulted in rapidly increased tacrolimus exposure within 36 to 48 hours in an observational study 4. If these agents are coadministered, frequently monitor tacrolimus whole blood concentrations, and reduce dosage as needed. Monitor for adverse effects including changes in renal function and QT prolongation 23.
Why it happens (mechanism)
Inhibition of CYP3A-mediated tacrolimus metabolism
Literature reports
1 report — tap to read
a) Tacrolimus is primarily metabolized by CYP3A4 and CYP3A5. NiCARdipine has been shown to inhibit CYP3A4 metabolism and therefore may cause excessive tacrolimus exposure in patients not genetically expressing CYP3A5. During an observational study, 12 patients identified as receiving continuous IV niCARdipine. Of these 12 patients, 8 were identified as homozygous CYP3A5 non-expressors and 4 were homozygous CYP3A5 expressors. Concomitant administration of niCARdipine and tacrolimus in CYP3A5 non-expressors resulted in rapidly increased tacrolimus exposure within 36 to 48 hours. Median 12-hours tacrolimus trough levels (maxC0) was 24.3 ng/mL in patients not expressing CYP3A5 compared with 13.9 ng/mL in patients expressing CYP3A5 and 14.6 ng/mL for patients not receiving niCARdipine. Dose adjusted MaxC0 was also significantly higher in CYP3A5 non-expressors compared with all other patients 4.
Common questions
Can I take Tacrolimus and Nicardipine together?
Increased tacrolimus exposure and an increased risk of toxicity Always confirm with your pharmacist or prescriber before making any change.
How serious is the Tacrolimus and Nicardipine interaction?
It is rated major. Potentially serious — often needs a change or close monitoring.
How quickly could this interaction happen?
The documented onset is "delayed". Effects tend to build up gradually over days to weeks.
How strong is the evidence for this interaction?
The evidence is graded "theoretical". Predicted from the drugs' pharmacology; not yet confirmed in people.
Questions for your pharmacist
- Does my dose of Tacrolimus or Nicardipine need adjusting while I take them together?
- What symptoms should prompt me to call you or my prescriber right away?
- Does the timing of my doses matter for this combination?
- Is there a safer alternative to one of these medications for me?
References (4)
- Product Information: CARDENE(R) oral capsules, nicardipine HCl oral capsules. Roche Laboratories Inc. (per FDA), Nutley, NJ, 2016. DailyMed
- Product Information: ENVARSUS XR(R) oral extended-release tablets, tacrolimus oral extended-release tablets. Veloxis Pharmaceuticals Inc (per FDA), Cary, NC, 2023. DailyMed
- Product Information: PROGRAF(R) oral capsules, oral granules for suspension, intravenous injection, tacrolimus oral capsules, oral granules for suspension, intravenous injection. Astellas Pharma US Inc (per FDA), Northbrook, IL, 2023. DailyMed
- Hooper DK, Fukuda T, Gardiner R, et al: Risk of tacrolimus toxicity in CYP3A5 nonexpressors treated with intravenous nicardipine after kidney transplantation. Transplantation 2012; 93(8):806-812. PubMed
Keep reading about Tacrolimus
Keep reading about Nicardipine
These medications also interact with supplements
Prescription drugs aren't the whole picture — herbal and dietary supplements can interact with them too. From the evidence-graded Natural Medicines database:
major · moderate · minor — check everything you take with our drug–supplement interaction checker.
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