Nifedipine with Tacrolimus Interaction Details

Brand Names Associated with Nifedipine

Brand Names Associated with Tacrolimus

Medical Content Editor Dr. Brian Staiger, PharmD
Last updated Nov 20, 2023

Interaction Effect

Increased tacrolimus concentration

Interaction Summary

Tacrolimus is primarily metabolized by the CYP3A hepatic enzyme systems. Coadministration with NIFEdipine has resulted in increased tacrolimus blood levels due to the competitive inhibition of CYP3A-mediated tacrolimus metabolism. If NIFEdipine and tacrolimus are used concurrently, monitor tacrolimus levels and make dose adjustments as appropriate .

Severity

Major

Onset

Delayed

Evidence

Established

How To Manage Interaction

Concomitant administration of NIFEdipine and tacrolimus may increase tacrolimus whole blood trough concentrations and increase the risk of serious adverse reactions (including neurotoxicity or QT prolongation). If these agents are coadministered, monitor tacrolimus levels, making dosage adjustments as necessary.

Mechanism Of Interaction

Inhibition of CYP3A4-mediated tacrolimus metabolism

Literature Reports

A) Concomitant use of tacrolimus and NIFEdipine significantly increased mean trough concentration/dose ratio of tacrolimus in adult transplant patients (N=10) compared with tacrolimus use alone (2.6 vs 1.5) in a prospective study. The mean trough concentration of tacrolimus significantly increased with concomitant use (14.4 vs 12.9 nanograms/mL), despite a significantly lower mean daily dose (7.8 vs 9.5 mg), compared to tacrolimus use alone. In addition, gingival hyperplasia occurred 7 and 16 days after beginning concomitant use of NIFEdipine and tacrolimus in 2 kidney transplant patients. Monitoring of therapeutic immunosuppressant concentrations and dosage reduction should be considered with concomitant use .

B) The possible interaction between NIFEdipine and tacrolimus was evaluated in a retrospective study of 50 liver transplant recipients. Of the 50 patients, 22 were hypertensive patients treated with NIFEdipine; the other 28 did not receive NIFEdipine. All patients also received immunosuppressive therapy with tacrolimus. Data from the two patient groups were obtained from medical records, and consisted of tacrolimus dosages, cumulative dosages, tacrolimus serum concentrations, and cumulative prednisone dosages. Absolute tacrolimus daily dosages in the NIFEdipine group were significantly lower than for the non-NIFEdipine group after 90 days (26.2% lower), 6 months (29.8% lower), and 12 months (38.1% lower) of tacrolimus therapy. The cumulative dosages of tacrolimus were also significantly lower for the NIFEdipine group after 6 months and 12 months of therapy, with a 25.5% and 31.4% lower tacrolimus dose, respectively. Tacrolimus blood concentrations in the NIFEdipine group were 55% higher after 30 days of therapy, with a average concentration of 13.8 nanograms/milliliter (ng/mL; 17.2 nanomol/L) compared to 8.9 ng/mL (11.1 nanomol/L) for the non-NIFEdipine group. Tacrolimus serum concentrations were not significantly different, indicating that dosage adjustments were made to keep tacrolimus concentrations within the therapeutic range. This drug interaction may be related to competitive inhibition of cytochrome P450 isoenzymes involved in the metabolism of tacrolimus by NIFEdipine. Tacrolimus concentrations should be closely monitored, and appropriate dosage adjustments made when NIFEdipine is added to or removed from therapy .

Nifedipine Overview

• Nifedipine is used to treat high blood pressure and to control angina (chest pain). Nifedipine is in a class of medications called calcium-channel blockers. It lowers blood pressure by relaxing the blood vessels so the heart does not have to pump as hard. It controls chest pain by increasing the supply of blood and oxygen to the heart.

• High blood pressure is a common condition and when not treated, can cause damage to the brain, heart, blood vessels, kidneys and other parts of the body. Damage to these organs may cause heart disease, a heart attack, heart failure, stroke, kidney failure, loss of vision, and other problems. In addition to taking medication, making lifestyle changes will also help to control your blood pressure. These changes include eating a diet that is low in fat and salt, maintaining a healthy weight, exercising at least 30 minutes most days, not smoking, and using alcohol in moderation.

Tacrolimus Overview

• Tacrolimus (Astagraf XL, Envarsus XR, Prograf) is used along with other medications to prevent rejection (attack of a transplanted organ by the immune system of a person receiving the organ) in people who have received a kidney transplant. Tacrolimus (Prograf) is also used along with other medications to prevent rejection in people who have received a liver, lung, or heart transplant. Tacrolimus is in a class of medications called immunosupressants. It works by decreasing the activity of the immune system to prevent it from attacking the transplanted organ.

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Definitions

Severity Categories

Contraindicated

These drugs, generally, should not be used together simultaneously due to the high risk of severe adverse effects. Combining these medications can lead to dangerous health outcomes and should be strictly avoided unless otherwise instructed by your provider.

Major

This interaction could result in very serious and potentially life-threatening consequences. If you are taking this drug combination, it is very important to be under close medical supervision to minimize severe side effects and ensure your safety. It may be necessary to change a medication or dosage to prevent harm.

Moderate

This interaction has the potential to worsen your medical condition or alter the effectiveness of your treatment. It's important that you are monitored closely and you potentially may need to make adjustments in your treatment plan or drug dosage to maintain optimal health.

Minor

While this interaction is unlikely to cause significant problems, it could intensify side effects or reduce the effectiveness of one or both medications. Monitoring for changes in symptoms and your condition is recommended, and adjustments may be made if needed to manage any increased or more pronounced side effects.

Onset

Rapid: Onset of drug interaction typically occurs within 24 hours of co-administration.

Delayed: Onset of drug interaction typically occurs more than 24 hours after co-administration.

Evidence

Level of documentation of the interaction.

Established: The interaction is documented and substantiated in peer-reviewed medical literature.

Theoretical: This interaction is not fully supported by current medical evidence or well-documented sources, but it is based on known drug mechanisms, drug effects, and other relevant information.

How To Manage The Interaction

Provides a detailed discussion on how patients and clinicians can approach the identified drug interaction as well as offers guidance on what to expect and strategies to potentially mitigate the effects of the interaction. This may include recommendations on adjusting medication dosages, altering the timing of drug administration, or closely monitoring for specific symptoms.

It's important to note that all medical situations are unique, and management approaches should be tailored to individual circumstances. Patients should always consult their healthcare provider for personalized advice and guidance on managing drug interactions effectively.

Mechanism Of Interaction

The theorized or clinically determined reason (i.e., mechanism) why the drug-drug interaction occurs.

Disclaimer: The information provided on this page is for informational purposes only and should not be considered medical advice. Always consult with a qualified healthcare professional regarding your specific circumstances and medical conditions.

Where Does Our Information Come From?

Information for our drug interactions is compiled from several drug compendia, including:

• Gold Standard Drug Database
• Micromedex
• Lexicomp
• DrugBank

The prescribing information for each drug, as published on DailyMED, is also used. 

Individual drug-drug interaction detail pages contain references specific to that interaction. You can click on the reference number within brackets '[]' to see what reference was utilized.

The information posted is fact-checked by HelloPharmacist clinicians and reviewed quarterly.