Methylprednisolone with Diltiazem Interaction Details

Brand Names Associated with Methylprednisolone

Brand Names Associated with Diltiazem

Medical Content Editor Dr. Brian Staiger, PharmD
Last updated Dec 03, 2023

Interaction Effect

Increased methylPREDNISolone plasma concentrations and enhanced adrenal-suppressant effects

Interaction Summary

The coadministration of diltiazem 60 mg three times daily for three days and a single dose of methylPREDNISolone 16 mg resulted in a 2.6-fold increase in the methylPREDNISolone area under the concentration-time curve (AUC) and a 1.6-fold increase in the maximum concentration (Cmax). Additionally, the morning plasma cortisol concentration was only 12% of that during the placebo phase, indicating enhanced adrenal-suppressant effects of methylPREDNISolone during diltiazem treatment. Diltiazem is a potent inhibitor of cytochrome P450 3A4 (CYP3A4), and methylPREDNISolone relies on this pathway for its metabolism.

Severity

Moderate

Onset

Rapid

Evidence

Probable

How To Manage Interaction

The dose of methylPREDNISolone may need to be reduced in patients receiving long-term methylPREDNISolone therapy and diltiazem if steroid-related adverse effects become apparent or increase.

Mechanism Of Interaction

Inhibition of cytochrome P450 3A4-mediated methylPREDNISolone metabolism

Literature Reports

A) Nine subjects completed a randomized, double-blind, placebo-controlled, crossover study to examine the effects of diltiazem and mibefradil on the pharmacokinetics of and adrenal suppression from a single dose of oral methylPREDNISolone. Study participants received diltiazem 60 mg three times daily, mibefradil 50 mg once daily, or placebo three times daily for three days. MethylPREDNISolone was given on the morning of day 3. Diltiazem increased the area under the concentration-time curve (AUC) of methylPREDNISolone from 483 ng/h/mL to 1227 ng/h/mL and also increased the maximum concentration (Cmax) from 118 ng/mL to 183 ng/mL (315 to 489 nanomol/L). The nighttime exposure to methylPREDNISolone (AUC (12-23)) was increased 28.2-fold (from 6.2 ng/h/mL to 99 ng/h/mL). The morning plasma cortisol concentration, measured 23 hours after ingestion of methylPREDNISolone, was 22 ng/mL as compared to 186 ng/mL during the placebo phase. Caution should be exercised if methylPREDNISolone is administered long-term to a patient also receiving diltiazem .

Methylprednisolone Overview

• Methylprednisolone, a corticosteroid, is similar to a natural hormone produced by your adrenal glands. It is often used to replace this chemical when your body does not make enough of it. It relieves inflammation (swelling, heat, redness, and pain) and is used to treat certain forms of arthritis; skin, blood, kidney, eye, thyroid, and intestinal disorders (e.g., colitis); severe allergies; and asthma. Methylprednisolone is also used to treat certain types of cancer.

• This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information.

Diltiazem Overview

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

• High blood pressure is a common condition, and when not treated it 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.

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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.