Diltiazem with Buspirone Interaction Details

Brand Names Associated with Diltiazem

Brand Names Associated with Buspirone

Medical Content Editor Dr. Brian Staiger, PharmD
Last updated Mar 06, 2024

Interaction Effect

An increased risk of enhanced busPIRone effects

Interaction Summary

Diltiazem has been shown to increase the area under the concentration-time curve (AUC) and the maximum concentration (Cmax) of busPIRone by 5.5-fold (range 3.3-fold to 7.4-fold) and 4.1-fold, respectively. Because the elimination half-life of busPIRone was not altered by the presence of diltiazem, it can be assumed that this interaction is a result of inhibition of the cytochrome P450 3A4-mediated first-pass metabolism of busPIRone in the gut wall and liver[1].

Severity

Moderate

Onset

Rapid

Evidence

Probable

How To Manage Interaction

Monitor patients who are receiving diltiazem and busPIRone for enhanced sedative effects of busPIRone. Low doses of busPIRone should be employed.

Mechanism Of Interaction

Inhibition of cytochrome P450 3A4-mediated first-pass metabolism of busPIRone

Literature Reports

A) Nine healthy volunteers participated in a randomized, placebo-controlled, three-phase crossover study to investigate possible interactions of busPIRone with verapamil and diltiazem. Subjects received verapamil 80 mg, diltiazem 60 mg, or placebo orally three times daily for five doses, with busPIRone 10 mg being administered orally following the fifth dose. During the placebo phase, the maximum concentration (Cmax) and area under the concentration-time curve (AUC) of busPIRone was 2.6 ng/mL (6.7 nanomoles/L (nmol/L)) and 6.9 ng/mL/hr, respectively. In the presence of diltiazem, the Cmax was 10.3 ng/mL (26.7 nmol/L) and the AUC was 36.8 ng/mL/hr. The elimination half-life and the time to Cmax (tmax) were not significantly altered by diltiazem. While this pharmacokinetic interaction was associated with only a minor impairment of psychomotor performance, an increased frequency of side effects of busPIRone was seen in the diltiazem phase [1].

References

1 ) Lamberg TS, Kivisto KT, & Neuvonen PJ: Effects of verapamil and diltiazem on the pharmacokinetics and pharmacodynamics of buspirone. Clin Pharmacol Ther 1998; 63:640-645.

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.

Buspirone Overview

• Buspirone is used to treat anxiety disorders or in the short-term treatment of symptoms of anxiety. Buspirone is in a class of medications called anxiolytics. It works by changing the amounts of certain natural substances in the brain.

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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.