Buspirone and grapefruit

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Interaction Between Buspirone and Grapefruit Juice

Introduction to Buspirone and Grapefruit Juice Interaction

Buspirone is a medication commonly used to treat anxiety disorders. It is metabolized in the liver primarily by the enzyme cytochrome P450 3A4 (CYP3A4). Grapefruit juice is known to inhibit CYP3A4, which can lead to increased levels of drugs metabolized by this enzyme in the bloodstream, potentially causing adverse effects.

Mechanism of Interaction: CYP3A4 Inhibition

Grapefruit juice inhibits the activity of intestinal CYP3A4, which increases the maximum plasma concentration (Cmax) and the area under the plasma concentration-time curve (AUC) of oral CYP3A4 substrates, including buspirone . This inhibition can lead to higher levels of buspirone in the blood, increasing the risk of side effects.

Clinical Evidence of Interaction

Studies have shown that grapefruit juice significantly increases the AUC of buspirone. In one study, the geometric mean ratio (GMR) of the AUC of buspirone with grapefruit juice compared to water was 2.12, indicating more than a twofold increase in buspirone levels when taken with grapefruit juice . This suggests a significant interaction that could enhance the effects and side effects of buspirone.

Case Reports and Adverse Effects

There are documented cases where individuals consuming large amounts of buspirone along with grapefruit juice experienced significant side effects. One such case involved a person who developed a state of altered consciousness, including frequent occurrences of a twilight state, while taking high doses of buspirone with grapefruit juice . This highlights the potential for serious adverse effects when these substances are combined.

Comparison with Other Juices

Interestingly, not all fruit juices have the same effect. For example, blueberry juice (BBJ) was studied for its potential to inhibit CYP3A4 and CYP2C9. While BBJ did inhibit these enzymes in vitro, its effect in clinical settings was not significant. The GMR for buspirone with BBJ was 1.39, which was not statistically significant, indicating that BBJ does not have the same level of interaction with buspirone as grapefruit juice .

Conclusion

The interaction between buspirone and grapefruit juice is clinically significant due to the inhibition of CYP3A4 by grapefruit juice, leading to increased levels of buspirone in the bloodstream and a higher risk of adverse effects. Patients taking buspirone should be advised to avoid grapefruit juice to prevent potential side effects. Other fruit juices, such as blueberry juice, do not appear to have the same level of interaction and may be safer alternatives.

Sources and full results

Most relevant research papers on this topic

Effect of blueberry juice on clearance of buspirone and flurbiprofen in human volunteers.

Blueberry juice has no significant effect on the clearance of buspirone or flurbiprofen, and there is no evidence of clinically important drug interactions with CYP3A or CYP2C9.

In Vitro StudyVery Rigorous Journal

2013·

17citations

·M. Hanley et al.

How Long Does Grapefruit Juice Inhibit CYP3A4

Grapefruit juice inhibits intestinal CYP3A4 activity for up to 12 hours, increasing the maximum plasma concentration and area under the plasma concentration-time curve of oral CYP3A4 substrates.

2000·

0citations

·S. Dubovsky

Buspirone an Example of Generalized Social Anxiety Disorder that Caused a State of Consciousness Change During Taking Large Quantities

Taking large quantities of buspirone can cause a change in consciousness, causing frequent twilight states from dreamy states.

Preprint

2018·

0citations

·Toshiro Takami

Grapefruit-Drug Interactions

Grapefruit juice and products can interact with certain drugs, increasing their bioavailability and potentially impacting their clinical significance.

Highly Cited

2010·

137citations

·K. Seden et al.

Buspirone in the treatment of alcoholic patients.

Buspirone may reduce alcohol cravings and improve psychopathology in patients with mild to moderate alcohol abuse, warranting further evaluation in this area.

RCTHighly Cited

1989·

129citations

·Francesco Bruno

Grapefruit juice-drug interactions.

Grapefruit juice can increase oral drug bioavailability by reducing presystemic metabolism, potentially impacting medications with low oral bioavailability.

Highly Cited

1998·

774citations

·D. Bailey et al.

Drug-grapefruit juice interactions.

Grapefruit juice can increase the serum concentrations of various medications, leading to increased dose-dependent adverse effects.

Highly Cited

2000·

219citations

·Garvan C. Kane et al.

Drug Interactions with Grapefruit Juice

Grapefruit juice can significantly increase the oral bioavailability of certain drugs, potentially altering their action, and its effects should be evaluated on an individual drug basis.

In Vitro StudyHighly Cited

1997·

352citations

·B. Ameer et al.

Drug Interactions with Grapefruit Juice

Grapefruit juice can increase drug concentrations, potentially affecting drug effects or tolerability, and should be avoided when taking extensively metabolized drugs.

Highly Cited

1998·

172citations

·U. Fuhr

A combined therapeutic regimen of buspirone and environmental enrichment is more efficacious than either alone in enhancing spatial learning in brain-injured pediatric rats.

A combined treatment of buspirone and environmental enrichment is more effective than either therapy alone in enhancing spatial learning and reducing lesion size in brain-injured pediatric rats.

RCTAnimal StudyVery Rigorous Journal

2014·

40citations

·Christina M. Monaco et al.

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