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Buspirone and Grapefruit Juice

North Dakota State University · FDA-approved active Small molecule

Buspirone acts as a serotonin 5-HT1A receptor partial agonist, while grapefruit juice inhibits CYP3A4 metabolism, increasing buspirone bioavailability and plasma concentrations.

Buspirone acts as a serotonin 5-HT1A receptor partial agonist, while grapefruit juice inhibits CYP3A4 metabolism, increasing buspirone bioavailability and plasma concentrations. Used for Generalized anxiety disorder (buspirone monotherapy), Drug-drug interaction study / pharmacokinetic investigation (buspirone + grapefruit juice combination).

At a glance

Generic nameBuspirone and Grapefruit Juice
SponsorNorth Dakota State University
Drug classSerotonin 5-HT1A receptor partial agonist (buspirone component)
Target5-HT1A receptor (buspirone); CYP3A4 enzyme (grapefruit juice inhibition)
ModalitySmall molecule
Therapeutic areaPsychiatry / Neurology
PhaseFDA-approved

Mechanism of action

Buspirone is an anxiolytic that binds to and partially activates serotonin 5-HT1A receptors in the brain, reducing anxiety symptoms. Grapefruit juice contains furanocoumarins that irreversibly inhibit intestinal and hepatic CYP3A4 enzyme, significantly reducing first-pass metabolism of buspirone and elevating its systemic exposure. This interaction is clinically relevant as it can increase buspirone levels and potentially enhance both therapeutic and adverse effects.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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