PsychRounds: The Psychiatry Podcast The Anxiolytics: Buspirone (Buspar)
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Jul 2, 2025 Dive into the world of buspirone, a medication used to tackle anxiety, and uncover its rich history and recent FDA approval of jepirone for depression. Learn about the unique pharmacodynamics of buspirone, including its partial agonist function and impressive safety profile. The conversation delves into off-label uses, such as aiding in movement disorders and addressing antidepressant-related sexual dysfunction. Plus, discover how buspirone combines with new treatments like jepirone to enhance outcomes for those battling depression.
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Buspirone's Development History
- Buspirone was initially developed as an antipsychotic at very high doses but failed those trials.
- It was repurposed and FDA approved in 1986 as an anxiolytic for generalized anxiety disorder at much lower doses.
Buspirone's Mechanism of Action
- Buspirone acts as a weak partial agonist at presynaptic dopamine-2, 3, and 4 receptors, but this isn’t linked to its anxiolytic effect.
- It also partially agonizes alpha-1 adrenergic receptors, likely causing dizziness.
Buspirone's Side Effect Profile
- Buspirone is very well tolerated with mild side effects like dizziness and GI distress only slightly more than placebo.
- It does not cause sedation, weight gain, anticholinergic effects, or QTc prolongation, making it safer than many anxiolytics.