Buspirone (Buspar)

Class

Azapirone anxiolytic

Mechanism

Partial agonist at serotonin 5-HT1A receptors, modulating serotonergic neurotransmission; minimal effects on GABA receptors, contributing to anxiolytic effects without sedation or dependence.

FDA-Approved Use

Generalized anxiety disorder (GAD)

Off-Label Use

Social anxiety disorder (SoAD), augmentation for depression (major depressive disorder [MDD]), agitation and aggression in neurodevelopmental disabilities (sometimes with risperidone)

Formulation

Oral tablets (5 mg, 7.5 mg, 10 mg, 15 mg, 30 mg)

Titration

5–10 mg p.o. twice daily, titrating as clinically appropriate

Dose Range

15–60 mg/day divided doses

Kinetics

Half-life ~2–3 hours; metabolized by CYP3A4; steady state in ~1 week

Common AEs

Dizziness, headache, nausea, nervousness, lightheadedness, restlessness

Serious/Rare AEs

Rare hypersensitivity reactions; no significant risk of sedation or dependence

Monitoring

Monitor clinical response over weeks; assess for anxiety symptom improvement and tolerability

Black Box Warning

None

Considerations

Buspirone has minimal risk of dependence or withdrawal and lacks sedative or muscle-relaxant properties. It requires regular dosing and several weeks to reach full effect. May be helpful for agitation and anxiety in patients with intellectual disability, though evidence is limited. It is generally safe and effective in patients with seizure disorders as it does not lower seizure threshold. Dose adjustments may be necessary in hepatic or renal impairment.