Selective 5-HT1A receptor partial agonist
Partial agonist at serotonin 5-HT1A receptors, modulating serotonergic neurotransmission with minimal activity at other receptors.
Major depressive disorder (MDD)
Various anxiety disorders, hypoactive sexual desire disorder (HSDD)
Oral extended-release tablets (18.2 mg)
18.2 mg p.o. daily; increase to 36.3 mg/day on day 4, 54.5 mg/day on day 7, up to 72.6 mg/day by day 14 based on response and tolerability
18.2–72.6 mg/day
Half-life approximately 12 hours; metabolized primarily via CYP3A4
Dizziness, nausea, headache, somnolence
Serotonin syndrome (when combined with other serotonergic agents)
Monitor for serotonergic effects and tolerability, especially when combined with other serotonergic drugs
Increased risk of suicidal thoughts and behaviors in children, adolescents, and young adults with MDD
Gepirone lacks the sedating, anticholinergic, and sexual side effects commonly seen with selective serotonin reuptake inhibitors (SSRIs) and serotonin-norepinephrine reuptake inhibitors (SNRIs). It is not associated with withdrawal symptoms or abuse potential, making it potentially preferable in patients sensitive to serotonergic or activating agents.