Gepirone
Gepirone (brand name EXXUA) is an antidepressant medication used to treat major depressive disorder in adults. It works by selectively targeting serotonin 5-HT1A receptors in the brain to modulate serotonergic activity. Unlike many other antidepressants, it is not a serotonin reuptake inhibitor but rather a selective agonist at the 5-HT1A receptor.
Gepirone is an antidepressant that treats depression by acting on serotonin receptors in the brain.
This medication carries a boxed (black box) warning — the strongest type of FDA warning. Review the full prescribing information before use.
Key facts at a glance
- ATC
- N06AX19
- RxNorm
- 2672253
- Generic
- Gepirone
- Class
- atc-n06
- Brands
- Exxua
- Availability
- rx
- Lactation
- unknown
- Routes
- oral
- Forms
- tablet
- Regions
- US, EU, CN, JP
- Monitoring
- —
This page is for informational purposes only.
Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Dosage and administration
- Usual dose
- 500mg twice daily
- Maximum
- consult physician
- Frequency
- every 12 hours
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 250mg twice daily
- Maximum
- consult physician
- Frequency
- every 12 hours
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 400mg daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
Overdose information
Special Populations
9 groupspregnancy
first trimesteravoid if possible
avoid use during pregnancy unless benefits outweigh risks
regular fetal monitoring
Use with caution and monitor for adverse effects.
pregnancy
third trimesteravoid if possible
avoid use near term unless benefits outweigh risks
fetal monitoring and assessment of newborn
Use with caution and monitor for adverse effects.
lactation
breastfeedingavoid
not recommended during breastfeeding due to unknown excretion in breast milk
monitor infant for sedation or feeding changes
geriatric
elderlyreduce dose
start with lowest effective dose and titrate slowly; monitor for sedation and dizziness
regular assessment of blood pressure and sedation
Use with caution and monitor for adverse effects.
pediatric_age
children adolescentsnot recommended
not approved for use in patients under 18 years due to lack of safety and efficacy data
not applicable
Use of this medication in this population requires careful consideration of risks and benefits.
renal_impairment
moderate renal impairmentreduce dose
use with caution; consider dose reduction in patients with creatinine clearance 30-50 mL/min
monitor renal function and adjust dose accordingly
Use with caution and monitor for adverse effects.
renal_impairment
severe renal impairmentavoid or significantly reduce dose
not recommended in patients with creatinine clearance less than 30 mL/min
closely monitor renal function and for adverse effects
Use with caution and monitor for adverse effects.
hepatic_impairment
moderate hepatic impairmentreduce dose
use with caution; may require dose reduction in moderate impairment
monitor liver function tests and for sedation
Use with caution and monitor for adverse effects.
hepatic_impairment
severe hepatic impairmentavoid
not recommended in severe hepatic impairment due to limited data
monitor closely if use is necessary
Use with caution and monitor for adverse effects.
Statistics and clinical data
FDA approval year
FDA approval for Exxua (gepirone ER) for major depressive disorder
Drug class
Pharmacological classification
Common uses
Therapeutic indications
Mechanism of action
Pharmacodynamic properties
Gepirone is indicated for the treatment of major depressive disorder (MDD) in adult patients. It is prescribed when depressive symptoms significantly impact daily functioning and quality of life.
Gepirone exerts its antidepressant effects primarily through selective agonist activity at serotonin 5-HT1A receptors. By activating these receptors, it modulates serotonergic neurotransmission in the central nervous system. The exact pathway through which this produces antidepressant effects is not yet fully understood.
As with other antidepressants, gepirone may take several weeks to produce full therapeutic effects. Patients should be monitored for worsening depression or suicidal thoughts, particularly when starting treatment. The medication should not be discontinued abruptly. Common side effects may include nausea, dizziness, and headache. Patients should inform their healthcare provider of all medications and supplements they are taking to avoid potential interactions.
Contraindications
Conditions and patient states where this medication should be avoided or used with caution.
Do not use (1)
Known allergy to this medication or its components
Use caution (1)
Consult healthcare provider for benefits vs risks assessment
Official drug label
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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed July 26, 2026. · Read our editorial policy