II. Indications
III. Contraindications
- QTc Prolongation (>450 msec)
- Severe hepatic Impairment (Child Pugh C)
V. Medications
- Gepirone ER (Exxua)
- Extended-release tablets: 18.2 mg, 36.3 mg, 54.5 mg and 72.6 mg
VI. Dosing: Adults
- Standard Adult Protocol
- Start Gepirone ER 18.2 mg orally daily with food
- Titration schedule as needed
- Day 4: May increase to 36.3 mg
- Day 7: May increase to 54.5 mg
- Day 14: May increase to 72.6 mg
- Lower Dose Adult Protocol
- Indications
- Elderly
- Renal Impairment (eGFR <50 ml/min)
- Moderate hepatic Impairment (Child Pugh B)
- Protocol
- Start Gepirone ER 18.2 mg orally daily
- May increase up to 36.3 mg orally daily after 7 days
- Indications
VII. Adverse Effects
- Suicidality in pediatric patients (FDA black box warning)
-
QTc Prolongation
- More than other Antidepressants
- Obtain Electrocardiogram (EKG) before use
-
Serotonin Syndrome
- Avoid in combination with other serotinergic medications
- Other reported adverse effects
VIII. Safety
- Unknown safety in Lactation
- Avoid in pregnancy
- Third trimester
- Associated with persistent Pulmonary Hypertension
- Neonatal
- Poor adaptation (respiratory distress, Temperature instability, feeding difficulty, hypotonia, irritability)
- Third trimester
IX. Drug Interactions
-
MAO Inhibitors
- Avoid within 14 days of Gepirone
-
Drugs That Prolong the QTc Interval
- Avoid in combination with Gepirone
- Strong CYP3A4 inhibitor and inducers
- Avoid in combination with Gepirone
X. Efficacy
- Developed 1986 and rejected by the FDA 3 times in 20 years (2002, 2004, 2007) up to its approval in 2023
- Studies showed low efficacy compared to Placebo
- Approved based on short-term studies (8 weeks)
- No proven efficacy in children (and carries the same Suicidality black box warning as other Antidepressants)
XI. Resources
XII. References
- (2024) Presc Lett 31(5): 25