gepirone (Exxua)
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Indications
- treatment of major depression in adult
Contraindications
- QTc interval > 450 msec
- concurrent strong CYP3A4 inhibitors
- severe hepatic impairmment
- concurrent use of MAOI inhibitor (within 14 days)
* lack of sufficient data on pregnancy & lactation
Dosage
- start 18.2 mg PO QD with food
- may increase to 36.3 mg on day 4 if tolerated; day 7 geriatric/renal dosing
- may increase to 54.5 mg on day 7
- may increase to 72.6 mg after additional week
Dosage adjustment in renal failure
* same as geriatric dosing
Pharmacokinetics
- absolute bioavailability: 14-17%
- maximum plasma concentration reached after 6 hours (3 hours after high fat meal)
- volume of distribution: 94.5 liters
- protein binding: 72%
- mean terminal 1/2life: 5 hours
- metabolized by CYP3A4 to 3-OH gepirone & gepirone 1-pyrophosphate, both present in plasma at higher concentrations than the parent compound
Monitor
- correct electrolytes & obtain ECG prior to initiation of
- ECGs during titration & periodically thereafter
Adverse effects
- prolongation of QR interval
- activation of mania/hypomania in patients with bipolar affective disorder
Drug interactions
- serotonin syndrome when used concurrently with other serotonergic agents
- 36.3 mg dose of gepirone reduces plasma levels of glyburide by 20%
- > 5%
- drug interaction(s) of benzodiazepines with antidepressants
- drug interaction(s) of antidepressants with benzodiazepines
- drug interaction(s) of NSAIDs with antidepressants
More general terms
References
- ↑ U.S. Food & Drug Administration (FDA) https://www.accessdata.fda.gov/drugsatfda_docs/appletter/2023/021164Orig1s000ltr.pdf
- ↑ Medscape: gepirone (Rx) https://reference.medscape.com/drug/exxua-gepirone-1000091
- ↑ HIGHLIGHTS OF PRESCRIBING INFORMATION EXXUA (gepirone) extended-release tablets, for oral use https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/021164s000lbl.pdf