Dosing & Uses
Dosage Forms & Strengths
extended-release tablettablet
- 18.2mg
- 36.3mg
- 54.5mg
- 72.6mg
Major Depressive Disorder
Indicated for treatment of major depressive disorder (MDD)
Initial: 18.2 mg PO qDay
Based on clinical response and tolerability
- May increase to 36.3 mg qDay on Day 4
- Further titrate to 54.5 mg qDay after Day 7
- Then, 72.6 mg qDay after an additional week; maximum recommended daily dosage 72.6 mg qDay
Dosage Modifications
Coadministration of CYP3A4 Inhibitors
- Moderate CYP3A4 inhibitors: Reduce gepirone dose by 50%
- Strong CYP3A4 inhibitors: Contraindicated
Switching to or from a monoamine oxidase inhibitor (MAOI) antidepressant
- At least 14 days must elapse between discontinuation of an MAOI and initiating gepirone
- Allow at least 14 days after stopping gepirone before starting an MAOI antidepressant
Renal impairment
- CrCl ≥50 mL/min: No dosage adjustment necessary
- CrCl <50 mL/min: Start at 18.2 mg qDay; may increase to maximum recommended dosage of 36.3 mg qDay after Day 7 based on clinical response and tolerability
Hepatic impairment
- Mild (Child-Pugh A): No dosage adjustment necessary
- Moderate (Child-Pugh B): Start at 18.2 mg qDay; may increase to maximum recommended dosage of 36.3 mg qDay after Day 7 based on clinical response and tolerability
- Severe (Child-Pugh C): Contraindicated
Dosing Considerations
Screen for a personal or family history of bipolar disorder, mania, or hypomania before initiating treatment
Advise patients to inform healthcare provider if taking, or plan to take, any prescription or over-the-counter medications due to an increased risk for drug interactions with this medication
Electrolyte abnormalities and electrocardiogram (ECG)
- Correct electrolyte abnormalities before initiating for patients with electrolyte abnormalities, or who are receiving diuretics or glucocorticoids, or who have a history of hypokalemia or hypomagnesemia
- Monitor electrolytes during dose titration and periodically during treatment
- Perform an ECG before initiating, during dosage titration, and periodically during treatment
- Do not initiate if QTc is >450 msec at baseline
-
Monitor ECGs more frequently if used with:
- Drugs known to prolong the QT interval
- Patients who develop QTc ≥450 msec during treatment
- Patients with a significant risk of developing torsade de pointes
- Do not escalate dosage if QTcF is 450 msec
Safety and efficacy not established
Major Depressive Disorder
Indicated for treatment of major depressive disorder (MDD)
Initial: 18.2 mg PO qDay
Aged >65 years: Based on clinical response and tolerability, may increase dosage to maximum recommended dosage of 36.3 mg qDay after Day 7
Interactions
Interaction Checker
No Results
Contraindicated
Serious
Significant - Monitor Closely
Minor
Contraindicated (31)
- atazanavir
atazanavir will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- chlorambucil
chlorambucil will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- clarithromycin
clarithromycin will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- cobicistat
cobicistat will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- conivaptan
conivaptan will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- darunavir
darunavir will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
elvitegravir/cobicistat/emtricitabine/tenofovir DF will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- grapefruit
grapefruit will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- idelalisib
idelalisib will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- isocarboxazid
isocarboxazid and gepirone both increase serotonin levels. Contraindicated. Gepirone is contraindicated in patients taking monoamine oxidase inhibitors (MAOIs), including linezolid or IV methylene blue or in patients who have taken MAOIs within the preceding 14 days. Allow at least 14 days after stopping gepirone before starting an MAOI.
- itraconazole
itraconazole will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- ketoconazole
ketoconazole will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- levoketoconazole
levoketoconazole will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- lonafarnib
lonafarnib will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- lopinavir
lopinavir will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- mifepristone
mifepristone will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- nefazodone
nefazodone will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- nelfinavir
nelfinavir will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- nirmatrelvir/ritonavir
nirmatrelvir/ritonavir will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- phenelzine
phenelzine and gepirone both increase serotonin levels. Contraindicated. Gepirone is contraindicated in patients taking monoamine oxidase inhibitors (MAOIs), including linezolid or IV methylene blue or in patients who have taken MAOIs within the preceding 14 days. Allow at least 14 days after stopping gepirone before starting an MAOI.
- posaconazole
posaconazole will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- rasagiline
rasagiline and gepirone both increase serotonin levels. Contraindicated. Gepirone is contraindicated in patients taking monoamine oxidase inhibitors (MAOIs), including linezolid or IV methylene blue or in patients who have taken MAOIs within the preceding 14 days. Allow at least 14 days after stopping gepirone before starting an MAOI.
- ritonavir
ritonavir will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- rucaparib
rucaparib will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- safinamide
safinamide and gepirone both increase serotonin levels. Contraindicated. Gepirone is contraindicated in patients taking monoamine oxidase inhibitors (MAOIs), including linezolid or IV methylene blue or in patients who have taken MAOIs within the preceding 14 days. Allow at least 14 days after stopping gepirone before starting an MAOI.
- selegiline
selegiline and gepirone both increase serotonin levels. Contraindicated. Gepirone is contraindicated in patients taking monoamine oxidase inhibitors (MAOIs), including linezolid or IV methylene blue or in patients who have taken MAOIs within the preceding 14 days. Allow at least 14 days after stopping gepirone before starting an MAOI.
- selegiline transdermal
selegiline transdermal and gepirone both increase serotonin levels. Contraindicated. Gepirone is contraindicated in patients taking monoamine oxidase inhibitors (MAOIs), including linezolid or IV methylene blue or in patients who have taken MAOIs within the preceding 14 days. Allow at least 14 days after stopping gepirone before starting an MAOI.
- stiripentol
stiripentol will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- tranylcypromine
tranylcypromine and gepirone both increase serotonin levels. Contraindicated. Gepirone is contraindicated in patients taking monoamine oxidase inhibitors (MAOIs), including linezolid or IV methylene blue or in patients who have taken MAOIs within the preceding 14 days. Allow at least 14 days after stopping gepirone before starting an MAOI.
- tucatinib
tucatinib will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- voriconazole
voriconazole will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
Serious (13)
- apalutamide
apalutamide will decrease the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- carbamazepine
carbamazepine will decrease the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- enzalutamide
enzalutamide will decrease the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- fosphenytoin
fosphenytoin will decrease the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- linezolid
linezolid and gepirone both increase serotonin levels. Contraindicated. Gepirone is contraindicated in patients taking monoamine oxidase inhibitors (MAOIs), including linezolid or IV methylene blue or in patients who have taken MAOIs within the preceding 14 days. Allow at least 14 days after stopping gepirone before starting an MAOI.
- lumacaftor/ivacaftor
lumacaftor/ivacaftor will decrease the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- mitotane
mitotane will decrease the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- olopatadine intranasal
gepirone and olopatadine intranasal both increase sedation. Avoid or Use Alternate Drug. Coadministration increases risk of CNS depression, which can lead to additive impairment of psychomotor performance and cause daytime impairment.
- phenytoin
phenytoin will decrease the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- primidone
primidone will decrease the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rifampin
rifampin will decrease the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- St John's Wort
St John's Wort will decrease the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- zuranolone
gepirone, zuranolone. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration of zuranolone with other CNS depressants may increase impairment of psychomotor performance or CNS depressant effects. If unavoidable, consider dose reduction. .
Monitor Closely (196)
- adagrasib
adagrasib will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
gepirone and adagrasib both increase QTc interval. Modify Therapy/Monitor Closely. - alfuzosin
gepirone and alfuzosin both increase QTc interval. Modify Therapy/Monitor Closely.
- almotriptan
gepirone and almotriptan both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- amiodarone
amiodarone will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
gepirone and amiodarone both increase QTc interval. Modify Therapy/Monitor Closely. - amitriptyline
gepirone and amitriptyline both increase QTc interval. Modify Therapy/Monitor Closely.
gepirone and amitriptyline both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug. - amoxapine
gepirone and amoxapine both increase QTc interval. Modify Therapy/Monitor Closely.
- amphetamine
gepirone and amphetamine both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- apomorphine
gepirone and apomorphine both increase QTc interval. Modify Therapy/Monitor Closely.
- aprepitant
aprepitant will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- arsenic trioxide
gepirone and arsenic trioxide both increase QTc interval. Modify Therapy/Monitor Closely.
- artemether/lumefantrine
gepirone and artemether/lumefantrine both increase QTc interval. Modify Therapy/Monitor Closely.
- asenapine
gepirone and asenapine both increase QTc interval. Modify Therapy/Monitor Closely.
- azithromycin
gepirone and azithromycin both increase QTc interval. Modify Therapy/Monitor Closely.
- bedaquiline
gepirone and bedaquiline both increase QTc interval. Modify Therapy/Monitor Closely.
- bicalutamide
bicalutamide will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- bupropion
gepirone and bupropion both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- buspirone
gepirone and buspirone both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- ceritinib
ceritinib will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- chlorpromazine
gepirone and chlorpromazine both increase QTc interval. Modify Therapy/Monitor Closely.
- ciprofloxacin
gepirone and ciprofloxacin both increase QTc interval. Modify Therapy/Monitor Closely.
- citalopram
gepirone and citalopram both increase QTc interval. Modify Therapy/Monitor Closely.
gepirone and citalopram both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug. - clarithromycin
gepirone and clarithromycin both increase QTc interval. Modify Therapy/Monitor Closely.
- clofazimine
gepirone and clofazimine both increase QTc interval. Modify Therapy/Monitor Closely.
- clomipramine
gepirone and clomipramine both increase QTc interval. Modify Therapy/Monitor Closely.
gepirone and clomipramine both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug. - clotrimazole
clotrimazole will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- clozapine
gepirone and clozapine both increase QTc interval. Modify Therapy/Monitor Closely.
- cocaine topical
gepirone and cocaine topical both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- crizotinib
crizotinib will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
gepirone and crizotinib both increase QTc interval. Modify Therapy/Monitor Closely. - cyclobenzaprine
gepirone and cyclobenzaprine both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- cyclosporine
cyclosporine will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- daridorexant
gepirone and daridorexant both increase sedation. Modify Therapy/Monitor Closely. Coadministration increases risk of CNS depression, which can lead to additive impairment of psychomotor performance and cause daytime impairment.
- dasatinib
gepirone and dasatinib both increase QTc interval. Modify Therapy/Monitor Closely.
- degarelix
gepirone and degarelix both increase QTc interval. Modify Therapy/Monitor Closely.
- desipramine
gepirone and desipramine both increase QTc interval. Modify Therapy/Monitor Closely.
gepirone and desipramine both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug. - desvenlafaxine
gepirone and desvenlafaxine both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- deutetrabenazine
gepirone and deutetrabenazine both increase QTc interval. Modify Therapy/Monitor Closely.
- dextroamphetamine
gepirone and dextroamphetamine both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- dextroamphetamine transdermal
gepirone and dextroamphetamine transdermal both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- dextromethorphan
gepirone and dextromethorphan both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- diazepam buccal
diazepam buccal, gepirone. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration may potentiate the CNS-depressant effects of each drug.
- diazepam intranasal
diazepam intranasal, gepirone. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration may potentiate the CNS-depressant effects of each drug.
- difelikefalin
difelikefalin and gepirone both increase sedation. Use Caution/Monitor.
- diltiazem
diltiazem will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- disopyramide
gepirone and disopyramide both increase QTc interval. Modify Therapy/Monitor Closely.
- dofetilide
gepirone and dofetilide both increase QTc interval. Modify Therapy/Monitor Closely.
- dolasetron
gepirone and dolasetron both increase QTc interval. Modify Therapy/Monitor Closely.
- doxepin
gepirone and doxepin both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- dronedarone
dronedarone will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
gepirone and dronedarone both increase QTc interval. Modify Therapy/Monitor Closely. - droperidol
gepirone and droperidol both increase QTc interval. Modify Therapy/Monitor Closely.
- duloxetine
gepirone and duloxetine both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- eletriptan
gepirone and eletriptan both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- encorafenib
encorafenib will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
gepirone and encorafenib both increase QTc interval. Modify Therapy/Monitor Closely. - entacapone
entacapone will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- entrectinib
gepirone and entrectinib both increase QTc interval. Modify Therapy/Monitor Closely.
- eribulin
gepirone and eribulin both increase QTc interval. Modify Therapy/Monitor Closely.
- erythromycin base
erythromycin base will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
gepirone and erythromycin base both increase QTc interval. Modify Therapy/Monitor Closely. - erythromycin ethylsuccinate
erythromycin ethylsuccinate will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
gepirone and erythromycin ethylsuccinate both increase QTc interval. Modify Therapy/Monitor Closely. - erythromycin lactobionate
erythromycin lactobionate will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
gepirone and erythromycin lactobionate both increase QTc interval. Modify Therapy/Monitor Closely. - erythromycin stearate
erythromycin stearate will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
gepirone and erythromycin stearate both increase QTc interval. Modify Therapy/Monitor Closely. - escitalopram
gepirone and escitalopram both increase QTc interval. Modify Therapy/Monitor Closely.
gepirone and escitalopram both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug. - ezogabine
gepirone and ezogabine both increase QTc interval. Modify Therapy/Monitor Closely.
- fedratinib
fedratinib will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- fenfluramine
fenfluramine, gepirone. Either increases effects of the other by serotonin levels. Use Caution/Monitor. Coadministration with drugs that increase serotoninergic effects may increase the risk of serotonin syndrome.
- fexinidazole
fexinidazole will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- flecainide
gepirone and flecainide both increase QTc interval. Modify Therapy/Monitor Closely.
- fluconazole
fluconazole will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
gepirone and fluconazole both increase QTc interval. Modify Therapy/Monitor Closely. - fluoxetine
gepirone and fluoxetine both increase QTc interval. Modify Therapy/Monitor Closely.
gepirone and fluoxetine both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug. - fluphenazine
gepirone and fluphenazine both increase QTc interval. Modify Therapy/Monitor Closely.
- fluvoxamine
fluvoxamine will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
gepirone and fluvoxamine both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug. - formoterol
gepirone and formoterol both increase QTc interval. Modify Therapy/Monitor Closely.
- fosamprenavir
fosamprenavir will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
gepirone and fosamprenavir both increase QTc interval. Modify Therapy/Monitor Closely. - fosaprepitant
fosaprepitant will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- foscarnet
gepirone and foscarnet both increase QTc interval. Modify Therapy/Monitor Closely.
- fostamatinib
fostamatinib will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- frovatriptan
gepirone and frovatriptan both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- gabapentin
gabapentin, gepirone. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of CNS depressants can result in serious, life-threatening, and fatal respiratory depression. Use lowest dose possible and monitor for respiratory depression and sedation.
- gabapentin enacarbil
gabapentin enacarbil, gepirone. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of CNS depressants can result in serious, life-threatening, and fatal respiratory depression. Use lowest dose possible and monitor for respiratory depression and sedation.
- ganaxolone
gepirone and ganaxolone both increase sedation. Use Caution/Monitor.
- gemifloxacin
gepirone and gemifloxacin both increase QTc interval. Modify Therapy/Monitor Closely.
- gemtuzumab
gepirone and gemtuzumab both increase QTc interval. Modify Therapy/Monitor Closely.
- givinostat
gepirone and givinostat both increase QTc interval. Use Caution/Monitor. If coadministered, obtain ECGs when initiating, during concomitant use, and as clinically indicated. Withhold if QTc interval >500 ms or a change from baseline >60 ms.
- glasdegib
gepirone and glasdegib both increase QTc interval. Modify Therapy/Monitor Closely.
- haloperidol
haloperidol will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
gepirone and haloperidol both increase QTc interval. Modify Therapy/Monitor Closely. - hydroxychloroquine sulfate
gepirone and hydroxychloroquine sulfate both increase QTc interval. Modify Therapy/Monitor Closely.
- ibrexafungerp
ibrexafungerp will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- ibutilide
gepirone and ibutilide both increase QTc interval. Modify Therapy/Monitor Closely.
- iloperidone
iloperidone will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
gepirone and iloperidone both increase QTc interval. Modify Therapy/Monitor Closely. - imatinib
imatinib will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- imipramine
gepirone and imipramine both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- indacaterol, inhaled
gepirone and indacaterol, inhaled both increase QTc interval. Modify Therapy/Monitor Closely.
- indapamide
gepirone and indapamide both increase QTc interval. Modify Therapy/Monitor Closely.
- inotuzumab
gepirone and inotuzumab both increase QTc interval. Modify Therapy/Monitor Closely.
- isavuconazonium sulfate
isavuconazonium sulfate will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- isocarboxazid
gepirone and isocarboxazid both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- isoniazid
isoniazid will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
gepirone and isoniazid both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug. - isradipine
gepirone and isradipine both increase QTc interval. Modify Therapy/Monitor Closely.
- ivacaftor
ivacaftor will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- L-tryptophan
gepirone and L-tryptophan both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- lapatinib
gepirone and lapatinib both increase QTc interval. Modify Therapy/Monitor Closely.
- lasmiditan
lasmiditan, gepirone. Either increases effects of the other by sedation. Use Caution/Monitor. Coadministration of lasmiditan and other CNS depressant drugs, including alcohol have not been evaluated in clinical studies. Lasmiditan may cause sedation, as well as other cognitive and/or neuropsychiatric adverse reactions.
- lefamulin
gepirone and lefamulin both increase QTc interval. Modify Therapy/Monitor Closely.
- lenacapavir
lenacapavir will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- letermovir
letermovir will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- levofloxacin
gepirone and levofloxacin both increase QTc interval. Modify Therapy/Monitor Closely.
- linezolid
gepirone and linezolid both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- lisdexamfetamine
gepirone and lisdexamfetamine both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- lithium
gepirone and lithium both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- lofexidine
gepirone and lofexidine both increase QTc interval. Modify Therapy/Monitor Closely.
- lopinavir
gepirone and lopinavir both increase QTc interval. Modify Therapy/Monitor Closely.
- lorcaserin
gepirone and lorcaserin both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- lumefantrine
gepirone and lumefantrine both increase QTc interval. Modify Therapy/Monitor Closely.
- maprotiline
gepirone and maprotiline both increase QTc interval. Modify Therapy/Monitor Closely.
gepirone and maprotiline both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug. - mefloquine
gepirone and mefloquine both increase QTc interval. Modify Therapy/Monitor Closely.
- meperidine
gepirone and meperidine both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- methadone
gepirone and methadone both increase QTc interval. Modify Therapy/Monitor Closely.
- methamphetamine
gepirone and methamphetamine both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- metronidazole
metronidazole will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- mifepristone
gepirone and mifepristone both increase QTc interval. Modify Therapy/Monitor Closely.
- milnacipran
gepirone and milnacipran both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- mirtazapine
gepirone and mirtazapine both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- moxifloxacin
gepirone and moxifloxacin both increase QTc interval. Modify Therapy/Monitor Closely.
- naratriptan
gepirone and naratriptan both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- nefazodone
gepirone and nefazodone both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- netupitant/palonosetron
netupitant/palonosetron will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- nilotinib
gepirone and nilotinib both increase QTc interval. Modify Therapy/Monitor Closely.
- nortriptyline
gepirone and nortriptyline both increase QTc interval. Modify Therapy/Monitor Closely.
gepirone and nortriptyline both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug. - octreotide
gepirone and octreotide both increase QTc interval. Modify Therapy/Monitor Closely.
- ofloxacin
gepirone and ofloxacin both increase QTc interval. Modify Therapy/Monitor Closely.
- olanzapine
gepirone and olanzapine both increase QTc interval. Modify Therapy/Monitor Closely.
- olanzapine/samidorphan
gepirone, olanzapine/samidorphan. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration of diazepam, alcohol, or other CNS acting drugs may potentiate orthostatic hypotension observed with olanzapine. Additive sedation may also occur.
- ondansetron
gepirone and ondansetron both increase QTc interval. Modify Therapy/Monitor Closely.
- osilodrostat
gepirone and osilodrostat both increase QTc interval. Modify Therapy/Monitor Closely.
- osimertinib
gepirone and osimertinib both increase QTc interval. Modify Therapy/Monitor Closely.
- ozanimod
gepirone and ozanimod both increase QTc interval. Modify Therapy/Monitor Closely.
- paliperidone
gepirone and paliperidone both increase QTc interval. Modify Therapy/Monitor Closely.
- panobinostat
gepirone and panobinostat both increase QTc interval. Modify Therapy/Monitor Closely.
- paroxetine
gepirone and paroxetine both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- pasireotide
gepirone and pasireotide both increase QTc interval. Modify Therapy/Monitor Closely.
- pazopanib
gepirone and pazopanib both increase QTc interval. Modify Therapy/Monitor Closely.
- pentamidine
gepirone and pentamidine both increase QTc interval. Modify Therapy/Monitor Closely.
- perphenazine
gepirone and perphenazine both increase QTc interval. Modify Therapy/Monitor Closely.
gepirone and perphenazine both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug. - phenelzine
gepirone and phenelzine both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- pimavanserin
gepirone and pimavanserin both increase QTc interval. Modify Therapy/Monitor Closely.
- pimozide
gepirone and pimozide both increase QTc interval. Modify Therapy/Monitor Closely.
- pitolisant
gepirone and pitolisant both increase QTc interval. Modify Therapy/Monitor Closely.
- ponesimod
gepirone and ponesimod both increase QTc interval. Modify Therapy/Monitor Closely.
- posaconazole
gepirone and posaconazole both increase QTc interval. Modify Therapy/Monitor Closely.
- pregabalin
pregabalin, gepirone. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of CNS depressants can result in serious, life-threatening, and fatal respiratory depression. Use lowest dose possible and monitor for respiratory depression and sedation.
- procainamide
gepirone and procainamide both increase QTc interval. Modify Therapy/Monitor Closely.
- protriptyline
gepirone and protriptyline both increase QTc interval. Modify Therapy/Monitor Closely.
gepirone and protriptyline both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug. - quetiapine
gepirone and quetiapine both increase QTc interval. Modify Therapy/Monitor Closely.
- quinidine
gepirone and quinidine both increase QTc interval. Modify Therapy/Monitor Closely.
- quinine
gepirone and quinine both increase QTc interval. Modify Therapy/Monitor Closely.
- quinupristin/dalfopristin
quinupristin/dalfopristin will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- quizartinib
gepirone and quizartinib both increase QTc interval. Modify Therapy/Monitor Closely.
- ranolazine
gepirone and ranolazine both increase QTc interval. Modify Therapy/Monitor Closely.
- rasagiline
gepirone and rasagiline both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- remimazolam
remimazolam, gepirone. Either increases toxicity of the other by sedation. Modify Therapy/Monitor Closely. Coadministration may result in profound sedation, respiratory depression, coma, and/or death. Continuously monitor vital signs during sedation and recovery period if coadministered. Carefully titrate remimazolam dose if administered with opioid analgesics and/or sedative/hypnotics.
- ribociclib
ribociclib will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
gepirone and ribociclib both increase QTc interval. Modify Therapy/Monitor Closely. - rilpivirine
gepirone and rilpivirine both increase QTc interval. Modify Therapy/Monitor Closely.
- risperidone
gepirone and risperidone both increase QTc interval. Modify Therapy/Monitor Closely.
- ritlecitinib
ritlecitinib will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- rizatriptan
gepirone and rizatriptan both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- safinamide
gepirone and safinamide both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- schisandra
schisandra will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- selegiline
gepirone and selegiline both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- selpercatinib
gepirone and selpercatinib both increase QTc interval. Modify Therapy/Monitor Closely.
- sertraline
sertraline will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
gepirone and sertraline both increase QTc interval. Modify Therapy/Monitor Closely.
gepirone and sertraline both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug. - solifenacin
gepirone and solifenacin both increase QTc interval. Modify Therapy/Monitor Closely.
- sorafenib
gepirone and sorafenib both increase QTc interval. Modify Therapy/Monitor Closely.
- sotalol
gepirone and sotalol both increase QTc interval. Modify Therapy/Monitor Closely.
- St John's Wort
gepirone and St John's Wort both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- sumatriptan
gepirone and sumatriptan both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- sunitinib
gepirone and sunitinib both increase QTc interval. Modify Therapy/Monitor Closely.
- tacrolimus
gepirone and tacrolimus both increase QTc interval. Modify Therapy/Monitor Closely.
- telavancin
gepirone and telavancin both increase QTc interval. Modify Therapy/Monitor Closely.
- tetrabenazine
gepirone and tetrabenazine both increase QTc interval. Modify Therapy/Monitor Closely.
- tetracycline
tetracycline will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- thioridazine
gepirone and thioridazine both increase QTc interval. Modify Therapy/Monitor Closely.
- thiotepa
gepirone and thiotepa both increase QTc interval. Modify Therapy/Monitor Closely.
- toremifene
gepirone and toremifene both increase QTc interval. Modify Therapy/Monitor Closely.
- tramadol
gepirone and tramadol both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- tranylcypromine
gepirone and tranylcypromine both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- trazodone
gepirone and trazodone both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- trimipramine
gepirone and trimipramine both increase QTc interval. Modify Therapy/Monitor Closely.
- vandetanib
gepirone and vandetanib both increase QTc interval. Modify Therapy/Monitor Closely.
- vardenafil
gepirone and vardenafil both increase QTc interval. Modify Therapy/Monitor Closely.
- vemurafenib
gepirone and vemurafenib both increase QTc interval. Modify Therapy/Monitor Closely.
- venlafaxine
gepirone and venlafaxine both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- verapamil
verapamil will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.
- vilanterol/fluticasone furoate inhaled
gepirone and vilanterol/fluticasone furoate inhaled both increase QTc interval. Modify Therapy/Monitor Closely.
- vilazodone
gepirone and vilazodone both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- voriconazole
gepirone and voriconazole both increase QTc interval. Modify Therapy/Monitor Closely.
- vorinostat
gepirone and vorinostat both increase QTc interval. Modify Therapy/Monitor Closely.
- ziprasidone
gepirone and ziprasidone both increase QTc interval. Modify Therapy/Monitor Closely.
gepirone and ziprasidone both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug. - zolmitriptan
gepirone and zolmitriptan both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
Minor (0)
Adverse Effects
>10%
Dizziness (49%)
Nausea (35%)
Headache (31%)
Feeling sleepy or tired (15%)
Insomnia (14%)
1-10%
Diarrhea (10%)
Upper respiratory tract infection (8%)
Dry mouth (8%)
Vomiting (7%)
Abdominal pain (7%)
Dyspepsia (6%)
Increased appetite (5%)
Constipation (4%)
Nasopharyngitis (4%)
Nasal congestion (4%)
Paresthesia (4%)
Hyperhidrosis (4%)
Palpitations (4%)
Weight increased (3%)
Agitation (3%)
Feeling jittery (3%)
Heart rate increased (2%)
Lethargy (2%)
Breast tenderness (<2%)
Confusional state (<2%)
Dyspnea(<2%)
Edema peripheral (<2%)
Energy increased (<2%)
Feeling abnormal (<2%)
Hypoesthesia (<2%)
Poor quality sleep (<2%)
Thinking abnormal (<2%)
Frequency not defined
Hypersensitivity reactions
Warnings
Black Box Warnings
Suicidal thoughts and behaviors
- Antidepressants increased risk of suicidal thoughts and behaviors in pediatric and young adults in short-term studies
- Closely monitor all antidepressant-treated patients for clinical worsening and emergence of suicidal thoughts and behaviors
- Not approved for use in pediatric patients
Contraindications
Known hypersensitivity to gepirone or components
Prolonged QTc interval >450 msec at baseline
Congenital long QT syndrome
Concomitant use of strong CYP3A4 inhibitors
Severe hepatic impairment
Use with an MAOI or within 14 days of stopping treatment; do not use within 14 days of discontinuing an MAOI
Cautions
History of bipolar disorder
Antidepressant treatment can precipitate a manic, mixed, or hypomanic manic episode; risk appears to be increased in patients with bipolar disorder or who have risk factors for bipolar disorder, before initiating treatment, screen for history of bipolar disorder and the presence of risk factors for bipolar disorder (eg, family history of bipolar disorder, suicide, or depression)
Not approved for use in treating bipolar depression
Suicidal thoughts and behaviors in adolescents and young adults
- Incidence of suicidal thoughts and behaviors in antidepressant-treated patients aged ≤24 years was greater than in placebo-treated patients
- Risk of suicidal thoughts and behaviors varies among drugs, but there was an increased risk identified in young patients for most drugs studied
- Monitor for clinical worsening and emergence of suicidal thoughts and behaviors, especially during initial few months of drug therapy, and when dose is adjusted
- Counsel family members or caregivers of patients to monitor for changes in behavior and to alert healthcare provider
- Consider changing therapeutic regimen, including possibly discontinuing, in patients whose depression is persistently worse, or who are experiencing emergent suicidal thoughts or behaviors
QT prolongation
- May prolongs QTc interval
- Contraindicated in patients with congenital long QT syndrome
- Do not initiate if QTc is >450 msec at baseline
- Correct electrolyte abnormalities before initiating
- Monitor electrolytes during dose titration and periodically in patients with electrolyte abnormalities who are receiving diuretics or glucocorticoids, or have a history of hypokalemia or hypomagnesemia
- Perform an ECG before initiation, during dosage titration, and periodically during treatment.
-
Monitor ECGs more frequently
- Coadministration with drugs known to prolong the QT interval
- Patients who develop QTc ≥450 msec during treatment; do not escalate dosage if QTcF is >450 msec
- Patients with a significant risk of developing torsade de pointes, including those with uncontrolled or significant cardiac disease, recent myocardial infarction, heart failure, unstable angina, bradyarrhythmias, uncontrolled hypertension, high degree atrioventricular block, severe aortic stenosis, or uncontrolled hypothyroidism
Serotonin syndrome
- Coadministration of gepirone with selective serotonin reuptake inhibitors (SSRIs) or tricyclic antidepressants may cause serotonin syndrome, a potentially life-threatening condition with changes including altered mental status, hypertension, restlessness, myoclonus, hyperthermia, hyperreflexia, diaphoresis, shivering, and tremor
Drug interaction overview
-
CYP3A4 inhibitors
- Strong CYP3A4 inhibitor: Contraindicated
- Moderate CYP3A4 inhibitor: Reduce gepirone dose
- Strong and moderate CYP3A4 inhibitors increases gepirone exposure by ~5-fold and ~2.4 fold
-
CYP3A4 inducers
- Strong CYP3A4 inducers: Avoid coadministration
- Strong CYP3A4 inducers reduce gepirone exposure by 20- to 29-fold
-
MAOIs
- Coadministration with MAOIs is contraindicated; do not initiate in patients with MAOIs (eg, linezolid, IV methylene blue)
- If MAOI (eg, linezolid, IV methylene blue) is necessary in a gepirone-treated patient, discontinue gepirone before initiating a MAOI
-
Serotonergic drugs
- Monitor for symptoms of serotonin syndrome
- If concomitant use of gepirone with other serotonergic drugs is clinically warranted, inform patients of increased risk for serotonin syndrome and monitor for symptoms
- Immediately discontinue gepirone and/or concomitant serotonergic drugs if symptoms occur and initiate supportive symptomatic treatment
-
QT prolonging drugs
- Monitor patients with ECGs more frequently
- Drugs that prolong QTc interval may potentiate to QTc prolonging effects of gepirone and increase the risk of cardiac arrhythmias
Pregnancy & Lactation
Pregnancy
There are insufficient clinical data on gepirone use during pregnancy to evaluate for a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes
There are clinical considerations regarding neonates exposed to serotonergic antidepressants during third trimester of pregnancy
Pregnancy exposure registry
- Registry monitors pregnancy outcomes in women exposed to antidepressants during pregnancy
- Encourage patients to register patients by calling the National Pregnancy Registry for Antidepressants at 1-866-961-2388 or visiting online at https://womensmentalhealth.org/research/pregnancyregistry/antidepressants/
Animal data
- Gepirone has been shown to have adverse effects on embryofetal and postnatal development
- In rats, increased mortality during the first 4 days after birth and persistent reduction in body weight through lactation and weaning were observed at all doses and increased still births were seen with no observed adverse effect level (NOAEL) at 3 times the maximum recommended human dose (MRHD) on a mg/m2 basis
- In embryofetal development studies in rats and rabbits, decreased embryofetal growth, body weights and lengths, with accompanying skeletal variations were seen with a NOAEL at 9 and 12x the MRHD on a mg/m2 basis, respectively
Disease-associated maternal and/or embryofetal risk
- Women who discontinue antidepressants during pregnancy are more likely to experience a relapse of major depression than women who continue antidepressants
- Consider the risk of untreated depression when discontinuing or changing treatment with antidepressant medication during pregnancy and postpartum
Fetal/neonatal adverse reactions
- Neonates exposed to other serotonergic antidepressants in the third trimester have developed complications requiring prolonged hospitalization, respiratory support, and tube feeding. Complications can arise immediately upon delivery
- Reported clinical findings include respiratory distress, cyanosis, apnea, seizures, temperature instability, feeding difficulty, vomiting, hypoglycemia, hypotonia, hypertonia, hyperreflexia, tremors, jitteriness, irritability, and constant crying
Lactation
There are no data on the presence of gepirone in human milk, the effects on the breastfed infant, or the effects on milk production
Present in rat milk; when a drug is present in animal milk, it is likely that drug will be present in human milk
There are reports of breastfed infants exposed to other serotonergic antidepressants experiencing irritability, restlessness, excessive somnolence, decreased feeding, and weight loss
Monitor breastfeeding infants for adverse reactions (eg, irritability, restlessness, excessive somnolence, decreased feeding, weight loss)
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Serotonin (5HT)-1a agonist
Mechanism of the antidepressant effect is not fully understood
May be related to its modulation of serotonergic activity in the CNS through selective agonist activity at 5HT1A receptors
Absorption
Bioavailability: 14-17%
Steady-state achieved within 2-4 days
Effects of food
- High-fat meal: Peak plasma time reached 3 hr
- Systemic gepirone exposure and major metabolites were consistently higher under fed conditions as compared to the fasted state
- Gepirone peak plasma concentration after intake of low-fat (~200 calories) breakfast was 27% higher, after medium-fat (~500 calories) breakfast 55% higher and after a high-fat (~850 calories) breakfast 62% higher as compared to the fasted state
Distribution
Vd: 94.5 L
Protein-bound
- Gepirone: 72% and is not concentration dependent
- Metabolite: 59% (3’-OH gepirone) and 42% (1-PP)
Metabolism
Primarily metabolized by CYP3A4 to its major pharmacologically active metabolites
Both major metabolites 1-PP and 3’-OH-gepirone are present in plasma in higher concentrations than parent compound
Elimination
Half-life: 5 hr
Excretion
- Feces: 13%
- Urine: 81%
Administration
Oral Administration
Take with food
Swallow tablets whole; do not cut, crush, or chew
Storage
Store at 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)
Protect from high humidity and moisture
Images
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
