Comparative Pharmacology
Head-to-head clinical analysis: AUVELITY versus ZULRESSO.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AUVELITY versus ZULRESSO.
AUVELITY vs ZULRESSO
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
AUVELITY (dextromethorphan HBr and bupropion HCl) is an NMDA receptor antagonist (via dextromethorphan) and a norepinephrine-dopamine reuptake inhibitor (via bupropion). Dextromethorphan also modulates sigma-1 receptor activity.
Allopregnanolone is a positive allosteric modulator of GABAA receptors, enhancing phasic and tonic inhibition via binding to delta-subunit-containing receptors.
45 mg orally once daily, given as dextromethorphan hydrobromide 45 mg and bupropion hydrochloride 105 mg combination tablet.
Initial: 30 mcg/min IV infusion for 0-4 hours, then increase by 30 mcg/min every 4 hours if tolerated, maximum 120 mcg/min; typical duration up to 60 hours.
None Documented
None Documented
Dextromethorphan: 13.5 hours (terminal half-life; prolonged due to CYP2D6 inhibition by bupropion, allowing sustained NMDA antagonism; bupropion: 13.7 hours)
Terminal elimination half-life is approximately 18 hours (range 15-23 hours) following intravenous administration; clinically, this supports once-daily dosing.
Renal 81% (dextromethorphan and metabolites: 78% as unchanged drug and 3% as dextrorphan conjugates), fecal 9% (dextromethorphan and metabolites), biliary <1%
Primarily via renal excretion as unchanged drug (approximately 90% of dose) and minor fecal elimination (approximately 5%); no active metabolites identified.
Category C
Category C
Antidepressant
Antidepressant