Comparative Pharmacology
Head-to-head clinical analysis: APLENZIN versus AUVELITY.
Peer-Reviewed Evidence
Head-to-head clinical analysis: APLENZIN versus AUVELITY.
APLENZIN vs AUVELITY
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Bupropion is an aminoketone antidepressant that inhibits the reuptake of norepinephrine and dopamine, with no significant effect on serotonin. The exact mechanism of antidepressant action is unknown but is thought to be mediated by noradrenergic and dopaminergic pathways.
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.
APLENZIN (bupropion hydrobromide) extended-release tablets: Initial dose 174 mg orally once daily in the morning; after 4 days, increase to 348 mg once daily. Maximum dose 348 mg/day.
45 mg orally once daily, given as dextromethorphan hydrobromide 45 mg and bupropion hydrochloride 105 mg combination tablet.
None Documented
None Documented
Mean terminal half-life of bupropion is 21 hours (SD ±9 hours). Steady state achieved within 8 days. Metabolites have longer half-lives: hydroxybupropion ~24 hours, threohydrobupropion ~37 hours, erythrohydrobupropion ~34 hours.
Dextromethorphan: 13.5 hours (terminal half-life; prolonged due to CYP2D6 inhibition by bupropion, allowing sustained NMDA antagonism; bupropion: 13.7 hours)
Primarily renal (87% recovered in urine) with 10% fecal elimination. Unchanged bupropion accounts for <1% of renal excretion; metabolites (hydroxybupropion, threohydrobupropion, erythrohydrobupropion) predominate.
Renal 81% (dextromethorphan and metabolites: 78% as unchanged drug and 3% as dextrorphan conjugates), fecal 9% (dextromethorphan and metabolites), biliary <1%
Category C
Category C
Antidepressant
Antidepressant