Comparative Pharmacology
Head-to-head clinical analysis: AUVELITY versus ZYBAN.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AUVELITY versus ZYBAN.
AUVELITY vs ZYBAN
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.
Bupropion is a selective dopamine and norepinephrine reuptake inhibitor with weak inhibition of serotonin reuptake. Its mechanism in smoking cessation and depression is not fully understood.
45 mg orally once daily, given as dextromethorphan hydrobromide 45 mg and bupropion hydrochloride 105 mg combination tablet.
150 mg orally once daily for 3 days, then increase to 150 mg twice daily for a total treatment duration of 7-12 weeks.
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)
The terminal elimination half-life of bupropion is approximately 21 hours (range 18-24 h), while its active metabolites have longer half-lives: hydroxybupropion ~20 h, threohydrobupropion ~37 h, erythrohydrobupropion ~33 h. Steady state is achieved within 8 days.
Renal 81% (dextromethorphan and metabolites: 78% as unchanged drug and 3% as dextrorphan conjugates), fecal 9% (dextromethorphan and metabolites), biliary <1%
Renal excretion accounts for approximately 87% of an oral dose, with 42% as unchanged bupropion and its active metabolites (hydroxybupropion, threohydrobupropion, erythrohydrobupropion). Fecal excretion is minimal at <10%.
Category C
Category C
Antidepressant
Antidepressant, Smoking Cessation Aid