Comparative Pharmacology
Head-to-head clinical analysis: BUPROPION HYDROCHLORIDE versus DESYREL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BUPROPION HYDROCHLORIDE versus DESYREL.
BUPROPION HYDROCHLORIDE vs DESYREL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Bupropion is a relatively weak inhibitor of neuronal dopamine and norepinephrine reuptake, but its clinical effects are thought to be mediated by these mechanisms. It also has weak antagonistic properties at nicotinic acetylcholine receptors.
Selective serotonin reuptake inhibitor (SSRI) that potentiates serotonergic activity by blocking serotonin reuptake at the presynaptic neuron. Also has secondary antagonistic effects at 5-HT2A receptors, contributing to its antidepressant and anxiolytic effects.
150 mg orally once daily (immediate-release) or 150 mg orally twice daily (sustained-release); maximum 300 mg/day for immediate-release and 400 mg/day for sustained-release. Extended-release: 150 mg orally once daily, titrate to 300 mg once daily. Typical target 300 mg/day in divided doses.
Initial dose: 150 mg orally once daily, increased by 50 mg/day every 3-4 days. Maximum: 400 mg/day. For severe depression, up to 600 mg/day in hospitalized patients.
None Documented
None Documented
Bupropion: ~21 hours (11-30 hours); hydroxybupropion: ~20 hours; threohydrobupropion: ~37 hours; erythrohydrobupropion: ~33 hours. Clinical context: Steady-state reached in 5-8 days; extended half-life of metabolites contributes to prolonged effects and accumulation.
Terminal elimination half-life is approximately 5-11 hours (mean 7 hours); for elderly patients, half-life may be prolonged.
Renal: 87% (primarily as metabolites, <0.5% unchanged); biliary/fecal: 10%; hepatic metabolism by CYP2B6 to active metabolites (hydroxybupropion, threohydrobupropion, erythrohydrobupropion).
Primarily renal (approximately 75% as metabolites, less than 1% unchanged); fecal excretion accounts for about 20%.
Category A/B
Category C
Atypical Antidepressant
Atypical Antidepressant