Therapeutic Classification: antidepressants, smoking deterrents
Pharmacologic Classification: aminoketones
Absorption: Although well absorbed, rapidly and extensively metabolized by the liver.
Distribution: Unknown.
Metabolism/Excretion: Extensively metabolized by the liver into 3 active metabolites (CYP2B6 isoenzyme involved in formation of one of the active metabolites).
Half-Life: 14 hr (active metabolites may have longer half-lives).
Depression
- PO (Adults ): Immediate-release: 100 mg twice daily initially; after 3 days may ↑ to 100 mg 3 times daily; after at least 4 wk of therapy, may ↑ up to 450 mg/day in divided doses (not to exceed 150 mg/dose; wait at least 6 hr between doses at the 300 mg/day dose or at least 4 hr between doses at the 450-mg/day dose). 12hr sustained-release: 150 mg once daily in the morning; after 3 days, may ↑ to 150 mg twice daily with at least 8 hr between doses; after at least 4 wk of therapy, may ↑ to a maximum daily dose of 400 mg given as 200 mg twice daily. 24hr extended-release (Wellbutrin XL): 150 mg once daily in the morning, may be ↑ after 4 days to 300 mg once daily; some patients may require up to 450 mg/day as a single daily dose. 24hr extended-release (Aplenzin): 174 mg once daily in the morning, may be ↑ after 4 days to 348 mg once daily; some patients may require up to 522 mg/day as a single daily dose. 24hr extended-release (Forfivo XL): 450 mg once daily (should NOT be used as initial therapy; it should only be used in patients who have been receiving 300 mg/day of another bupropion formulation for at least 2 wk and require titration up to 450 mg/day or in those patients receiving 450 mg/day of another bupropion formulation).
Hepatic Impairment
- PO (Adults ): Moderate-to-severe hepatic impairment (Aplenzin): Max dose: 174 mg every other day.
Seasonal Affective Disorder
- PO (Adults ): 24hr extended-release (Wellbutrin XL): 150 mg/day in the morning; if dose is well tolerated, ↑ to 300 mg/day in one wk. Doses should be tapered to 150 mg/day for 2 wk before discontinuing; 24hr extended-release (Aplenzin): 174 mg once daily in the morning, may be ↑ after 7 days to 348 mg once daily.
Hepatic Impairment
- PO (Adults ): Moderate-to-severe hepatic impairment (Aplenzin): Max dose: 174 mg every other day.
Smoking cessation
- PO (Adults ): 12hr sustained release: 150 mg once daily for 3 days, then 150 mg twice daily for 712 wk (doses should be at least 8 hr apart).