Bupropion

Norepinephrine-dopamine reuptake inhibitor (NDRI), Antidepressant, Smoking cessation medicine

Bupropion

Wellbutrin (IR, SR, XL), Zyban (smoking cessation), Aplenzin (hydrobromide salt), Forfivo XL

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Titration strategies

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Effects

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Pharmacy

Starting dose

SR 150 mg PO once daily for 3 days, then 150 mg BID. XL 150 mg PO once daily for 4 days, then 300 mg once daily. Zyban (smoking cessation) 150 mg daily for 3 days, then 150 mg BID

Preparations

SR tablets 100, 150, 200 mg; XL tablets 150, 300 mg; IR tablets 75, 100 mg (less common); Aplenzin (bupropion hydrobromide) 174, 348, 522 mg

US FDA Max

450 mg/day; doses above this raise seizure risk steeply

Common uses

Classification(s)

Classes

Norepinephrine-dopamine reuptake inhibitor (NDRI), Antidepressant, Smoking cessation medicine

Pharmacology

Routes

Oral

Onset

1-2 weeks for antidepressant effect; smoking-cessation effect builds over the first 1-2 weeks

Duration

SR ~12 hours; XL 24 hours

Half-life

Bupropion ~21 hours; hydroxybupropion (active metabolite) ~20-37 hours

Bioavailability

~5-20% (extensive first-pass), highly variable between individuals

Pregnancy

Limited human data; some animal cardiac signal not clearly replicated in human cohort studies; observational signals inconclusive.^{[citation needed]}

Legal status

Rx-only in US. Carries the antidepressant Boxed Warning for suicidality in children, adolescents, and young adults. Not controlled

Purported mechanism

Selective norepinephrine and dopamine reuptake inhibitor with minimal serotonergic activity, distinguishing it sharply from the SSRI/SNRI antidepressants. Also a non-competitive nicotinic acetylcholine receptor antagonist, the proposed mechanism behind smoking-cessation efficacy. CYP2B6 produces the active metabolite hydroxybupropion, which contributes substantially to clinical effect.▲0▼ Lowers seizure threshold in a dose-dependent way; contraindicated in bulimia, anorexia nervosa, seizure disorder, and abrupt alcohol or benzodiazepine discontinuation. Bupropion is a strong CYP2D6 inhibitor, raising plasma levels of many CYP2D6 substrates including tricyclic antidepressants, certain β-blockers, and certain neuroleptics.