Bupropion
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Bupropion
Wellbutrin (IR, SR, XL), Zyban (smoking cessation), Aplenzin (hydrobromide salt), Forfivo XL
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Summary
Classes
Common uses
Major depressive disorder (FDA)0, Seasonal affective disorder (FDA, Wellbutrin XL)0, Smoking cessation (FDA, Zyban)0, Attention-deficit/hyperactivity disorder (off-label, especially with comorbid depression)0, SSRI-induced sexual dysfunction (off-label adjunct)0, Weight management (off-label, also as a component of Contrave)0
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
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[1]
Bioavailability
~5-20% (extensive first-pass), highly variable between individuals[1]
Pregnancy
Limited human data; some animal cardiac signal not clearly replicated in human cohort studies; observational signals inconclusive.[citation needed]
Legal status
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[1].
References
- ↑ 1.0 1.1 1.2 1.3 FDA Prescribing Information, Wellbutrin XL (bupropion hydrochloride extended-release), GSK/Bausch, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021515s039lbl.pdf