Bupropion: Difference between revisions
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{{MedTemplate | {{MedTemplate | ||
| generic | | generic = Bupropion | ||
| brand | | brand = Wellbutrin (IR, SR, XL), Zyban (smoking cessation), Aplenzin (hydrobromide salt), Forfivo XL | ||
| structure | | structure = | ||
| classes | | classes = [[:Category:NDRIs|Norepinephrine-dopamine reuptake inhibitor (NDRI)]], [[:Category:Antidepressants|Antidepressant]], [[:Category:Smoking cessation medicines|Smoking cessation medicine]] | ||
| | | uses = <vote slug="major-depressive-disorder-use">Major depressive disorder (FDA)</vote>, <vote slug="seasonal-affective-disorder-use">Seasonal affective disorder (FDA, Wellbutrin XL)</vote>, <vote slug="smoking-cessation-use">Smoking cessation (FDA, Zyban)</vote>, <vote slug="adhd-bupropion-use">Attention-deficit/hyperactivity disorder (off-label, especially with comorbid depression)</vote>, <vote slug="ssri-induced-sexual-dysfunction-use">SSRI-induced sexual dysfunction (off-label adjunct)</vote>, <vote slug="weight-loss-adjunct-use">Weight management (off-label, also as a component of Contrave)</vote> | ||
| uses | | 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 | ||
| starting_dose | | 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 | ||
| preparations | | fda_max = 450 mg/day; doses above this raise seizure risk steeply | ||
| fda_max = | | pill_id = | ||
| routes | | routes = Oral | ||
| onset | | onset = 1-2 weeks for antidepressant effect; smoking-cessation effect builds over the first 1-2 weeks | ||
| duration | | duration = SR ~12 hours; XL 24 hours | ||
| halflife | | halflife = Bupropion ~21 hours; hydroxybupropion (active metabolite) ~20-37 hours<ref name="wellbutrin-label">FDA Prescribing Information, Wellbutrin XL (bupropion hydrochloride extended-release), GSK/Bausch, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021515s039lbl.pdf</ref> | ||
| bioavailability = ~5-20% (extensive first-pass), highly variable between individuals<ref name="wellbutrin-label" /> | |||
| pregnancy = Limited human data; some animal cardiac signal not clearly replicated in human cohort studies; observational signals inconclusive.{{citation needed}} | |||
| legal = [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults. Not controlled<ref name="wellbutrin-label" /> | |||
| | | mechanism = <vote slug="bupropion-mech-claim">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.</vote> 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<ref name="wellbutrin-label" />. | ||
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== References == | |||
<references /> | |||
[[Category:NDRIs]] | |||
[[Category:Antidepressants]] | [[Category:Antidepressants]] | ||
[[Category:Smoking cessation medicines]] | |||