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Bupropion

WELLBUTRIN

What it isNorepinephrine-dopamine reuptake inhibitor; depression and smoking cessation.

Why this oneFar less sexual dysfunction and weight gain than SSRIs, which is why it is added to or substituted for one.

What limits itLowers the seizure threshold, so avoid in eating disorders and with alcohol withdrawal. A strong CYP2D6 inhibitor.

FDA-approved for

Off-label

FDA label

BOXED WARNING Suicidal thoughts and behaviors: increased risk in children, adolescents, and young adults; monitor closely
FDA dosingPopulationStartTargetMax
Major depressive disorderAdults150 mg QAM300 mg QD450 mg/day
Seasonal affective disorder (prevention)Adults150 mg QD300 mg QD300 mg/day

Titration MDD: may increase to 300 mg QD after 4 days; SAD: may increase to 300 mg QD after 7 days

Renal Consider reduced dose and/or frequency (GFR <90 mL/min)

Hepatic Moderate-severe (Child-Pugh 7–15): max 150 mg every other day; mild (5–6): consider reduced dose/frequency

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy Epidemiologic data do not show increased overall malformation risk; weigh against risks of untreated depression

Lactation Bupropion and metabolites present in human milk (~2% maternal dose); seizures reported in breastfed infants

⚠ BOXED WARNING

Cost, est. cash$300–$2,500/month

Generic entry1999

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger4 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk1 / 4

Legacy pregnancy categoryC

Defining liabilityDose-related seizures and delayed cardiotoxicity are prominent in overdose, especially with extended-release products.

Active metabolites

Mechanism of action: Bupropion ballicule

Bupropion ballicule: receptor binding, kinetics and half-life diagram

Open Bupropion in the interactive console ↗

Memory aids: mascots and interaction avatars

Bupropion WELLBUTRIN mascot mnemonic cartoon
“Boop ropin’ Well booty”
Strong CYP2D6 inHibitor
Skinny → weight loss possible
Bupropion CYP2B6 substrate avatar
CYP2B6 substrate
Bupropion CYP2D6 inhibitor avatar
CYP2D6 inhibitor (strong)

Open Bupropion in the interactive console ↗