Bupropion

WELLBUTRIN

Open Bupropion in the interactive console ↗

Pronunciation: byoo-PROE-pee-on (WEL-byoo-trin)

Bupropion ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Bupropion ballicule

Bupropion WELLBUTRIN mascot mnemonic cartoon — Visual mnemonic: Bupropion mascot
**“Boop ropin’ Well booty”**
Strong CYP2D6 inHibitor
Skinny → weight loss possible

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.

Bupropion molecular structure (skeletal formula) — Molecular structure: Bupropion

FDA-approved for

depression (1985)
smoking cessation (1997)
seasonal affective disorder (2006)

Off-label

ADHD
antidepressant sexual dysfunction

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Suicidal thoughts and behaviors: increased risk in children, adolescents, and young adults; monitor closely.

FDA dosing	Population	Start	Target	Max
Major depressive disorder	Adults	100 mg BID	100 mg TID (300 mg/day)	450 mg/day (≤150 mg per dose)

Titration After 3 days may increase to 300 mg/day; increases ≤100 mg/day per 3-day period

Renal GFR <90 mL/min: consider reduced dose and/or frequency

Hepatic Moderate–severe (Child-Pugh 7–15): max 75 mg/day; mild (Child-Pugh 5–6): consider reduced dose and/or frequency

Not approved for smoking cessation; pediatric safety and effectiveness not established.

Instructions

Swallow whole; do not crush, divide, or chew
With or without food
At least 6 h between doses
Above 300 mg/day use 75- or 100-mg tablets; 450 mg/day as 150 mg TID or 100 mg 4 times daily (≤150 mg per dose)

Available strengths

tab 75, 100 mg

Contraindications

Seizure disorder
Current or prior bulimia or anorexia nervosa
Abrupt discontinuation of alcohol, benzodiazepines, barbiturates, or antiepileptic drugs
MAOIs (psychiatric) concurrently or within 14 days; starting in patients on linezolid or IV methylene blue — hypertensive reactions

Cautions

Suicidal thoughts and behaviors in children, adolescents, young adults
Neuropsychiatric adverse events in smoking cessation
Seizure (dose-related; ≤450 mg/day, titrate gradually)
Hypertension
Activation of mania/hypomania
Psychosis and other neuropsychiatric reactions
Angle-closure glaucoma
Hypersensitivity reactions

Adverse reactions

Agitation
Dry mouth
Constipation
Headache/migraine
Nausea/vomiting
Dizziness
Excessive sweating
Tremor
Insomnia
Blurred vision
Tachycardia
Confusion, rash, hostility, cardiac arrhythmias, auditory disturbance

Pregnancy First-trimester epidemiologic data show no increased overall malformation risk; weigh risks of untreated depression.

Lactation Bupropion and metabolites present in milk (~2% of maternal weight-adjusted dose); seizures reported in breastfed infants (relationship unclear).

Cost

Bupropion (WELLBUTRIN)

What pharmacies pay · NADAC 9/30/26

Strength		#/mo	generic $/mo	CostPlus
75 mg	tab	30 qd	$2.78	offered
100 mg	tab	30 qd	$3.39	offered

Other forms: Bupropion hydrobromide ER (APLENZIN) · Bupropion SR (WELLBUTRIN SR) · Bupropion XL (WELLBUTRIN XL) · Bupropion XL 450 mg (FORFIVO XL)

Available combined with: dextromethorphan / bupropion · naltrexone / bupropion

Generic entry1999

⚠ BOXED WARNING

Suicidal thoughts and behaviors in patients under 25

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.

Serotonicity

This drug is routinely called serotonergic. By Gillman’s human-effect criteria it does not raise serotonin in the synapse.

No clinically significant SRI activity.

Label contraindicationMAOIs (psychiatric) concurrently or within 14 days; starting in patients on linezolid or IV methylene blue — hypertensive reactions. The label governs prescribing; Gillman’s point concerns serotonin toxicity only.

Gillman’s four human testsA measurable SERT affinity that fails all four is not clinical serotonicity.