bupropion

Quick answers

What is bupropion?

Bupropion is an atypical antidepressant (NDRI) used for major depressive disorder, bipolar depression augmentation, and smoking cessation, valued for weight neutrality and low sexual side effects.

What is WELLBUTRIN?

WELLBUTRIN is a brand name for bupropion.

What is WELLBUTRIN (bupropion) used for?

Label indications include: MDD; seasonal affective disorder; smoking cessation (SR).

What drug class is WELLBUTRIN (bupropion)?

NDRI Antidepressant.

What is the mechanism of action of WELLBUTRIN (bupropion)?

Norepinephrine–dopamine reuptake inhibitor (NDRI).

What strengths does WELLBUTRIN (bupropion) come in?

SR tablets 100–200 mg (BID) and XL tablets 150–450 mg (QD).

General information

Activating profile can be useful for fatigue and low motivation, but it is contraindicated in seizure disorders and in current/prior eating disorders; screening for risk factors (alcohol withdrawal, electrolyte disturbances) is important before initiation.

Mechanism of action

Refer to the Glossary entry on Neurotransmitters for background on receptor systems involved in serious mental illness.

• Norepinephrine-dopamine reuptake inhibitor with nicotinic receptor antagonism.

Metabolism & pharmacokinetics

• Metabolized by CYP2B6 to active hydroxybupropion; parent half-life ~14 h, metabolite half-life 20–37 h.
• Exposure can shift with strong CYP2B6 inhibitors/inducers; interaction checks are particularly important when carbamazepine or ritonavir are in a regimen.

Dosing & administration

• XL: start 150 mg qAM for 3–7 days, increase to 300 mg qAM; may increase to 450 mg qAM if needed.
• SR: 150 mg qAM ×3 days then 150 mg BID (≥8 h apart).
• For smoking cessation (SR), a common approach is 150 mg daily for several days, then 150 mg twice daily; coordinate quit date planning and behavioral supports.
• SR/XL tablets should not be crushed, split, or chewed; dose timing (often morning dosing) can help limit insomnia, and staying within labeled maximums helps reduce seizure risk.

Monitoring & labs

• Blood pressure at baseline and after dose changes, especially when nicotine replacement is used.
• Seizure risk factors (eating disorder history, alcohol/benzodiazepine withdrawal, electrolyte disturbances) before initiation and at follow-up.
• Sleep and anxiety during early titration; dose timing and titration speed are common levers for tolerability.
• Mood elevation or agitation in bipolar-spectrum illness; coordinate prevention plans via the bipolar disorder hub.
• Medication list review to ensure only one bupropion-containing product is active (to reduce accidental dose escalation across brands).

Bupropion’s activating profile can be helpful for low energy, but tolerability depends heavily on seizure-risk screening and on a predictable titration plan. Alcohol reduction and minimizing abrupt sedative withdrawal reduce seizure risk; document plans when alcohol use disorder is present. SR/XL tablets should remain intact, and gradual dose changes can reduce insomnia and seizure risk.

Adverse effects

Interactions

• CYP2B6 inhibitors (clopidogrel, ticlopidine) raise levels; CYP2B6 inducers (carbamazepine, ritonavir) lower levels.
• As a strong CYP2D6 inhibitor, bupropion can increase concentrations of coadministered CYP2D6 substrates (antidepressants, antipsychotics).
• Contraindicated with MAO inhibitors; a 14-day washout is used to reduce hypertensive crisis risk.

Other useful information

• Combination with SSRIs for augmentation is sometimes used; anxiety and insomnia are common early tolerability issues to watch.
• Alcohol moderation can reduce seizure risk.
• Duplicate bupropion across products (e.g., antidepressant plus smoking-cessation brand) can lead to accidental dose escalation; a medication list review helps prevent this.

References