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Bupropion

Norepinephrine–dopamine reuptake inhibitor (aminoketone) · Antidepressant, Smoking Cessation Aid

Also known as Bupropion Hydrochloride

START
Depression XL 150 mg AM → 300 mg/day; smoking cessation 150 mg/day ×3 days → 150 mg BID
TYPICAL MAX
450 mg/day (XL); single dose ≤150 mg SR / ≤450 mg XL — minimise seizure risk
STOP IF
Seizure, severe hypertension, suicidality/psychiatric deterioration, severe hypersensitivity
WATCH
Mood/suicidality (esp. <25, early), BP (esp. with nicotine), seizure risk factors, sleep
CDSCO approvedSchedule HATC N06AX12
Dose laddermg/d
150start/day300target/day (XL)400SR max/day450XL ceiling/day
Renal dose adjustmenteGFR mL/min/1.73m²
FULLUsual dosing60REDUCEReduce dose/frequency (metabolite ac…30REDUCELowest dose, reduced frequency; moni…90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
5hONSET5hPEAK21h1dDURATION
ONSET
5h · absorption (XL)
PEAK
5h · Cmax (XL)
21h · plasma t½
DURATION
1d · once-daily (XL)
EXCRETION
Hepatic CYP2B6; ~87% renal metabolites
route + CYP
INTERACTIONS
12 major
incl. contraindicated
PREGNANCY
Use only if benefit outweighs risk — possible small cardiac malformation signal; individualise
FDA category + note
Top interactionssee all 12
  • MaoisContraindicatedDatabaseKimi deep-research + Cla
  • AldesleukinSevereDatabaseDDInter
  • AlfentanilSevereDatabaseDDInter
  • AlimemazineSevereDatabaseDDInter
Available in India

35 branded formulations. Look up specific brands in the Drugs workspace.

Mechanism

Inhibits noradrenaline and dopamine reuptake (and is a nicotinic acetylcholine receptor antagonist); no significant serotonergic activity — antidepressant and smoking-cessation efficacy without sexual dysfunction/weight gain.

Indications

Major depressive disorderSeasonal affective disorder (prophylaxis)Smoking cessation (Zyban)ADHD; obesity (with naltrexone) — off-label/combination

Dosing

Adult
Depression: SR 150 mg AM, increase to 150 mg BID (max 400 mg/day); XL 150 mg AM → 300 mg/day (max 450 mg). Smoking cessation: 150 mg/day ×3 days then 150 mg BID for 7–12 weeks (start 1–2 weeks before quit date).
Pediatric
Not first-line; specialist only.
Renal adjustment
Reduce dose/frequency in renal impairment (active metabolites accumulate); eGFR <30 use lowest dose.
Hepatic adjustment
Mild–moderate: reduce dose/frequency. Severe (cirrhosis): max 150 mg every other day.
Geriatric
Lower starting dose; reduced clearance.
Max dose
450 mg/day (XL); 400 mg/day (SR)

Pharmacokinetics

Onset
Antidepressant 2–4+ weeks
Peak effect
SR ~3 h; XL ~5 h
Duration
SR BID / XL once daily
Half-life
~21 h (parent); active metabolites longer (hydroxybupropion ~20 h)
Bioavailability
Low absolute (extensive first-pass)
Protein binding
~84%
Metabolism
Hepatic CYP2B6 → active hydroxybupropion; strong CYP2D6 inhibitor
Excretion
Renal (~87% as metabolites; <1% unchanged)

Contraindications

  • Seizure disorder
  • Current/prior bulimia or anorexia nervosa
  • Abrupt discontinuation of alcohol/benzodiazepines/sedatives (seizure risk)
  • MAOI within 14 days
  • Hypersensitivity to bupropion

Side effects

Common
InsomniaDry mouthHeadacheAgitation/anxietyNausea, tremorReduced appetite
Serious
  • Dose-related seizures
  • Hypertension (esp. with nicotine patch)
  • Neuropsychiatric: suicidality (boxed — young patients), psychosis/mania
  • Severe hypersensitivity (serum sickness-like, SJS)
  • Angle-closure glaucoma

Pregnancy & lactation

Pregnancy

Use only if benefit outweighs risk — possible small cardiac malformation signal; individualise

Lactation

Excreted in milk; monitor infant (seizure case reports) — use lowest dose, caution

Drug interactions

Maois
Contraindicated
Database

Hypertensive reaction/serotonin-independent crisis

Do not use within 14 days of an MAOI

Source: Kimi deep-research + Cla

Aldesleukin
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Alfentanil
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Alimemazine
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Amantadine
Severe
Database

Drug interaction classified as: synergy.

Source: DDInter

Amifampridine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Aminophylline
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amitriptyline
Severe
Database

May increase plasma exposures of TCAs.

The possibility of drug interactions should be kept in mind until the safety of the combination is firmly established.

Source: DDInter

Amoxapine
Severe
Database

May increase plasma exposures of TCAs.

The possibility of drug interactions should be kept in mind until the safety of the combination is firmly established.

Source: DDInter

Amphetamine
Severe
Database

Drug interaction classified as: metabolism.

Source: DDInter

Apalutamide
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Aripiprazole
Severe
Database

Increased AUC of parent drug (up to double AUC of parent drug).

Reduce aripiprazole dose by 50%.

Source: DDInter

Related guidelines

Ask House about Bupropion

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: KD Tripathi 7e, Goodman & Gilman 14e, Harrison 22e, Katzung·Verified: 2026-05-19 · House clinical team·Cockpit curated: 2026-05-19