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NERVOUS SYSTEM › PSYCHOANALEPTICS › ANTIDEPRESSANTS › Other antidepressants
bupropion
N06AX12
Forms & Strengths
- Tablet (Immediate Release - IR): 75 mg, 100 mg
- Tablet (Sustained Release - SR): 100 mg, 150 mg, 200 mg
- Tablet (Extended Release - XL): 150 mg, 300 mg
Adult Dosing
- Major Depressive Disorder (IR): 100 mg TID; start 100 mg BID, increase to 100 mg TID after 3 days; max 450 mg/day (max 150 mg/dose)
- Major Depressive Disorder (SR): 150 to 400 mg/day; start 150 mg once daily in the morning, may increase to 150 mg BID after 3 days; max 200 mg/dose
- Major Depressive Disorder (XL): 150 to 300 mg/day; start 150 mg once daily, may increase to 300 mg once daily after 4 days; max 300 mg/day
- Smoking Cessation (SR): 150 mg once daily for 3 days, then 150 mg BID for 7 to 12 weeks; max 300 mg/day
Pediatric Dosing
- Safety and efficacy not established in pediatric patients <18 years for major depressive disorder or smoking cessation
Indications
- Major depressive disorder (MDD)
- Prevention of seasonal affective disorder (SAD)
- Smoking cessation aid (as sustained-release formulation, Zyban)
Mechanism of Action
- Relatively weak inhibitor of the neuronal reuptake of norepinephrine and dopamine (NDRI)
- Minimal effect on neuronal reuptake of serotonin and does not inhibit monoamine oxidase (MAO)
Contraindications
- Seizure disorder
- Current or prior diagnosis of bulimia or anorexia nervosa
- Abrupt discontinuation of alcohol, benzodiazepines, barbiturates, or antiepileptic drugs
- Concomitant use of MAO inhibitors (or within 14 days of discontinuing)
- Known hypersensitivity to bupropion or any component of the formulation
Adverse Reactions
- Common: Insomnia, dry mouth, headache, nausea, agitation, dizziness, constipation, tachycardia, sweating
- Serious: Seizures (dose-dependent risk), hypertension, hepatotoxicity, neuropsychiatric events (suicidality, psychosis), angle-closure glaucoma
Drug Interactions
- CYP2B6 substrates/inhibitors: Bupropion is metabolized by CYP2B6; inhibitors (e.g., ticlopidine, clopidogrel) may increase levels, inducers (e.g., ritonavir, lopinavir, efavirenz) may decrease levels
- CYP2D6 inhibitors/substrates: Bupropion and its metabolite hydroxybupropion are strong inhibitors of CYP2D6; may increase plasma concentrations of CYP2D6 substrates (e.g., antidepressants, antipsychotics, beta-blockers)
- Drugs lowering seizure threshold: Coadministration with antipsychotics, antidepressants, theophylline, systemic steroids, or quinolones increases seizure risk
- MAO inhibitors: Hypertensive crisis risk; contraindicated
- Levodopa and amantadine: Increased risk of adverse CNS effects such as CNS toxicity and jitteriness
Curated Content: Needs Vetting Before Put to Clinical Use