Bupropion

The mechanism of action of bupropion is unknown, as is the case with other antidepressants. However, it is presumed that this action is mediated by noradrenergic and/or dopaminergic mechanisms.

• Bupropion hydrochloride extended-release tablets (XL) are an aminoketone antidepressant, indicated for: treatment of major depressive disorder (MDD) (1.1) prevention of seasonal affective disorder (SAD) ( 1.2) 1.1 Major Depressive Disorder (MDD) Bupropion hydrochloride extended-release tablets (XL) are indicated for the treatment of major depressive disorder (MDD), as defined by the Diagnostic and Statistical Manual (DSM). The efficacy of the immediate-release formulation of bupropion was established in two 4-week controlled inpatient trials and one 6-week controlled outpatient trial of adult patients with MDD.ICD-10: F32.9

• Bupropion hydrochloride extended-release tablets (XL) are contraindicated in patients with seizure disorder. Bupropion hydrochloride extended-release tablets (XL) are contraindicated in patients with a current or prior diagnosis of bulimia or anorexia nervosa as a higher incidence of seizures was observed in such patients treated with bupropion hydrochloride extended-release tablets (XL) [see Warnings and Precautions (5.3) ].contraindicated

General: Increase dose gradually to reduce seizure risk. ( 2.1 , 5.3 ) Periodically reassess the dose and need for maintenance treatment. ( 2.2 ) Major Depressive Disorder Starting dose: 150 mg once daily. Usual target dose: 300 mg once daily ( 2.2 ) After 4 days, may increase the dose to 300 mg once daily. ( 2.2 ) Seasonal Affective Disorder Initiate treatment in the autumn prior to onset of seasonal depressive symptoms. ( 2.3 ) Starting dose: 150 mg once daily. Usual target dose: 300 mg once daily. ( 2.3 ) After one week, may increase the dose to 300 mg once daily. ( 2.3 ) Continue treatment through the winter season. ( 2.3 ) Hepatic Impairment Moderate to severe hepatic impairment: 150 mg every other day ( 2.6 ) Mild hepatic impairment: Consider reducing the dose and/or frequency of dosing. ( 2.6 , 8.7 ) Renal Impairment Consider reducing the dose and/or frequency of dosing. ( 2.7 , 8.6 ) 2.1 General Instructions for Use To minimize the risk of seizure, increase the dose gradually [see Warnings and Precautions (5.3) ]. Bupropion hydrochloride extended-release tablets (XL) should be swallowed whole and not crushed, divided, or chewed. Bupropion hydrochloride extended-release tablets (XL) should be administered in the morning and may be taken with or without food. 2.2 Dosage for Major Depressive Disorder (MDD) The recommended starting dose for MDD is 150 mg once daily in the morning. After 4 days of dosing, the dose may be increased to the target dose of 300 mg once daily in the morning.

Neuropsychiatric Adverse Events During Smoking Cessation: Postmarketing reports of serious or clinically significant neuropsychiatric adverse events have included changes in mood (including depression and mania), psychosis, hallucinations, paranoia, delusions, homicidal ideation, aggression, hostility, agitation, anxiety, and panic, as well as suicidal ideation, suicide attempt, and completed suicide. Observe patients attempting to quit smoking with bupropion hydrochloride extended-release tablets (XL) for the occurrence of such symptoms and instruct them to discontinue bupropion hydrochloride extended-release (XL) tablets and contact a healthcare provider if they experience such adverse events. ( 5.2 ) Seizure Risk: The risk is dose-related. Can minimize risk by limiting daily dose to 450 mg and gradually increasing the dose. Discontinue if seizure occurs. ( 4 , 5.3 , 7.3 ) Hypertension: Bupropion hydrochloride extended-release tablets (XL) can increase blood pressure. Monitor blood pressure before initiating treatment and periodically during treatment. ( 5.4 ) Activation of Mania/Hypomania: Screen patients for bipolar disorder and monitor for these symptoms. ( 5.5 ) Psychosis and Other Neuropsychiatric Reactions: Instruct patients to contact a healthcare professional if such reactions occur. ( 5.6 ) Angle-Closure Glaucoma: Angle-closure glaucoma has occurred in patients with untreated anatomically narrow angles treated with antidepressants.

The following adverse reactions are discussed in greater detail in other sections of the labeling: Suicidal thoughts and behaviors in children, adolescents, and young adults [see Warnings and Precautions (5.1) ] Neuropsychiatric adverse events and suicide risk in smoking cessation treatment [see Warnings and Precautions (5.2) ] Seizure [see Warnings and Precautions (5.3) ] Hypertension [see Warnings and Precautions (5.4) ] Activation of mania or hypomania [see Warnings and Precautions (5.5) ] Psychosis and other neuropsychiatric events [see Warnings and Precautions (5.6) ] Angle-Closure Glaucoma [see Warnings and Precautions (5.7) ] Hypersensitivity reactions [see Warnings and Precautions (5.8) ] Most common adverse reactions are (incidence ≥5%; ≥2× placebo rate): dry mouth, nausea, insomnia, dizziness, pharyngitis, abdominal pain, agitation, anxiety, tremor, palpitation, sweating, tinnitus, myalgia, anorexia, urinary frequency, rash. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Oryza Pharmaceuticals, Inc. at 1-866-637-4281, or FDA at 1-800-FDA-1088, or visit www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to antidepressants during pregnancy. Healthcare providers are encouraged to register patients by calling the National Pregnancy Registry for Antidepressants at 1-844-405-6185 or visiting online at https://womensmentalhealth.org/clinical-and-research-programs/pregnancyregistry/antidepressants/. Risk Summary Data from epidemiological studies of pregnant women exposed to bupropion in the first trimester have not identified an increased risk of congenital malformations overall (see Data ). There are risks to the mother associated with untreated depression (see Clinical Considerations) . When bupropion was administered to pregnant rats during organogenesis, there was no evidence of fetal malformations at doses up to approximately 10 times the maximum recommended human dose (MRHD) of 450 mg/day. When given to pregnant rabbits during organogenesis, non-dose-related increases in incidence of fetal malformations and skeletal variations were observed at doses approximately equal to the MRHD and greater. Decreased fetal weights were seen at doses twice the MRHD and greater (see Animal Data ). The estimated background risk for major birth defects and miscarriage are unknown for the indicated population.

Metabolism

Bupropion is a racemic mixture. The pharmacologic activity and pharmacokinetics of the individual enantiomers have not been studied.

10.1 Human Overdose Experience Overdoses of up to 30 grams or more of bupropion have been reported. Seizure was reported in approximately one third of all cases. Other serious reactions reported with overdoses of bupropion alone included hallucinations, loss of consciousness, mental status changes, sinus tachycardia, ECG changes such as conduction disturbances or arrhythmias, clonus, myoclonus, and hyperreflexia. Fever, muscle rigidity, rhabdomyolysis, hypotension, stupor, coma, and respiratory failure have been reported mainly when bupropion was part of multiple drug overdoses. Although most patients recovered without sequelae, deaths associated with overdoses of bupropion alone have been reported in patients ingesting large doses of the drug. Multiple uncontrolled seizures, bradycardia, cardiac failure, and cardiac arrest prior to death were reported in these patients. 10.2 Overdosage Management Consult a Certified Poison Control Center for up-to-date guidance and advice. Call 1-800-222-1222 or refer to www.poison.org. There are no known antidotes for bupropion. In case of an overdose, provide supportive care, including close medical supervision and monitoring.

• Oct 4, 1996NDANDA020358Glaxosmithkline
• Feb 7, 2000ANDAANDA075584Senores Pharms
• Apr 17, 2000ANDAANDA075491Aurobindo Pharma Usa
• Aug 28, 2003NDANDA021515Bausch
• Apr 23, 2008NDANDA022108Bausch
• Nov 10, 2011NDANDA022497Twi Pharms
• Sep 10, 2014NDANDA200063Nalpropion
• Aug 18, 2022NDANDA215430Axsome

Recent PubMed references pinned to Bupropion as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Bupropion-induced early-onset urticaria.
  BMJ case reports · 2026 · Saini VK, Raj AB, Tyagi S, et al.
  PMID 42173537DOI 10.1136/bcr-2026-273117
• Recurrent Seizure Induced an Overdose of Bupropion Hydrochloride Sustained-Release Tablets in an<br /> Adolescent: A Management Analysis.
  Journal of the College of Physicians and Surgeons--Pakistan : JCPSP · 2026 · Shi Y, Ruan P, Chen H, et al.
  PMID 42152219DOI 10.29271/jcpsp.2026.05.694
• A rapid GC-MS method for the simultaneous determination of bupropion and hydroxybupropion in plasma using SALLME and microwave-assisted derivatization.
  Journal of chromatography. A · 2026 · Neşetoğlu M, Al S, Neşetoğlu N, et al.
  PMID 42070463DOI 10.1016/j.chroma.2026.467049
• Early Extracorporeal Membrane Oxygenation Support in Bupropion-Induced Cardiogenic Shock: A Case Series.
  The Journal of emergency medicine · 2026 · DeGraaf L, Bhatnagar G, Ovakim DH, et al.
  PMID 41934731DOI 10.1016/j.jemermed.2025.12.009
• Use of Naltrexone-Bupropion in Persons With Overweight/Obesity and Symptoms of Depression: A Pooled Analysis.
  Obesity (Silver Spring, Md.) · 2026 · Tronieri JS, Kushner RF, Apovian CM, et al.
  PMID 41914839DOI 10.1002/oby.70183
• Bupropion-Memantine Combination in the Treatment of Major Depressive Disorder and Treatment-Resistant Depression.
  Human psychopharmacology · 2026 · Riestra JM, Levin-Carrion Y, Sutar R, et al.
  PMID 41913380DOI 10.1002/hup.70039
• Pharmacological modulation of anxiety‑like and depression‑like behaviors in nerve‑ligated mice: regarding the effects of citicoline and bupropion.
  Acta neurobiologiae experimentalis · 2026 · Hajikarimloo B, Raissi-Dehkordi N, Raissi-Dehkordi N, et al.
  PMID 41885748DOI 10.55782/c6vq8k73
• Protective effect of concurrent bupropion and citicoline treatment on lipopolysaccharide-induced depression- and anxiety-like behavior in mice: The role of neuroinflammation.
  Experimental and clinical psychopharmacology · 2026 · Mousavi SE, Afrand Khalilabad Z, Ghasemi M, et al.
  PMID 41870376DOI 10.1037/pha0000845

The 10 most recently updated of 497 ClinicalTrials.gov registrations naming Bupropion as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Weight Loss Study: Genetics and Response to Naltrexone/Bupropion
  Recruiting · Phase 4 · Interventional · 120 enrolled · Columbia University
  NCT05919797updated 2026-06-10
• Pharmacological and Behavioral Treatment After Bariatric Surgery
  Active not recruiting · Phase 3 · Interventional · 84 enrolled · Yale University
  NCT05157698updated 2026-06-10
• A Study to Evaluate the Safety of Exposure to Wegovy During Pregnancy
  Enrolling by invitation · Observational · 1,139 enrolled · Novo Nordisk A/S
  NCT05503927updated 2026-06-09
• A Phase 1, First-in-human Study of VX-433
  Recruiting · Phase 1 · Interventional · 118 enrolled · Vertex Pharmaceuticals Incorporated
  NCT07584434updated 2026-06-08
• Trial of Naltrexone/Bupropion for the Treatment of Methamphetamine Use Disorder
  Recruiting · Phase 3 · Interventional · 360 enrolled · National Institute on Drug Abuse (NIDA)
  NCT06233799updated 2026-06-04
• A Study in Healthy Men and Women to Test Whether BI 1569912 Influences the Amount of Repaglinide, Midazolam and Bupropion in the Blood
  Completed · Phase 1 · Interventional · 18 enrolled · Boehringer Ingelheim
  NCT06367153updated 2026-05-22
• Effectiveness of a Smoking Cessation Algorithm Integrated Into HIV Primary Care
  Completed · Phase 4 · Interventional · 371 enrolled · University of Alabama at Birmingham
  NCT03670316updated 2026-05-22
• Predictors of Cognitive Outcomes in Geriatric Depression
  Active not recruiting · Phase 4 · Interventional · 75 enrolled · David Steffens
  NCT05273996updated 2026-05-22
• Bupropion Hydrochloride in Improving Sexual Desire in Women With Breast or Gynecologic Cancer
  Completed · Phase 2 · Interventional · 230 enrolled · NRG Oncology
  NCT03180294updated 2026-05-19
• BRE-06: Study to Increase Tolerance to Aromatase Inhibitors for Patients With Early-Stage Hormone Receptor Positive Breast Cancer Who Developed Hypoactive Sexual Desire Disorder
  Not yet recruiting · Phase 1 · Phase 2 · Interventional · 100 enrolled · University of Illinois at Chicago
  NCT07596212updated 2026-05-19

CPIC-curated drug–gene pairs for Bupropion. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

• CYP2B6CPIC B/C (provisional)ClinPGx 2A

Frequently asked questions

How does Bupropion work?

The mechanism of action of bupropion is unknown, as is the case with other antidepressants. However, it is presumed that this action is mediated by noradrenergic and/or dopaminergic mechanisms.

What is Bupropion used for?

According to FDA labeling, Bupropion carries indications including: Bupropion hydrochloride extended-release tablets (XL) are an aminoketone antidepressant, indicated for: treatment of major depressive disorder (MDD) (1.1) prevention of seasonal affective disorder (SAD) ( 1.2) 1.1 Major Depressive Disorder (MDD) Bupropion hydrochloride extended-release tablets (XL) are indicated for the treatment of major depressive disorder (MDD), as defined by the Diagnostic and Statistical Manual (DSM). The efficacy of the immediate-release formulation of bupropion was established in two 4-week controlled inpatient trials and one 6-week controlled outpatient trial of adult patients with MDD.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Bupropion?

Bupropion is classified as Other antidepressants, Aminoketone, Cytochrome P450 2D6 Inhibitors, Dopamine Uptake Inhibitors, Monoamine Oxidase Inhibitors, Norepinephrine Uptake Inhibitors, Serotonin Uptake Inhibitors, Increased Dopamine Activity, Increased Norepinephrine Activity, Increased Serotonin Activity.

What are the brand names for Bupropion?

Bupropion is marketed under brand names including Aplenzin, Auvelity, Contrave, Forfivo, Wellbutrin.

What are the contraindications for Bupropion?

Bupropion labeling lists contraindications including: Bupropion hydrochloride extended-release tablets (XL) are contraindicated in patients with seizure disorder. Bupropion hydrochloride extended-release tablets (XL) are contraindicated in patients with a current or prior diagnosis of bulimia or anorexia nervosa as a higher incidence of seizures was observed in such patients treated with bupropion hydrochloride extended-release tablets (XL) [see Warnings and Precautions (5.3) ].. Always consult the full prescribing information and a clinician.