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Bupropion

    DEA Class;  Rx

    Common Brand Names; Budeprion SR, Aplenzin, Buproban, Wellbutrin SR, Wellbutrin XL, Forfivo XL, Zyban (DSC)

    • Antidepressants, Dopamine Reuptake Inhibitors; 
    • Antidepressants, Other; 
    • Smoking Cessation Aids

    Oral antidepressant of the aminoketone class; unrelated to other antidepressants
    Brand-specific FDA approvals for major depression, seasonal affective disorder, and smoking cessation in adults
    Greater potential for causing seizures than many other antidepressants; a boxed warning exists for use in pediatric depression

    Indicated for treatment of major depressive disorder (MDD)

    For use as an adjunct to psychosocial interventions in the management of tobacco cessation (smoking cessation).
    For the treatment of attention-deficit hyperactivity disorder (ADHD).
    For the symptomatic treatment of neuropathic pain due to various causes, including pain associated with peripheral diabetic neuropathy or postherpetic neuralgia.

    Hypersensitivity to bupropion or other ingredients

    History of anorexia/bulimia; patients undergoing abrupt discontinuation of ethanol or sedatives including anticonvulsants, barbiturates, or benzodiazepines

    Coadministration of any other medications that contain bupropion, because seizures are dose dependent

    • Headache (25-34%)
    • Dry mouth (17-28%)
    • Nausea (1-18%)
    • Weight loss (15-20%)
    • Insomnia (11-20%)
    • Agitation (2-32%)
    • Dizziness (6-22%)
    • Pharyngitis (3-13%)
    • Constipation (5-10%)
    • Infection (8-9%)
    • Abdominal pain (2-9%)
    • Anxiety (5-7%)
    • Diarrhea (5-7%)
    • Tinnitus (3-6%)
    • Tremor (3-6%)
    • Nervousness (3-5%)
    • Anorexia (3-5%)
    • Palpitation (2-6%)
    • Myalgia (2-6%)
    • Sweating (2-5%)
    • Rash (1-5%)
    • Sinusitis (1-5%)
    • Weight gain (4%)
    • Chest pain (3-4%)
    • Urinary frequency (2%)
    • Vaginal hemorrhage (2%)
    • Pruritus (2-4%)
    • Vomiting (2-4%)
    • Arthralgia (1-4%)
    • Flushing (1-4%)
    • Migraine (1-4%)
    • Decreased memory (<3%)
    • Irritability (2-3%)
    • Somnolence (2-3%)
    • Dysphagia (<2%)
    • Arthritis (2%)

    Caution in severe hepatic cirrhosis (do not exceed 150 mg every other day), mild-moderate hepatic impairment, head trauma and prior seizure history, CNS tumor, concomitant meds lowering seizure threshold

    Observe patients for neuropsychiatric symptoms, such as changes in behavior, hostility, agitation, depressed mood, and suicide-related events, including ideation, behavior, and attempted suicide (see Black Box Warnings); therapy may cause delusions, hallucinations, psychosis, paranoia, confusion, and concentration disturbance; symptoms may abate with dose reduction

    Healthcare provider should evaluate severity of adverse events and extent to which patient is benefiting from treatment, and consider options including continued treatment under closer monitoring, or discontinuing treatment; in many postmarketing cases, resolution of symptoms after discontinuation of bupropion reported; however, symptoms persisted in some cases; ongoing monitoring and supportive care should be provided until symptoms resolve

    Potential risk of hepatotoxicity

    Assess blood pressure before initiating treatment with sustained release formulation, and monitor periodically during treatment; risk of hypertension is increased if sustained release formulation is used concomitantly with MAOIs or other drugs that increase dopaminergic or noradrenergic activity; use caution in patients with cardiovascular disease

    May cause weight loss; use caution if weight loss not desirable

    May cause CNS depression and impair ability to operate heavy machinery

    Extended-release: Do not administer less than 8 hr apart

    Seizure risk is dose-related; can minimize risk by limiting daily dose to 522 mg and gradually increasing dose; discontinue permanently in patients who experience seizures

    May cause sexual dysfunction

    There is an independent pregnancy exposure registry that monitors pregnancy outcomes in women exposed to any antidepressants during pregnancy

    Data from published literature report presence of drug and its metabolites in human milk

    Adults

    Immediate-release tablets: 450 mg/day PO, no single dose should exceed 150 mg.
    Wellbutrin SR: 400 mg/day PO; no single dose should exceed 200 mg.
    Zyban: 300 mg/day PO for smoking cessation; no single dose should exceed 150 mg.
    Wellbutrin XL: 450 mg/day PO.
    Aplenzin: 522 mg/day PO; no single dose should exceed 522 mg.
    Forfivo XL: 450 mg/day PO.

    Geriatric

    Immediate-release tablets: 450 mg/day PO, no single dose should exceed 150 mg.
    Wellbutrin SR: 400 mg/day PO; no single dose should exceed 200 mg.
    Zyban: 300 mg/day PO for smoking cessation; no single dose should exceed 150 mg.
    Wellbutrin XL: 450 mg/day PO.
    Aplenzin: 522 mg/day PO; no single dose should exceed 522 mg.
    Forfivo XL: 450 mg/day PO.

    Adolescents

    Safety and efficacy have not been established; however, a total daily dosage up to 300 mg/day PO for immediate-release tablets has been suggested for the treatment of attention-deficit hyperactivity disorder (ADHD); doses up to 6 mg/kg/day (not to exceed 300 or 400 mg/day) PO of the bupropion SR products have been used in studies for treatment of depression.

    Children

    6 to 12 years: Safety and efficacy have not been established; however, a total daily dosage up to 300 mg/day PO for immediate-release tablets has been suggested for the treatment of attention-deficit hyperactivity disorder (ADHD).
    5 years and younger: Safety and efficacy have not been established.

    Infants

    Safety and efficacy have not been established.

    Neonates

    Safety and efficacy have not been established.

    Bupropion hydrobromide 

    tablet (Wellbutrin – Discontinued)

    • 75mg
    • 100mg

    tablet, sustained-release (Wellbutrin SR)

    • 100mg
    • 150mg
    • 200mg

    tablet, extended-release (Wellbutrin XL)

    • 150mg
    • 300mg

    tablet, extended-release (Aplenzin)

    • 174mg
    • 348mg
    • 522mg

    tablet, extended-release (Forfivo XL)

    • 450mg

    tablet, extended-release (Zyban – Discontinued)

    • 150mg