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

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