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Generic Name: bupropion hydrochloride
Brands: Wellbutrin, Wellbutrin SR, Wellbutrin XL, Zyban

Pregnancy Category B

Drug classes
Antidepressant
Smoking deterrent

Therapeutic actions
The neurochemical mechanism of the antidepressant effect of bupropion is not understood; it is chemically unrelated to other antidepressant agents; it is a weak blocker of neuronal uptake of serotonin and norepinephrine and inhibits the reuptake of dopamine to some extent.

Indications
• Treatment of depression (effectiveness if used > 6 wk is unknown)
• Aid to smoking cessation treatment (Zyban)

Contraindications and cautions
• Contraindicated with hypersensitivity to bupropion; history of seizure disorder, bulimia or anorexia, head trauma, CNS tumor (increased risk of seizures); treatment with MAOIs; lactation.
• Use cautiously with renal or liver disease; heart disease, history of MI, pregnancy.

Available forms
Tablets—75, 100 mg; SR tablets—100, 150, 200 mg; ER tablets—150, 300 mg

Dosages
ADULTS
• Depression: 300 mg PO given as 100 mg tid; begin treatment with 100 mg PO bid; if clinical response warrants, increase 3 days after beginning treatment. If 4 wk after treatment, no clinical improvement is seen, dose may be increased to 150 mg PO tid (450 mg/day). Do not exceed 150 mg in any one dose. Discontinue drug if no improvement occurs at the 450 mg/day level. Sustained release: 150 mg PO bid; allow at least 8 hr between doses. Extended release: Initially, 150 mg/day PO as a once-a-day dose; range 300–450 mg/day.
• Smoking cessation: 150 mg (Zyban) PO daily for 3 days, then increase to 300 mg/day in 2 divided doses at least 8 hr apart. Treat for 7–12 wk.
PEDIATRIC PATIENTS
Safety and efficacy in children < 18 yr not established.
GERIATRIC PATIENTS
Bupropion is excreted through the kidneys; use with caution, and monitor older patients carefully.

Pharmacokinetics

Metabolism: Hepatic; T1/2: 14 hr; 21 hr (SR)
Distribution: May cross placenta; may enter breast milk
Excretion: Urine and feces