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bupropion hydrochloride

(byoo proe' pee on)


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.

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 weeks.
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
Route Onset Peak Duration
Oral Varies 2 hr 8–12 hr
SR Oral Varies 3 hr 16–20 hr
ER Oral Varies 5 hr 15–25 hr

Metabolism: Hepatic; T1/2: 8–24 hr


Distribution: May cross placenta; may enter breast milk
Excretion: Urine and feces

Adverse effects
• CNS: Agitation, insomnia, headache, migraine, tremor, ataxia, incoordination,
seizures, mania, increased libido, hallucinations, visual disturbances
• CV: Dizziness, tachycardia, edema, ECG abnormalities, chest pain, shortness of
breath
• Dermatologic: Rash, alopecia, dry skin
• GI: Dry mouth, constipation, nausea, vomiting, stomatitis
• GU: Nocturia, vaginal irritation, testicular swelling
• Other: Weight loss, flulike symptoms

Interactions
Drug-drug
• Increased risk of adverse effects with levodopa
• Increased risk of toxicity with MAOIs
• Increased risk of seizures with drugs that lower seizure threshold, including
alcohol

Nursing considerations
Assessment
• History: Hypersensitivity to bupropion, history of seizure disorder, bulimia or
anorexia, head trauma, CNS tumor, treatment with MAOI, renal or liver disease,
heart disease, lactation
• Physical: Skin, weight; orientation, affect, vision, coordination; P, rhythm,
auscultation; R, adventitious sounds; bowel sounds, condition of mouth

Interventions
• Administer drug three times a day for depression; do not administer more than
150 mg in any one dose. Administer sustained-release forms twice a day with at
least 8 hr between doses.
• Increase dosage slowly to reduce the risk of seizures.
• Administer 100-mg tablets qid for depression, with at least 4 hr between doses, if
patient is receiving > 300 mg/day; use combinations of 75-mg tablets to avoid
giving > 150 mg in any single dose.
• Arrange for patient evaluation after 6 wk; effects of drug after 6 wk are not
known.
• Discontinue MAOI therapy for at least 14 days before beginning bupropion.
• Monitor liver and renal function tests in patients with a history of liver or renal
impairment.
• Have patient quit smoking within first 2 wk of treatment for smoking cessation;
may be used with transdermal nicotine.
• Monitor response and behavior; suicide is a risk in depressed patients.

Teaching points
• Take this drug in equally divided doses three to four times a day as prescribed for
depression. Take sustained-release forms twice a day, at least 8 hr apart. Do not
combine doses or make up missed doses. Take once a day, or divided into two
doses at least 8 hr apart for smoking cessation.
• Avoid or limit the use of alcohol while on this drug. Seizures can occur if these
are combined.
• These side effects may occur: Dizziness, lack of coordination, tremor (avoid
driving or performing tasks that require alertness); dry mouth (use frequent mouth
care; suck sugarless lozenges); headache, insomnia (consult with care provider if
these become a problem; do not self-medicate); nausea, vomiting, weight loss (eat
small, frequent meals).
• May be used with transdermal nicotine; most effective for smoking cessation if
combined with behavioral support program.
• Report dark urine, light-colored stools; rapid or irregular heart beat;
hallucinations; severe headache or insomnia; fever, chills, sore throat.

Adverse effects in Italic are most common; those in Bold are life-threatening.