(byoo proe‘ pee on)
- Wellbutrin SR
- Wellbutrin XL
- Smoking deterrent
- Pregnancy Category B
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 norepinephrineand inhibits the reuptake of dopamine to some extent.
- 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.
Tablets—75, 100 mg; SR tablets—100, 150, 200 mg; ER tablets—150, 300 mg
- 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.
Safety and efficacy in children < 18 yr not established.
Bupropion is excreted through the kidneys; use with caution, and monitor older patients carefully.
|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: 14 hr; 21 hr (SR)
Distribution: May cross placenta; may enter breast milk
Excretion: Urine and feces
- 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
- 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
- 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
- Give 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 four times a day 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.
- 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.
- WARNING: Monitor response and behavior; suicide is a risk in depressed patients.
- Take this drug in equally divided doses three to four times a day as prescribed for depression. Take SR 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.
- May be used with transdermal nicotine; most effective for smoking cessation if combined with behavioral support program.
- You may experience these side effects: 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 frequent small meals).
- Report dark urine, light-colored stools; rapid or irregular heart beat; hallucinations; severe headache or insomnia; fever, chills, sore throat.