bupropion hcl (Wellbutrin)

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bupropion-hcl

Description

Bupropion HCl or Wellbutrin is an antidepressant and a smoking deterrent.

Generic Name

bupropion hydrochloride

(byoo proe pee on)

Brand Names

  • Wellbutrin
  • Wellbutrin SR
  • Wellbutrin XL
  • Zyban

Drug classes

  • Antidepressant
  • Smoking deterrent
  • Pregnancy Category B

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 norepinephrineand 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

RouteOnsetPeakDuration
OralVaries2 hr8–12 hr
SR OralVaries3 hr16–20 hr
ER OralVaries5 hr15–25 hr

Metabolism: Hepatic; T1/2: 14 hr; 21 hr (SR)

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

  • 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.

Teaching points

  • 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.

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