Generic Name : bupropion hydrochloride
Brand Name: Wellbutrin, Wellbutrin SR, Wellbutrin XL, Zyban
Classification: Antidepressant, Smoking deterrent
Pregnancy Category B
Dosage & Route
- Smoking cessation
- Adult: Modified-release preparation: Initially, 150 mg once daily for 6 days then increased to 150 mg bid. Period of treatment: 7-12 wk. To discontinue treatment if abstinence is not achieved by 7th wk. Max: 300 mg/day.
- Elderly: 150 mg/day.
- Adult: Initially, 100 mg bid increased to 100 mg tid after 3 days if necessary. Increased further to 150 mg tid if no improvement has been observed after several wk of therapy. Max: 150 mg tid. As a modified-release preparation: 150 mg once daily in the morning, increased to 150 mg bid after 3 days if necessary, may further increase to 200 mg bid after several wk if needed. Max: 450 mg as a single dose.
- Bupropion HCl is a relatively weak inhibitor of the neuronal uptake of norepinephrine, serotinin and dopamine. The mechanism by which it aids in smoking cessation is presumed to be mediated by its noradrenergic and/or dopaminergic actions.
- Absorption: Well absorbed from the GI tract but undergoes extensive first pass effect.
- Distribution: ≥80% bound to plasma proteins. Crosses the placenta and distributed into breast milk.
- Excretion: Terminal half-life of immediate-release preparation: about 14 hr. Mainly excreted in the urine as metabolites.
- Treatment of depression
- Aid to smoking cessation treatment (Zyban)
- Unlabeled uses: Treatment of neuropathic pain, ADHD
- Facial edema; nausea, dry mouth, constipation, diarrhea, anorexia; mouth ulcer; thirst; myalgia, arthralgia; insomnia, dream, abnormality, anxiety, disturbed concentration, dizziness, nervousness, tremor, dysphoria; rhinitis, increased cough, pharyngitis, sinusitis; dyspnea, epistaxis, agitation, insomnia, tremor, headache, weight loss, vomiting, skin rash.
- Potentially Fatal: Stevens-Johnson syndrome.
- Epilepsy; eating disorders (e.g. bulimia or anorexia nervosa); hypersensitivity.
- History: Hypersensitivity to bupropion, history of seizure disorder, bulimia or anorexia, head trauma, CNS tumor, treatment with MAOI, renal or hepatic 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 hepatic and renal function tests in patients with a history of hepatic or renal impairment.
- Have patient quit smoking within first 2 wk of treatment for smoking cessation; may be used with transdermal nicotine.
- BLACK BOX WARNING: Monitor response and behavior; suicide is a risk in depressed patients, children, and adolescents.
- 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 hours apart. Do not combine doses or make up missed doses. Take once a day, or divided into two doses at least 8 hours 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 heartbeat; hallucinations; severe headache or insomnia; fever, chills, sore throat.