What is the proper dosing and administration of Wellbutrin (bupropion) for smoking cessation and depression?

From the Guidelines

For smoking cessation, Wellbutrin (bupropion SR) is typically started at 150 mg once daily for 3 days, then increased to 150 mg twice daily for 7-12 weeks, as recommended by the most recent guidelines 1.

Proper Dosing and Administration

The treatment should begin 1-2 weeks before the quit date.

• The standard dosing information for bupropion is as follows:
  • Initiate dosing 1–2 weeks prior to quitting
  • Days 1–3: 150 mg orally, once daily
  • Day 4–12 weeks: 150 mg orally, twice daily, if tolerated
  • Maximum 300 mg per day
• For depression, Wellbutrin is available in three formulations:
  • Immediate-release (100-150 mg three times daily, maximum 450 mg/day)
  • Sustained-release (150 mg twice daily, maximum 400 mg/day)
  • Extended-release (150-300 mg once daily in the morning, maximum 450 mg/day)

Important Considerations

Treatment usually begins with a lower dose and gradually increases to minimize side effects.

• Wellbutrin works by inhibiting the reuptake of dopamine and norepinephrine, which helps regulate mood and reduce nicotine cravings.
• Common side effects include dry mouth, insomnia, headache, and nausea.
• Wellbutrin should be taken with food to minimize stomach upset, and doses should be spaced at least 8 hours apart to reduce seizure risk.
• It's contraindicated in patients with seizure disorders, eating disorders, or those taking MAOIs.
• Alcohol consumption should be minimized during treatment as it increases seizure risk, as noted in recent studies 1.

Key Points to Consider

• Bupropion reduces the seizure threshold and has a 0.1% seizure risk among those receiving the drug for smoking cessation 1.
• Neuropsychiatric effects have also been identified as a safety concern with bupropion, although to a lesser extent than varenicline 1.
• Recent meta-analyses do not show elevated risk of serious adverse cardiovascular effects as a result of bupropion use for smoking cessation 1.
• The most common adverse effects associated with drug discontinuation in clinical trials with bupropion have been tremor, rash, headache, and urticaria, with typical dropout rates attributed to adverse effects ranging from 7% to 12% 1.

From the FDA Drug Label

The initial bupropion dose was 150 mg once daily for 1 week, followed by up-titration to 300 mg once daily. Although there are no independent trials demonstrating the efficacy of bupropion hydrochloride extended-release tablets (XL) in the acute treatment of MDD, studies have demonstrated similar bioavailability between the immediate-, sustained-, and extended-release formulations of bupropion HCl under steady-state conditions

The proper dosing and administration of Wellbutrin (bupropion) for depression is an initial dose of 150 mg once daily for 1 week, followed by up-titration to 300 mg once daily. For smoking cessation, the FDA drug label does not provide direct information on the dosing and administration of Wellbutrin (bupropion). 2 2 2

• Key points:
  • Initial dose for depression: 150 mg once daily for 1 week
  • Up-titration for depression: 300 mg once daily
  • No direct information for smoking cessation dosing and administration
• Important consideration: The FDA drug label does not provide direct information on the dosing and administration of Wellbutrin (bupropion) for smoking cessation.

From the Research

Proper Dosing and Administration of Wellbutrin (Bupropion)

• Wellbutrin (bupropion) is available as three oral formulations: immediate release (IR), sustained release (SR), and extended/modified release (XR) 3.
• For smoking cessation, a study used 300 mg of bupropion over a 4-week period combined with 12 weeks of nicotine patch application, resulting in a 69% abstinence rate after 6 months of follow-up 4.
• For depression, bupropion SR 150 mg administered either once or twice daily was more effective than placebo in treating depression, with once-daily dosing appearing to be at least as effective as twice-daily dosing 5.
• The combination therapy of varenicline and sustained release bupropion (bupropion SR) for cigarette smoking cessation can increase smoking abstinence rates, but has also been associated with increases in self-reported depressive symptoms 6.

Comparison of Bupropion with Other Medications

• Varenicline yielded a greater cessation rate at both 3 and 12 months compared to bupropion and/or placebo 7.
• Bupropion demonstrated a higher efficacy for cessation both at 3 and 12 months compared to placebo 7.
• The efficacy of bupropion XR in terms of primary efficacy measures was established in two of six well-designed placebo-controlled studies, and it was similar to the SSRI escitalopram in two placebo-controlled trials 3.

Administration and Efficacy

• Oral three-times-daily bupropion IR was effective and generally well tolerated in the treatment of major depressive disorder (MDD) 3.
• Twice-daily bupropion SR was also efficacious and generally well tolerated in the treatment of MDD, with a similar tolerability profile to some SSRIs but with less somnolence and sexual dysfunction 3.
• Bupropion XR was generally as well tolerated as escitalopram and venlafaxine XR, but was associated with less sexual dysfunction than escitalopram 3.