THERAPEUTICS

Brands

• Wellbutrin, Wellbutrin SR, Wellbutrin XL, Aplenzin, Forfivo XL, Zyban, Contrave

Generic?

• Yes

Class

• Atypical antidepressant

Commonly Prescribed for

(FDA approved in bold)

• Major depressive disorder

• Seasonal affective disorder (Wellbutrin XL only)

• Smoking cessation (Zyban only)

• Weight loss (Contrave only)

• Neuropathic pain

• Attention deficit hyperactivity disorder

• Hypoactive sexual desire disorder

• Methamphetamine withdrawal

How the Drug Works

• Both bupropion and its metabolite (hydroxybupropion; half as potent as bupropion) inhibit reuptake of norepinephrine and dopamine

• It also blocks nicotinic acetylcholine receptors

• It does not block reuptake of serotonin nor inhibit monoamine oxidase

How Long Until It Works

• It may take more than 1 month for full effect

If It Works

• Continue to use and monitor for AEs. May continue for 1 year following first depression episode or indefinitely if > 1 episode of depression

If It Doesn't Work

• Increase to highest tolerated dose. Change to another agent or add a second agent

Best Augmenting Combos for Partial Response or Treatment-Resistance

• Low-dose polytherapy with 2 or more drugs may be better tolerated and more effective than high-dose monotherapy

Tests

• Not available. Monitor blood pressure, seizures, suicidality, and unusual psychiatric behavior

ADVERSE EFFECTS (AEs)

How the Drug Causes AEs

• By increasing dopamine and norepinephrine concentrations at non-therapeutic responsive receptors throughout the body. Most AEs are dose- and time-dependent

Notable AEs

• ≥ 5%: agitation, dry mouth, constipation, headache, nausea, vomiting, dizziness, hyperhidrosis, tremor, insomnia, blurred vision, tachycardia, confusion, rash, hostility, cardiac arrhythmia, hypertension, auditory disturbance

Life-Threatening or Dangerous AEs

• Worsening of depression and suicidality

• Rare hepatitis

• Rare activation of mania or suicidal ideation

• Rare worsening of coexisting seizure disorders

Weight Gain

• Unusual

Sedation

• Unusual

What to Do About AEs

• For minor AEs, lower dose, titrate slower, or switch to another agent. For serious AEs, lower dose and consider stopping, taper to avoid withdrawal symptoms