Bupropion extended-release tablets for major depressive disorder and seasonal affective disorder

Bupropion hydrochloride extended-release tablets (XL) are a prescription antidepressant medication approved for treating major depressive disorder (MDD) and preventing seasonal depressive episodes in patients with seasonal affective disorder (SAD). They work as an aminoketone antidepressant and are taken orally once daily.

Approved uses:

• Major depressive disorder (MDD): Treatment of MDD in adults, as defined by the Diagnostic and Statistical Manual (DSM).
• Seasonal affective disorder (SAD): Prevention of seasonal major depressive episodes in adults with a history of seasonal MDD episodes, typically starting treatment in autumn before symptoms begin and continuing through winter.

Bupropion hydrochloride

Bupropion is an aminoketone antidepressant believed to exert its effects by influencing the balance of neurotransmitters in the brain involved in mood regulation, although the exact mechanism is not fully established.

General dosing instructions

• Swallow tablets whole; do not crush, chew, or divide.
• Administer in the morning, with or without food.
• Increase the dose gradually to reduce seizure risk.

Major Depressive Disorder (MDD)

• Start at 150 mg once daily.
• After 4 days, may increase to 300 mg once daily.
• Maintenance dose and duration should be periodically reassessed and individualized.

Seasonal Affective Disorder (SAD)

• Start at 150 mg once daily, initiated in autumn before symptom onset.
• After 7 days, may increase to 300 mg once daily.
• Continue treatment throughout the winter season.
• In early spring, taper dose from 300 mg to 150 mg once daily prior to discontinuation.
• Doses above 300 mg were not studied for SAD.

Use in hepatic impairment

• Moderate to severe impairment (Child-Pugh 7-15): Limit to 150 mg every other day.
• Mild impairment (Child-Pugh 5-6): Consider dose/frequency reduction.

Use in renal impairment

• Consider reducing dose and/or frequency in patients with glomerular filtration rate below 90 mL/min.

Switching and discontinuation

• When switching from other bupropion formulations, use equivalent total daily dose.
• Before stopping treatment at 300 mg/day, reduce to 150 mg once daily.
• Allow at least 14 days between stopping monoamine oxidase inhibitors (MAOIs) and starting bupropion, and vice versa.
• Do not start bupropion concurrently with reversible MAOIs such as linezolid or intravenous methylene blue.

• Seizure disorder
• Current or prior diagnosis of bulimia or anorexia nervosa
• Abrupt discontinuation of alcohol, benzodiazepines, barbiturates, or antiepileptic drugs
• Use with MAOIs intended to treat psychiatric disorders or within 14 days before or after bupropion
• Concomitant use with reversible MAOIs such as linezolid or intravenous methylene blue
• Hypersensitivity to bupropion or any tablet ingredients

Suicidal thoughts and behaviors

Antidepressants, including bupropion, increase the risk of suicidal ideation and behavior in children, adolescents, and young adults (up to age 24) during short-term treatment. There is no increased risk in adults over 24; adults 65 and older demonstrated reduced risk. Close monitoring for worsening depression and suicidal thoughts is essential, especially during treatment initiation and dose changes.

Seizure risk

Bupropion can cause seizures; this risk increases with higher doses. Do not exceed 300 mg once daily for the extended-release formulation. Dose escalation should be gradual, and treatment discontinued if a seizure occurs.

Hypertension

Monitor blood pressure before and during treatment as bupropion may increase blood pressure.

Neuropsychiatric reactions

Serious events such as mood changes, psychosis, hallucinations, paranoia, aggression, agitation, anxiety, and suicidality have been reported, including in patients using bupropion for smoking cessation (not this product). Stop medication and seek medical help if these symptoms appear.

Activation of mania/hypomania

Screen for bipolar disorder and monitor for symptoms.

Angle-closure glaucoma

Use cautiously in patients with untreated narrow-angle glaucoma.

Common side effects

• Insomnia
• Dry mouth
• Headache
• Nausea

Serious side effects

• Seizures
• Hypertension
• Serious allergic reactions, including anaphylaxis and Stevens-Johnson syndrome
• Neuropsychiatric symptoms including suicidal thoughts, psychosis, mania, and aggression

• Monoamine oxidase inhibitors (MAOIs): Contraindicated if used together or within 14 days of each other due to risk of hypertensive crisis.
• Reversible MAOIs (e.g., linezolid, intravenous methylene blue): Do not start bupropion in patients on these agents; discontinue bupropion before initiating them if alternatives are unavailable.
• Drugs that lower seizure threshold or increase bupropion levels may increase seizure risk.