Bupropion Hydrochloride

Bupropion Hydrochloride is an atypical antidepressant used for depression and smoking cessation. It is a selective inhibitor of neuronal catecholamine (norepinephrine and dopamine) reuptake, with minimal effect on indolamine (serotonin) reuptake, and does not inhibit monoamine oxidase.

While the mechanism of action as an antidepressant is not fully understood, it is presumed to be mediated by noradrenergic and/or dopaminergic mechanisms. In smoking cessation, it reduces nicotine withdrawal symptoms and craving through noradrenergic and dopaminergic actions.

• Depression
• Smoking cessation

Adults (Depression - Immediate-release): Initially 100 mg twice daily; if needed, increase to 100 mg three times daily after 3 days; further increase to 150 mg three times daily if no improvement after several weeks. Max: 150 mg three times daily.

Adults (Depression - Modified-release/Sustained-release): Initially 150 mg once daily in the morning; if needed, increase to 150 mg twice daily after 3 days; further increase to 200 mg twice daily if needed after several weeks. Max: 450 mg/day (as a single dose).

Adults (Smoking cessation - Modified-release): Initially 150 mg once daily for 6 days, then 150 mg twice daily. Treatment duration: 7-12 weeks. Discontinue if abstinence not achieved by week 7. Max: 300 mg/day.

Elderly (Depression - Immediate-release): Initially 37.5 mg twice daily.

Elderly (Depression - Sustained-release): Initially 100 mg/day; increase by 37.5-100 mg every 3-4 days. Max: 300 mg/day in divided doses.

Hepatic impairment: Mild-moderate: Reduce dose or dosing frequency. Severe (immediate-release): Max 75 mg once daily; (modified-release): Max 100 mg once daily or 150 mg every other day.

Renal impairment: Caution; consider dose reduction.

Children and adolescents (under 18 years): Not recommended.

Common side effects: Insomnia, allergic reaction, impaired concentration, sweating, headache, nausea, vomiting, dizziness, dry mouth, taste change, abdominal pain, agitation, anxiety, fever, constipation, tremor.

Hypersensitivity reactions: Pruritus, urticaria, angioedema, dyspnea, anaphylactoid reactions (rare).

Serious (rare): Seizures (dose-dependent; higher risk with history of seizures, bulimia/anorexia, abrupt alcohol/benzodiazepine withdrawal, hepatic cirrhosis).

• Agitation, anxiety, and insomnia may occur during initial stages of therapy.
• Avoid alcohol (may lower seizure threshold).
• Inform your doctor if you notice sudden mood and behavior changes or develop suicidal thoughts.
• Caution in patients with history of seizure disorders, head trauma, diabetes, alcohol abuse, bulimia/anorexia, hepatic cirrhosis, CNS tumor.
• May cause dizziness and impaired concentration; know your response before driving.
• Wait 14 days between stopping MAO inhibitor and starting bupropion.
• Caution during pregnancy and lactation.

• Seizure disorder (epilepsy)
• Treatment with other medications containing bupropion (seizure risk is dose-dependent)
• Current or prior diagnosis of bulimia or anorexia nervosa (higher seizure incidence)
• Concurrent administration with MAO inhibitor (wait 14 days after MAO inhibitor discontinuation)
• Allergic response to bupropion or other ingredients

• MAO inhibitors: Concurrent use may cause acute toxicity and increased risk of fatality (potentially fatal); 14-day interval required.
• Alcohol, other antidepressants, antimalarials, antipsychotics, sedating antihistamines, quinolones, tramadol, theophylline, systemic corticosteroids: May lower seizure threshold; use with extreme caution.
• Neuroleptics, lithium, TCAs, benzodiazepine: Interactions.
• Levodopa: Increased risk of side effects.
• Fluoxetine: Reduced hepatic clearance.
• Carbamazepine, phenobarbital, phenytoin: May induce bupropion metabolism.
• Cimetidine, ritonavir: May inhibit bupropion metabolism.
• Orphenadrine, cyclophosphamide, ifosfamide: Interactions may occur.