Bupropion SR (sustained-release) is a prescription medication primarily indicated for the treatment of major depressive disorder and as an aid to smoking cessation. As a norepinephrine-dopamine reuptake inhibitor (NDRI), it offers a distinct mechanism of action compared to traditional SSRIs, making it a valuable option for patients who may not tolerate or respond adequately to other antidepressants. Its sustained-release formulation ensures stable plasma concentrations, supporting consistent therapeutic effects with twice-daily dosing. This profile provides a comprehensive overview of its clinical use, benefits, and safety considerations for healthcare professionals and informed patients.

Features

• Active ingredient: Bupropion hydrochloride
• Dosage form: Sustained-release (SR) oral tablets
• Available strengths: 100 mg, 150 mg, 200 mg
• Mechanism: Norepinephrine-dopamine reuptake inhibitor (NDRI)
• Dosing frequency: Typically twice daily
• Bioavailability: Approximately 85%
• Half-life: 21 hours (± 9 hours)
• Metabolism: Hepatic, primarily via CYP2B6
• Excretion: Renal (87%) and fecal (10%)

Benefits

• Effective reduction of depressive symptoms with a unique mechanism of action
• Supports smoking cessation by reducing nicotine cravings and withdrawal symptoms
• Generally associated with less sexual dysfunction and weight gain than SSRIs
• May improve energy levels and focus due to its dopaminergic activity
• Sustained-release formulation provides stable drug levels and improved compliance
• Non-habit forming when used as prescribed for depression treatment

Common use

Bupropion SR is FDA-approved for the treatment of major depressive disorder (MDD) and as an aid to smoking cessation. In depression management, it is particularly valuable for patients who experience SSRI-associated sexual dysfunction or excessive sedation. For smoking cessation, it helps reduce nicotine cravings and withdrawal symptoms when used as part of a comprehensive cessation program. Off-label uses may include attention deficit hyperactivity disorder (ADHD) and seasonal affective disorder, though these applications require careful medical supervision.

Dosage and direction

For depression: Initial dose is 150 mg once daily in the morning, increasing after 3 days to 150 mg twice daily (with at least 8 hours between doses). Maximum dose is 400 mg daily, given as 200 mg twice daily. For smoking cessation: Begin with 150 mg once daily for 3 days, then increase to 150 mg twice daily. Treatment should continue for 7-12 weeks as part of a comprehensive cessation program. Tablets should be swallowed whole and not crushed, chewed, or divided. Doses should be taken at the same times each day to maintain steady blood levels.

Precautions

Patients should be monitored for emergence of anxiety, agitation, panic attacks, insomnia, irritability, hostility, aggressiveness, impulsivity, akathisia, hypomania, and mania. Use with caution in patients with hepatic or renal impairment, and dose adjustment may be necessary. May lower seizure threshold; use cautiously in patients with history of seizure, head trauma, or eating disorders. May increase blood pressure; monitor regularly during treatment. Use caution when operating machinery until response to therapy is known. Abrupt discontinuation should be avoided; taper gradually when discontinuing treatment.

Contraindications

Bupropion SR is contraindicated in patients with seizure disorder or history of seizures. Contraindicated in patients with current or prior diagnosis of bulimia or anorexia nervosa due to increased seizure risk. Should not be used concomitantly with monoamine oxidase inhibitors (MAOIs) or within 14 days of discontinuing MAOI treatment. Contraindicated in patients undergoing abrupt discontinuation of alcohol or sedatives. Not recommended for patients with known hypersensitivity to bupropion or any component of the formulation.

Possible side effects

Common side effects (≥10%) include dry mouth, nausea, insomnia, dizziness, and headache. Less common effects (1-10%) include constipation, anxiety, agitation, tremor, sweating, tinnitus, taste disturbance, and weight loss. Serious side effects requiring medical attention include seizures (dose-related), allergic reactions, hypertension, hallucinations, confusion, and severe skin reactions. Sexual side effects are generally less frequent than with SSRIs. Most side effects are dose-dependent and may diminish with continued treatment.

Drug interaction

MAOIs: Risk of hypertensive crisis—contraindicated within 14 days of MAOI use. CYP2B6 inhibitors (e.g., ticlopidine, clopidogrel) may increase bupropion levels. Bupropion inhibits CYP2D6 and may increase levels of drugs metabolized by this enzyme (e.g., antidepressants, antipsychotics, beta-blockers, type 1C antiarrhythmics). May potentiate effects of levodopa and amantadine. Use caution with other drugs that lower seizure threshold. Alcohol may increase risk of neuropsychiatric events. Nicotine replacement therapy may increase hypertension risk.

Missed dose

If a dose is missed, take it as soon as remembered unless it is almost time for the next dose. In that case, skip the missed dose and resume the regular dosing schedule. Do not double the dose to make up for a missed dose. Taking two doses too close together may increase the risk of side effects, including seizures. If multiple doses are missed, contact a healthcare provider for guidance on resuming therapy.

Overdose

Symptoms may include seizures, hallucinations, loss of consciousness, sinus tachycardia, and ECG changes (e.g., QRS prolongation). Fatal outcomes have been reported, often involving multiple drug ingestion. Management includes supportive care with attention to maintaining airway and monitoring cardiac function. Gastric lavage may be considered if presentation is early. Activated charcoal may be effective. Seizures should be treated with benzodiazepines; status epilepticus may require additional anticonvulsants. There is no specific antidote; hemodialysis is not likely to be beneficial.

Storage

Store at room temperature (20-25°C or 68-77°F) in a dry place. Keep in the original container with the lid tightly closed. Protect from light and moisture. Do not store in bathroom or kitchen where humidity and temperature variations may occur. Keep out of reach of children and pets. Properly dispose of expired or unused medication through medication take-back programs or according to FDA guidelines.

Disclaimer

This information is for educational purposes only and does not constitute medical advice. Always consult with a qualified healthcare professional before starting, changing, or stopping any medication. Individual response to medication may vary. Only a healthcare provider can determine the appropriate treatment based on individual medical history, current health status, and specific needs. Do not disregard professional medical advice or delay seeking it because of information contained herein.

Reviews

Clinical studies demonstrate bupropion SR’s efficacy in depression treatment with response rates comparable to SSRIs. In smoking cessation trials, approximately 30-35% of patients achieve continuous abstinence at one year follow-up. Many patients report preference over SSRIs due to lower incidence of sexual dysfunction and weight gain. Some users note initial side effects like insomnia and dry mouth that often diminish with continued use. Healthcare providers appreciate its unique mechanism and utility in treatment-resistant cases. However, individual experiences vary, and careful patient selection and monitoring are essential for optimal outcomes.