Bupropion SR: Effective Relief for Major Depressive Disorder
Bupropion
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Bupropion SR (sustained-release) is a widely prescribed antidepressant belonging to the aminoketone class, distinct from SSRIs and SNRIs. It functions primarily as a norepinephrine–dopamine reuptake inhibitor (NDRI), offering a unique mechanism of action for managing major depressive disorder. This formulation provides steady plasma concentrations over 12 hours, supporting consistent therapeutic effect with twice-daily dosing. Clinicians often favor bupropion SR for its favorable side effect profile, particularly the low incidence of sexual dysfunction and weight gain associated with other antidepressants.
Features
- Sustained-release formulation for stable drug delivery
- Available in 100 mg, 150 mg, and 200 mg tablet strengths
- White to off-white, round, biconvex film-coated tablets
- NDRI mechanism targeting norepinephrine and dopamine
- Bioavailability of approximately 87% with high protein binding
- Median time to peak plasma concentration: 3 hours
- Half-life of approximately 21 hours (±9 hours)
Benefits
- Redymptoms of depression with minimal sexual side effects
- Lower risk of weight gain compared to many antidepressants
- May improve energy, motivation, and concentration
- Does not typically cause sedation or significant serotonin-related effects
- Suitable for long-term maintenance therapy
- May aid smoking cessation as an off-label benefit
Common use
Bupropion SR is indicated for the treatment of major depressive disorder (MDD) in adults. It is also used off-label for seasonal affective disorder, attention deficit hyperactivity disorder (ADHD), and as an aid to smoking cessation. The sustained-release formulation is particularly valuable for patients who require steady-state plasma concentrations to maintain stable mood throughout the day, and for those who have experienced undesirable effects with serotonin-focused antidepressants.
Dosage and direction
The initial recommended dose is 150 mg once daily in the morning. After at least 3 days, the dose may be increased to 150 mg twice daily, with at least 8 hours between doses. The maximum recommended dose is 400 mg per day, given as 200 mg twice daily. Tablets should be swallowed whole and not crushed, chewed, or divided. Administration with food may decrease the incidence of gastrointestinal side effects. Dose adjustments are necessary in patients with hepatic or renal impairment.
Precautions
Patients should be monitored for worsening depression, suicidality, or unusual changes in behavior, particularly during initial treatment or dose adjustments. Bupropion SR may lower the seizure threshold; caution is advised in patients with history of seizure, head trauma, or eating disorders. Use cautiously in patients with hepatic or renal impairment, and in those taking medications that affect hepatic enzymes. Blood pressure monitoring is recommended due to potential hypertensive effects. Avoid alcohol consumption during treatment.
Contraindications
Bupropion SR is contraindicated in patients with seizure disorder or history of epilepsy. It should not be used in patients with current or prior diagnosis of bulimia or anorexia nervosa due to increased seizure risk. Concomitant use with MAO inhibitors is contraindicated; a 14-day washout period is required when switching between these medications. Hypersensitivity to bupropion or any component of the formulation prohibits use. Not recommended for patients undergoing abrupt discontinuation of alcohol or sedatives.
Possible side effects
Common side effects (≥1%) include dry mouth, nausea, insomnia, dizziness, headache, constipation, and increased sweating. Less frequently, patients may experience tremor, blurred vision, tachycardia, rash, or weight changes. Serious side effects requiring immediate medical attention include seizures, allergic reactions, hypertension, hallucinations, and suicidal thoughts. Approximately 10% of patients discontinue treatment due to adverse effects, most commonly insomnia and headache.
Drug interaction
Bupropion SR is metabolized primarily by CYP2B6 and inhibits CYP2D6. Significant interactions occur with MAO inhibitors (contraindicated), other antidepressants, antipsychotics, beta-blockers, and antiarrhythmics. Concurrent use with drugs that lower seizure threshold (e.g., antipsychotics, antidepressants, steroids) increases seizure risk. Caution with drugs that affect hepatic enzymes (e.g., ritonavir, carbamazepine) may require dose adjustment. Avoid concomitant use with levodopa and amantadine.
Missed dose
If a dose is missed, take it as soon as remembered unless it is close to the next scheduled dose. Do not double the dose to make up for a missed one. If remembering becomes a consistent issue, consider using a pill organizer or alarm system. Consistent timing maintains stable plasma concentrations and therapeutic effect.
Overdose
Bupropion overdose may cause seizures, hallucinations, sinus tachycardia, and cardiac arrest. Other symptoms include nausea, vomiting, and loss of consciousness. Fatalities have occurred with doses exceeding 4,500 mg. Management includes gastric lavage if presented early, activated charcoal, and supportive care with ECG monitoring. Benzodiazepines are first-line for seizure control. There is no specific antidote; treatment is symptomatic and supportive.
Storage
Store at room temperature (20-25°C or 68-77°F) in a dry place protected from light and moisture. Keep in the original container with the lid tightly closed. Do not store in bathroom or kitchen where humidity and temperature fluctuations may occur. Keep out of reach of children and pets. Properly dispose of expired or unused medication through take-back programs.
Disclaimer
This information is for educational purposes only and does not constitute medical advice. Always consult a healthcare professional before starting or changing medication. Individual response to bupropion SR may vary. Proper diagnosis and monitoring by a qualified physician are essential for safe and effective treatment. Not all side effects or interactions are listed here.
Reviews
Clinical studies demonstrate bupropion SR’s efficacy with response rates of 50-65% in major depressive disorder. Patients frequently report improved energy levels and fewer sexual side effects compared to SSRIs. Some note initial insomnia or anxiety that often resolves with continued use. Healthcare providers appreciate its unique mechanism and utility in treatment-resistant depression. Long-term studies support its safety profile for maintenance therapy up to 52 weeks.