Bupropion SR: Effective Relief for Major Depressive Disorder
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Bupropion SR (sustained-release) is a prescription antidepressant medication belonging to the aminoketone class, distinct from many other agents due to its unique mechanism of action. It functions primarily as a norepinephrine–dopamine reuptake inhibitor (NDRI), modulating key neurotransmitters in the brain to help restore emotional balance. This formulation is designed for twice-daily dosing, providing stable plasma concentrations over a 12-hour period to support consistent therapeutic effect. It is indicated for the treatment of major depressive disorder (MDD) in adults and may also be used as part of a comprehensive smoking cessation treatment plan. Clinicians often consider bupropion SR when patients require an option with a lower risk of sexual side effects or weight gain compared to SSRIs.
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: Twice daily (approximately 12 hours apart)
- Bioavailability: Approximately 20% under fasting conditions
- Half-life: 21 hours (± 9 hours) for bupropion; active metabolites have longer half-lives
- Excretion: Primarily renal (87%) and fecal (10%)
Benefits
- Reduces symptoms of depression such as low mood, loss of interest, and fatigue
- Lower incidence of sexual dysfunction and weight gain compared to many SSRIs
- May improve concentration, energy, and motivation in some patients
- Can support smoking cessation efforts when used as part of a structured program
- Sustained-release formulation supports adherence with twice-daily dosing
- Does not typically cause significant sedation, allowing for daytime use
Common use
Bupropion SR is primarily prescribed for the treatment of major depressive disorder (MDD) in adults. It may be used as a first-line treatment, particularly when concerns about sexual side effects or weight gain are significant, or as an augmentation strategy when response to other antidepressants is inadequate. Additionally, it is FDA-approved as an aid to smoking cessation treatment, often under the brand name Zyban. Off-label uses may include attention-deficit/hyperactivity disorder (ADHD), bipolar depression (with mood stabilizer), and seasonal affective disorder, though these applications require careful clinical judgment and monitoring.
Dosage and direction
The initial recommended dose for bupropion SR is 150 mg once daily for the first three days, increasing to 150 mg twice daily (with at least 8 hours between doses) from day 4 onward. 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, as this could alter the release profile and increase the risk of adverse effects including seizures. Dosing should be consistent with regard to meals, though it may be taken with food to minimize gastrointestinal discomfort. Dose adjustments may be necessary in patients with hepatic or renal impairment, and elderly patients may require lower doses.
Precautions
Patients should be monitored for emerging anxiety, agitation, panic attacks, insomnia, irritability, hostility, aggressiveness, impulsivity, akathisia, hypomania, and mania, particularly during initial treatment and dose adjustments. There is an increased risk of suicidal thoughts and behaviors in children, adolescents, and young adults, particularly during early treatment; close supervision is essential. Use with caution in patients with a history of seizure disorder, cranial trauma, or conditions that lower seizure threshold. May elevate blood pressure; monitor regularly during treatment. Avoid use in patients with eating disorders (bulimia or anorexia nervosa) due to increased seizure risk.
Contraindications
Bupropion SR is contraindicated in patients with a seizure disorder or history of seizures. It must not be used in patients with a current or prior diagnosis of bulimia or anorexia nervosa due to the increased seizure risk. Concurrent use with monoamine oxidase inhibitors (MAOIs) is contraindicated; allow at least 14 days between discontinuing an MAOI and initiating bupropion SR. Hypersensitivity to bupropion or any component of the formulation is an absolute contraindication. Should not be used in patients undergoing abrupt discontinuation of alcohol or sedatives (including benzodiazepines).
Possible side effects
Common side effects (≥10%) include dry mouth, nausea, insomnia, dizziness, and headache. Less frequently (1-10%), patients may experience constipation, anxiety, agitation, tremor, sweating, tinnitus, blurred vision, tachycardia, hypertension, or weight loss. Serious but rare adverse effects include seizures (dose-dependent), allergic reactions, angle-closure glaucoma, hepatotoxicity, and severe skin reactions. Neuropsychiatric symptoms including suicidal ideation, hostility, and unusual behaviors have been reported. Any persistent or severe side effects should be reported to a healthcare provider immediately.
Drug interaction
Bupropion SR is a moderate inhibitor of CYP2D6 and may increase concentrations of drugs metabolized by this enzyme (e.g., certain antidepressants, antipsychotics, beta-blockers, and Type 1C antiarrhythmics). Concurrent use with other dopamine/norepinephrine-affecting drugs may increase the risk of adverse effects. MAOIs are absolutely contraindicated. May lower seizure threshold when combined with other drugs that predispose to seizures (e.g., antipsychotics, antidepressants, systemic corticosteroids). Use caution with drugs that affect hepatic metabolism. Alcohol consumption should be minimized or avoided due to increased seizure risk and potential for neuropsychiatric reactions.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is close to the time for the next scheduled dose. In that case, the missed dose should be skipped and the regular dosing schedule resumed. Doubling doses to make up for a missed dose is not recommended, as this may increase the risk of adverse effects including seizures. Patients should be advised to maintain a consistent dosing routine and use reminders if necessary to support adherence.
Overdose
Bupropion overdose may result in 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 requires immediate medical attention with supportive care, including airway protection and ECG monitoring. Gastrointestinal decontamination may be considered if presentation is early, though activated charcoal may be of limited benefit due to bupropion’s rapid absorption. Seizures should be managed with benzodiazepines; barbiturates or phenytoin may be considered if seizures persist. There is no specific antidote.
Storage
Store at room temperature (20-25°C or 68-77°F), with excursions permitted between 15-30°C (59-86°F). Keep in the original container, tightly closed, and protect from light and moisture. Do not store in bathrooms or other humid areas. Keep out of reach of children and pets. Dispose of unused medication properly through take-back programs or according to FDA guidelines; do not flush unless specifically instructed.
Disclaimer
This information is for educational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional for diagnosis and treatment decisions. Do not initiate, adjust, or discontinue medication without medical supervision. Individual response to bupropion SR may vary, and not all uses, precautions, or side effects may be listed here. Full prescribing information should be reviewed before use.
Reviews
Clinical studies demonstrate that bupropion SR is effective in reducing depressive symptoms, with response rates comparable to other antidepressants. Many patients report improved energy levels and minimal sexual side effects compared to SSRI alternatives. Some note initial side effects such as insomnia or dry mouth, which often diminish over time. Smoking cessation trials show significantly higher abstinence rates versus placebo. Critical reviews emphasize the importance of careful patient selection, particularly regarding seizure risk, and note that individual tolerance varies. Overall, it remains a valuable option within the antidepressant arsenal, particularly for patients prioritizing certain side effect profiles.