Bupropion: A Leading Solution for Major Depressive Disorder
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Bupropion is a widely prescribed antidepressant belonging to the norepinephrine-dopamine reuptake inhibitor (NDRI) class, offering a distinct mechanism of action compared to traditional selective serotonin reuptake inhibitors (SSRIs). It is approved for the treatment of major depressive disorder (MDD), seasonal affective disorder (SAD), and as an aid to smoking cessation. Clinicians value bupropion for its favorable side effect profile, particularly the absence of significant weight gain or sexual dysfunction commonly associated with other antidepressants. Its efficacy, tolerability, and dual neurotransmitter activity make it a cornerstone in modern psychiatric pharmacotherapy.
Features
- Active ingredient: Bupropion hydrochloride
- Available formulations: Immediate-release (IR), sustained-release (SR), and extended-release (XL) tablets
- Mechanism: Norepinephrine-dopamine reuptake inhibitor (NDRI)
- FDA-approved indications: Major depressive disorder (MDD), seasonal affective disorder (SAD), smoking cessation
- Half-life: Approximately 21 hours (XL formulation), 12 hours (IR)
- Metabolism: Hepatic, primarily via CYP2B6
- Excretion: Renal (87%) and fecal (10%)
Benefits
- Effective relief from symptoms of depression, including low mood, anhedonia, and fatigue
- Lower incidence of sexual dysfunction and weight gain compared to SSRIs
- Supports smoking cessation by reducing nicotine cravings and withdrawal symptoms
- May improve focus, energy, and motivation due to its dopaminergic activity
- Suitable for long-term maintenance therapy in recurrent depression
Common use
Bupropion is primarily indicated for the treatment of major depressive disorder in adults. It is also prescribed for preventing seasonal affective disorder and as a non-nicotine aid for smoking cessation. Off-label uses may include attention-deficit/hyperactivity disorder (ADHD), bipolar depression (with caution), and augmentation in treatment-resistant depression. It is typically used as monotherapy but may be combined with other antidepressants under specialist supervision.
Dosage and direction
Dosage must be individualized based on clinical response and tolerability. For MDD:
- Immediate-release: Initial dose 100 mg twice daily, may increase to 100 mg three times daily after at least 3 days; maximum 450 mg/day in divided doses.
- Sustained-release: Initial dose 150 mg once daily in the morning, may increase to 150 mg twice daily after at least 3 days; maximum 400 mg/day.
- Extended-release: Initial dose 150 mg once daily in the morning, may increase to 300 mg once daily after at least 4 days; maximum 450 mg/day.
Tablets should be swallowed whole; do not crush, chew, or divide. Administer with or without food. For smoking cessation, begin treatment 1–2 weeks before the target quit date.
Precautions
- Risk of seizure: Dose-dependent; incidence increases at doses above 450 mg/day. Use with caution in patients with history of seizure, head trauma, CNS tumors, or eating disorders.
- Hypertension: Monitor blood pressure regularly, especially during dose escalation.
- Hepatic impairment: Use lower doses and titrate slowly in patients with severe hepatic cirrhosis.
- Renal impairment: Consider reduced dosing in severe renal impairment.
- Suicidal ideation: Monitor for worsening depression or emergent suicidality, particularly in adolescents and young adults.
- Angle-closure glaucoma: May precipitate acute attacks in susceptible individuals.
Contraindications
- Known hypersensitivity to bupropion or any component of the formulation
- Current or prior diagnosis of bulimia or anorexia nervosa
- Concomitant use of monoamine oxidase inhibitors (MAOIs); allow at least 14 days between discontinuation of an MAOI and initiation of bupropion
- Patients undergoing abrupt discontinuation of alcohol or sedatives
- History of seizure disorder
- Use of other bupropion-containing products
Possible side effect
Common (≥1%):
- Dry mouth
- Nausea
- Headache
- Insomnia
- Constipation
- Dizziness
- Tremor
- Sweating
Less common:
- Tinnitus
- Rash
- Agitation
- Tachycardia
- Weight loss
- Blurred vision
Serious (seek medical attention):
- Seizures
- Severe allergic reactions (angioedema, Stevens-Johnson syndrome)
- Hypertension crisis
- Hallucinations or psychotic episodes
- Suicidal thoughts or behaviors
Drug interaction
- MAOIs: Risk of hypertensive crisis; contraindicated.
- Antidepressants (e.g., SSRIs, TCAs): Increased risk of serotonin syndrome.
- Antipsychotics: May lower seizure threshold.
- CYP2B6 inhibitors (e.g., ticlopidine, clopidogrel): Increase bupropion exposure.
- CYP2B6 inducers (e.g., ritonavir, carbamazepine): Decrease bupropion efficacy.
- Beta-blockers (e.g., metoprolol): Bupropion may increase their levels.
- Alcohol: Increases seizure risk; avoid or limit use.
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. For once-daily formulations (XL), if missed, take the next dose at the regular time. Consistent daily dosing is important to maintain steady-state plasma concentrations.
Overdose
Symptoms may include seizures, hallucinations, tachycardia, arrhythmias, hypotension, loss of consciousness, and fever. Fatal outcomes have been reported, particularly with large ingestions (>4 g). Management is supportive and symptomatic; ensure airway protection, administer activated charcoal if presented early, and treat seizures with benzodiazepines. ECG monitoring is essential. There is no specific antidote.
Storage
Store at room temperature (20–25°C/68–77°F), in a tightly closed container, away from light, moisture, and heat. Keep out of reach of children and pets. Do not use beyond the expiration date printed on the packaging.
Disclaimer
This information is for educational purposes only and does not constitute medical advice. Always consult a qualified healthcare provider for diagnosis, treatment decisions, and individualized dosing. Do not initiate or discontinue bupropion without professional supervision. Full prescribing information is available in the package insert or from the manufacturer.
Reviews
Clinical studies and meta-analyses consistently demonstrate bupropion’s efficacy in treating depression, with response rates comparable to SSRIs. Patients often report improved energy levels and fewer sexual side effects. In smoking cessation trials, bupropion doubles abstinence rates compared to placebo. However, individual experiences vary; some report initial anxiety or insomnia, which often subside with continued use. Long-term data support its safety and effectiveness for maintenance therapy.