Bupropion: Effective Relief for Depression and Smoking Cessation
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Bupropion is a widely prescribed antidepressant medication belonging to the norepinephrine-dopamine reuptake inhibitor (NDRI) class. It is primarily indicated for the treatment of major depressive disorder (MDD) and to support smoking cessation. Unlike many other antidepressants, bupropion has a unique mechanism of action that avoids significant serotonergic activity, which contributes to its distinct side effect profile. It is available in various formulations, including immediate-release, sustained-release (SR), and extended-release (XL), allowing for tailored therapeutic approaches based on individual patient needs and tolerability.
Features
- Active ingredient: Bupropion hydrochloride
- Available formulations: Immediate-release (IR), sustained-release (SR), extended-release (XL)
- Standard strengths: 75 mg, 100 mg, 150 mg, 200 mg, 300 mg
- Administration: Oral tablet
- Prescription status: Schedule IV controlled substance in some jurisdictions due to abuse potential
- Half-life: Approximately 21 hours (XL formulation), 12 hours (IR formulation)
- Metabolism: Hepatic, primarily via CYP2B6
- Excretion: Renal
Benefits
- Effectively alleviates symptoms of major depressive disorder by enhancing norepinephrine and dopamine activity in the brain.
- Supports smoking cessation by reducing nicotine cravings and withdrawal symptoms, doubling the chances of quitting successfully compared to placebo.
- Lacks significant serotonergic effects, minimizing sexual dysfunction and weight gain commonly associated with SSRIs and SNRIs.
- May improve energy levels, focus, and motivation in some patients due to its dopaminergic activity.
- Can be used as an adjunctive treatment for seasonal affective disorder (SAD) and off-label for ADHD.
Common use
Bupropion is FDA-approved for the treatment of major depressive disorder (MDD) and as an aid to smoking cessation treatment. It is also commonly used off-label for attention-deficit/hyperactivity disorder (ADHD), seasonal affective disorder (SAD), and as an augmenting agent in treatment-resistant depression. The extended-release formulation (XL) is additionally approved for preventing major depressive episodes in patients with seasonal affective disorder.
Dosage and direction
For major depressive disorder: The initial dose is typically 100 mg twice daily (IR), 150 mg once daily (SR), or 150 mg once daily (XL). Dosage may be increased to a maximum of 450 mg/day (IR), 400 mg/day (SR), or 450 mg/day (XL) based on clinical response and tolerability. For smoking cessation: Initiate with 150 mg once daily for 3 days, then increase to 150 mg twice daily (SR formulation). Treatment should continue for 7-12 weeks as part of a comprehensive smoking cessation program. All doses should be taken with food to minimize gastrointestinal upset. Tablets should be swallowed whole and not crushed, chewed, or divided.
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 history of seizure disorder, cranial trauma, or conditions that lower seizure threshold. May increase blood pressure; regular monitoring recommended. Use cautiously in patients with hepatic or renal impairment, requiring dosage adjustment. May cause weight loss; monitor nutritional status in underweight patients. Not recommended during acute phase of myocardial infarction.
Contraindications
Hypersensitivity to bupropion or any component of the formulation. Current or prior diagnosis of bulimia or anorexia nervosa. Concomitant use with monoamine oxidase inhibitors (MAOIs); allow at least 14 days between discontinuation of MAOI and initiation of bupropion. Patients undergoing abrupt discontinuation of alcohol or sedatives. History of seizure disorder. Use of other formulations containing bupropion.
Possible side effects
Common (≥1%): Dry mouth, nausea, constipation, headache, dizziness, insomnia, tremor, sweating, tinnitus, blurred vision. Less common: Anxiety, agitation, tachycardia, hypertension, rash, weight loss, taste perversion. Serious: Seizures (dose-dependent), allergic reactions, angioedema, Stevens-Johnson syndrome, hallucinations, psychosis, suicidal ideation (particularly in young adults), hepatitis, hypoglycemia.
Drug interaction
MAOIs: Risk of hypertensive crisis. Antipsychotics, antidepressants, tramadol: Lowered seizure threshold. Drugs metabolized by CYP2D6 (e.g., beta-blockers, SSRIs, antipsychotics): Bupropion may increase their plasma concentrations. Carbamazepine, phenobarbital, phenytoin: May decrease bupropion levels. Alcohol: Increases seizure risk. Nicotine replacement therapy: May increase hypertension risk. Levodopa, amantadine: Increased dopaminergic effects.
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 twice-daily regimens, if missed and next dose is due within 4 hours, skip the missed dose. For once-daily regimens, take when remembered unless next dose is due within 8 hours.
Overdose
Symptoms may include seizures, hallucinations, loss of consciousness, sinus tachycardia, ECG changes (e.g., QRS prolongation), fever, muscle rigidity, rhabdomyolysis, and respiratory failure. Fatal outcomes have been reported, particularly with mixed overdoses. Management includes supportive care, ECG monitoring, and control of seizures with benzodiazepines. Gastric lavage may be considered if presented early. There is no specific antidote.
Storage
Store at room temperature (20-25°C or 68-77°F). Keep in original container, tightly closed. Protect from light and moisture. Do not store in bathroom or other humid areas. 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 with a qualified healthcare professional before starting, changing, or stopping any medication. Individual response to bupropion may vary. Not all side effects or interactions are listed here. Proper diagnosis and monitoring by a healthcare provider are essential for safe and effective treatment.
Reviews
Clinical studies demonstrate bupropion’s efficacy in depression treatment with response rates comparable to SSRIs. Smoking cessation trials show approximately 30% continuous abstinence rates at end of treatment versus 16% for placebo. Patient reviews often highlight benefits for energy and motivation with fewer sexual side effects than other antidepressants, though some report initial anxiety or insomnia. Many successful quitters describe reduced cigarette cravings without weight gain. However, individual experiences vary significantly, and some patients report inadequate response or intolerable side effects requiring discontinuation.