Bupropion: A Leading Antidepressant for Depression and Smoking Cessation
Bupropion
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Bupropion is a widely prescribed antidepressant medication belonging to the class of norepinephrine-dopamine reuptake inhibitors (NDRIs). It is primarily indicated for the treatment of major depressive disorder (MDD) and to aid in smoking cessation. Unlike many other antidepressants, bupropion does not significantly affect serotonin levels, which contributes to its distinct side effect profile and makes it a favorable option for patients who cannot tolerate serotonergic agents. Its dual mechanism of action enhances norepinephrine and dopamine neurotransmission, which is associated with improvements in mood, energy, and motivation.
Features
- Active ingredient: Bupropion hydrochloride
- Available formulations: Immediate-release (IR), sustained-release (SR), and extended-release (XL) tablets
- Mechanism of action: Norepinephrine-dopamine reuptake inhibitor (NDRI)
- FDA-approved indications: Major depressive disorder (MDD), seasonal affective disorder (SAD), and smoking cessation
- Half-life: Approximately 21 hours (bupropion XL)
- Metabolism: Hepatic, primarily via CYP2B6
- Excretion: Renal (87%) and fecal (10%)
Benefits
- Effective relief from symptoms of depression, including low mood, anhedonia, and fatigue
- Supports smoking cessation by reducing nicotine cravings and withdrawal symptoms
- Lower risk of sexual dysfunction compared to SSRIs and SNRIs
- Minimal weight gain, and may promote weight loss in some patients
- Does not cause sedation; may improve energy and focus
- Suitable for long-term maintenance therapy in depression
Common use
Bupropion is commonly prescribed for the management of major depressive disorder in adults. It is also utilized as an aid to smoking cessation treatment, helping individuals reduce their dependence on nicotine. Off-label uses may include attention-deficit/hyperactivity disorder (ADHD), bipolar depression (with caution due to seizure risk), and augmentation in treatment-resistant depression. It is not indicated for use in children or adolescents due to increased risk of suicidal ideation.
Dosage and direction
Dosage must be individualized based on clinical response and tolerability. For depression: The initial dose for bupropion XL is 150 mg once daily in the morning; may be increased to 300 mg once daily after 4 days if tolerated. Maximum dose is 450 mg per day, administered as a single dose. For smoking cessation: Begin with 150 mg once daily for 3 days, then increase to 150 mg twice daily (at least 8 hours apart). Treatment duration for smoking cessation is typically 7–12 weeks. Tablets should be swallowed whole; do not crush, chew, or divide. Take with or without food.
Precautions
Patients should be monitored for worsening depression, suicidal thoughts, or unusual changes in behavior, especially at the beginning of treatment or after dosage changes. Use with caution in patients with hepatic or renal impairment; dosage adjustment may be necessary. May lower seizure threshold; avoid in patients with history of seizure disorder, eating disorders, or undergoing abrupt discontinuation of alcohol or sedatives. May cause hypertension; monitor blood pressure regularly. Inform healthcare provider of all medications being taken.
Contraindications
Bupropion is contraindicated in patients with a known hypersensitivity to bupropion or any component of the formulation. It must not be used in individuals with a current or prior diagnosis of bulimia or anorexia nervosa due to increased seizure risk. Contraindicated in patients undergoing abrupt discontinuation of alcohol or sedatives (including benzodiazepines). Concomitant use with monoamine oxidase inhibitors (MAOIs) is contraindicated; allow at least 14 days between discontinuing an MAOI and initiating bupropion.
Possible side effect
Common side effects include dry mouth, nausea, headache, insomnia, tremor, and excessive sweating. Less frequently, patients may experience anxiety, dizziness, tinnitus, rash, or weight loss. Serious side effects requiring immediate medical attention include seizures, allergic reactions (e.g., angioedema, Stevens-Johnson syndrome), hypertension, hallucinations, and suicidal ideation. Incidence of sexual dysfunction is lower compared to SSRIs.
Drug interaction
Bupropion is a substrate of CYP2B6 and may interact with inhibitors (e.g., ticlopidine, clopidogrel) or inducers (e.g., ritonavir, carbamazepine) of this enzyme. Concomitant use with other dopaminergic agents (e.g., levodopa, amantadine) may increase risk of adverse effects. May potentiate effects of drugs that lower seizure threshold (e.g., antipsychotics, antidepressants, tramadol). Use caution with drugs metabolized by CYP2D6 (e.g., beta-blockers, SSRIs, antipsychotics), as bupropion is a strong inhibitor and may increase their plasma concentrations.
Missed dose
If a dose is missed, take it as soon as remembered unless it is close to the time of the next scheduled dose. Do not double the dose to make up for a missed one. For twice-daily regimens, if missed, skip and resume the regular dosing schedule. Consistent daily dosing is important for maintaining therapeutic effect.
Overdose
Overdose may lead to seizures, hallucinations, tachycardia, arrhythmias, fever, muscle rigidity, and loss of consciousness. Fatal outcomes have been reported, often involving multiple drug ingestion. Management is supportive and symptomatic; ensure airway protection and monitor vital signs. Activated charcoal may be considered if ingestion was recent. There is no specific antidote; seizures should be controlled with benzodiazepines. Contact a poison control center immediately.
Storage
Store at room temperature (20–25°C or 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 if tablets are discolored or show signs of deterioration. Dispose of unused medication via take-back programs or according to local regulations; do not flush.
Disclaimer
This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or medication. Do not disregard professional medical advice or delay in seeking it because of something you have read here.
Reviews
Clinical studies and patient reports indicate bupropion is effective for depression and smoking cessation, with many users appreciating its activating effects and lower incidence of weight gain and sexual side effects. Some note initial side effects like insomnia or anxiety, which often subside with continued use. Adherence to dosing instructions and regular follow-up with a healthcare provider are emphasized for optimal outcomes.