Bupropion: A Leading Antidepressant for Depression and Smoking Cessation

Bupropion

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 support smoking cessation. Unlike many other antidepressants, bupropion does not significantly affect serotonin levels, which contributes to its unique side effect profile, including a lower risk of sexual dysfunction and weight gain. Its mechanism involves increasing the availability of norepinephrine and dopamine in the brain, neurotransmitters associated with mood, motivation, and pleasure. This makes it a valuable option both as monotherapy and as an adjunct in treatment-resistant cases.

Features

  • Active ingredient: Bupropion hydrochloride
  • Available formulations: Immediate-release (IR), sustained-release (SR), and extended-release (XL) tablets
  • Therapeutic class: Norepinephrine-dopamine reuptake inhibitor (NDRI)
  • Common brand names: Wellbutrin, Zyban, Aplenzin
  • Prescription status: Available by prescription only
  • Standard strengths: 75 mg, 100 mg, 150 mg, 200 mg, 300 mg, 450 mg

Benefits

  • Effectively alleviates symptoms of major depressive disorder, including low mood, anhedonia, and fatigue.
  • Supports smoking cessation by reducing nicotine cravings and withdrawal symptoms.
  • Lower incidence of sexual side effects and weight gain compared to SSRIs and SNRIs.
  • May improve focus, energy, and motivation in certain patient populations.
  • Can be used as an augmentation strategy in treatment-resistant depression.
  • Non-addictive with no known abuse potential when used as prescribed.

Common use

Bupropion is FDA-approved for the treatment of major depressive disorder and as an aid to smoking cessation. Off-label uses include attention-deficit/hyperactivity disorder (ADHD), seasonal affective disorder (SAD), and bipolar depression (with caution due to seizure risk). It is often selected for patients who cannot tolerate the sexual side effects or weight gain associated with other antidepressants, or for those with comorbid nicotine dependence.

Dosage and direction

Dosage must be individualized based on clinical response and tolerability. For depression, the initial dose is typically 100 mg twice daily for immediate-release, 150 mg once daily for sustained-release, or 150 mg once daily for extended-release, with possible titration to a maximum of 450 mg per day. For smoking cessation, dosing usually begins at 150 mg once daily for three days, then increases to 150 mg twice daily, with treatment duration of 7–12 weeks. Tablets should be swallowed whole, not crushed or divided, and may be taken with or without food. Doses should be spaced to minimize the risk of seizures—avoid single doses exceeding 200 mg for immediate-release or 300 mg for sustained-/extended-release formulations.

Precautions

Patients should be monitored for emergence of anxiety, agitation, panic attacks, insomnia, irritability, hostility, impulsivity, akathisia, hypomania, mania, or suicidality, especially at treatment initiation or dose changes. Use with caution in patients with hepatic or renal impairment—dose adjustment may be necessary. Avoid use in patients with a history of seizures, eating disorders, or abrupt discontinuation of alcohol or sedatives. May cause elevated blood pressure; monitor periodically. Inform healthcare provider of all medications, including over-the-counter drugs and supplements.

Contraindications

Bupropion is contraindicated in patients with a seizure disorder or history of seizures. It must not be used in individuals with a current or prior diagnosis of bulimia or anorexia nervosa due to increased seizure risk. Concomitant use with monoamine oxidase inhibitors (MAOIs) is contraindicated; allow a 14-day washout period after discontinuing an MAOI before initiating bupropion. Hypersensitivity to bupropion or any component of the formulation is also a contraindication.

Possible side effects

Common side effects include dry mouth, nausea, headache, insomnia, dizziness, and constipation. Less frequently, patients may experience tremors, agitation, anxiety, sweating, tinnitus, or blurred vision. Serious side effects, though rare, include seizures, allergic reactions, hypertension, hallucinations, confusion, and severe skin reactions. Any unusual or severe symptoms should be reported to a healthcare provider immediately.

Drug interaction

Bupropion is metabolized primarily by CYP2B6 and may interact with drugs that inhibit or induce this enzyme. Concomitant use with other antidepressants, antipsychotics, systemic corticosteroids, theophylline, or tramadol may increase seizure risk. It may increase levels of drugs metabolized by CYP2D6, such as certain beta-blockers, antipsychotics, and antidepressants. Avoid use with MAOIs. Alcohol consumption may lower seizure threshold and should be minimized or avoided.

Missed dose

If a dose is missed, take it as soon as remembered unless it is close to the time of the next dose. In that case, skip the missed dose and resume the regular schedule. Do not double the dose to make up for a missed one, as this may increase the risk of adverse effects, including seizures.

Overdose

Overdose may lead to seizures, hallucinations, loss of consciousness, tachycardia, or cardiac arrest. Symptoms can include nausea, vomiting, and agitation. In case of suspected overdose, seek emergency medical attention immediately. Treatment is supportive and may include activated charcoal, anticonvulsants, and ECG monitoring.

Storage

Store at room temperature (20–25°C or 68–77°F), away from light, moisture, and heat. Keep in the original container, tightly closed, and out of reach of children and pets. Do not use beyond the expiration date.

Disclaimer

This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider for personalized recommendations and to discuss potential risks and benefits based on individual health status and history.

Reviews

Clinical studies and patient reports generally indicate bupropion is effective for depression and smoking cessation, with many users appreciating the lack of weight gain and sexual side effects. Some note initial side effects like insomnia or anxiety, which often subside with continued use. Effectiveness varies by individual; a healthcare provider can help determine if bupropion is appropriate.