Bupropion

1. Introduction

Bupropion is an atypical antidepressant that acts as a norepinephrine-dopamine reuptake inhibitor (NDRI). It is used for major depressive disorder (MDD), smoking cessation, and attention deficit hyperactivity disorder (ADHD) (off-label). Unlike SSRIs, bupropion does not cause sexual dysfunction or weight gain and has stimulant-like properties.

2. Indications

  • Major Depressive Disorder (MDD)
  • Seasonal Affective Disorder (SAD) (Depression Associated with Seasonal Changes)
  • Smoking Cessation (Helps Reduce Nicotine Cravings)

Off-Label Uses:

  • Attention Deficit Hyperactivity Disorder (ADHD)
  • Obesity (Appetite Suppression Effect)
  • Sexual Dysfunction (Caused by SSRIs or SNRIs)

3. Dosage

For Major Depressive Disorder (MDD):

  • Immediate-Release (IR):
    • Starting dose: 100 mg twice daily
    • Increase to: 100 mg three times daily (max 450 mg/day, divided doses)
  • Extended-Release (SR/XR):
    • Starting dose: 150 mg once daily
    • Increase to: 300 mg once daily
    • Max dose: 450 mg/day

For Smoking Cessation:

  • Start 150 mg once daily for 3 days, then increase to 150 mg twice daily.
  • Continue for 7–12 weeks; set a quit date within the first 2 weeks.

For ADHD (Off-Label):

  • 150 mg once daily, increase to 300 mg/day if needed.

Elderly (>65 years):

  • Start with 75 mg once daily, increase cautiously due to seizure risk.

Renal Impairment:

  • Reduce dose to 75 mg once daily (CrCl <30 mL/min).

Hepatic Impairment:

  • Mild-moderate: Reduce dose to 150 mg/day.
  • Severe: Use with caution, max 75 mg/day.

4. Administration

  • Take with or without food (food reduces nausea risk).
  • Avoid taking near bedtime (may cause insomnia).
  • Do not crush or chew extended-release tablets.

5. Forms Available

  • Immediate-Release (IR): 75 mg, 100 mg
  • Sustained-Release (SR): 100 mg, 150 mg, 200 mg
  • Extended-Release (XL): 150 mg, 300 mg

6. Side Effects

6.1 Common Side Effects:

  • Insomnia
  • Dry mouth
  • Anxiety or agitation
  • Headache
  • Nausea

6.2 Less Common Side Effects:

  • Increased sweating
  • Weight loss
  • Dizziness
  • Tremors

6.3 Rare but Serious Side Effects:

  • Seizures (especially at high doses >450 mg/day)
  • Suicidal thoughts (especially in young adults and adolescents)
  • Hypertension (especially when combined with nicotine patches)
  • Manic episodes (in bipolar disorder patients)

7. Warnings

  • Seizure Risk:
    • Avoid in patients with seizure disorders or conditions that lower seizure threshold (e.g., eating disorders, alcohol withdrawal, head trauma).
    • Do not exceed 450 mg/day (high doses increase seizure risk).
  • Suicidal Thoughts & Behaviour:
    • Monitor mood changes in young adults, especially in the first few weeks of treatment.
  • Hypertension:
    • Increases blood pressure, especially when used with nicotine patches.
  • Mania Risk in Bipolar Disorder:
    • May trigger manic episodes—use cautiously in undiagnosed bipolar patients.

8. Precautions

  • Avoid alcohol—may increase seizure risk.
  • Do not stop suddenly—gradual tapering is recommended to avoid withdrawal effects.
  • Use with caution in anxiety disorders—may increase agitation.

9. Interactions

  • MAOIs (e.g., phenelzine, selegiline): Contraindicated—risk of hypertensive crisis.
  • Alcohol: Increases seizure risk—avoid or limit alcohol.
  • SSRIs (e.g., fluoxetine, sertraline): Increases serotonin syndrome risk.
  • Stimulants (e.g., amphetamines, methylphenidate): Increases seizure risk.
  • CYP2B6 Inhibitors (e.g., ticlopidine, clopidogrel): Increase bupropion levels—monitor for toxicity.

10. Monitoring Parameters

  • Mental health symptoms (suicidal ideation, mood changes).
  • Blood pressure (especially in patients on nicotine patches).
  • Weight (due to weight loss effects in some patients).
  • Seizure risk (especially if risk factors are present).

11. Use in Children

  • Not FDA-approved for children, but used off-label for ADHD in adolescents.

12. Use in Pregnancy

  • Category C:
    • Considered safer than SSRIs, but use only if benefits outweigh risks.
    • Can be used in pregnant smokers under medical supervision.

13. Use in Elderly

  • Start with lower doses (75 mg/day) due to seizure risk.

14. Use in Kidney Disease

  • Reduce dose to 75 mg once daily if CrCl <30 mL/min.

15. Use in Liver Disease

  • Mild-moderate impairment: Reduce dose to 150 mg/day.
  • Severe impairment: Max 75 mg/day.

16. Patient Counselling Points

  • Expect delayed onset—effects take 2–4 weeks to appear.
  • Avoid alcohol—increases risk of seizures.
  • Take in the morning to avoid insomnia.
  • Do not crush or chew SR/XL tablets.
  • Report mood changes or suicidal thoughts immediately.

17. Table of Brand Names, Manufacturer, and Prices in USD

Brand NameManufacturerStrength/Dosage FormPrice (USD)
WellbutrinGlaxoSmithKline75 mg, 100 mg IR Tablets$100 (30 tabs)
Wellbutrin SRGlaxoSmithKline100 mg, 150 mg, 200 mg SR$150 (30 tabs)
Wellbutrin XLGlaxoSmithKline150 mg, 300 mg XL Tablets$200 (30 tabs)
ZybanGlaxoSmithKline150 mg SR Tablets (Smoking Cessation)$180 (30 tabs)
Generic BupropionVarious75 mg, 100 mg, 150 mg, 200 mg$50 (30 tabs)

18. 15 FAQs (Frequently Asked Questions)

1. What is Bupropion used for?
Bupropion is used to treat major depressive disorder (MDD), seasonal affective disorder (SAD), and smoking cessation. It is also used off-label for ADHD and SSRI-induced sexual dysfunction.

2. How does Bupropion work?
It is a norepinephrine-dopamine reuptake inhibitor (NDRI) that increases these neurotransmitters, improving mood, focus, and motivation.

3. How long does it take for Bupropion to work?
It may take 2–4 weeks for initial improvement and 6–8 weeks for full effects. For smoking cessation, effects appear within 7–10 days.

4. Can I stop taking Bupropion suddenly?
No, stopping suddenly may cause withdrawal effects such as irritability, anxiety, or mood swings. Tapering is recommended under medical supervision.

5. Does Bupropion cause weight gain?
No, Bupropion is weight-neutral or may cause weight loss. It is sometimes used off-label for weight management.

6. Can I drink alcohol while taking Bupropion?
No, alcohol increases the risk of seizures and worsens mood instability. It is best to avoid or limit alcohol intake.

7. Does Bupropion cause sexual dysfunction?
Unlike SSRIs, Bupropion does not cause sexual dysfunction. It is often used to counteract SSRI-induced sexual side effects.

8. Can Bupropion cause insomnia?
Yes, Bupropion has stimulant-like properties and may cause insomnia. It is best to take it in the morning to reduce sleep disturbances.

9. Can Bupropion be taken with caffeine?
Yes, but high caffeine intake may increase anxiety or jitteriness. Moderation is advised.

10. Can Bupropion increase anxiety?
Yes, some people may experience increased anxiety, restlessness, or agitation, especially in the first few weeks. Adjusting the dose or taking with food may help.

11. Is Bupropion addictive?
No, Bupropion is not addictive and has no withdrawal symptoms like benzodiazepines or opioids.

12. Can Bupropion be used for ADHD?
Yes, it is sometimes used off-label for ADHD, particularly in adults who cannot tolerate stimulant medications.

13. Does Bupropion raise blood pressure?
Yes, it can increase blood pressure. Patients with hypertension should monitor their BP regularly.

14. Can Bupropion cause seizures?
Yes, high doses (>450 mg/day) increase seizure risk, especially in those with a history of epilepsy, eating disorders, or alcohol withdrawal.

15. Can I take Bupropion long-term?
Yes, Bupropion is safe for long-term use under medical supervision. Regular monitoring is advised to assess its effectiveness and side effects.