Bupropion is a distinctive antidepressant used to treat major depressive disorder (MDD), seasonal affective disorder (SAD), and aid in smoking cessation. Unlike most antidepressants, it primarily targets dopamine and norepinephrine rather than serotonin, offering unique therapeutic advantages.

It is available as a prescription drug in two forms: immediate-release tablets and extended-release tablets. The immediate-release tablets work quickly, while the extended-release tablets are designed to release the drug slowly over time.

Bupropion is marketed under several brand names, including Wellbutrin SR, Wellbutrin XL, Aplenzin, Forfivo XL, and Zyban. It is also available as a generic drug, which is typically less expensive than the brand-name versions.

What is Bupropion Tablet?

Bupropion is a norepinephrine-dopamine reuptake inhibitor (NDRI) , a class of antidepressants that enhances mood by increasing levels of dopamine and norepinephrine in the brain. It lacks the sexual dysfunction and weight gain risks common with SSRIs/SNRIs, making it a preferred choice for many patients.

Approved for MDD, SAD, and smoking cessation (under the brand Zyban), it is unique among antidepressants for its dual action on mood and nicotine craving reduction.

What are the Uses of Bupropion?

Bupropion offers several therapeutic benefits that make it a versatile medication in psychiatric and addiction medicine. The medication's unique mechanism provides advantages for patients who may not respond well to traditional antidepressants.

Conditions Bupropion Treats

  • Major Depressive Disorder: Bupropion is FDA-approved as a first-line treatment for major depressive disorder in adults. The CANMAT 2024 guidelines recommend bupropion as both a first-line treatment option and a second-line adjunctive treatment for difficult-to-treat depression.
  • Seasonal Affective Disorder: Bupropion XL is approved explicitly for preventing seasonal affective disorder, typically starting in autumn before depressive symptoms appear and continuing through winter months.
  • Smoking Cessation: Under the brand name Zyban, bupropion demonstrates significant effectiveness in helping people quit'smoking, with clinical studies showing a 40-45% success rate compared to 20-25% with placebo treatments.

Secondary Uses of Bupropion

Beyond its FDA-approved indications, bupropion is commonly prescribed off-label for several conditions. These include antidepressant-induced sexual dysfunction, attention deficit hyperactivity disorder (ADHD) in pediatric patients, and as an adjunct treatment for weight management.

Some healthcare providers also consider bupropion for patients with cocaine use disorder to support abstinence efforts, particularly when combined with tobacco cessation treatment.

How Does Bupropion Work?

Bupropion is a unique antidepressant that functions primarily as a norepinephrine-dopamine reuptake inhibitor (NDRI). Unlike SSRIs or SNRIs, it has minimal impact on serotonin levels, which reduces the risk of sexual side effects and weight gain commonly associated with other antidepressants.

Bupropion Mechanism of Action

Bupropion works by:

  • Inhibiting dopamine and norepinephrine reuptake: It blocks the dopamine transporter (DAT) and norepinephrine transporter (NET), increasing the concentration of these neurotransmitters in the brain.

  • Enhancing activity in specific brain regions:

    • Nucleus accumbens: Increases dopamine activity, which is associated with mood regulation and reward.

    • Locus coeruleus: Modulates noradrenaline levels, impacting energy and alertness.

  • Acting as a nicotinic acetylcholine receptor antagonist: This mechanism helps reduce nicotine cravings, making Bupropion effective for smoking cessation.

How to Take Bupropion (Wellbutrin)?

Take Bupropion exactly as prescribed by your doctor. Follow the instructions on your prescription label carefully. Do not take more or less than the recommended dose.

  • Avoid taking the medication in larger or smaller amounts than directed. Overconsumption of Bupropion can increase the risk of seizures.
  • Swallow extended-release tablets whole. Do not crush, chew, or break them.
  • Do not stop taking Bupropion suddenly without consulting your doctor, as this can increase the risk of seizures.
  • If you're using Bupropion to quit'smoking, your doctor may also prescribe a nicotine replacement product (such as patches or gum). Start using the nicotine replacement product on the same day you stop smoking or using tobacco products.
  • Be aware that some people using Bupropion (Wellbutrin or Zyban) have experienced severe high blood pressure, especially when using nicotine replacement products.
  • Nicotine Withdrawal Symptoms: When you stop smoking, you may experience withdrawal symptoms such as:
    • Increased appetite
    • Weight gain
    • Trouble sleeping
    • Difficulty concentrating
    • Slower heart rate
    • Urges to smoke
    • Feelings of anxiety, restlessness, depression, anger, frustration, or irritation
  • These symptoms can occur with or without the use of medications like Zyban. Quitting smoking can also lead to new or worsening mental health issues, including depression.

Bupropion Dosage

Proper dosing of bupropion tablets is crucial for both effectiveness and safety, as the medication has a dose-dependent risk of seizures. Healthcare providers carefully titrate doses based on the specific condition being treated and individual patient factors.

Depression

  • Generic: Bupropion Tablet (75 mg, 100 mg)
  • Brand:
    • Wellbutrin XL (150 mg, 300 mg)
    • Wellbutrin SR (100 mg, 150 mg)
    • Aplenzin (174 mg, 348 mg, 522 mg)
    • Forfivo XL (450 mg)

Seasonal Affective Disorder (SAD)

  • Generic: Bupropion Tablet (100 mg, 150 mg, 200 mg, 300 mg)
  • Brand:
    • Aplenzin (174 mg, 348 mg, 522 mg)
    • Wellbutrin XL (150 mg, 300 mg)

Smoking Cessation

  • Generic: Bupropion (100 mg, 150 mg, 200 mg, 300 mg)
  • Brand: Zyban (150 mg)

What Happens If You Miss a Dose of Wellbutrin?

Missing a dose of Wellbutrin (bupropion) can affect your treatment, but it's important to stay calm and act wisely. If you forget to take Wellbutrin in the morning or miss a single dose, take it as soon as you remember unless it's close to your next scheduled dose. In that case, skip the missed dose and resume your usual routine.

Is it bad to miss a dose of Wellbutrin? Occasionally missing one dose is not usually dangerous, but never double the next dose to catch up. Doing so may increase the risk of seizures, especially if doses are taken too close together.

If you skip Wellbutrin for two days or more, contact your doctor. Restarting without guidance can lead to mood swings, withdrawal-like symptoms, or a return of depression or cravings (if using it for smoking cessation).

What Happens If an Overdose Occurs?

Bupropion overdose is a serious medical emergency that requires immediate attention. The medication has a relatively narrow therapeutic window, meaning the difference between an effective dose and a toxic dose is smaller than with many other medications.

What to Avoid: Never exceed the prescribed dose, avoid taking multiple doses close together, and don't crush or break extended-release tablets as this can lead to rapid absorption and increased overdose risk. Alcohol consumption should be limited or avoided entirely while taking bupropion, as it can lower the seizure threshold.

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What are the Side Effects of Bupropion (Wellbutrin)?

Like all medications, bupropion can cause side effects, though many people tolerate it well. Understanding potential side effects helps patients and healthcare providers make informed decisions about treatment.

Common Side Effects

The most frequently reported side effects of bupropion include:

Mental Health Effects:

  • Worsening depression
  • Anxiety
  • Feeling agitated or restless
  • Panic attacks
  • Sleeping disorders
  • Increased irritability
  • Dangerous impulses

Eye Problems:

  • Eye pain
  • Swelling or redness near the eye
  • Changes in vision

Seizures:

  • Staring spells
  • Jerking in arms and legs
  • Loss of consciousness

If you experience any severe symptoms, contact your doctor immediately. Avoid using Bupropion if you have any adverse reactions.

Allergy Warnings

Be aware of potential allergic reactions to Bupropion, which can include:

  • Rash
  • Swelling of the lips
  • Itching
  • Hives
  • Fever
  • Swollen lymph glands
  • Painful sores in the mouth
  • Trouble breathing

Warnings for Serious Health Conditions

  • Pregnancy: Bupropion is a Category C pregnancy drug, indicating that animal studies have shown adverse effects on the fetus. It should be used during pregnancy only if necessary and the benefits outweigh the risks.
  • Breastfeeding: Bupropion passes into breast milk and may affect a nursing baby. Consult your doctor before using Bupropion if you are breastfeeding.

Precautions and Warnings

Bupropion requires careful consideration of patient factors before prescribing, as certain conditions significantly increase the risk of severe adverse effects.

Who Should Avoid This Medicine

Absolute Contraindications: Patients with seizure disorders, eating disorders (anorexia nervosa or bulimia nervosa), or those currently taking monoamine oxidase inhibitors (MAOIs) should not use bupropion. The medication is also contraindicated in patients who have suddenly stopped alcohol or sedative use, as withdrawal can lower the seizure threshold.

Conditions Where Caution Is Needed

Healthcare providers exercise special caution when prescribing bupropion to patients with:

  • History of head trauma or brain injury
  • Liver or kidney disease
  • Diabetes
  • Narrow-angle glaucoma
  • Bipolar disorder
  • History of substance abuse

Patients with these conditions may require dose adjustments, more frequent monitoring, or alternative treatment options.

Are There Any Age Restrictions for Using Bupropion?

Bupropion is not approved for use in children under 18 years of age for depression treatment. The FDA black box warning specifically highlights increased suicide risk in patients under 25 years old. For elderly patients, lower starting doses are often recommended due to increased sensitivity to side effects and potential for drug interactions.

Alcohol and Food Interactions

  • Alcohol: Patients should limit or avoid alcohol consumption while taking bupropion, as alcohol can significantly lower the seizure threshold and increase the risk of serious side effects. The combination can also exacerbate side effects such as dizziness and poor concentration.
  • Food: Bupropion can be taken with or without food. However, taking it with food may help reduce stomach upset in sensitive individuals.

Possible Interactions with Other Medications

Bupropion's metabolism through liver enzymes creates potential for significant drug interactions that healthcare providers must carefully consider.

Drug Interactions Overview

Bupropion is metabolised primarily by the CYP2B6 enzyme system, making it'susceptible to interactions with medications that either inhibit or induce these enzymes. The medication can also affect the metabolism of other drugs, creating bidirectional interaction potential.

Major Interactions:

  • MAOIs: Concurrent use is contraindicated due to the risk of hypertensive crisis
  • Other antidepressants: May increase serotonin syndrome risk when combined with SSRIs or SNRIs
  • Seizure threshold-lowering medications: Antipsychotics, tricyclic antidepressants, and certain antibiotics can increase seizure risk
  • CYP2D6 substrates: Bupropion inhibits this enzyme, potentially increasing levels of medications like certain beta-blockers and antiarrhythmics

Interactions with Supplements and Herbal Products

St. John's Wort: This herbal supplement can induce liver enzymes, potentially reducing bupropion effectiveness. Ginkgo biloba may lower seizure threshold when combined with bupropion.

Patients should inform their healthcare providers about all supplements and herbal products they use, as these can significantly impact bupropion's safety and effectiveness.

How Should Bupropion Be Stored?

Proper storage of bupropion ensures medication'stability and prevents accidental ingestion by children or pets. Following storage guidelines helps maintain the medication's effectiveness throughout its shelf life.

Recommended Storage Temperature for Bupropion

Bupropion should be stored at room temperature between 68°F and 77°F (20°C to 25°C). The medication can tolerate brief temperature excursions between 59°F and 86°F (15°C to 30°C), such as during transportation, but should not be exposed to extreme temperatures for extended periods.

What Happens If Bupropion Is Not Stored Properly?

Improper storage can lead to medication degradation, reducing effectiveness and potentially creating harmful breakdown products. Exposure to excessive heat, moisture, or light can alter the chemical composition of the medication.

Extended-release formulations are particularly sensitive to environmental conditions, as damage to the tablet coating can result in rapid drug release and an increased risk of side effects.

Bupropion vs Sertraline

Bupropion Sertraline
Bupropion is an antidepressant medication used to treat major depressive disorder and seasonal affective disorder. It is available by prescription in immediate-release or extended-release tablet forms. Sertraline is an antidepressant belonging to the selective serotonin reuptake inhibitor (SSRI) class. It helps balance chemicals in the brain associated with depression and anxiety.
Bupropion is used for treating depression and seasonal affective disorder (SAD). It is also used as a smoking cessation aid. It works by increasing certain types of brain activity. Sertraline is used to treat depression, panic attacks, social anxiety disorder, and post-traumatic stress disorder. It helps improve mood, sleep, and energy levels.
Most common side effects of Bupropion:
  • Agitation
  • Dry mouth
  • Constipation
  • Headache
  • Nausea
  • Vomiting
  • Dizziness
  • Sweating
  • Sleeping disorder
Most common side effects of Sertraline:
  • Nausea
  • Dizziness
  • Loss of appetite
  • Sweating
  • Diarrhea

References

Bupropion - StatPearls
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Frequently Asked Questions

Bupropion is used to treat depression and seasonal affective disorder (SAD). It also helps people quit smoking. As an antidepressant, it increases certain brain activities.

Bupropion may cause several serious side effects, including agitation, dry mouth, constipation, headache, nausea, vomiting, dizziness, sweating, and sleeping disorders. Patients should monitor these symptoms and consult their healthcare provider if they experience any of these effects while taking the medication.

Bupropion is an effective antidepressant used to treat major depressive disorder and seasonal affective disorder. It is a prescription drug available as immediate-release or extended-release tablets.

Doctors may avoid bupropion due to its seizure risk, especially in patients with certain conditions, or prefer other antidepressants based on patient needs.

Alternatives include SSRIs (e.g., sertraline, fluoxetine), SNRIs (e.g., venlafaxine), or other atypical antidepressants like mirtazapine, depending on the condition.

Bupropion may aid weight loss in some patients, often combined with naltrexone, but it’s not primarily prescribed for this purpose and requires medical supervision.

Missing a single dose occasionally isn’t usually harmful, but skipping multiple doses or taking doses too close together can raise your seizure risk.

Skipping Wellbutrin for two or more days may lead to withdrawal symptoms such as irritability, low mood, or increased cravings (if used for smoking cessation). It may also disrupt the stability of your treatment. Contact your doctor if this happens frequently.

Take bupropion as prescribed by your doctor, following the directions on the prescription label. Do not take more or less than recommended, as excessive use can increase the risk of seizures.

Bupropion primarily affects dopamine and norepinephrine, not serotonin, by inhibiting their reuptake, making it unique among antidepressants.


Disclaimer: The information provided is accurate and up-to-date to the best of our knowledge. However, it should not be considered a substitute for medical advice or consultation. We do not guarantee its completeness or accuracy. The absence of specific warnings does not mean a medicine is safe for all users. We are not responsible for any outcomes based on this information and strongly recommend consulting a doctor for any medical concerns or questions.

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