Bupropion (Wellbutrin): Uses, Mechanism of Action, Side Effects

Bupropion (Aplenzin, Wellbutrin, Wellbutrin SR, Wellbutrin XL) is a medication used to treat depression. Bupropion (Aplenzin, Wellbutrin XL) is also used to treat seasonal affective disorder (SAD; episodes of depression that occur at the same time each year [usually in the fall and winter but rarely may occur in the spring or summer months]). Bupropion (Zyban) is used to help people stop smoking. Bupropion is in a class of medications called antidepressants.

How does Bupropion (Wellbutrin) work?

Bupropion is a selective inhibitor of the neuronal reuptake of catecholamines (noradrenaline and dopamine) with minimal effect on the re-uptake of indolamines (serotonin). It works by increasing certain types of activity in the brain.

What Is Bupropion (Wellbutrin) And What Does It Treat?

Bupropion (Wellbutrin) is an antidepressant medication that works in the brain. It is approved for the treatment of major depressive disorders (MDD), seasonal affective disorder (SAD), and to help people quit smoking (smoking cessation).

Symptoms of depression include:

•          Depressed mood – feeling sad, empty, or tearful

•          Feeling worthless, guilty, hopeless, and helpless

•          Loss of interest or pleasure in your usual activities

•          Sleep and eat more or less than usual (for most people it is less)

•          Low energy, trouble concentrating, or thoughts of death (suicidal thinking)

•          Psychomotor agitation (‘nervous energy’)

•          Psychomotor retardation (feeling like you are moving and thinking in slow motion)

•          Suicidal thoughts or behaviors

SAD is a type of depression that occurs mainly during the autumn-winter season. Although the common term SAD is now referred to as Major Depression with Seasonal Pattern, this fact sheet will continue to use SAD as it is more commonly known.

Bupropion (Wellbutrin) may also be helpful when prescribed “off-label” for bipolar disorder, attention deficit hyperactivity disorder (ADHD, and sexual dysfunction due to SSRI antidepressants. “Off-label” means that it hasn’t been approved by the Food and Drug Administration for this condition. Your mental health provider should justify his or her thinking in recommending an “off-label” treatment. They should be clear about the limits of the research around that medication and if there are any other options.

What Is The Most Important Information I Should Know About Bupropion (Wellbutrin)?

After starting bupropion, symptoms gradually decrease over a period of weeks. In MDD and SAD, sleep and other physical symptoms may improve before there is a noticeable improvement in mood or interest in activities. Once symptoms are under control, MDD usually requires long-term treatment to help prevent the return of depressive symptoms. If you are using bupropion for SAD or smoking cessation, the length of your treatment may be shorter. With input from you, your health care provider will assess how long you will need to take the medicine.

Do not stop taking bupropion or change your dose without talking with your health care provider first.

Depression is also a part of bipolar illness. People with bipolar disorder who take antidepressants may be at risk for “switching” from depression into mania. Symptoms of mania include “high” or irritable mood, very high self-esteem, decreased need for sleep, pressure to keep talking, racing thoughts, being easily distracted, frequently involved in activities with a large risk for bad consequences (for example, excessive buying sprees).

What Should I Discuss With My Health Care Provider Before Taking Bupropion (Wellbutrin)?

•          Symptoms of your condition that bother you most

•          If you have thoughts of suicide or harming yourself

•          Medications you have taken in the past for your condition, whether they were effective or caused any adverse effects

•          If you experience side effects from your medications, discuss them with your provider. Some side effects may pass with time, but others may require an adjustment in the medication.

•          Any other psychiatric or medical problems you have, including a history of bipolar disorder

•          All other medications you are currently taking and any medication allergies you have. This will help your prescriber assess for potential drug interactions.

•          Other non-medication treatment you are receiving (such as psychotherapy (i.e., talk therapy) or substance abuse treatment). Your provider can explain how these different treatments work with the medication.

•          If you are pregnant, plan to become pregnant, or are breastfeeding

•          If you drink alcohol or use drugs

How Should I Take Bupropion (Wellbutrin)?

Bupropion hydrochloride is available in 3 different forms: immediate-release (IR), sustained-release (SR), and extended-release (XL).

Bupropion IR is usually taken 2 or 3 times per day with 4-6 hours between doses. The dose usually ranges from 100 mg twice daily to 150 mg three times daily, with the last dose taken mid-afternoon.

Bupropion SR is usually taken twice daily in the morning and mid-afternoon. The dose usually ranges from 100 mg twice daily up to 200 mg twice daily.

Bupropion (Wellbutrin) XL is usually taken once daily in the morning. The dose ranges from 150 mg to 450 mg.

Bupropion hydrobromide (Aplenzin®) is usually taken once daily in the morning. The dose ranges from 174 mg to 522 mg.

While there are dose ranges for each form, your health care provider will determine the form and dose that is right for you based on your response.

The dose for SAD is bupropion XL 150 mg once daily in the morning. The dose may be increased to 300 mg once daily.

The dose for smoking cessation is bupropion SR 150 mg once daily for 3 days and then twice daily for 7 to 12 weeks.

You should not take more than one product that contains bupropion, including the products that are used to quit smoking. Do not take more than your prescribed dose since higher doses may increase your risk of having a seizure. Since quickly increasing the dose of bupropion can cause seizures in some people, your doctor will slowly increase your dose.

You can take bupropion on an empty stomach or with food. The SR and XL forms should be swallowed whole — not chewed, crushed, or broken — so that the medication can work correctly in your body and reduce the risk of serious side effects. The tablet shell from the SR and XL forms may appear in your feces.

Consider using a calendar, pillbox, alarm clock, or cell phone alert to help you remember to take your medication. You may also ask a family member or friend to remind you or check in with you to be sure you are taking your medication.

What Happens If I Miss A Dose Of Bupropion (Wellbutrin)?

For bupropion IR or SR, if you miss a dose, take it as soon as you remember. Take the remaining doses for the day at evenly spaced times at least 4 hours apart. DO NOT take 2 doses at once. You should not take more than your prescribed dose and doing so may increase your risk of having a seizure.

For bupropion XL, do not take an extra tablet to make up for the dose you forgot. Wait and take your next dose at your regular time the next day.

What Should I Avoid While Taking Bupropion (Wellbutrin)?

Avoid drinking alcohol or using illegal drugs while you are taking bupropion because the beneficial effects of the medication may be decreased and the risk of seizures may be increased. If you are dependent on drugs or alcohol and would like to stop, consult your healthcare provider for help. Abruptly stopping these substances can result in a seizure, especially when taking bupropion.

What Happens If I Overdose With Bupropion (Wellbutrin)?

If an overdose occurs, call your doctor or 911. You may need urgent medical care. You may also contact the poison control center at 1-800-222-1222.

How Long Does It Take For Bupropion (Wellbutrin) To Work?

Sleep, energy, or appetite may show some improvement within the first 1-2 weeks. Improvement in these physical symptoms can be an important early signal that the medication is working. Depressed mood and lack of interest in activities may need up to 6-8 weeks to fully improve.

Can a pregnant woman take Bupropion (Wellbutrin)?

If you are planning on becoming pregnant, notify your health care provider to best manage your medications. People living with MDD who wish to become pregnant face important decisions, each with risks and benefits as they relate to how the illness, medications, and risks to the fetus may interact. Untreated MDD has risks to the fetus, as well as the mother. It is important to discuss the risks and benefits of treatment with your doctor and caregivers.

Bupropion (Wellbutrin) has also been evaluated for smoking cessation during pregnancy and is recommended only after other therapies have failed.

Can a breastfeeding woman take Bupropion (Wellbutrin)?

Caution is advised with breastfeeding since bupropion does pass into breast milk.

Are There Any Risks For Taking Bupropion (Wellbutrin) For Long Periods Of Time?

To date, there are no known problems associated with the long-term use of bupropion. It is a safe and effective medication when used as directed.

What Are The Possible Side Effects Of Bupropion (Wellbutrin)?

Bupropion may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

•          anxiety

•          changes in your sense of taste

•          constipation

•          difficulty falling asleep or staying asleep

•          dizziness

•          drowsiness

•          dry mouth

•          excessive sweating

•          excitement

•          frequent urination

•          headache

•          loss of appetite

•          nausea

•          ringing in the ears

•          sore throat

•          stomach pain

•          uncontrollable shaking of a part of the body

•          vomiting

•          weight loss

Some side effects can be serious. If you experience any of the following symptoms, call your doctor immediately or get emergency medical treatment:

•          confusion

•          hallucinating (seeing things or hearing voices that do not exist)

•          irrational fears

•          muscle or joint pain

•          rapid, pounding, or irregular heartbeat

•          seizures

If you experience any of the following symptoms, stop taking bupropion and call your doctor immediately or get emergency medical treatment:

•          chest pain

•          difficulty breathing or swallowing

•          fever

•          hives

•          hoarseness

•          itching

•          rash or blisters

•          swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs

Bupropion may cause other side effects. Call your doctor if you have any unusual problems while taking this medication.


What Other Medications May Interact With Bupropion (Wellbutrin)?

Bupropion (Wellbutrin) should not be taken with or within two weeks of taking monoamine oxidase inhibitors (MAOIs). These include phenelzine (Nardil®), tranylcypromine (Parnate®), isocarboxazid (Marplan®), and selegiline (Emsam®).

There are several products with the active ingredient bupropion. Do not take more than one product that contains bupropion since this may increase your risk of having a seizure.

Certain medications may increase your risk of having a seizure when combined with bupropion. These include other antidepressants, antipsychotics, theophylline, isoniazid, tramadol, stimulants, steroids, hypoglycemic agents (including insulin), certain antibiotics (e.g., Cipro®), and abrupt discontinuation of benzodiazepines (e.g., Ativan®).

Notify your doctor and pharmacist if you are taking any of the following medications: phenytoin (Dilantin®), carbamazepine (Tegretol®, Equetro®), phenobarbital, cimetidine (Tagamet®), ritonavir (Norvir®), lopinavir (Kaletra™), nelfinavir (Viracept®), or efavirenz (Sustiva®). These medications can change the way your body reacts to bupropion.

Notify your doctor and pharmacist if you are taking any of the following medications: atomoxetine (Stratterra®), codeine, tamoxifen, tetrabenazine, thioridazine (Mellaril®), tramadol (Ultram®), or a tricyclic antidepressant. Bupropion (Wellbutrin) can change the way your body reacts to these medications.


Dr. Oche Otorkpa PG Cert, MPH, PhD

Dr. Oche is a seasoned Public Health specialist who holds a post graduate certificate in Pharmacology and Therapeutics, an MPH, and a PhD both from Texila American University. He is a member of the International Society of Substance Use Professionals and a Fellow of the Royal Society for Public Health in the UK. He authored two books: "The Unseen Terrorist," published by AuthorHouse UK, and "The Night Before I Killed Addiction."
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