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Stopping smoking (smoking cessation) is difficult. Of those attempting to quit without support, only 3-5% are successful after a year.[1] There are two main categories of support for smoking cessation: psychological/behavioral support (talking therapies) and pharmacological support (medications).
Bupropion is a medication that can help reduce the unpleasant withdrawal effects and cravings associated with smoking cessation and help individuals stop smoking. It should only be used as prescribed by a medical professional.
- Bupropion supports smoking cessation and aims to reduce the probability of relapse.
- Bupropion can reduce common issues associated with smoking cessation, including weight gain, depression, and cravings.
- Bupropion doesn’t help with any of the social or emotional challenges of smoking cessation. It can cause side effects, including insomnia, vivid dreams, headaches, and (rarely) seizures.
What is bupropion?
Bupropion was first developed as an antidepressant. During clinical trials, researchers noticed that veterans who were prescribed bupropion also stopped smoking. Since then, ample research has demonstrated that bupropion can help people struggling with nicotine dependence.[2]
Bupropion was first approved by the FDA in 1985 and is commonly sold under the brand names Wellbutrin, Zyban, Aplenzin, and Forfivo. It is widely used, with over 25 million prescriptions per year in the US alone.[3] As Wellbutrin, bupropion is licensed and prescribed as an antidepressant, including for people with recurring seasonal affective disorder (SAD) or bipolar disorder. Wellbutrin is also FDA-approved for smoking cessation. Zyban is the same drug and is licensed to assist with smoking cessation, although this brand may be discontinued.
How bupropion works for nicotine dependence
Bupropion is a nicotinic acetylcholine receptor antagonist and a norepinephrine–dopamine reuptake inhibitor (NDRI).[4] In both of these roles, it increases the levels of dopamine in the brain.
Nicotine withdrawal usually leads to a reduction in dopamine levels in the brain. Bupropion reduces how much dopamine is reabsorbed and increases the overall dopamine effects, which thereby reduces the depressed mood associated with smoking cessation.[5]
Bupropion may also play a small role in reducing the pleasurable feelings associated with smoking by binding with nicotinic acetylcholine receptors and reducing the dopamine release that follows cigarette use.[6]
Is bupropion effective for smoking cessation?
Using bupropion is effective in supporting smoking cessation. Individuals taking bupropion are approximately twice as likely to have successfully quit after 12 months as those taking a placebo medication. Overall, studies show that around 20% of smokers using bupropion successfully quit.[2] This is similar to other smoking cessation medications, such as nicotine replacement therapy (NRT) and varenicline, although some studies show varenicline to be more effective.[7][8]
Bupropion dosage guidelines for nicotine addiction treatment
For smoking cessation, bupropion is frequently started 1–2 weeks prior to the quit date. Bupropion will usually be given in 150 mg tablets, and the initial dose will usually be once per day for 3 days. After that, bupropion is typically increased to twice per day, with doses at least 8 hours apart. The maximum dosage is 450 mg per day or 150 mg in a single dose, although total daily doses of 300 mg are most common.
These tablets should be taken whole, without being crushed or chewed. They can be taken with food to reduce stomach upset. Avoid taking bupropion shortly before bedtime, as it can cause difficulty sleeping.
Precautions for use
Bupropion can carry risks for some individuals. Before taking it, be aware of the following:[9]
- Antidepressants, including bupropion, can cause suicidal thoughts. Anyone experiencing depression or suicidal thoughts should discuss those with their medical practitioner before taking it.
- Bupropion can lower the seizure threshold and cause seizures, so it may not be appropriate for anyone who has experienced seizures in the past.
- Individuals who have experienced an allergic reaction to bupropion or its ingredients should not take the drug.
- Bupropion should also not be used by anyone with a history of eating disorders, including anorexia nervosa or bulimia.
- Bupropion should not be taken while taking a monoamine oxidase (MAO) inhibitor or within 14 days after stopping.
- Anyone suddenly stopping using alcohol or sedatives should speak with their medical practitioner before taking bupropion.
Bupropion side effects and risks
As with all medications, bupropion can lead to various side effects.
Common side effects of bupropion include: [10]
- Loss of appetite/weight loss
- Dry mouth
- Rash
- Sweating
- Ringing in the ears
- Shakiness
- Stomach pain
- Nausea
- Anxiety or agitation
- Dizziness
- Headache
- Trouble sleeping
- Muscle pain
- Racing heart
- Sore throat
- Increased need to urinate
More serious side effects can include:
- Seizures
- Suicidal thoughts
- Psychosis
- Severe allergic reactions
Anyone taking bupropion should speak to their medical practitioner immediately if they experience suicidal thoughts, agitation, or hallucinations.
If you experience a rash, fever, swelling of the mouth or tongue, chest pain, or trouble breathing, stop taking bupropion immediately and seek urgent medical care by contacting your primary care provider or calling 911. These may indicate a severe allergic reaction which can be life-threatening.
Bupropion interactions
Bupropion can interact with other medications. Always inform your doctor of any medications or other drugs you may be taking.
Bupropion can slow down how quickly the body metabolizes (gets rid of) certain medications, including some antidepressants (including nortriptyline, imipramine, desipramine, paroxetine, fluoxetine, and sertraline), antipsychotic medications (including haloperidol, risperidone, and thioridazine) and heart medications known as antiarrhythmics (including amiodarone, propafenone, and flecainide). These may need to be prescribed at a lower dose to anyone taking bupropion.
MAO inhibitors should not be used concurrently with bupropion.
Medications that lower seizure threshold should not usually be taken at the same time as bupropion. These may include certain antipsychotics, specific antidepressants, theophylline, and some systemic steroids.
Levodopa and amantadine, which are used to treat Parkinson's disease, may also increase the risks of adverse reactions to bupropion and should be used carefully in conjunction with bupropion.
Bupropion overdose
Bupropion overdose can lead to seizures, hallucinations, increased heart rate, coma, and death.
Call 911 immediately if someone seems confused, struggles to breathe, loses consciousness, or starts to convulse after taking bupropion.
Speaking to your provider about bupropion
Bupropion is only available as a prescription, so you will need to talk to your healthcare provider to consider it for smoking cessation. Most providers will be strongly supportive of people trying to stop smoking, but they will need to be sure that bupropion is right (and safe) for you.
Your healthcare provider will need to know of these potential concerns:
- Whether you have had depression, suicidal thoughts, or other mental health issues in the past
- Any history of eating disorders
- If you have experienced heart problems or high blood pressure
- If you have a history of seizures
- Any current or previous liver or kidney problems
- Whether you are pregnant, planning to become pregnant, or breastfeeding
- Any drugs or medications you take, including prescriptions, over-the-counter medications, supplements, alcohol, and illegal drugs
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