There are more than six million smokers in the United Kingdom alone. This number underscores the profound challenge public health faces in combating tobacco use, especially as smoking remains one of the leading causes of premature death, with associated health complications ranging from cardiovascular diseases to various forms of cancer. Nicotine addiction can be incredibly difficult to overcome due to its powerful cravings and withdrawal symptoms, but bupropion can be a useful tool for those looking to quit. Originally developed as an antidepressant, bupropion can help alleviate nicotine withdrawal symptoms, reduce cravings and provide solid foundations for a nicotine-free life.

What is bupropion?

Bupropion serves as a medication utilised in the treatment of major depressive disorder and as a support for smoking cessation. Originally developed in 1969, this drug falls under the category of a norepinephrine-dopamine reuptake inhibitor (NDRI). It gained approval from the US Food and Drug Administration (FDA) in 1985 specifically for addressing depression.

However, one of the most serious bupropion side effects was an increase in the risk of seizures. This caused bupropion to be withdrawn in 1986 but after reassessment, it was discovered that seizures were primarily a risk at high doses, so the drug was re-introduced in 1989 but with a reduced prescribed dose.

Bupropion was later discovered to have significant benefits for individuals looking to quit smoking, leading to its FDA approval for this use in 1997 under the brand name Zyban. In the UK, bupropion is only approved for smoking cessation, not for depression treatment.

There is also research being carried out on bupropion’s effectiveness in treating a range of other conditions including attention deficit hyperactivity disorder (ADHD), seasonal affective disorder (SAD), obesity and methamphetamine addiction.

Brand names for bupropion include:

    Zyban
    Wellbutrin
    Forfivo
    Voxra
    Prexaton
    Aplenzin

How bupropion is used in nicotine addiction treatment

The brain uses chemicals called neurotransmitters to send messages from one neuron (or brain cell) to another. Two of these neurotransmitters, dopamine and norepinephrine, are particularly important for regulating mood and behaviour.

Dopamine is often called the “feel-good” neurotransmitter due to its role in the pleasure and reward systems in the brain. Norepinephrine affects attention and response actions, playing a role in energy and alertness. Nicotine triggers the release of these neurotransmitters, and the increased levels create positive feelings and reinforce the behaviour.

Bupropion works by blocking the reuptake of dopamine and norepinephrine. “Reuptake” is a process where neurotransmitters are reabsorbed by the neuron that released them. By blocking this reabsorption, Bupropion keeps more dopamine and norepinephrine available in the spaces between neurons. This means these feel-good and energy-related signals can be more effective, which helps reduce the nicotine withdrawal symptoms that emerge when quitting smoking. These include:

    Cravings for nicotine: One of the most challenging aspects of quitting smoking is the intense desire to smoke. By increasing dopamine and norepinephrine levels, Bupropion helps reduce these cravings, making it easier for individuals to resist the urge to smoke.

    Mood swings: Quitting smoking can lead to feelings of irritability, anxiety and sadness due to the sudden drop in neurotransmitter levels that nicotine used to boost. Bupropion’s mechanism helps stabilise mood by ensuring that dopamine and norepinephrine remain available, reducing the severity of mood swings.

    Difficulty concentrating: Nicotine withdrawal can also affect cognitive functions, making it hard to focus or concentrate. The boosted levels of norepinephrine, associated with attention and alertness, help counteract this effect, helping to maintain mental clarity during the quitting process.

    Fatigue: The lack of nicotine, which many smokers rely on for a quick energy boost, can lead to feelings of tiredness and lethargy. Bupropion helps mitigate this fatigue by increasing norepinephrine, which aids energy and alertness.

    Increased appetite: Quitting smoking leads to an increase in appetite, which can be a concern for those worried about weight gain. By modulating the brain’s reward and pleasure centres, bupropion can potentially help normalise appetite changes that come with nicotine withdrawal.

Administering Bupropion requires careful consideration of dosing schedules, typically starting with a lower dose and gradually increasing to minimise the risk of side effects. For smoking cessation, treatment usually begins one to two weeks before the quit date to allow the medication to reach effective levels in the body. The full course of treatment typically lasts for 7 to 12 weeks. However, some individuals may benefit from extended treatment to prevent relapse.

Potential bupropion side effects

While Bupropion is an effective and generally safe medication, there are potential bupropion side effects that individuals and healthcare providers should be aware of. It is important for individuals taking Bupropion to communicate openly with their healthcare provider about any side effects they experience as many can be managed through dose adjustments, timing of doses or supportive measures.

Common bupropion side effects

Many of the side effects of Bupropion are similar to those of other antidepressants, though some are more specific to its unique mechanism of action.  Common bupropion side effects include:

    Dry mouth: A frequently reported side effect.

    Headache: Some users experience headaches, which are usually temporary and diminish as the body adjusts to bupropion.

    Insomnia: The stimulating effect of bupropion can lead to difficulties falling or staying asleep, particularly if taken later in the day.

    Nausea: This can occur, especially in the early stages of treatment, but often subsides over time.

    Appetite changes: Some people may experience increased or decreased appetite, though bupropion is less likely than other antidepressants to cause significant weight gain.

    Constipation: A common side effect of bupropion that can usually be managed with dietary adjustments and increased fluid intake.

More serious bupropion side effects

While less common, these bupropion side effects can be very serious and require immediate attention:

    Seizures: Bupropion carries a risk of seizures, which is higher at doses above the recommended maximum or in individuals with certain medical conditions.

    High blood pressure: Treatment with Bupropion can lead to elevated blood pressure in some individuals, necessitating regular monitoring.

    Psychiatric symptoms: Some people may experience worsening depression, suicidal thoughts or unusual changes in behaviour, especially in the first few weeks of treatment or when the dose is changed.

    Allergic reactions: Rarely, Bupropion can cause allergic reactions, including itching, hives or swelling of the face, lips or tongue.

Bupropion withdrawal symptoms

While not typically associated with dependency, discontinuing bupropion abruptly can lead to withdrawal symptoms in some individuals. Bupropion withdrawal symptoms may include irritability, aggression, confusion or an intense craving for the drug. Tapering off under medical supervision is recommended to minimise withdrawal effects.

Regular monitoring by a healthcare provider is crucial, especially during the initial stages of treatment or when adjusting the dose. This can ensure that any bupropion side effects or complications are identified early and managed promptly.

 

Is bupropion addictive?

Bupropion is not generally considered to be addictive but there are some cases of people crushing the pills and snorting them to enhance the effects. While bupropion can create some degree of euphoria when abused like this at extremely high doses, the greater concern is the increased risk of seizures this creates.

Get help to quit smoking today

If you are looking for professional support to quit smoking, make an appointment with your GP. They can assess your health goals and individual needs and decide whether bupropion is a suitable option for you. The sooner you give up smoking, the better your chances of avoiding the most serious health risks.
 

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FAQ’s

What is bupropion used for?
Bupropion is primarily prescribed for treating major depressive disorder and for aiding in smoking cessation. It operates as a norepinephrine-dopamine reuptake inhibitor (NDRI), which helps to balance certain chemicals in the brain, thereby improving mood and reducing cravings and withdrawal symptoms associated with quitting smoking. Bupropion is also sometimes used off-label for conditions such as seasonal affective disorder (SAD) and to help manage symptoms of attention deficit hyperactivity disorder (ADHD).