Bupropion is an antidepressant drug approved by the U.S Food and Drug Administration (FDA) for the treatment of Major Depressive Disorder (MDD), Seasonal Affective Disorder (SAD), and as an aid for smoking cessation. This medication works by improving your mood and your sense of well-being. This is achieved by restoring the chemical balance of dopamine and norepinephrine in the brain. Bupropion is also used off-label for the treatment of a variety of health conditions such as:
Attention Deficit Hyperactivity Disorder (ADHD)
Social anxiety disorder
Obesity
Certain forms of nerve pain
Bupropion is available in three main forms:
Immediate-release tablet
A sustained-release tablet
An extended-release tablet for oral administration
One of the key differences between bupropion and other antidepressants is that it doesn’t affect the user’s libido, and it doesn’t cause any weight gain as other antidepressants usually do. In fact, it’s often prescribed along with other antidepressants to help counteract the sexual side effects of other medications.
Most antidepressants are selective serotonin reuptake inhibitors (SSRI), which means that they boost the levels of serotonin in the brain. Bupropion, on the other hand, is different. It is a norepinephrine-dopamine reuptake inhibitor (NDRI). An NDRI boosts levels of the neurotransmitters norepinephrine, also known as noradrenaline and dopamine.
As well as being an antidepressant, bupropion is an antagonist to nicotinic receptors. This means that it blocks receptors where nicotine normally binds, making it useful in helping people quit smoking.
The overall effects of bupropion are complex, and its neurological effects and mechanism of action are only partly understood.
Major depressive disorder, also referred to as clinical depression, is a significant mental health condition that can affect many areas of a person’s life. It impacts mood and behavior as well as various physical functions, such as appetite and sleep. According to the National Survey on Drug Use and Health (NSDUH), major depressive disorder is characterized as a period of at least two or more weeks of depressed mood, loss of interest, pleasure in daily activities, and other symptoms, such as sleep problems, low in appetite, energy, concentration, and self-worth.
MDD is one of the most common mental health conditions in the United States. The National Institute of Mental Health (NIMH) suggests that 8.4% of U.S. adults, experienced a major depressive episode in 2020.
Bupropion is an ideal medication for the treatment of depression as it works by inhibiting the reuptake of dopamine, serotonin, and norepinephrine and helps balance out the neurotransmitter imbalance that causes depression.
The American Psychiatric Association (APA) identifies seasonal affective disorder as a type of major depressive disorder with seasonal patterns. People with SAD experience mood changes and symptoms that are quite similar to depression. The symptoms usually occur during the fall and winter months when there is less sunlight but usually improve with the arrival of spring. Common symptoms of SAD include fatigue and weight gain.
The most difficult months for people with SAD in the U.S. tend to be between January and February. It is estimated that around 5% of the U.S. adult population experience SAD. Additionally, the disorder is more common in women than in men and in younger adults than older adults.
SAD has been linked to a biochemical imbalance in the brain caused by shorter daylight hours and less sunlight during winter. Seasonal changes cause certain people to experience a shift in their internal biological clock or a circadian rhythm that causes them to be out of step with their daily schedule.
According to the American Academy of Family Physicians (AAFP), extended-release bupropion in 300 mg taken once daily effectively prevents recurrent symptoms in high-risk adults with a history of SAD and those at a lower risk.
Studies reveal bupropion to be a great aid for smoking cessation as it helps reduce nicotine withdrawal and cravings to a great extent.
The type of bupropion used for smoking cessation is sold under the brand name of Zyban. It is described as a safe and cost-effective treatment for nicotine addiction. Zyban helps around one in 5 people quit smoking in the U.S each year. The effectiveness of this medication as an aid against nicotine dependence increases when bupropion is used in conjunction with other nicotine replacement products such as the nicotine patch, gum, and lozenges. However, Zyban may only be recommended for people who smoke ten or more cigarettes per day.
You should not take bupropion if you have ever had an allergic reaction to bupropion.
Bupropion can cause seizures, especially in people with certain medical conditions or when it interacts with certain other drugs. So it is important to inform your doctor of any other medications you’re on to avoid adverse reactions.
It is also helpful to inform your doctor of any medical condition you may have as bupropion may not be suitable for certain medical conditions such as:
Liver or kidney disease
Bipolar disorder
Diabetes
High blood pressure
Patients with alcohol use disorder or substance use disorder
Seizures
Eating disorder such as anorexia or bulimia
Abruptly stopped using alcohol, seizure medications, or sedatives
Though bupropion is often used in children and adolescents, it is not FDA approved for use by anyone younger than 18 years of age. Bupropion has been associated with a risk of suicidal ideation in children.
Even though bupropion treats various health conditions, it also comes with its own set of side effects that range from mild to severe. The more common side effects of bupropion may emerge within a few days of use and disappear within a few weeks.
Some of the most common side effects include:
Stomach pain
Appetite loss
Changes in the way food tastes
Constipation
Drowsiness
Dizziness
Dry mouth
Flushing
Gas
Hair Loss
Headache
Profuse sweating
Insomnia
Joint aches
Nausea
Nervousness
Tremors
Restlessness
Vomiting
Ringing in the ears
Weakness
Weight loss
Urinating more often
Sleeping troubles
Bupropion can also cause severe side effects that can potentially be life-threatening. Some such side effects include:
Aggressiveness
Agitation
Changes in the menstrual cycle
Changes in vision
Changes in sexual function
Dark urine
Chest pain
Breathing difficulties
Hearing problems
Rapid or irregular heart rate
Swollen, blistered, or peeling skin
Yellow skin or eyes
Unusual swelling in parts of the body
Severe or lingering muscle or joint pain
Severe headache
Pale-colored stools
Hallucinations
Bupropion comes with a black box warning to help alert doctors and patients about the drug’s adverse effects. This is the most serious type of warning from the U.S. Food and Drug Administration (FDA).
Taking this drug may cause you to have changes in behavior such as hostility, agitation, depressed moods, or suicidal thoughts. The potential risk of suicidal thoughts and behavior is higher in children, adolescents, and young adults who consume bupropion. It is vital that you inform your doctor immediately should you experience any of these adverse effects.
In rare instances, bupropion can cause seizures that can be severe and potentially life-threatening. As such, it is not recommended for patients who are prone to seizures or to be consumed with other drugs that lower the seizure threshold. The risk of seizures increases when the doses of bupropion are increased.
Some other factors that increase the risk of seizure in bupropion are:
Past history of seizures or epilepsy
Previous head traumas
Active brain tumors or anorexia or bulimia nervosa
Withdrawal from benzodiazepines or alcohol
Current use of drugs such as antipsychotics, antidepressants, theophylline, systematic steroids, and others that lower seizure threshold.
Even though bupropion is an effective treatment option for most patients with anxiety disorders, it can also cause anxiety as a side effect in certain patients. Bupropion can also cause severe high blood pressure and periods of mania.
Bupropion is a non-habit-forming drug that is considered to have a low risk of addiction and dependence. And it doesn’t produce much of the side effects seen by other antidepressants. However, it can produce a high that is quite similar to that of amphetamines and crack cocaine when the pills are crushed and snorted.
When bupropion is misused, dangerous doses of the drug enter the body and increase the risk of an overdose. Although there is little evidence provided to show fatal bupropion overdose, it can trigger severe symptoms such as:
Seizures
Hallucinations
Loss of consciousness
Abnormal heart rhythms
As with any medication, bupropion has both pros and cons to its use. Even though it has tremendous benefits in treating conditions such as depression and its effectiveness in treating nicotine addiction, it also comes with its own set of adverse side effects. It is important to consult your healthcare provider before you take bupropion to avoid any potential risks associated with its use.
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