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Bupropion - Mechanism of Action, Indications, Contraindications, and Side Effects

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Bupropion - Mechanism of Action, Indications, Contraindications, and Side Effects

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Bupropion is an atypical antidepressant drug mainly used in adults for depressive disorders. The below article discusses Bupropion in detail.

Written by

Dr. Deepiha. D

Medically reviewed by

Dr. Siva Anoop Yella

Published At July 20, 2022
Reviewed AtJanuary 20, 2023

Introduction:

Atypical antidepressants are drugs that do not fall under regular antidepressant drugs. The mechanism of action of atypical antidepressants differs in each type of drug. These drugs work by restoring the neurotransmitters (chemical messengers) in brain cells. Thereby altering the brain's chemical reaction and communication between the nerve cells. Some of the FDA (Food and drug administration) approved atypical antidepressant drugs are:

  • Bupropion.

  • Trazodone.

  • Mirtazapine.

  • Agomelatine

  • Nefazodone.

What Is Bupropion?

Bupropion refers to Bupropion hydrochloride. Burroughs Wellcome (a multinational pharmaceutical company) patented the Bupropion formulation in 1974. Bupropion was approved by the FDA in 1985. Later, the sustained release and extended-release preparation were brought in. They are commercially available as Bupropion, Bupropion-SR, and Bupropion-XL.

Where Is Bupropion Indicated?

Bupropion is specifically approved for usage in the adult population.

  • Bupropion is prescribed for depression attacks like:

  • Bupropion has been used in the treatment of smoking cessation.

  • They have been used for non-FDA-approved conditions like obesity, anti-depressant-induced sexual dysfunction, and depression associated with bipolar disorder.

  • Bupropion is also used off-label for attention deficit hyperactivity disorder (ADHD) in the pediatric group.

How Does Bupropion Work?

The chemical composition of Bupropion hydrochloride is an aminoketone derivative.

The active mechanism of Bupropion is not well understood.

Dopamine, serotonin, and norepinephrine are three neurotransmitters that are fundamental for brain function. These substances in the brain help to elevate mood and emotions.

Bupropion has been attributed to inhibiting the reuptake of dopamine and norepinephrine. The effect on dopamine is high, while on norepinephrine, it is low. By hindering the uptake of these substances into the bloodstream, Bupropion helps to sustain them in the brain.

The concentration of the drug in the blood reaches its maximum by two hours for immediate release, three hours for sustained release, and five hours for extended release. These formulations were introduced to carry the therapeutic effect further for an elongated period of time. The action of the drug can be felt during the second week of medicine intake. Bupropion is metabolized in the liver and eliminated via urine and feces.

How to Take Bupropion?

Bupropion is a tablet to be taken orally. The following are the formulations of Bupropion available in the market,

  • Immediate-release category - 75 mg and 100 mg strength.

  • Sustained-release category - 100 mg,150 mg, and 200 mg strength.

  • Extended-release category - 150 mg and 300 mg strength.

Bupropion has to be taken as instructed by the healthcare professional. Patients can have them before or after meals. Generally, it is recommended to swallow the tablet as a whole without crushing, dividing, or chewing them. It is not advisable to change the dosage or quit taking the tablet without the knowledge of the doctor who prescribed it. The dosage and the number of tablets taken are to be noted by the caregiver or well-wisher because the extra dosage can have severe consequences. Missing the dose or mistakenly taking the tablet twice should be addressed immediately to the health care provider. The maximum dosage of Bupropion one can have in a day is 450 mg, and that too is in divided doses.

What Are the Side Effects of Bupropion?

Studies have revealed some serious adverse effects of Bupropion. They are,

Abnormal Behavior and Unusual Thoughts:

  • Delusions - Believing and behaving like some other person.

  • Hallucination - Hearing or seeing things that are actually not present.

  • Paranoia - Having a feeling that others are against you.

  • Mania - Elevated level of energy, mood, or emotions.

  • Depression Thoughts - Suicidal feelings, panic attacks, aggressive or violent behavior, and hyperactive actions.

Cardiovascular:

Neurological:

  • Seizure is one of the major side effects.

The other common side effects are

  • Insomnia - Difficulty getting sleep.

  • Diaphoresis - Excessive abnormal sweating.

  • Weight loss.

  • Dizziness and headache.

  • Nausea and vomiting.

  • Tremor.

  • Vision problems.

  • Constipation.

  • Dry mouth.

  • Anxiety.

  • Stuffy nose.

  • Joint pain.

Where Is Bupropion Contraindicated?

  • People with a known history of allergy and hypersensitivity to Bupropion or its constituents should not take medicine.

  • Patients with a seizure disorder or epilepsy refrained from having Bupropion. In addition, Bupropion is also contraindicated in other risk factors of seizures like stroke, head injury, neurological diseases, brain tumor, drug or alcohol addiction, or withdrawal.

  • Patients under monoamine oxidase inhibitors that are present in antibiotic linezolid should not take Bupropion.

  • Bupropion formulation should not be given to people who are already taking other medicines that contain Bupropion.

  • It is advisable to discuss with the healthcare provider about preexisting conditions like liver or kidney problems, seizures, eating disorders, head injury, heart issues, debilitating diseases, usage of drugs or alcohol, other medication histories, and pregnancy or breastfeeding.

  • Pregnant ladies, recently delivered women, nursing mothers, and children are contraindicated to take Bupropion.

  • Research has shown an increased aggregation of Bupropion metabolites in the geriatric population as well.

Can Excess Bupropion Be Toxic?

  • Seizures are very common in the overdose of Bupropion. More than 15 % of patients had seizures due to overdose exposure.

  • Other things with the same side effects include confusion, mental instability, heart rate changes, and palpitations.

  • Larger doses of Bupropion have shown an increased risk of liver toxicity and kidney impairment.

  • Immediately visit the healthcare provider if there seems to be an overdose exposure.

Conclusion:

Bupropion is not a medicine for all kinds of people. It is a prescription drug and is carefully administered to the patients by physicians with extra precaution. The medication guidelines should be well understood and strictly followed. The mental and physical status of the patients is well assessed before and during the treatment of Bupropion. There is a suicidal risk in patients taking Bupropion, and hence they are to be monitored and observed carefully for mental wellbeing or worsening of existing symptoms. An interprofessional team will be needed to handle the outcomes of Bupropion therapy.

The advice is to discuss with the healthcare provider regarding all the body status and doubts before taking and continuing the drug Bupropion.

Frequently Asked Questions

1.

What is bupropion?

Bupropion is an antidepressant medication, prescribed to treat conditions like depression, seasonal affective disorder, and even helps in overcoming the habit of smoking in cases with chronic smoking. Bupropion acts on the brain and helps in feeling calm.

2.

Bupropion is what type of antidepressant?

 
Bupropion is an effective antidepressant, which can be used effectively to treat depression in short term as well as long term treatments and is well tolerated by the patients.

3.

How does a person feel after taking bupropion?

 
Bupropion is an antidepressant which is effective in most of the patients, but in some cases it can cause irritability, agitations or abnormal behaviours during the initial days. Some patients can even have sucidal thoughts therefore bupripion must be taken only as advised by your physician.

4.

Can bupropion be used to treat anxiety?

Bupropion is an antidepressant medication which is effective and safe in treating patients with short-term or chronic depression, but it has also proved to effectively cure anxiety associateted with depression. Bupropion is more effective than sertraline and fluoxetine in patients with anxiety.

5.

Does Bupropruon make you feel energetic?

Bupropion is a antidepressant which is widely used, studies have shown that other antidepressants act on the brain and promote enzymes release which makes you feel energetic, bupripion can have a similar effect, but any such effect has not been proved in accordance with bupropion till date.

6.

Can bupropion make you gain weight?

Most antidepressants have the effect on the weight, and people on long term antidepressants do gain some weight, but buprion on the other hand results in weight loss,  therefore if you experience any alteration in the weight while on medication do inform your doctor.

7.

Who can be prescribed bupripion?

Bupropion being a stimulating antidepressant is very effective in treating chronic depression, or person who feels lack of energy, but the patient with anxiety disorders with depression should not be prescribed bupripion.

8.

Is bupropion effective in patients with ADHD?

 
Bupropion can be used to treat ADHD more effectively than placebo, it helps by reducing the symptoms of ADHD and it can also be effectively used in improving condition in patients with ADHD who cannot be prescribed stimulant drugs.

9.

Is bupropion a stimulant?

 
Bupropion is a antidepressant that acts as a norepinephrine-dopamine reuptake inhibitor, it helps in treating depression by retaining the neurotransmitters dopamine and norepinephrine, but it is not a stimulant.

10.

When we can take bupropion ?

Bupropion mainly taken in the morning.avoid taking last dose after 5 pm.if you take at night it will cause problem with falling asleep.

11.

Does bupropion and adderall have similar affects?

 
No both are very defferent. Bupropion is a antidepressant and adderall is a stimulant and amphitamine.bupropion is used for to stop smoking and adderall is used to treat narcolepsy
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Dr. Siva Anoop Yella
Dr. Siva Anoop Yella

Psychiatry

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