Bupropion

What is Buproprion?

Bupropion is one of the FDA approved medications for smoking cessation. Many smokers desire to quit, and using the available treatments gives them a better chance of being successful. The combination of behavior modifications, behavior counseling, and medications significantly improves the chance of success. Some of the barriers to quitting include Nicotine withdrawal symptoms and cravings. Bupropion has been shown to help with these symptoms, in combination with Nicotine replacement.  

How does Bupropion work?

The exact mechanism of how Bupropion works for smoking cessation is not known, but it is thought to be related to modulation of noradrenergic and dopaminergic neurotransmission. The medication was first used to treat depression, but due to reports of people having decreased cravings for cigarettes while being treated for depression with Bupropion, the manufacturer studied the drug for use in smoking cessation.

How effective is Bupropion?

Bupropion has been studied in randomized trials for smoking cessation. People who took Bupropion had higher rates (1.6x) of smoking cessation than people on placebo. In another study, people who took Bupropion 150mg twice a day had greater rates of abstinence after 7 weeks (44% compared to 19% on placebo) and at one year (23% vs. 12% on placebo). In another trial of over 8000 people, bupropion was more effective than placebo. It had comparable cessation rates to the nicotine patch. In that study, Varenicline did have higher quit rates than bupropion, however. 

Active ingredients

Each tablet contains 150 mg of bupropion hydrochloride.

Inactive ingredients

The inactive ingredients in Bupropion are: carnauba wax, cysteine hydrochloride, hypromellose, magnesium stearate, 625 microcrystalline cellulose, polyethylene glycol, polysorbate 80, and titanium dioxide and is 626 printed with edible black ink. In addition, the 150-mg tablet contains FD&C Blue No. 2 Lake 627 and FD&C Red No. 40 Lake.

Bupropion Dosage

Bupropion is dosed 150mg daily. After three days, the dose may be increased to 150mg twice a day (maximum 300mg/day). However, if this is not tolerated due to side effects as discussed below, the lower dose of 150mg a day has been shown to be effective. Bupropion does not have to be taken with meals. Bupropion must be swallowed whole (do not chew or crush tablets).

Treatment should begin at least two weeks before your target quit date (while still smoking, because it takes 1-2 weeks for the drug to start being effective). If you successfully quit smoking after 7-12 weeks, may consider continuing Bupropion as maintenance therapy afterwards for up to 1 year.  On the other hand, if there is no progress after the seventh week of treatment, then Bupropion is not likely to work, and your provider can consider stopping this medication.

How should I take Bupropion?

You should take Bupropion as prescribed by your doctor. The dose for smoking cessation is 150mg daily or 150 mg twice a day. It must be started 1-2 weeks before the planned “quit date” as the medication takes that long to start working. It does not need to be taken with food. The tablets should be taken whole, not chewed or crushed.

Precautions

When used for smoking cessation, serious neuropsychiatric events have occured in patients taking Bupropion. These include mood changes (depression, mania), psychosis, hallucinations, paranoia, delusions, homicidal thoughts, agitation, suicidal thoughts and suicide attempts. These symptoms may be related to nicotine withdrawal. These effects happened in patients both with and without psychiatric conditions (such as depression). It is important to stop taking Bupropion and contact a health care provider if any side effects occur.

Bupropion is also used to treat psychiatric disorders such as depression. The medication carries psychiatric warnings when used to treat psychiatric disorders, including suicidal thinking/behaviors especially in young adults.

Bupropion should not be used if you have a history of seizures, epilepsy, or are stopping alcohol use suddenly as it can increase the risk of seizures.

Bupropion may cause mild pupil dilation, which can cause an episode of narrow-angle glaucoma in susceptible patients.

Side Effects

The most common side effects (>10%) include:

• Fast heart rate
• Insomnia
• Headache
• Dizziness
• Sweatiness
• Weight Loss
• Dry Mouth
• Constipation
• Nausea/Vomiting
• Tremor

Drug Interactions

Bupropion has the potential to interact with the following medications:

• Ticlopidine
• Clopidogrel (Plavix)
• HIV Medications (Ritonavir, Lopinavir, Efavirenz)
• Carbamazepine, Phenobarbital, Phenytoin
• Antidepressants (Venlafaxine, Nortriptyline, Imipramine, Desipramine, Paroxetine, Fluoxetine, Sertraline)
• Antipsychotics (haloperidol, risperidone, thioridazine)
• Beta-blockers (metoprolol)
• Antiarrhythmics (propafenone, flecainide) and other Type 1C antiarrhythmics.
• Levodopa, amantadine
• Contraindicated with MAOIs

Contraindications

Bupropion is contraindicated in the the following patients:

• History of seizure disorder or seizures
• History of Bulimia or anorexia nervosa
• Undergoing abrupt discontinuation of alcohol, benzodiazepines (such as Xanax) or anti-seizure medications.
• Taking MAOIs (monoamine oxidase inhibitors) for psychiatric disorders
• Allergy to bupropion or any of its ingredients

Is Bupropion safe in pregnancy?

Studies of pregnant women who took Bupropion during the first trimester did not show any increased risk of birth defects. However, it has not been studied extensively and there is no long-term data. Bupropion should only be used in pregnancy if the benefit justifies the potential risk to the fetus. The long-term effect on development and behavior of Bupropion has not been studied.

Is Bupropion safe for breastfeeding?

Bupropion is present in breast-milk. Seizures and sleep disturbances were reported in breastfeeding infants whose mothers were using Bupropion, and infants should be closely monitored. However, the use of bupropion is not considered a contraindication to breastfeeding. The risks and benefits of breastfeeding should be discussed with your doctor.