Bupropion HCl SR (Zyban)

What is Buproprion?

Bupropion is an antideperessant medication, which along with nicotine replacement therapy, and Varinecline (Chantix), is also FDA-approved for smoking cessation. For smokers who want to quit, a combination of behavioral modification, counseling, and medication, can significantly improve the chance of success. When used with nicotine replacement therapy, Bupropion has been shown to help with symptoms of nicotine withdrawal such as cravings and anxiety.

How does Bupropion work?

The exact mechanism by which Bupropion helps with smoking cessation is not known.  It may work in part by extending the activity of dopamine in the brain, which in turn can reduce nicotine withdrawal symptoms. Bupropion was developed to treat depression.  Individuals who were being treated for depression with Bupropion reported decreased cigarette cravings, which led the manufacturer to study the drug for the purpose of smoking cessation.

How effective is Bupropion?

Bupropion has been studied in randomized trials for smoking cessation. People treated with Bupropion had higher rates of smoking cessation than people taking a placebo. In one study, patients treated with Bupropion 150 mg twice a day, had greater rates of abstinence after 7 weeks (44% compared to 19%) and one year (23% vs. 12%), than patients who received a placebo. In a large trial of over 8000 people, Bupropion was found to be more effective than placebo and comparable in effect to the nicotine patch.  In the same study Varenicline (Chantix) proved more effective than Bupropion.

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, titanium dioxide and 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 at 150 mg daily. After three days, the dose can be increased to 150 mg twice a day (maximum 300 mg/day). If the higher dose is not well tolerated (due to side effects as discussed below), the lower dose of 150 mg a day can be resumed as it has been shown to be effective. 

Treatment should begin at least two weeks before a target quit date, while you are still smoking, as it takes 1-2 weeks for the drug to start taking effect. If you successfully quit smoking after 7-12 weeks, you may consider continuing Bupropion as maintenance therapy for up to an additional year.  Alternatively, if there is no progress after the seventh week of treatment, then Bupropion is not likely to work, and your provider can consider stopping the medication.

How should I take Bupropion?

You should take Bupropion as prescribed by your doctor. The dose for smoking cessation is 150 mg 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.

What to do if you miss a dose of Bupropion

If you miss a scheduled dose of Bupropion, take it as soon as you remember.  Try to space the remaining doses evenly throughout the day, at least 4 hours apart. If you are closer than 4 hours to your next dose, you should skip the missed dose altogether and take the next dose as scheduled. It is important not to ingest an extra dose to make up for a missed one, as this could produce dangerous side-effects.

What to do if you take too much Bupropion

If you take more Bupropion than recommended, you may have dangerous levels of the drug in your body, which could prove to be fatal. Symptoms of an overdose include:

• Seizures
• Muscle stiffness
• Hallucinations
• Abnormal heart rhythms
• Shallow breathing
• Loss of consciousness

If you think you may have overdosed on Bupropion, seek emergency medical assistance by either calling your doctor or local poison control center. If your symptoms are severe, call 911 immediately.  

Precautions

When used for smoking cessation, serious neurologic and psychiatric events have occurred 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 and have occurred in patients with and without underlying 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 important warnings when used to treat psychiatric disorders, including risk of suicidal ideation and related behavior, 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)
• Antiseizure medications (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)
• Parkinson’s disease medications (levodopa, amantadine)
• MAOIs (rasagiline, selegiline) are contraindicated when taking Bupropion

Contraindications

Bupropion should not be taken by patients with the following conditions:

• 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 potential for long-term effects on child development and behavior from Bupropion use has not been studied.  Always talk to your obstetrician before starting any new medication if you are pregnant, planning to become pregnant or if you are breastfeeding.

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.