Worst Pills, Best Pills

An expert, independent second opinion on more than 1,800 prescription drugs, over-the-counter medications, and supplements

Drug Profile

The information on this site is intended to supplement and enhance, not replace, the advice of a physician who is familiar with your medical history. Decisions about your health should always be made ONLY after detailed conversation with your doctor.

Limited Use [what does this mean?]
Generic drug name: bupropion [smoking] (byu PRO pee on)
Brand name(s): ZYBAN
GENERIC: available FAMILY: Other Drugs for Smoking Cessation
Find the drug label by searching at DailyMed.

Pregnancy and Breast-feeding Warnings [top]

Pregnancy Warning

Because smoking is extremely dangerous to the developing fetus, the safest thing you can do is not smoke while pregnant (or afterward). Educational and behavioral methods to quit smoking are the first choice. If you cannot stop smoking on your own, use this medicine, if advised to do so by your doctor. However, bupropion crosses the placenta, exposing the fetus to the drug. Tell your doctor if you are pregnant or thinking of becoming pregnant before you take this drug.

Breast-feeding Warning

Bupropion and its metabolites are excreted at high levels in human milk and have caused serious adverse reactions, including seizures, in the infant. Because of the potential for adverse effects in nursing infants, you should not take this drug while nursing.

Safety Warnings For This Drug [top]

Product Warnings

Ask a doctor or pharmacist before use if you are taking antibiotics.

When using this product, tiredness, drowsiness or dizziness may occur. Be careful driving or operating machinery.

Stop using and ask a doctor if symptoms get worse, diarrhea lasts more than two days or you get abdominal swelling or bulging. These may be signs of a serious condition.

If pregnant or breast-feeding, ask a health care professional before use.

Older adults are especially sensitive to the harmful anticholinergic effects of this drug. Drugs in this family should not be used unless absolutely necessary.

Mental Effects: confusion, delirium, short-term memory problems, disorientation and impaired attention.

Physical Effects: dry mouth, constipation, difficulty urinating (especially for a man with an enlarged prostate), blurred vision, decreased sweating with increased body temperature, sexual dysfunction and worsening of glaucoma.

Extreme Caution

Bupropion has been approved by the FDA for use in smoking cessation for people 18 years of age and older under the brand name Zyban. Zyban and Wellbutrin are exactly the same drug. Taking Zyban and Wellbutrin together will increase the risk of seizure. See the warning about bupropion-induced seizure below.

Bupropion, marketed as Wellbutrin, is used to treat severe depression that is not caused by other drugs, alcohol, or emotional losses (such as death in the family). Antidepressants increase the risk of suicidal thinking and behavior (suicidality) in short term studies in children and adolescents with major depressive disorder (MDD) and other psychiatric disorders.

Facts About This Drug [top]

 

FDA BLACK-BOX WARNING

 

WARNING: SUICIDAL THOUGHTS AND BEHAVIORS


SUICIDALITY AND ANTIDEPRESSANT DRUGS

Although ZYBAN is not indicated for treatment of depression, it contains the same active ingredient as the antidepressant medications WELLBUTRIN, WELLBUTRIN SR, and WELLBUTRIN XL. Antidepressants increased the risk of suicidal thoughts and behavior in children, adolescents and young adults in short-term trials. These trials did not show...

 

FDA BLACK-BOX WARNING

 

WARNING: SUICIDAL THOUGHTS AND BEHAVIORS


SUICIDALITY AND ANTIDEPRESSANT DRUGS

Although ZYBAN is not indicated for treatment of depression, it contains the same active ingredient as the antidepressant medications WELLBUTRIN, WELLBUTRIN SR, and WELLBUTRIN XL. Antidepressants increased the risk of suicidal thoughts and behavior in children, adolescents and young adults in short-term trials. These trials did not show an increase in the risk of suicidal thoughts and behavior with antidepressant use in subjects over age 24; there was a reduction in risk with antidepressant use in subjects aged 65 and older.

In patients of all ages who are started on antidepressant therapy, monitor closely for worsening, and for emergence of, suicidal thoughts and behaviors. Advise families and caregivers of the need for close observation and communication with the prescriber.

Bupropion (ZYBAN) is a non-nicotine aid to smoking cessation and is approved by the Food and Drug Administration (FDA) as an aid to smoking cessation treatment.

Side effects

Seizures

Because the use of bupropion is associated with an increased risk of seizures, doses over 300 milligrams (mg) per day for smoking cessation should not be used. The risk of seizures is also related to patient factors, clinical situation and other drugs taken with bupropion, all of which must be considered when selecting treatment with this drug. Use of bupropion should be discontinued and not restarted in patients who experience a seizure during treatment.

The seizure rate associated with doses of sustained-release bupropion up to 300 mg per day is approximately 0.1 percent (1/1,000). This rate was determined during eight weeks of treatment in approximately 3,100 depressed patients. Data for the immediate-release formulation of bupropion revealed a seizure rate of approximately 0.4 percent (4/1,000) in depressed patients treated at doses  ranging from 300 to 450 mg per day. In addition, the estimated seizure incidence increases almost tenfold with doses from 450 to 600 mg per day.

Predisposing factors that may increase the risk of seizure with bupropion use include history of head trauma or prior seizure, central nervous system tumor, the presence of severe hepatic (liver) cirrhosis and concomitant medications that lower seizure threshold.

Situations associated with an increased seizure risk include, among others, excessive use of alcohol or sedatives (including benzodiazepines); addiction to opiates, cocaine or stimulants; use of over-the-counter stimulants and anorectics; and use of insulin or oral diabetes drugs.

Many other drugs (for example, antipsychotics, antidepressants, theophylline and systemic steroids) are known to lower seizure threshold.

Bupropion should be used with extreme caution in patients with severe liver cirrhosis. In these patients, a reduced frequency of dosing is required, as peak bupropion levels are substantially increased and higher-than-usual accumulation is likely to occur. The dose should not exceed 150 mg every other day in these patients.[1]

Psychiatric behaviors

Patients treated with bupropion should be observed for abnormal psychiatric behaviors. These behaviors can include hostility, agitation, depression and suicidality. Most of these symptoms were reported in patients during treatment with bupropion, but some were also reported in patients after stopping bupropion.[2] Patients treated with the drug have also experienced delusions, hallucinations, psychosis, problems with concentration, paranoia and confusion.

Antidepressants and pregnancy

An article published in Prescrire International in January 2012 examined the use of bupropion during pregnancy and the increased risk of congenital heart defects in children. The data showed that children born to mothers who used bupropion during pregnancy had an increased risk of cardiac malformations.[3]

Cardiovascular events

Bupropion can cause elevated blood pressure and hypertension, which can increase the risk of adverse cardiovascular events.

In October 2014, the Australian Department of Health Therapeutic Goods Administration, a regulatory agency similar to the FDA, issued an advisory that the drug product information for bupropion would be updated to include information on reports of cardiovascular adverse events, including 24 heart attacks and five strokes, in patients taking the drug.[4]

Regulatory actions surrounding bupropion 

2004: In October, the FDA issued a public health advisory requiring manufacturers to add a black-box warning (see “FDA Black-Box Warning” at the top of this page) to the professional product labeling of all antidepressants. A black-box warning is the strongest type of warning that the FDA can require.

The FDA also required that a Medication Guide be given to patients receiving this drug to advise them of the risks and of precautions that can be taken.

2007: The FDA announced in May that it would require new warnings concerning the increased risk of suicidal thoughts and behavior in young adults ages 18 to 24 during the first one to two months of treatment with antidepressants. The agency required the new warnings to be black-box warnings, printed on the professional product labels for all antidepressants sold in the U.S. The warnings amended an existing black-box warning for children and adolescents.[5]

The FDA-approved professional product labeling for antidepressant drugs sold in the U.S. carries the following statement:

Suicide: The possibility of a suicide attempt is inherent in major depressive disorder and may persist until significant remission occurs. Close supervision of high-risk patients should accompany initial drug therapy. Prescriptions for Drug X should be written for the smallest quantity of tablets consistent with good patient management, in order to reduce the risk of overdose. 

Before You Use This Drug [top]

Do not use if you have or have had:

  • eating disorders, such as anorexia or bulimia
  • seizures

Tell your doctor if you have or have had:

  • pregnancy or are breast-feeding
  • allergies to drugs
  • bipolar disorder (manic depression)
  • brain tumor
  • head injury
  • neurologic disease
  • seizures
  • drug abuse
  • heart disease
  • liver disease
  • kidney disease
  • high blood pressure
  • psychosis

Tell your doctor about any other drugs you take, including aspirin, herbs, vitamins, and other nonprescription products; buproprion comes under different brand names, including Wellbutrin and Zyban.

 

 

When You Use This Drug [top]

  • Participate in a smoking cessation program.
  • Until you know how you react to this drug, do not drive or perform other activities requiring alertness.
  • Do not drink alcohol.
  • Do not take bupropion under different brand names at the same time that you are taking it for smoking cessation.

How to Use This Drug [top]

  • If you miss a dose, take it as soon as you remember, but skip it if it is almost time for the next dose. Do not take double doses.
  • Do not share your medication with others.
  • Take the drug at the same time(s) each day.
  • Take with or without food.
  • Do not break, chew, or crush long-acting forms of this drug.
  • Store at room temperature with lid on tightly. Do not store in the bathroom. Do not expose to heat, moisture, or strong light. Keep out of reach of children.
  • Take doses of prompt-release tablets at least four hours apart.
  • Take doses of extended-release tablets at least eight hours apart.
  • Take this drug for seven or more days prior to the date on which smoking will be stopped.

Interactions with Other Drugs [top]

The following drugs, biologics (e.g., vaccines, therapeutic antibodies), or foods are listed in Evaluations of Drug Interactions 2003 as causing “highly clinically significant” or “clinically significant” interactions when used together with any of the drugs in this section. In some sections with multiple drugs, the interaction may have been reported for one but not all drugs in this section, but we include the interaction because the drugs in this section are similar to one another. We have also included potentially serious interactions listed in the drug’s FDA-approved professional package insert or in published medical journal articles. There may be other drugs, especially those in the families of drugs listed below, that also will react with this drug to cause severe adverse effects. Make sure to tell your doctor and pharmacist the drugs you are taking and tell them if you are taking any of these interacting drugs:

At least two weeks should elapse after you stop taking a monoamine oxidase (MAO) inhibitor and before you start taking bupropion. The same is true if you stop taking bupropion and then start one of these MAO inhibitors: deprenyl, ELDEPRYL, EUTONYL, furazolidone, FUROXONE, isocarboxazid, MARPLAN, MATULANE, NARDIL, PARNATE, phenelzine, procarbazine, selegiline, tranylcypromine.

AVENTYL, carbamazepine, cyclophosphamide, CYTOXIN, desipramine, digoxin, DILANTIN, flecainide, fluoxetine, HALDOL, haloperidol, imipramine, LANOXIN, LOPRESSOR, MELLARIL, metoprolol, NORFLEX, NORPRAMINE, nortriptyline, orphenadrine, paroxetine, PAXIL, phenobarbital, phenytoin, propafenone, PROZAC, RISPERDAL, risperidone, RYTHMOL, sertraline, TAMBOCOR, TEGRETOL, thioridazine, TOFRANIL, ZOLOFT.

Taking bupropion with other drugs that also affect the central nervous system adds to adverse effects, including risk of seizures: alcohol, amitriptyline, chlorpromazine, clozapine, CLOZARIL, DESYREL, ELAVIL, fluoxetine, HALDOL, haloperidol, lithium, LITHOBID, LITHONATE, loxapine, LOXITANE, LUDIOMIL, maprotiline, meclobemide, MOBAN, molindone, NAVANE, NORVIR, pargyline, PROZAC, ritonavir, thiothixene, THORAZINE, trazodone.

Adverse Effects [top]

Call your doctor immediately if you experience:

  • agitation
  • anxiety
  • severe headache
  • skin rash, hives, or itching
  • ringing in ears
  • fainting
  • confusion
  • delusions
  • hallucinations
  • paranoia
  • trouble concentrating
  • seizures

Call your doctor if these symptoms continue:

  • abdominal pain
  • decrease in appetite
  • constipation
  • dizziness
  • dry mouth
  • increased sweating
  • insomnia
  • muscle pain
  • nausea or vomiting
  • sore throat
  • tremor
  • unusual weight loss
  • blurred vision
  • drowsiness
  • fast or irregular heartbeat
  • change in sense of taste
  • unusual feeling of well-being
  • frequent urination

Signs of overdose:

  • hallucinations
  • loss of consciousness
  • nausea or vomiting
  • seizures
  • fast heartbeat

If you suspect an overdose, call this number to contact your poison control center: (800) 222-1222.

Periodic Tests[top]

Ask your doctor which of these tests should be done periodically while you are taking this drug:

  • supervision for suicidal tendencies
  • blood pressure

last reviewed February 28, 2021