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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 [mind] (byu PROP pee on)
Brand name(s): APLENZIN, FORFIVO XL, WELLBUTRIN SR, WELLBUTRIN XL
GENERIC: available FAMILY: Other Drugs for Depression
Find the drug label by searching at DailyMed.

Pregnancy and Breast-feeding Warnings [top]

Pregnancy Warning

There is concern about the safety of bupropion use in pregnant women: the drug is both genotoxic (damages DNA) and carcinogenic in animal studies. Use in pregnancy only if clearly needed. GlaxoSmithKline maintains a pregnancy registry for which health care providers are encouraged to register their patients.

Breast-feeding Warning

Bupropion and its metabolites are excreted in human milk. Because of the potential for serious adverse effects in nursing infants, you should not take this drug while nursing.

Safety Warnings For This Drug [top]

FDA BLACK BOX WARNING

Suicidality and Antidepressant Drugs

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 patients over age 24; there was a reduction in risk with antidepressant use in patients aged 65 and older. In patients of all ages who are started on antidepressant therapy, monitor closely for clinical worsening and emergence of suicidal thoughts and behaviors. Advise families and caregivers of the need for close observation and communication with the prescriber.

Anticholinergic Effects

Warning: Special Mental and Physical Adverse Effects

Older adults are especially sensitive to the harmful anticholinergic effects of these drugs. 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]

Bupropion (APLENZIN, FORFIVO XL, WELLBUTRIN SR, WELLBUTRIN XL) is used to control, but not cure, severe depression that is not caused by other drugs, alcohol or emotional losses (such as a death in the family). Bupropion is related to drugs in the amphetamine family (ADDERALL, ADDERALL XR) and to diethylpropion (TENUATE, TEPANIL) but purportedly is not habit-forming. Although bupropion is preferred by some doctors for use in elderly patients,[1] it has not been studied much in such patients.

...

Bupropion (APLENZIN, FORFIVO XL, WELLBUTRIN SR, WELLBUTRIN XL) is used to control, but not cure, severe depression that is not caused by other drugs, alcohol or emotional losses (such as a death in the family). Bupropion is related to drugs in the amphetamine family (ADDERALL, ADDERALL XR) and to diethylpropion (TENUATE, TEPANIL) but purportedly is not habit-forming. Although bupropion is preferred by some doctors for use in elderly patients,[1] it has not been studied much in such patients.

We have designated bupropion as Limited Use. For patients who need an antidepressant drug, we recommend trying one of the newer selective serotonin reuptake inhibitors (SSRIs) (for example, fluoxetine [PROZAC, SARAFEM, SELFEMRA]) first, as these are the safest antidepressants. If symptoms do not improve sufficiently on an SSRI and remain severe, further treatment with other antidepressants is warranted.

Bupropion can take up to four weeks to be effective. The length of time it takes an antidepressant to work can overlap with spontaneous recovery — recovery that might occur without the use of medications — especially if the depression is situational (for example, caused by a death or other external circumstances). Most people recover from depression with friends, spiritual resources or activities such as exercise, work, reading, play, art and travel. If depression is not overcome by these measures, patients should seek help from mental health professionals, such as therapists or psychiatrists. Antidepressant drugs should be reserved for major depression in which the patient does not respond to psychotherapy alone.

Adverse effects

Weight loss is a common adverse effect of this drug. A number of people become restless when taking bupropion. Also, people aged 60 and older are more likely to experience adverse effects such as heart complications.

In October 2014, the Australian Department of Health Therapeutic Goods Administration, a regulatory agency similar to the Food and Drug Administration (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.[2]

Antidepressants and pregnancy

On Aug. 9, 2004, Health Canada, a regulatory agency similar to the FDA, issued a public advisory warning to Canadians that newborns may be adversely affected when their mothers take a selective serotonin reuptake inhibitor (SSRI) and other newer antidepressants during the third trimester of pregnancy. Health Canada reported that some newborns whose mothers took these drugs during pregnancy have developed complications at birth requiring prolonged hospitalization, breathing support and tube feeding. The symptoms reported include feeding and breathing difficulties, seizures, muscle rigidity, jitteriness and constant crying. In most cases, the mothers were prescribed newer antidepressants during the third trimester of pregnancy.[3]

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.[4]

Psychiatric behaviors

Patients treated with bupropion should be observed for changes in psychiatric behaviors. These behaviors can include hostility, agitation, depression and suicidality. Most of these symptoms were reported in patients who were currently taking bupropion, but some were also reported in patients after they had stopped taking bupropion.

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 patients for 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 between 450 and 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 oral hypoglycemics or insulin to treat diabetes.

Many drugs (e.g., antipsychotics, antidepressants, theophylline and systemic steroids) are known to lower the seizure threshold. Bupropion should be used with extreme caution in patients with severe hepatic 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.

Studies show ...

A major meta-analysis (a study that combines data from multiple clinical trials) commissioned by the U.S. Department of Health and Human Services failed to find any significant differences in effectiveness between older antidepressants (such as bupropion) and newer antidepressants (such as SSRIs).

In terms of adverse drug reactions, there was no significant difference between the new and old antidepressants in overall discontinuation rates by patients.[5] (Drug discontinuation rates can be used to compare adverse reactions between drugs.)

Higher Doses Increase Likelihood of Harmful Effects

Bupropion doses higher than 450 milligrams (mg) per day increase the risk of seizures tenfold.[6] According to the drug’s labeling, even dosages higher than 300 mg (but lower than 450 mg) per day have been associated with seizures. Bupropion was temporarily banned in the U.S. for this reason.

Dosages should be limited to no more than 300 mg per day. People aged 60 and older are more likely to experience side effects such as heart complications. Due to age-related decreases in kidney and liver function, the lowest effective dose should be used.

 

Drug Interaction

In 2017, the FDA approved a change to the product label of bupropion that indicated that the blood level of heart drug digoxin may increase when bupropion and digoxin are used together.[7]

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. Bupropion is one of a limited number of drugs for which the FDA requires an FDA-approved Medication Guide to be dispensed when the prescription is filled. (Click here to view the WELLBUTRIN Medication Guide.) An FDA advisory committee has unanimously recommended that all prescription drugs be accompanied by such Medication Guides, but at present, less than 5% of drugs are. The other 95% of drugs are accompanied by unregulated, often dangerously incomplete information leaflets not approved by the FDA.

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.[8]

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.

2020: The Medicines and Healthcare products Regulatory Agency (an agency in the U.K. similar to the FDA) issued an advisory that serotonin syndrome has been reported with use of bupropion.[9]

Symptoms of serotonin syndrome include restlessness, hallucinations, loss of coordination, fast heartbeat, increased body temperature, rapid changes in blood pressure, overactive reflexes, diarrhea, coma, nausea and vomiting.

Before You Use This Drug [top]

Do not use if you have or have had:

  • eating disorders, such as anorexia or bulimia
  • seizures
  • pregnancy or are breast-feeding (drug crosses placenta and accumulates in breast milk)

Tell your doctor if you have or have had:

  •   allergies to drugs
  •   bipolar disorder (manic depression)
  •   drug abuse
  •   electroshock therapy[10]
  •   head injury
  •   heart, kidney, or liver problems
  •   heart attack
  •   psychosis
  •   tumor of the central nervous system
  •   brain tumor
  •   seizures

Tell your doctor about any other drugs you take, including aspirin, herbs, vitamins, and other nonprescription products.

When You Use This Drug [top]

  • Until you know how you react to this drug, do not drive or perform other activities requiring alertness.
  • Do not drink alcohol.

How to Use This Drug [top]

  • If you miss a dose, take it as soon as you remember, but skip it if it is within four hours of 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 food.
  • Swallow extended-release tablets whole.
  • Space doses evenly apart during the day, but avoid taking at bedtime.
  • Store tablets 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.

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:

Do not take bupropion within 14 days of starting or stopping these monoamine oxidase (MAO) inhibitors: deprenyl, ELDEPRYL, furazolidone, FUROXONE, isocarboxazid, MARPLAN, MATULANE, NARDIL, PARNATE, phenelzine, procarbazine, selegiline, tranylcypromine.

The beta blocker drugs such as metoprolol (LOPRESSOR). Click here for a list of beta blockers.

These drugs also can interact with bupropion: alcohol, amitriptyline, AVENTYL, chlorpromazine, clozapine, CLOZARIL, desipramine, DESYREL, ELAVIL, fluoxetine, HALDOL, haloperidol, imipramine, lithium, LITHOBID, LITHONATE, loxapine, LOXITANE, LUDIOMIL, maprotiline, MOBAN, moclobemide, molindone, NAVANE, NORPRAMIN, nortriptyline, NORVIR, pargyline, paroxetine, PAXIL, PROZAC, RISPERDAL, risperidone, ritonavir, sertraline, thioridazine, thiothixene, THORAZINE, TOFRANIL, trazodone, ZOLOFT.

Adverse Effects [top]

Call your doctor immediately if you experience:

  • agitation, anxiety, confusion
  • seizures
  • convulsions
  • fainting
  • hallucinations
  • delusions
  • trouble concentrating
  • severe headache
  • skin rash, itching, hives
  • tinnitus (buzzing or ringing in ears)[11]

Call your doctor if these symptoms continue:

  •   anger, hostility
  •   low or high blood pressure
  •   constipation
  •   diarrhea
  •   dizziness
  •   drowsiness
  •   dry mouth
  •   increased saliva
  •   fever
  •   chills
  •   sore throat
  •   impotence
  •   incoordination
  •   inflammation of the mouth
  •   loss of appetite, weight loss
  •   muscle spasms, tremor, twitching
  •   muscle pain
  •   nausea or vomiting
  •   abdominal pain
  •   tinnitus (buzzing or ringing in ears)[11]
  •   increased sweating
  •   weight change
  •   unusual tiredness, sleep disturbance
  •   tremor
  •   difficulty concentrating
  •   increase in frequency of urination, especially at night, or difficult urination
  •   blurred vision
  •   fast or irregular heartbeat
  •   change in sense of taste

Periodic Tests[top]

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

  • kidney function tests
  • liver function tests
  • supervision for suicidal tendencies

last reviewed January 31, 2021