Bupropion

Bupropion is used as a prescription medical treatment for depression. It can improve mood and feelings of well-being. It may work by helping to restore the balance of certain natural chemicals (neurotransmitters) in the brain.

• This prescription medication may also be used as a treatment to manage attention deficit hyperactivity disorder (ADHD).
• It may also be used as a prescription treatment to help people quit smoking by decreasing cravings and nicotine withdrawal effects.
• It may be used to prevent autumn-winter seasonal depression (seasonal affective disorder).
• This drug may also be used with other medications as a treatment for bipolar disorder (depression phase).
• It may also be used to treat anxiety in people with depression.
• This medication is available under the following different brand names: Wellbutrin, Zyban, Budeprion SR, Aplenzin, Buproban, Wellbutrin SR, Wellbutrin XL, and Forfivo XL.

Side effects of bupropion include:

• Headache
• Dry mouth
• Nausea
• Weight loss
• Insomnia
• Agitation
• Dizziness
• Sore throat
• Constipation
• Infection
• Abdominal pain
• Anxiety
• Diarrhea
• Ringing in the ears
• Tremor
• Nervousness
• Loss of appetite
• Palpitations
• Muscle pain
• Sweating
• Rash
• Sinus infection (sinusitis)
• Weight gain
• Chest pain
• Urinary frequency
• Vaginal bleeding
• Itching
• Vomiting
• Joint pain
• Flushing
• Migraine
• Decreased memory
• Irritability
• Drowsiness
• Difficulty swallowing
• Arthritis
• Numbness and tingling
• Fever
• Twitching
• Seizures (0.4% [less than 450 mg/day], greater than 3% [greater than 450 mg/day]; may be increased risk with concomitant ECT)

Other side effects of bupropion include:

• Confusion
• Cystitis
• Skin redness
• Loss of control of bodily movements
• Coma
• EEG abnormality
• Euphoria
• Gastric reflux

Other postmarketing side effects of bupropion reported include:

• Nervous system: Abnormal electroencephalogram (EEG), aggression, akinesia, aphasia, completed suicide, delirium, delusions, dysarthria, extrapyramidal syndrome (dyskinesia, dystonia, hypokinesia, parkinsonism), hallucinations, increased libido, manic reaction, neuralgia, neuropathy, paranoid ideation, restlessness, suicide attempt, and unmasking tardive dyskinesia

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors;
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheartedness, or passing out.

This document does not contain all possible side effects and others may occur. Check with your physician for additional information about side effects.

Dosages of Bupropion

Dosage Forms and Strengths

Tablet (Wellbutrin)

• 75 mg
• 100 mg

Tablet, sustained-release (Wellbutrin SR)

• 100 mg
• 150 mg
• 200 mg

Tablet, extended-release (Wellbutrin XL)

• 150 mg
• 300 mg

Tablet, extended-release (Aplenzin)

• 174 mg
• 348 mg
• 522 mg

Tablet, extended-release (Forfivo XL)

• 450 mg

Tablet, extended-release (Zyban), Adult Only

• 150 mg

Dosage Considerations – Should be Given as Follows:

Major Depressive Disorder

Immediate-release

• Initial: 100 mg orally every 12 hours; may adjust to 100 mg orally every 8 hours as early as day 4; may consider increasing up to a maximum of 150 mg every 8 hours after several weeks if no clinical improvement is observed with 100 mg every 8 hours
• Alternatively, may initiate with 75 mg orally every 8 hours

Sustained-release

• Initial: 150 mg orally once/day; may adjust to 150 mg every 12 hours after 3 days
• May increase to no more than 200 mg every 12 hours after more than 4 weeks if no clinical improvement is observed with 150 mg every 12 hours

Extended-release

• Initial: 150 mg orally once/day; may increase to 300 mg once/day on day 4
• May adjust not to exceed 450 mg once/day after more than 4 weeks if no clinical improvement is observed with 300 mg once/day; Forfivo may be used only after titrating initially with other bupropion drug products

Aplenzin

• Initial: 174 mg orally once/day; after 4 days, may adjust to a usual adult target dose of 348 mg orally once/day
• May increase not to exceed 522 mg once/day after more than 4 weeks

Forfivo XL

• 450 mg orally once/day without regard to food
• This drug can be used in people who have been receiving 300 mg/day of another bupropion formulation for at least 2 weeks and who require a dosage of 450 mg/day
• People who are currently being treated with other bupropion products at 450 mg/day can be switched to an equivalent dose of Forfivo XL once daily

Dosing considerations (Depression)

• Extended-release: When switching to XL, give the same total daily dose at the indicated frequencies: 3 times daily for immediate-release, twice daily for sustained-release, and once daily for extended-release
• Forfivo XL: Do not initiate treatment with Forfivo XL; use another bupropion formulation for the initial dosage
• Switching from hydrochloride salt formulation to hydrobromide salt (Aplenzin): 150 mg/day hydrochloride salt = 174 mg/day hydrobromide salt; 300 mg/day hydrochloride salt = 348 mg/day hydrobromide salt; 450 mg/day hydrochloride salt = 522 mg/day hydrobromide salt

Seasonal Affective Disorder (SAD)

Wellbutrin XL: 150 mg orally once/day; may increase to 300 mg once/day

Aplenzin (bupropion hydrobromide): 174 mg orally once/day initially (equivalent to 150 mg bupropion HCl); after 1 week, may increase to the usual target of 348 mg/day (equivalent to 300 mg bupropion HCL)

Dosing considerations (SAD)

• Initiate treatment in the autumn before the onset of seasonal depressive symptoms and continue through the winter season

Smoking Cessation

• Zyban: 150 mg orally once/day for 3 days, THEN
• Increase to 150 mg every 12 hours; should continue treatment for 7-12 weeks; if a patient successfully quits after 7-12 weeks, consider ongoing maintenance therapy based on the individual patient risk/benefit

Dosing considerations (Smoking Cessation)

• Begin therapy 1 week before the target quit date (usually the second week of treatment)
• It May be combined with the use of the nicotine patch

Attention Deficit Hyperactivity Disorder (ADHD) (Off-label)

Adult

• Initial: 150 mg/day orally
• Titrate to 150-450 mg/day based on tolerability and efficacy; may administer in divided doses or ER or SR formulations

Pediatric

Immediate-release

• Initial: 3 mg/kg/day or 150 mg/day orally
• Titrate to 6 mg/kg/day or 300 mg/day, maximum
• Single-dose should not exceed 150 mg; may administer as divided doses for safety and effectiveness (e.g., twice daily for children and three times daily for adolescents)

Extended-release

• Initial: Up to 3 mg/kg/day or 150 mg/day orally
• Titrate to 6 mg/kg/day or 300 mg/day, maximum

Sustained-release

• Initial: Up to 3 mg/kg/day or 150 mg/day orally
• Titrate to 6 mg/kg/day or 300 mg/day, maximum

Neuropathic Pain (Off-label)

• 150 mg bupropion SR orally twice daily for 6 weeks

Dosage Modifications

Hepatic impairment

• Mild to moderate: Use caution; consider reducing amount or frequency; Forfivo XL not recommended
• Moderate to severe (Buproban, Wellbutrin XL, Zyban): Not to exceed 150 mg every other day
• Moderate to severe (Aplenzin): Not to exceed 174 mg every other day
• Moderate to severe (Wellbutrin): 75 mg once daily
• Moderate to severe (Wellbutrin SR): 100 mg once daily or 150 mg every other day
• Moderate to severe (Zyban): 150 mg every other day
• Elderly: Lower dose/frequency may be required because of decreased renal/hepatic clearance

Renal impairment

• Use caution; consider reduction

Abuse warning

• XL and SR tablets are intended for oral use only
• Inhaling crushed tablets or injecting dissolved tablets has been reported to cause seizures and/or death

If your doctor has directed you to use this medication for diabetes, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Severe interactions of bupropion include:
  • eliglustat
  • isocarboxazid
  • phenelzine
  • pimozide
  • rasagiline
  • selegiline
  • selegiline transdermal
  • tranylcypromine
• Bupropion has serious interactions with at least 22 different drugs.
• Bupropion has moderate interactions with at least 91 different drugs.
• Bupropion has mild interactions with at least 22 different drugs.

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. Check with your physician if you have health questions or concerns.

Warnings

No FDA approved for bipolar depression

Suicidally

• In short-term studies, antidepressants increased t suicidal thinking and behavior in children, adolescents, and young adults (younger than 24 years) taking antidepressants for major depressive disorders and other psychiatric illnesses; this increase was not seen in patients older than 24 years
• A slight decrease in suicidal thinking was seen in adults older than 65 years
• In children and young adults, risks must be weighed against the benefits of taking antidepressants
• Patients should be monitored closely for changes in behavior, clinical worsening, and suicidal tendencies; this should be done during initial 1-2 months of therapy and dosage adjustments
• The patient's family should communicate any abrupt changes in behavior to the healthcare provider
• Worsening behavior and suicidal tendencies that are not part of the presenting symptoms may require discontinuation of therapy; this drug is not approved for use in pediatric patients

This medication contains bupropion. Do not take Wellbutrin, Zyban, Budeprion SR, Aplenzin, Buproban, Wellbutrin SR, Wellbutrin XL, or Forfivo XL if you are allergic to bupropion or any ingredients contained in this drug.

Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Contraindications

• Hypersensitivity to bupropion or other ingredients
• History of anorexia/bulimia; patients undergoing abrupt discontinuation of ethanol or sedatives including anticonvulsants, barbiturates, or benzodiazepines
• Co-administration of any other medications that contain bupropion, because seizures are dose-dependent

Aplenzin contraindications

• Seizure disorder or conditions that increase seizure risk (arteriovenous malformation, severe head injury, CNS tumor, CNS infection, severe stroke, anorexia nervosa, or bulimia (current or prior diagnosis)

Co-administration with MAOIs

• Co-administration may cause serotonin syndrome
• Do not use concomitantly or initiate bupropion within 14 days of stopping an MAOI
• Conversely, at least 14 days should be allowed after stopping bupropion before starting an MAOI antidepressant
• Starting bupropion in a patient who is being treated with linezolid or IV methylene blue is contraindicated because of an increased potential for serotonin syndrome
• If linezolid or IV methylene blue must be administered, discontinue bupropion immediately and monitor for CNS toxicity; may resume 24 hours after the last linezolid or methylene blue dose or after 2 weeks of monitoring, whichever comes first

Effects of Drug Abuse

Abuse warning

• XL and SR tablets are intended for oral use only
• Inhaling crushed tablets or injecting dissolved tablets has been reported to cause seizures and/or death

Short-Term Effects

• See "What Are Side Effects Associated with Using Bupropion?"

Long-Term Effects

• See "What Are Side Effects Associated with Using Bupropion?"

Cautions

• Caution in severe hepatic cirrhosis (do not exceed 150 mg every other day), mild-moderate hepatic impairment, head trauma, prior seizure history, CNS tumor, concomitant meds lowering the seizure threshold.
• Observe for neuropsychiatric symptoms, such as changes in behavior, hostility, agitation, depressed mood, and suicide-related events, including ideation, behavior, and attempted suicide; therapy may cause delusions, hallucinations, psychosis, paranoia, confusion, and concentration disturbance; symptoms may abate with dose reduction.
• The potential risk of hepatotoxicity.
• Assess blood pressure before initiating treatment with sustained-release formulation, and monitor periodically during treatment; risk of hypertension is increased if sustained release formulation is used concomitantly with MAOIs or other drugs that increase dopaminergic or noradrenergic activity; use caution in people with cardiovascular disease.
• May cause weight loss; use caution if weight loss is not desirable.
• May cause CNS depression and impair the ability to operate heavy machinery.

Extended-release: Do not administer less than 8 hours apart.

• Seizure risk is dose-related; can be minimized by limiting daily intake to 522 mg and gradually increasing; discontinue permanently in people who experience seizures.
• May cause sexual dysfunction.
• Screen patients for bipolar disorder and monitor for these symptoms; may precipitate manic, hypomanic, or mixed episodes in patients with bipolar disorder.
• Instruct patients to contact a healthcare professional if neuropsychiatric reactions occur.
• Perform a thorough cardiovascular assessment to identify risk factors of sudden cardiac death in pediatric ADHD patients.
• The risk of mydriasis; may trigger angle closure attack in people with angle-closure glaucoma with anatomically narrow angles without a patent iridectomy; use caution.
• False-positive urine immunoassay screening tests for bupropion have been reported; confirmatory tests (e.g., gas chromatography, mass spectrometry) will distinguish bupropion from bupropion
• Bupropion hydrobromide extended-release tablets are intended for oral use only; inhalation of crushed tablets or injection of dissolved bupropion reported; seizures and/or cases of death reported when administered intranasally or by parenteral injection.

Abuse warning

• XL and SR tablets are intended for oral use only
• Inhaling crushed tablets or injecting dissolved tablets has been reported to cause seizures and/or death

Pregnancy and Lactation

• Use bupropion with caution during pregnancy if the benefits outweigh the risks. Animal studies show potential for harm and human studies are not available or neither animal nor human studies done.
• Bupropion enters breast milk; use caution if breastfeeding.