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Bupropion

Brands and Forms

  • Wellbutrin
    • tablet: 75mg, 100mg
  • Wellbutrin SR
    • sustained-release tablet: 100mg, 150mg, 200mg
  • Wellbutrin XL
    • extended-release tablet: 150mg, 300mg
  • Zyban
    • sustained-release tablet: 150mg

Uses of Bupropion

Bupropion is commonly used for treating Depressive Episodes in Major Depressive Disorder. It may also be suitable for treating Depressive Episodes in Bipolar Disorder given that it may be less likely than other antidepressants to precipitate Manic or Mixed Episodes [ref] .

Bupropion is used to help people with Nicotine Addiction quit smoking.

Bupropion can help treat Attention-Deficit/ Hyperactivity Disorder (ADHD).

Unlike other antidepressants, Bupropion does not cause weight gain or much in the way of sexual side-effects, and can also be used to reverse the sexual side-effects caused by other SSRI antidepressants [ref]. It can also be a good choice for people with Depression who have hypersomnia (over-sleeping) and significant fatigue or low energy.

How Bupropion Works

Bupropion is an antidepressant, and is a norepinephrine dopamine reuptake inhibitor (NDRI). It blocks norepinephrine and dopamine reuptake in the central nervous system and thus increases norepinephrine and dopamine neurotransmission.

Cautions when Using Bupropion

In people with a seizure disorder, advice from a neurologist should be obtained before starting Bupropion. Risk of seizures may also be higher when Bupropion is used in individuals who are malnourished or severely underweight, including people with Eating Disorders.

Bupropion can worsen states of anxiety. It may worsen or induce psychosis in people with Psychotic Disorders, and may worsen or induce Manic or Mixed Episodes in people with Bipolar Disorder.

Bupropion should not be used during or within 14 days following the administration of an MAOI, because a hypertensive crisis may result.

Dosing of Bupropion

When used for Depression, the immediate release form of Bupropion (ie. not the SR or XL forms) should be started at 75mg twice a day (morning and afternoon) and as soon as 3 days into treatment can be increased to 100mg twice a day. The next step, depending on clinical response, would be to increase it to 100mg three times a day (morning, noon, and early evening), and then 150mg three times a day. Do not exceed a single dose of 150mg or a total daily dose of 450mg.

When used for Depression, the SR (sustained release) form should be started at 100mg twice a day (morning and late afternoon), and as soon as 4 days into treatment can be increased to 150mg twice a day. Thereafter, depending on clinical response, it can be increased to 200mg twice a day. Do not exceed a single dose of 200mg or a total daily dose of 400mg.

When used for Depression, the XL (extended release) form should be started at 150mg once a day in the morning, and can be increased to 300mg once a day as soon as 4 days into treatment. Thereafter, depending on clinical response, it can be increased to a maximum dose of 450mg once a day.

When used for Nicotine Addiction, Zyban, which is the SR (sustained release) form of Bupropion, should be started at 150mg once daily in the morning, and as soon as 3 days into treatment can be increased to 150mg twice a day (morning and late afternoon). It can be started while the individual is still smoking.

For Attention-Deficit/ Hyperactivity Disorder (ADHD), dose the same way as for Depression.

When wanting to stop this medication, the dose should be reduced gradually over a period of a few weeks.

Onset of action

It usually takes 3-4 weeks before any therapeutic effect occurs, and 12 weeks or more may be needed for maximum effects. If no significant effects occur after 6 weeks (during which time dose has been increased beyond the minimum for at least 2 weeks), then it may not work at all.

Kidney impairment

Use a lower dose, as kidney impairment can lead to increased blood concentrations of the medication.

Hepatic impairment

Use a lower dose. For severe liver cirrhosis, do not exceed 75mg once daily of the immediate release form, 100mg once daily or 150mg every other day of the SR (sustained release) form, and 150mg every other day of the XL form.

Side-effects of Bupropion

Below is a list of most of the reported side-effects of Bupropion. Most of these side-effects occur in only a minority of individuals, and many also resolve with time while the medication is continued.

Cardiovascular: tachycardia (rapid heart rate); palpitations; flushing; increased or decreased blood pressure; syncope (fainting; rare); edema; arrhythmias (rare); phlebitis (rare); pulmonary embolism (rare).

Central Nervous System: headache; insomnia; dizziness; tremor; sedation; disturbed concentration; sensory disturbance; abnormal dreams; paresthesia; incoordination (rare); myoclonus (rare); seizures (rare).

Dermatologic: rash; excessive perspiration; hair loss (rare).

Endocrine/Metabolic: weight loss; weight gain; hyperglycemia (rare); hypoglycemia (rare); SIADH (rare).

Eyes, Ears, Nose and Throat: blurred vision; dry mouth; nasopharyngitis; pharyngitis; tinnitus; amblyopia; increased intraocular pressure; mydriasis.

Gastrointestinal: nausea; constipation; vomiting; diarrhea; abdominal pain; dyspepsia; decreased appetite; flatulence; taste disturbance; intestinal inflammation (rare); pancreatitis (rare); hepatitis (rare).

Genitourinary: abnormal menstruation; frequent urination; urinary retention; abnormal ejaculation; dyspareunia (painful intercourse in women); painful urination; impotence (rare).

Musculoskeletal: muscle pains; joint pains; muscle weakness.

Psychiatric: anxiety; irritability; restlessness; agitation; psychosis (more likely in people with Psychotic Disorders or Bipolar Disorder); mania and mixed states (more likely in people with Bipolar Disorder); suicidal thoughts.

Respiratory: upper respiratory tract infection.

Common side-effects of Bupropion

Headache, agitation, insomnia, dizziness, tremor, sedation, tachycardia, excessive sweating, blurred vision, dry mouth, constipation, anorexia, nausea, abdominal pain, weight loss.

Rare but serious side-effects of note of Bupropion

  • Seizures

Bupropion overdose

Hallucinations, arrhythmias, loss of consciousness, seizures, cardiac arrest. Can be fatal in rare circumstances.

Bupropion and pregnancy

Category C: some animal studies show adverse effects at very high doses, but few controlled human studies have been done. One study on humans showed that rates of congenital malformations overall, and cardiovascular malformations, were not higher for Bupropion than for other antidepressants when used in the first trimester, and were not higher when Bupropion was used in the first trimester versus the later trimesters. Bupropion should be used in pregnancy only if potential benefits outweigh potential risks (see here for further discussion).

Medical Monitoring for Bupropion

Measure blood pressure and pulse a few weeks after starting the medication and after every dose increase.

Drug Interactions with Bupropion

  • Use caution when combining with other medications that increase dopamine neurotransmission, such as Levodopa, Amantadine, stimulants, and Atomoxetine.
  • Use caution when combining with other medications that can increase seizure risk, including Tricyclic Antidepressants, Lithium, and most Typical Antipsychotics.
  • Can increase plasma levels of some beta-blockers and Atomoxetine.
  • Blood concentrations of Bupropion can be lowered by Fluoxetine.
  • Should not be used during or within 14 days following the administration of an MAOI, because a hypertensive crisis may result.