Wellbutrin XL
Celexa (Citalopram)
Zoloft (Sertraline)
Effexor XR (Venlafaxine)

Bupropion SR (Zyban)

Generic Name: Bupropion hydrochloride

Brand Names: Wellbutrin, Wellbutrin SR

What is Bupropion?

Bupropion hydrochloride is an antidepressant of the aminoketone class with distinctive pharmacologic properties. It blocks the reuptake of norepinephrine and dopamine without significant effect at serotonin receptors. Its structure closely resembles that of the stimulant diethylpropion, and is related to phenylethylamines.

Bupropion Sustained-Release is indicated for the treatment of major depressive disorder and smoking cessation. Sometimes it is prescribed for weight loss and bipolar depression. Also, bupropion is frequently used to augment the efficacy and lessen the side effects of other antidepressants.

Most noteworthy about bupropion is the absence of weight gain, daytime drowsiness, sexual disturbances, and anticholinergic action. Evidence shows that other than the rare incident of seizures, bupropion causes no serious adverse reactions or clinical laboratory changes.

Good candidates for Bupropion (Wellbutrin)

Those who experience cravings, excessive eating, attention deficit hyperactivity disorder (ADHD), low libido, orgasm dysfunction 2, lethargy, or lack of motivation 3 may benefit from bupropion. It is a worthy choice if tobacco cessation or weight loss is a secondary goal. It may help to overcome retarded depression, depression with coexisting cognitive slowing or pseudo-dementia.

When Bupropion (Wellbutrin) is not appropriate

Bupropion is not a prescription of choice for excessively activated and agitated persons, those who use any other bupropion-containing product (ie, coadministration of Zyban for smoking cessation and Wellbutrin for depression).

It is contraindicated for those who have:

  • seizure disorder
  • current or prior diagnosis of bulimia or anorexia nervosa
  • been concurrently treated with or within 14 days of discontinuation of MAO inhibitors
  • abruptly discontinued alcohol or sedatives
  • hypersensitivity to bupropion or any other component of the product.

Bupropion dosing:


Although overshadowed by the SSRIs as first-line treatment for major depression, the efficacy of bupropion in depression is well established and is comparable to that of SSRIs.

Immediate-release: 100 mg two times per day initially; may increase to 100 mg tree times per day after 3 days (maximum 450 mg daily).

Sustained-release: 150 mg once daily initially; may increase to 150 mg two times per day as early as day 4 of therapy (max daily dose, 400 mg; max single dose, 200 mg).

Extended-release: 150 mg once daily in the morning initially; can increase to 300 mg once daily after 4 days; maximum single dose 450 mg once daily.

Dosing conversion between immediate, sustained, and extended release products: Convert using same total daily dose (up to the maximum recommended dose for a given dosage form), but adjust frequency as indicated for sustained (twice daily) or extended (once daily) release products.

Foods: May be taken without regard to meals.

How long until Bupropion works?

Onset of antidepressive effect usually not immediate, but often delayed 2-4 weeks. If it is not working within 6–8 weeks, it may require a dosage increase or it may not work at all.

Smoking cessation

By inhibiting dopamine reuptake, bupropion ensures anticraving and antiwithdrawal effects thanks to which it helps in a long-term abstinence from smoking.

Initial dose is 150 mg once a day, increase to 150 mg twice a day after at least 3 days (maximum 300 mg per day). Begin 1–2 weeks before smoking is discontinued and take for up to 6 months.

Side effects

Most common side effects include: agitation (32%); insomnia (31%); dry mouth (28%); headache (26%); weight loss (23%), nausea, vomiting (23%), dizziness (22%); sweating (22%); tremor (21%); sedation (20%); anorexia (18%), tachycardia (11%); abdominal discomfort (9%); and rash (8%).


  • Elderly. Use with caution. Because elderly patients are more likely to have decreased renal function, use care in dose selection and consider monitoring renal function.
  • Bipolar depression. May worsen psychosis in some patients or precipitate a shift to mania or hypomania in patients with bipolar disorder.
  • Cardiovascular disease. Use caution in patients with cardiovascular disease, history of hypertension, or coronary artery disease; treatment-emergent hypertension (including some severe cases) has been reported.
  • Seizures. The risk of seizures is dose-dependent and increased in patients with a history of seizures, anorexia/bulimia, head trauma, CNS tumor, severe hepatic cirrhosis, abrupt discontinuation of sedative-hypnotics or ethanol, drugs that lower seizure threshold (antipsychotics, other antidepressants, theophylline, systemic steroids, etc.)

Drug interactions

  • CYP2B6 Inhibitors (e.g. clopidogrel, cyclophosphamide, orphenadrine, thiotepa, ticlopidine): may increase bupropion plasma levels.
  • CYP2D6 Substrates (e.g. thioridazine, tamoxifen): decreased metabolism of CYP2D6 Substrates.
  • MAO inhibitors: can be fatal when combined with MAO inhibitors.
  • According to the latest reports, there is a potential for digoxin-bupropion drug interaction 4.

Pregnancy & Lactation

Pregnancy category C
A slight increase in malformations was observed in some animal studies.
In studies conducted in rats and rabbits, bupropion was administered orally at doses up to 450 and 150 mg/kg/day, respectively (approximately 11 and 7 times the maximum recommended human dose), during the period of organogenesis. No clear evidence of teratogenic activity was found in either species; however, in rabbits, slightly increased incidences of fetal malformations and skeletal variations were observed.

One study has been conducted in pregnant women. This retrospective, managed-care database study assessed the risk of congenital malformations overall, and cardiovascular malformations specifically, following exposure to bupropion in the first trimester compared to the risk of these malformations following exposure to other antidepressants in the first trimester and bupropion outside of the first trimester. The study showed no greater risk for congenital malformations overall, or cardiovascular malformations specifically, following first trimester bupropion exposure compared to exposure to all other antidepressants in the first trimester, or bupropion outside of the first trimester. The results of this study have not been corroborated.

Nursing mothers
Bupropion and its metabolites are secreted in human milk. Because of the potential harm for nursing infants, a decision should be made whether to discontinue nursing or to discontinue Bupropion.


  • 1. U.S. FDA. Bupropion SR Prescribing Information (PDF format)
  • 2. Modell JG, May RS, Katholi CR. J Sex Marital Ther. 2000 Jul-Sep;26(3):231-40. PubMed
  • 3. Jamerson BD, Krishnan KR, Roberts J, Krishen A, Modell JG. Psychopharmacol Bull. 2003 Spring;37(2):67-78. PubMed
  • 4. He J1, Yu Y, Prasad B, Chen X, Unadkat JD. Mechanism of an unusual, but clinically significant, digoxin-bupropion drug interaction. Biopharm Drug Dispos. 2014 Jan 16.

Last updated: February, 2015

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