Bupropion: 10 Clinical Facts

Bupropion: 10 Clinical Facts

Clinical Fact #1:

Bupropion is least likely to precipitate mania of all antidepressants in patient with bipolar disorder.

Reference: N Engl J Med 2007; 356:1711–1722​. (pdf)

Clinical Fact #2:

Incidence of seizure at 300mg/day for Sustained release Bupropion is worse than seizure incidence with other antidepressants.

Reference: Manual of Clinical Psychopharmacology, 7th Edition, Chapter 3, Antidepressants.

Clinical Fact #3:

Maximum recommended single dose and strength of Bupropion:

  • IR: < 150mg single dose

  • SR: < 200mg single dose

  • XL: < 450mg single dose

Clinical Fact #4:

Bupropion can cause false positive urine drug screen for amphetamines.

Reference: J Med Toxicol. 2011 Jun;7(2):105-8. (pdf)

Clinical Fact #5:

Two important clinical use of Bupropion as an adjunct to SSRIs:

(a) to augment the antidepressant effect.

(b) to counteract the sexual side effects of SSRIs.

Reference: J Clin Psychopharmacol. 2017 Apr;37(2):193-199. (pubmed)

Clinical Fact #6:

Caution with following co-morbid psychiatric disorders:

(a) Bupropion use in patient with psychotic disorder is known to worsen the psychosis.

(b) Probably not effective in the treatment of anxiety disorders: can worsen underlying anxiety.

Clinical Fact #7:

Bupropion Drug Interactions (CYP2D6):

Bupropion inhibits CYP2D6 and can increase concentrations of:

(a) antidepressants (e.g., venlafaxine, nortriptyline, imipramine, desipramine, paroxetine, fluoxetine, sertraline)

(b) antipsychotics (e.g., haloperidol, risperidone, thioridazine)

(c) beta-blockers (e.g., metoprolol),

(d) Type 1C antiarrhythmics (e.g., propafenone, flecainide).

Consider dose reduction when using with bupropion.

Clinical Fact #8:

Bupropion Drug Interactions (CYP2B6):

Bupropion is primarily metabolized to hydroxybupropion by CYP2B6:

(a) 2B6 inhibitors can increase bupropion exposure but decrease hydroxybupropion exposure: Ticlopidine and Clopidogrel.

(b) 2B6 inducers can decrease bupropion and hydroxybupropion exposure: ritonavir, lopinavir, or efavirenz

Clinical Fact #9:

Contraindications for bupropion:

  • Seizure disorder.

  • Current or prior diagnosis of bulimia or anorexia nervosa.

  • Abrupt discontinuation of alcohol, benzodiazepines, barbiturates, antiepileptic drugs.

  • Monoamine Oxidase Inhibitor

Clinical Fact #10:

Most common side effect of sustained release Bupropion are:

  • Insomnia

  • Anorexia

  • Dry mouth

  • Sweating

  • Tinitus 

  • Tremor (at dose of 100-300mg/day)

Reference: Bupropion SR package insert. (pdf)

Watch this Video for Bupropion’s Mechanism of Action:

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