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:
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:
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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