Bupropion in Depression

II. The Role of Metabolites in Clinical Outcome

Robert N. Golden, C. Lindsay Devane, Steven Laizure, Matthew V. Rudorfer, Michael A. Sherer, William Z. Potter

Research output: Contribution to journalArticle

101 Citations (Scopus)

Abstract

We studied the steady-state pharmacokinetics of bupropion hydrochloride, a unicyclic aminoketone antidepressant, in depressed patients. The metabolites hydroxybupropion (HB), threohydrobupropion, and erythrohydrobupropion predominated over the parent compound in plasma and cerebrospinal fluid at steady state. Plasma concentrations of each metabolite correlated with cerebrospinal fluid concentrations. Higher plasma metabolite concentrations were associated with poor clinical outcome. This relationship was most striking with HB; plasma HB levels were greater than 1250 ng/mL in all five nonresponders and less than 1200 ng/mL in all seven responders. Plasma HB levels correlated with postreatment plasma homovanillic acid levels. High levels of bupropion metabolites may be associated with poor clinical outcome due to toxic effects involving dopaminergic systems. Alternatively, a curvilinear dose-response relationship may exist for bupropion metabolites. Future studies should explore the clinical utility of plasma metabolite measurements in enhancing the efficacy of treatment with bupropion.

Original languageEnglish (US)
Pages (from-to)145-149
Number of pages5
JournalArchives of General Psychiatry
Volume45
Issue number2
DOIs
StatePublished - Jan 1 1988
Externally publishedYes

Fingerprint

Bupropion
Cerebrospinal Fluid
Homovanillic Acid
Poisons
Plasma
Antidepressive Agents
Pharmacokinetics
hydroxybupropion

All Science Journal Classification (ASJC) codes

  • Arts and Humanities (miscellaneous)
  • Psychiatry and Mental health

Cite this

Bupropion in Depression : II. The Role of Metabolites in Clinical Outcome. / Golden, Robert N.; Devane, C. Lindsay; Laizure, Steven; Rudorfer, Matthew V.; Sherer, Michael A.; Potter, William Z.

In: Archives of General Psychiatry, Vol. 45, No. 2, 01.01.1988, p. 145-149.

Research output: Contribution to journalArticle

Golden, Robert N. ; Devane, C. Lindsay ; Laizure, Steven ; Rudorfer, Matthew V. ; Sherer, Michael A. ; Potter, William Z. / Bupropion in Depression : II. The Role of Metabolites in Clinical Outcome. In: Archives of General Psychiatry. 1988 ; Vol. 45, No. 2. pp. 145-149.
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