Pharmacokinetics of bupropion and its major basic metabolites in normal subjects after a single dose

The pharmacokinetics of bupropion (BUP) and its three major basic metabolites (the erythroamino alcohol [EB], the threoamino alcohol [TB], and the hydroxy [HB] metabolites) were characterized after a single, oral, 200 mg dose of BUP in six healthy men. Twenty-one sequential plasma samples for analys...

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Published inClinical pharmacology and therapeutics Vol. 38; no. 5; p. 586
Main Authors Laizure, S C, DeVane, C L, Stewart, J T, Dommisse, C S, Lai, A A
Format Journal Article
LanguageEnglish
Published United States 01.11.1985
Subjects
Adult
Antidepressive Agents - metabolism
Bupropion
Humans
Kinetics
Male
Middle Aged
Propiophenones - metabolism
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Summary:The pharmacokinetics of bupropion (BUP) and its three major basic metabolites (the erythroamino alcohol [EB], the threoamino alcohol [TB], and the hydroxy [HB] metabolites) were characterized after a single, oral, 200 mg dose of BUP in six healthy men. Twenty-one sequential plasma samples for analysis by HPLC were drawn from each subject over the 56-hour period after dosing. Pharmacokinetic analyses were by noncompartmental methods. The mean elimination t1/2 values of BUP, TB, EB, and HB were 9.8, 19.8, 26.8, and 22.2 hours, respectively. The mean plasma AUCs of TB and HB were 2.4 and 10.3 times greater, respectively, than that for BUP. Because of the substantial presence of these metabolites in systemic circulation, further studies are recommended to understand further their roles in the clinical profile of this new antidepressant.
ISSN:0009-9236
DOI:10.1038/clpt.1985.228