Document Detail

Steady-state clinical pharmacokinetics of bupropion extended-release in youths.
MedLine Citation:
PMID:  17135996     Owner:  NLM     Status:  MEDLINE    
OBJECTIVE: To examine in children and adolescents the 24-hour, steady-state clinical pharmacokinetics of an extended-release (XL) formulation of bupropion (Wellbutrin XL).
METHOD: Subjects were six male and four female patients (ages 11.5-16.2 years) prescribed bupropion XL in morning daily doses of either 150 mg (n = 5) or 300 mg (n = 5) for at least 14 days. During an overnight hospitalization, subjects had serial blood draws every 1.5 to 3 hours from an intravenous port to measure plasma levels of bupropion and its metabolites. Pharmacokinetic variables were determined by noncompartmental analysis for bupropion and exponential analyses for metabolites.
RESULTS: Bupropion and metabolites demonstrated linear pharmacokinetics. Bupropion's mean maximum concentration (Cmax) was lower (p = .021) and its mean time to Cmax longer (p = .057) in the current sample on bupropion XL relative to a previously studied sample of youths on bupropion sustained-release (Wellbutrin SR). Mean 24-hour area under the curve ratios of metabolites to bupropion ranged from 1.0 for erythrohydrobupropion to 16.4 for hydroxybupropion.
CONCLUSIONS: Once-daily dosing is justified in youths prescribed bupropion XL. The active metabolite hydroxybupropion probably has key pharmacodynamic effects, given its higher and more sustained levels relative to the other metabolites or to bupropion.
W Burleson Daviss; James M Perel; Boris Birmaher; George R Rudolph; Imad Melhem; David A Axelson; David A Brent
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural    
Journal Detail:
Title:  Journal of the American Academy of Child and Adolescent Psychiatry     Volume:  45     ISSN:  0890-8567     ISO Abbreviation:  J Am Acad Child Adolesc Psychiatry     Publication Date:  2006 Dec 
Date Detail:
Created Date:  2006-11-30     Completed Date:  2006-12-28     Revised Date:  2014-01-07    
Medline Journal Info:
Nlm Unique ID:  8704565     Medline TA:  J Am Acad Child Adolesc Psychiatry     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1503-9     Citation Subset:  IM    
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MeSH Terms
Antidepressive Agents, Second-Generation / administration & dosage,  pharmacokinetics*,  therapeutic use*
Attention Deficit Disorder with Hyperactivity / drug therapy*
Bupropion / blood,  pharmacokinetics*,  therapeutic use*
Cytochrome P-450 CYP3A / metabolism
Cytochrome P-450 Enzyme System / metabolism
Delayed-Action Preparations / administration & dosage,  therapeutic use
Depressive Disorder, Major / drug therapy*
Grant Support
K23 MH065375/MH/NIMH NIH HHS; K23 MH065375-03/MH/NIMH NIH HHS; M-01 RR00084/RR/NCRR NIH HHS; P30 MH066371/MH/NIMH NIH HHS
Reg. No./Substance:
0/Antidepressive Agents, Second-Generation; 0/Delayed-Action Preparations; 01ZG3TPX31/Bupropion; 9035-51-2/Cytochrome P-450 Enzyme System; EC 1.14.13.-/cytochrome P-450 CYP2B6; EC P-450 CYP3A

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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