Literature DB >> 3931955

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

S C Laizure, C L DeVane, J T Stewart, C S Dommisse, A A Lai.   

Abstract

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.

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Year:  1985        PMID: 3931955     DOI: 10.1038/clpt.1985.228

Source DB:  PubMed          Journal:  Clin Pharmacol Ther        ISSN: 0009-9236            Impact factor:   6.875


  20 in total

Review 1.  Review of the pharmacology and clinical profile of bupropion, an antidepressant and tobacco use cessation agent.

Authors:  Linda P Dwoskin; Anthony S Rauhut; Kelley A King-Pospisil; Michael T Bardo
Journal:  CNS Drug Rev       Date:  2006 Fall-Winter

2.  The effect of experimentally-induced renal failure on accumulation of bupropion and its major basic metabolites in plasma and brain of guinea pigs.

Authors:  C L DeVane; S C Laizure; D F Cameron
Journal:  Psychopharmacology (Berl)       Date:  1986       Impact factor: 4.530

3.  Serum creatinine elevation caused by bupropion.

Authors:  Can Kinalp; Ilhan Kurultak; Mevlut Ceri; Ilkay Keskinel
Journal:  Wien Klin Wochenschr       Date:  2013-12-17       Impact factor: 1.704

4.  Metabolism of bupropion by carbonyl reductases in liver and intestine.

Authors:  Jamie N Connarn; Xinyuan Zhang; Andrew Babiskin; Duxin Sun
Journal:  Drug Metab Dispos       Date:  2015-04-22       Impact factor: 3.922

5.  Formation of threohydrobupropion from bupropion is dependent on 11β-hydroxysteroid dehydrogenase 1.

Authors:  Arne Meyer; Anna Vuorinen; Agnieszka E Zielinska; Petra Strajhar; Gareth G Lavery; Daniela Schuster; Alex Odermatt
Journal:  Drug Metab Dispos       Date:  2013-06-26       Impact factor: 3.922

6.  Effects of sertraline on the pharmacokinetics of bupropion and its major metabolite, hydroxybupropion, in mice.

Authors:  Jillissa C Molnari; Hazem E Hassan; Alan L Myers
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2011-09-17       Impact factor: 2.441

Review 7.  The Role of Metabolites of Antidepressants in the Treatment of Depression.

Authors:  M V Rudorfer; W Z Potter
Journal:  CNS Drugs       Date:  1997-04       Impact factor: 5.749

8.  Pharmacokinetics of Bupropion and Its Pharmacologically Active Metabolites in Pregnancy.

Authors:  Valentina M Fokina; Meixiang Xu; Erik Rytting; Sherif Z Abdel-Rahman; Holly West; Cheryl Oncken; Shannon M Clark; Mahmoud S Ahmed; Gary D V Hankins; Tatiana N Nanovskaya
Journal:  Drug Metab Dispos       Date:  2016-08-15       Impact factor: 3.922

Review 9.  Antidepressants. A comparative review of the clinical pharmacology and therapeutic use of the 'newer' versus the 'older' drugs.

Authors:  M V Rudorfer; W Z Potter
Journal:  Drugs       Date:  1989-05       Impact factor: 9.546

10.  Studies in formulation and pharmacotechnical evaluation of controlled release transdermal delivery system of bupropion.

Authors:  Deepak Gondaliya; Kilambi Pundarikakshudu
Journal:  AAPS PharmSciTech       Date:  2003       Impact factor: 3.246

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