Clinical Pharmacokinetics of Lofexidine, the [alpha] 2-Adrenergic Receptor Agonist, in Opiate Addicts Plasma Using a Highly Sensitive Liquid Chromatography Tandem Mass Spectrometric Analysis

The objective of this investigation was to characterize the pharmacokinetic profile of lofexidine. Lofexidine is an orally bioavailable α 2-adrenergic receptor agonist analogue of clonidine that acts centrally to suppress opiate withdrawal symptoms. During the detoxification period of a phase 3 plac...

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Bibliographic Details
Published in:The American journal of drug and alcohol abuse 2008-09, Vol.34 (5), p.611
Main Authors: Yu, Elmer, Miotto, Karen, Akerele, Evaristo, O'Brien, Charles P, Ling, Walter, Kleber, Herbert, Fischman, Marian W, Elkashef, Ahmed, Herman, Barbara H, Al-Ghananeem, Abeer M
Format: Article
Language:English
Subjects:
Chromatography
Drug abuse
Drug addiction
Drugs
Mass spectrometry
Medical research
Narcotics
Pharmacology
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Summary:The objective of this investigation was to characterize the pharmacokinetic profile of lofexidine. Lofexidine is an orally bioavailable α 2-adrenergic receptor agonist analogue of clonidine that acts centrally to suppress opiate withdrawal symptoms. During the detoxification period of a phase 3 placebo-controlled, randomized, double-blind trial, six subjects were entered in this preliminary pharmacokinetic study. Pharmacokinetic analysis of plasma samples collected during study day 7 indicated that C... was 3242 ± 917 ng/L. The mean trough levels between the study days were not significantly different (p > .05), suggesting that the subjects were at steady-state. Although preliminary due to the limited number of subjects, these findings are the first to document lofexidine clinical pharmacokinetics in opiate addicts using a highly sensitive liquid chromatography tandem mass spectrometric analysis. (ProQuest: ... denotes formulae/symbols omitted.)
ISSN:0095-2990
1097-9891
DOI:10.1080/00952990802308122